WO2002100347A3 - Prodrugs of gaba analogs, compositions and uses thereof - Google Patents

Prodrugs of gaba analogs, compositions and uses thereof Download PDF

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Publication number
WO2002100347A3
WO2002100347A3 PCT/US2002/018689 US0218689W WO02100347A3 WO 2002100347 A3 WO2002100347 A3 WO 2002100347A3 US 0218689 W US0218689 W US 0218689W WO 02100347 A3 WO02100347 A3 WO 02100347A3
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WO
WIPO (PCT)
Prior art keywords
prodrugs
gaba analogs
compositions
methods
gaba
Prior art date
Application number
PCT/US2002/018689
Other languages
French (fr)
Other versions
WO2002100347A2 (en
Inventor
Mark A Gallop
Kenneth C Cundy
Cindy X Zhou
Fayang G Qiu
Fenmei Yao
Jia-Ning Xiang
Ian R Ollman
Original Assignee
Xenoport Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27404495&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2002100347(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to DE60223923T priority Critical patent/DE60223923T3/en
Priority to HU0400167A priority patent/HUP0400167A3/en
Priority to JP2003516067A priority patent/JP4216713B2/en
Priority to KR1020037016230A priority patent/KR100926921B1/en
Priority to CA002449729A priority patent/CA2449729C/en
Priority to IL15930002A priority patent/IL159300A0/en
Priority to CN02814572.0A priority patent/CN1753673B/en
Priority to MXPA03011565A priority patent/MXPA03011565A/en
Priority to AU2002345664A priority patent/AU2002345664C1/en
Priority to NZ530109A priority patent/NZ530109A/en
Priority to EP02744314A priority patent/EP1404324B2/en
Application filed by Xenoport Inc filed Critical Xenoport Inc
Priority to DK02744314.2T priority patent/DK1404324T4/en
Publication of WO2002100347A2 publication Critical patent/WO2002100347A2/en
Publication of WO2002100347A3 publication Critical patent/WO2002100347A3/en
Priority to NO20035474A priority patent/NO333756B1/en
Priority to IL159300A priority patent/IL159300A/en
Priority to ZA2003/09678A priority patent/ZA200309678B/en
Priority to HK06107881.1A priority patent/HK1087628A1/en
Priority to AU2007203364A priority patent/AU2007203364B2/en
Priority to NO20083958A priority patent/NO20083958L/en
Priority to NO20083956A priority patent/NO20083956L/en
Priority to AU2008221505A priority patent/AU2008221505C1/en
Priority to IL197843A priority patent/IL197843A/en
Priority to IL213649A priority patent/IL213649A0/en

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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/12Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
    • C07C201/12Preparation of nitro compounds by reactions not involving the formation of nitro groups
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/19Carboxylic acids, e.g. valproic acid
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    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D317/34Oxygen atoms
    • C07D317/40Vinylene carbonate; Substituted vinylene carbonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Abstract

The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using phannaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
PCT/US2002/018689 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof WO2002100347A2 (en)

Priority Applications (22)

Application Number Priority Date Filing Date Title
JP2003516067A JP4216713B2 (en) 2001-06-11 2002-06-11 GABA analog prodrugs, compositions and uses thereof
MXPA03011565A MXPA03011565A (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof.
DK02744314.2T DK1404324T4 (en) 2001-06-11 2002-06-11 Preservatives of GABA analogues, compositions and uses thereof
KR1020037016230A KR100926921B1 (en) 2001-06-11 2002-06-11 Prodrugs of BAAA analogs, compositions and uses thereof
NZ530109A NZ530109A (en) 2001-06-14 2002-06-11 Prodrugs of GABA analogs, compositions and uses thereof
IL15930002A IL159300A0 (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof
CN02814572.0A CN1753673B (en) 2001-06-11 2002-06-11 Prodrugs of GABA analogs, compositions and uses thereof
CA002449729A CA2449729C (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof
AU2002345664A AU2002345664C1 (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof
HU0400167A HUP0400167A3 (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof
EP02744314A EP1404324B2 (en) 2001-06-11 2002-06-11 Prodrugs of gaba analogs, compositions and uses thereof
DE60223923T DE60223923T3 (en) 2001-06-11 2002-06-11 PROGRUGS OF GABA ANALOGUE, COMPOSITIONS AND ITS USES
NO20035474A NO333756B1 (en) 2001-06-11 2003-12-09 Compounds, their use, and pharmaceutical compositions
IL159300A IL159300A (en) 2001-06-11 2003-12-10 Prodrugs of gabapentin compounds, compositions and their use in the manufacture of a medicament
ZA2003/09678A ZA200309678B (en) 2001-06-11 2003-12-12 Prodrugs of gaba analogs compositions and uses thereof
HK06107881.1A HK1087628A1 (en) 2001-06-11 2006-07-14 Prodrugs of gaba analogs, compositions and uses thereof gaba
AU2007203364A AU2007203364B2 (en) 2001-06-11 2007-07-19 Prodrugs of gaba analogs, compositions and uses thereof
NO20083956A NO20083956L (en) 2001-06-11 2008-09-16 Prodrugs of GABA analogs, compositions and uses thereof
NO20083958A NO20083958L (en) 2001-06-11 2008-09-16 Prodrugs of GABA analogs, compositions and uses thereof
AU2008221505A AU2008221505C1 (en) 2001-06-11 2008-09-17 Prodrugs of gaba analogs, compositions and uses thereof
IL197843A IL197843A (en) 2001-06-11 2009-03-26 Prodrugs of gaba analogs, compositions and their use in the manufacture of a medicament
IL213649A IL213649A0 (en) 2001-06-11 2011-06-19 Prodrugs of gabapentin compounds, compositions and their use in the manufacture of a medicament

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US29752101P 2001-06-11 2001-06-11
US60/297,521 2001-06-11
US29851401P 2001-06-14 2001-06-14
US60/298,514 2001-06-14
US36609002P 2002-03-19 2002-03-19
US60/366,090 2002-03-19

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AT (2) ATE540678T1 (en)
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Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1077692T3 (en) * 1998-05-15 2004-12-06 Warner Lambert Co Amino acid stabilized gabapentin and pregabalin preparations and methods for their preparation
US7144877B2 (en) 2000-10-06 2006-12-05 Xenoport, Inc. Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
EP1361847A2 (en) 2000-10-06 2003-11-19 Xenoport, Inc. Bile-acid conjugates for providing sustained systemic concentrations of drugs
US6992076B2 (en) * 2000-10-06 2006-01-31 Xenoport, Inc. Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
EP1343515A4 (en) * 2000-10-06 2005-08-03 Xenoport Inc Compounds for sustained release of orally delivered drugs
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
AU2002345638A1 (en) * 2001-06-11 2002-12-23 Xenoport, Inc. Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
ATE540678T1 (en) * 2001-06-11 2012-01-15 Xenoport Inc GABA ANALOG PRODRUGS, COMPOSITIONS AND USES THEREOF
US7186855B2 (en) * 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7232924B2 (en) * 2001-06-11 2007-06-19 Xenoport, Inc. Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
US20040137052A1 (en) * 2001-12-25 2004-07-15 Yoshihiro Uchiyama Acid-containing preparations
WO2003077902A1 (en) 2002-02-19 2003-09-25 Xenoport, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
US7025745B2 (en) * 2002-10-07 2006-04-11 Advanced Cardiovascular Systems, Inc. Method of making a catheter balloon using a tapered mandrel
US20040162351A1 (en) * 2002-12-11 2004-08-19 Gallop Mark A. Orally administered dosage forms of fused GABA analog prodrugs having reduced toxicity
MXPA05006209A (en) * 2002-12-13 2005-08-19 Warner Lambert Co Pregabalin and derivates thereof for the treatment of fibromyalgia and other related disorders.
CA2451267A1 (en) 2002-12-13 2004-06-13 Warner-Lambert Company Llc Pharmaceutical uses for alpha2delta ligands
WO2004054560A1 (en) 2002-12-13 2004-07-01 Warner-Lambert Company Llc Alpha-2-delta ligand to treat lower urinary tract symptoms
US8641987B2 (en) 2003-01-24 2014-02-04 Applied Biosystems, Llc Sample chamber array and method for processing a biological sample
NZ543138A (en) * 2003-03-31 2009-02-28 Xenoport Inc Treating or preventing hot flashes using prodrugs of GABA analogs
US7169812B2 (en) * 2003-07-01 2007-01-30 Medtronic, Inc. Process for producing injectable gabapentin compositions
US7662987B2 (en) * 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds
CN1860101B (en) * 2003-08-20 2010-10-27 什诺波特有限公司 Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
PT1660440E (en) 2003-08-20 2012-05-15 Xenoport Inc Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
EP2354120A1 (en) * 2003-08-20 2011-08-10 XenoPort, Inc. Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
US7700652B2 (en) 2003-09-11 2010-04-20 Xenoport, Inc. Treating urinary incontinence using prodrugs of GABA analogs
WO2005025675A1 (en) 2003-09-12 2005-03-24 Pfizer Limited Combinations comprising alpha-2-delta ligands and serotonin / noradrenaline re-uptake inhibitors
RU2377234C2 (en) * 2003-09-17 2009-12-27 Ксенопорт, Инк. Treatment or prevention of restless legs syndrome with using promedicines of gaba analogues
CA2538802C (en) * 2003-09-17 2015-01-27 Xenoport, Inc. Treating or preventing restless legs syndrome using prodrugs of gaba analogs
SG147437A1 (en) 2003-10-14 2008-11-28 Xenoport Inc Crystalline form of gamma-aminobutyric acid analog
WO2005041976A2 (en) * 2003-10-23 2005-05-12 Medtronic, Inc. Injectable gabapentin compositions
EP2371815A1 (en) 2003-12-30 2011-10-05 XenoPort, Inc. Sythesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
CN1902175B (en) * 2003-12-30 2012-08-22 什诺波特有限公司 Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
EP1763503A1 (en) * 2004-03-17 2007-03-21 Hikal Limited 4-t-butylgabapentin and its synthesis
MXPA06012172A (en) * 2004-04-20 2007-01-17 Pfizer Prod Inc Combinations comprising alpha-2-delta ligands.
WO2006050472A2 (en) 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous and -phosphinic acids
WO2006050471A2 (en) * 2004-11-03 2006-05-11 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use
US8795725B2 (en) 2004-11-04 2014-08-05 Xenoport, Inc. GABA analog prodrug sustained release oral dosage forms
MX2007009923A (en) * 2005-02-15 2008-03-04 Jazz Pharmaceuticals Dosage form and method for sustained release of a substituted pyrazine compound.
JP4938771B2 (en) * 2005-06-20 2012-05-23 ゼノポート,インコーポレーテッド Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis, and uses
US20070049627A1 (en) * 2005-08-23 2007-03-01 Tran Pierre V Treating vulvodynia using prodrugs of GABA analogs
US20070049626A1 (en) * 2005-08-26 2007-03-01 Tran Pierre V Treating premature ejaculation using gabapentin and pregabalin prodrugs
RU2008108215A (en) * 2005-08-31 2009-10-10 Вайет (Us) 9-AMINOCARBONYL SUBSTITUTED DERIVATIVES OF GLYCYCLICLINS
US7727978B2 (en) * 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
WO2008033572A1 (en) 2006-09-15 2008-03-20 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
US7879906B2 (en) 2006-11-24 2011-02-01 Anchen Laboratories, Inc. GABA analogs, compositions and methods for manufacturing thereof
MX2009005676A (en) * 2006-11-30 2010-03-22 Cenerx Biopharma Inc Dialkylamino alkyl esters of pivagabine as medicaments for the treatment of central nervous system disorders.
US20080161393A1 (en) * 2006-12-08 2008-07-03 Barrett Ronald W Use of prodrugs of GABA analogs for treating disease
UA94979C2 (en) 2006-12-22 2011-06-25 Рекордати Айеленд Лимитед Combination therapy for lower urinary tract disorders with α2δ AND NSAIDs
TW200908957A (en) * 2007-06-15 2009-03-01 Xenoport Inc Use of prodrugs of GABA analogs, antispasticity agents, and prodrugs of GABAB receptor agonists for treating spasticity
CA2694982C (en) 2007-07-20 2013-06-25 Amyris Biotechnologies, Inc. Fuel compositions comprising tetramethylcyclohexane
TW200936123A (en) * 2007-11-06 2009-09-01 Xenoport Inc Use of prodrugs of GABAb agonists for treating neuropathic and musculoskeletal pain
US7872046B2 (en) 2008-01-25 2011-01-18 Xenoport, Inc. Crystalline form of a (3S)-aminomethyl-5-methyl-hexanoic acid prodrug and methods of use
US8062870B2 (en) 2008-01-25 2011-11-22 Xenoport, Inc. Enantiomerically resolving acyloxyalkyl thiocarbonates used in synthesizing acyloxyalkyl carbamate prodrugs
WO2009094577A2 (en) 2008-01-25 2009-07-30 Xenoport, Inc. Mesophasic forms of (3s)-aminomethyl-5-methyl-hexanoic acid prodrugs and methods of use
JP2010043063A (en) 2008-05-09 2010-02-25 Agency For Science Technology & Research Diagnosis and treatment of kawasaki disease
WO2010017498A1 (en) * 2008-08-07 2010-02-11 Xenoport, Inc. Methods of synthesizing n-hydroxysuccinimidyl carbonates
US8299291B2 (en) * 2008-08-07 2012-10-30 Xenoport, Inc. Methods of synthesizing 1-(acyloxy)-alkyl carbamate prodrugs
US8283487B2 (en) 2008-11-26 2012-10-09 Teva Pharmaceutical Industries Ltd. Processes for the preparation and purification of gabapentin enacarbil
JP5500164B2 (en) 2009-03-02 2014-05-21 アステラス製薬株式会社 Package of solid preparation
WO2010102252A1 (en) 2009-03-06 2010-09-10 Xenoport, Inc. Oral dosage forms having a high loading of a gabapentin prodrug
WO2011101245A1 (en) 2010-02-18 2011-08-25 Nicox S.A. Nitric oxide releasing compounds for the treatment of neuropathic pain
KR101786818B1 (en) 2010-07-30 2017-10-18 도레이 카부시키가이샤 Therapeutic agent or prophylactic agent for neuropathic pain
EP2844634B1 (en) * 2012-05-03 2021-04-14 DSM IP Assets B.V. Process for the preparation of intermediate compounds for preparing vitamin b6
WO2014134005A2 (en) 2013-02-26 2014-09-04 Xenoport, Inc. Method of making 1-(acyloxy)-alkyl carbamate compounds
KR102336426B1 (en) * 2013-11-05 2021-12-08 아스트라제네카 아베 Nmda antagonist prodrugs
US20190247331A1 (en) 2018-02-15 2019-08-15 Osmotica Kereskedelmi és Szolgáltató Korlátolt Felelõsségû Társaság Composition and method for treating neurological disease
US10213394B1 (en) 2018-02-15 2019-02-26 Osmotica Kereskedelmi és Szolgáltató Korlátolt Felelõsségû Társaság Composition and method for treating neurological disease
US10213393B1 (en) 2018-02-15 2019-02-26 Osmotica Kereskedelmi és Szolgáltató Korlátolt Feleõsségû Társaság Composition and method for treating neurological disease
WO2020074160A1 (en) * 2018-10-10 2020-04-16 Curovir Ab Condensed pyrimidine or pyridazine derivatives as antiviral agents
CN114306234A (en) * 2021-12-23 2022-04-12 江苏百奥信康医药科技有限公司 TPGS micelle oral liquid containing gabapentin compound and preparation method thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1178034A1 (en) * 2000-08-01 2002-02-06 Warner-Lambert Company Alkyl amino acid derivatives useful as pharmaceutical agents

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2002A (en) * 1841-03-12 Tor and planter for plowing
US2003A (en) * 1841-03-12 Improvement in horizontal windivhlls
US2996431A (en) * 1953-12-16 1961-08-15 Barry Richard Henry Friable tablet and process for manufacturing same
US3402240A (en) * 1957-06-25 1968-09-17 Pfizer & Co C Medicinal tablet and process of making same
US3139383A (en) * 1961-06-26 1964-06-30 Norton Co Encapsulated time release pellets and method for encapsulating the same
GB1364672A (en) * 1971-06-09 1974-08-29 Beecham Group Ltd Penicillins
US3962414A (en) * 1972-04-27 1976-06-08 Alza Corporation Structured bioerodible drug delivery device
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3811444A (en) * 1972-12-27 1974-05-21 Alza Corp Bioerodible ocular device
US3916899A (en) * 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
DE2336218C3 (en) * 1973-07-17 1985-11-14 Byk Gulden Lomberg Chemische Fabrik Gmbh, 7750 Konstanz Oral dosage form
US3992414A (en) * 1973-12-20 1976-11-16 Lever Brothers Company Process for the preparation of selectively halogenated ketals
US3992518A (en) * 1974-10-24 1976-11-16 G. D. Searle & Co. Method for making a microsealed delivery device
GB1478759A (en) * 1974-11-18 1977-07-06 Alza Corp Process for forming outlet passageways in pills using a laser
US4087544A (en) 1974-12-21 1978-05-02 Warner-Lambert Company Treatment of cranial dysfunctions using novel cyclic amino acids
DE2460891C2 (en) * 1974-12-21 1982-09-23 Gödecke AG, 1000 Berlin 1-aminomethyl-1-cycloalkaneacetic acids and their esters, processes for their preparation and medicaments containing these compounds
US4093709A (en) * 1975-01-28 1978-06-06 Alza Corporation Drug delivery devices manufactured from poly(orthoesters) and poly(orthocarbonates)
US4036064A (en) * 1975-09-11 1977-07-19 Gilford Instrument Laboratories, Inc. Pipette device
US4093571A (en) * 1976-01-14 1978-06-06 Celanese Corporation Process for making porous metal containing powder coating compositions
US4063064A (en) * 1976-02-23 1977-12-13 Coherent Radiation Apparatus for tracking moving workpiece by a laser beam
US4079038A (en) * 1976-03-05 1978-03-14 Alza Corporation Poly(carbonates)
US4066747A (en) * 1976-04-08 1978-01-03 Alza Corporation Polymeric orthoesters housing beneficial drug for controlled release therefrom
US4070347A (en) * 1976-08-16 1978-01-24 Alza Corporation Poly(orthoester) co- and homopolymers and poly(orthocarbonate) co- and homopolymers having carbonyloxy functionality
US4189571A (en) * 1978-02-07 1980-02-19 Fisons Limited Esters of cromoglycates
US4285987A (en) * 1978-10-23 1981-08-25 Alza Corporation Process for manufacturing device with dispersion zone
US4200098A (en) * 1978-10-23 1980-04-29 Alza Corporation Osmotic system with distribution zone for dispensing beneficial agent
FR2476087A1 (en) * 1980-02-18 1981-08-21 Roussel Uclaf NOVEL OXIMES DERIVED FROM 3-ALKYLOXY OR 3-ALKYL-THIOMETHYL 7-AMINO THIAZOLYL ACETAMIDO CEPHALOSPORANIC ACID, PROCESS FOR PREPARING THEM AND THEIR APPLICATION AS MEDICAMENTS
JPS57193489A (en) * 1981-05-21 1982-11-27 Fujisawa Pharmaceut Co Ltd Syn-isomer of 7-substituted-3-cephem-4-carboxylic acid ester and its preparation
US4434153A (en) * 1982-03-22 1984-02-28 Alza Corporation Drug delivery system comprising a reservoir containing a plurality of tiny pills
US4421736A (en) * 1982-05-20 1983-12-20 Merrel Dow Pharmaceuticals Inc. Sustained release diethylpropion compositions
US4721613A (en) * 1982-12-13 1988-01-26 Alza Corporation Delivery system comprising means for shielding a multiplicity of reservoirs in selected environment of use
US4760057A (en) * 1983-06-23 1988-07-26 Merck & Co., Inc. (Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs
EP0130119B1 (en) * 1983-06-23 1988-11-09 Merck & Co. Inc. (acyloxyalkoxy) carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs, their preparation and pharmaceutical compositions containing said derivatives
US4611056A (en) * 1983-10-05 1986-09-09 Merck Frosst Canada, Inc. Benzo[A]phenothiazines and hydro-derivatives
DE3479397D1 (en) * 1983-10-05 1989-09-21 Merck Frosst Canada Inc Benzoûa¨phenothiazines and hydro-derivatives and pharmaceutical compositions containing them
DE3484745D1 (en) * 1983-10-05 1991-08-01 Merck Frosst Canada Inc INHIBITORS FOR LEUKOTRIA BIOSYNTHESIS.
US4916230A (en) * 1984-07-02 1990-04-10 Merck & Co., Inc. Process for preparing novel N-(acyloxy-alkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for primary and secondary amine functions in drugs
US5051448A (en) * 1984-07-24 1991-09-24 The Mclean Hospital Corporation GABA esters and GABA analog esters
US4820523A (en) * 1986-04-15 1989-04-11 Warner-Lambert Company Pharmaceutical composition
US4752470A (en) * 1986-11-24 1988-06-21 Mehta Atul M Controlled release indomethacin
IL87710A (en) * 1987-09-18 1992-06-21 Ciba Geigy Ag Covered floating retard form for controlled release in gastric juice
US4816263A (en) * 1987-10-02 1989-03-28 Alza Corporation Dosage form for treating cardiovascular diseases comprising isradipine
US4853229A (en) * 1987-10-26 1989-08-01 Alza Corporation Method for adminstering tiny pills
DE3815221C2 (en) 1988-05-04 1995-06-29 Gradinger F Hermes Pharma Use of a retinol and / or retinoic acid ester-containing pharmaceutical preparation for inhalation for acting on the mucous membranes of the tracheo-bronchial tract, including the lung alveoli
PH26730A (en) * 1988-12-30 1992-09-28 Ciba Geigy Ag Coated adhesive tablets
DE3928183A1 (en) 1989-08-25 1991-02-28 Goedecke Ag LACTAM-FREE CYCLIC AMINO ACIDS
US5084169A (en) * 1989-09-19 1992-01-28 The University Of Colorado Foundation, Inc. Stationary magnetically stabilized fluidized bed for protein separation and purification
US5084479A (en) * 1990-01-02 1992-01-28 Warner-Lambert Company Novel methods for treating neurodegenerative diseases
GB9001405D0 (en) * 1990-01-22 1990-03-21 Leo Pharm Prod Ltd New intermediates,their production and use
EP0458751A1 (en) * 1990-05-25 1991-11-27 Warner-Lambert Company Delivery system for cyclic amino acids with improved taste, texture and compressibility
JPH04103574A (en) * 1990-08-22 1992-04-06 Kumiai Chem Ind Co Ltd Pyrimidine derivative and herbicide
US5827819A (en) * 1990-11-01 1998-10-27 Oregon Health Sciences University Covalent polar lipid conjugates with neurologically active compounds for targeting
AU9137091A (en) * 1990-11-27 1992-06-25 Northwestern University Gaba and l-glutamic acid analogs for antiseizure treatment
US6197819B1 (en) 1990-11-27 2001-03-06 Northwestern University Gamma amino butyric acid analogs and optical isomers
TW209174B (en) * 1991-04-19 1993-07-11 Takeda Pharm Industry Co Ltd
US5698155A (en) 1991-05-31 1997-12-16 Gs Technologies, Inc. Method for the manufacture of pharmaceutical cellulose capsules
GB9204918D0 (en) 1992-03-06 1992-04-22 Nycomed As Chemical compounds
DK0641330T3 (en) 1992-05-20 2001-12-03 Univ Northwestern Gaba and L-glutamic acid analogues for anticonvulsant therapy
EP0647133A4 (en) 1992-06-12 1997-10-29 Affymax Tech Nv Compositions and methods for enhanced drug delivery.
AU689809B2 (en) 1993-10-14 1998-04-09 Abbott Laboratories Quinolizinone type compounds
ZA953078B (en) * 1994-04-28 1996-01-05 Alza Corp Effective therapy for epilepsies
US5466811A (en) 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
US5684018A (en) * 1994-12-13 1997-11-04 Merck & Co., Inc. Acyloxyisopropyl carbamates as prodrugs for amine drugs
US5672584A (en) * 1995-04-25 1997-09-30 The University Of Kansas Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability
WO1996038435A1 (en) 1995-05-30 1996-12-05 Abbott Laboratories Dopamine agonists
AU720628B2 (en) 1996-02-07 2000-06-08 Warner-Lambert Company Novel cyclic amino acids as pharmaceutical agents
IL125364A0 (en) 1996-03-14 1999-03-12 Warner Lambert Co Novel bridged cyclic amino acids and pharmaceutical compositions containing them
PL185991B1 (en) * 1996-03-14 2003-09-30 Warner Lambert Co Novel substituted cyclic amino acids as pharmaceutic agents
DE69722426T3 (en) * 1996-07-24 2015-05-07 Warner-Lambert Company LLC (n.Ges. des Staates Delaware) ISOBUTYLGABA AND ITS DERIVATIVES FOR PAIN TREATMENT
JP2001509787A (en) 1996-07-30 2001-07-24 アクシス ファーマシューティカルズ,インコーポレイティド Novel compounds and compositions for treating diseases involving tryptase activity
US5962473A (en) 1996-08-16 1999-10-05 Eli Lilly And Company Methods of treating or ameliorating the symptoms of common cold or allergic rhinitis with serotonin 5-HT1F
US6375987B1 (en) * 1996-10-01 2002-04-23 Gattefossé, S.A. Process for the manufacture of pharmaceutical composition with modified release of active principle comprising the matrix
AU733896B2 (en) 1996-10-23 2001-05-31 Warner-Lambert Company Substituted gamma aminobutyric acids as pharmaceutical agents
EP1007037A4 (en) 1997-06-26 2004-10-06 Lilly Co Eli Antithrombotic agents
US6127418A (en) * 1997-08-20 2000-10-03 Warner-Lambert Company GABA analogs to prevent and treat gastrointestinal damage
AU8668598A (en) 1997-08-20 1999-03-08 University Of Oklahoma, The Gaba analogs to prevent and treat gastrointestinal damage
US6740682B2 (en) * 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
CU23048A3 (en) 1997-10-27 2005-06-24 Warner Lambert Co CYCLIC AMINO ACIDS AND DERIVATIVES OF THE SAME, USEFUL AS PHARMACEUTICAL AGENTS
CA2304965C (en) 1997-12-16 2007-08-21 Warner-Lambert Company ((cyclo)alkyl substituted)-gamma-aminobutyric acid derivatives (=gaba analogues), their preparation and their use in the treatment of neurological disorders
IL135315A0 (en) 1997-12-16 2001-05-20 Warner Lambert Co 4(3)-substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (gabapentin analogues), their preparation and their use in the treatment of neurological disorders
PT1047678E (en) 1997-12-16 2004-12-31 Warner Lambert Co 1-AMINOMETHYL-CYCLOALCAN DERIVATIVES SUBSTITUTED IN 1 (= GABAPENTINE ANALOGS) ITS PREPARATION AND ITS USE IN THE TREATMENT OF NEUROLOGICAL DISTURBLES
WO1999037296A1 (en) 1998-01-23 1999-07-29 Warner-Lambert Company Gabapentin and its derivatives for the treatment of muscular and skeletal pain
AU757445B2 (en) 1998-05-26 2003-02-20 Warner-Lambert Company Conformationally constrained amino acid compounds having affinity for the alpha2delta subunit of a calcium channel
FR2779651B1 (en) * 1998-06-16 2001-04-20 Gattefosse Ets Sa PROCESS FOR THE MANUFACTURE OF SUSTAINED RELEASE TABLETS OF ACTIVE INGREDIENT (S) HAVING ZERO-SIZE DISSOLUTION KINETICS
US6171615B1 (en) * 1998-07-06 2001-01-09 Gattefoss{acute over (e)} Sustained release theophylline formulations, excipient systems and methods of production
ATE280154T1 (en) 1998-09-14 2004-11-15 Warner Lambert Co BRANCHED ALKYLPYRROLIDINE-3-CARBONIC ACIDS
PT1121114E (en) 1998-10-16 2007-03-30 Warner Lambert Co Use of gaba analogs for the manufacture of a medicament for the treatment of mania and bipolar disorders
CO5210925A1 (en) * 1998-11-17 2002-10-30 Novartis Ag TETRASUSTITUID DIAMINUM NITROGUANIDINE DERIVATIVES
WO2000031020A1 (en) * 1998-11-25 2000-06-02 Warner-Lambert Company Improved gamma amino butyric acid analogs
EP1031350A1 (en) * 1999-02-23 2000-08-30 Warner-Lambert Company Use of a gabapentin-analog for the manufacture of a medicament for preventing and treating visceral pain
MXPA01012125A (en) * 1999-05-27 2002-06-04 Pfizer Prod Inc Mutual prodrugs of amlodipine and atorvastatin.
BR0011727A (en) * 1999-06-10 2002-03-05 Warner Lambert Co 3-propyl gamma-aminobutyric acids mono- and disubstituted
HN2000000224A (en) * 1999-10-20 2001-04-11 Warner Lambert Co BICYCLE AMINO ACIDS AS PHARMACEUTICAL AGENTS
DZ3141A1 (en) * 1999-12-08 2001-01-14 Warner Lambert Co Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of diabetic retinopathy.
IL150929A0 (en) * 2000-01-28 2003-06-24 Rohm & Haas Pharmaceutical compounds comprising a pharmaceutically active moiety and a moiety comprising a substituent that enhances its properties
WO2001062242A1 (en) * 2000-02-24 2001-08-30 Biocryst Pharmaceuticals, Inc. Prodrugs of substituted cyclopentane and cyclopentene compounds useful as neuraminidase inhibitors
NZ522411A (en) * 2000-05-25 2004-05-28 F Substituted 1-aminoalkyl-lactams and their use as muscarinic receptor antagonists
GB2362646A (en) * 2000-05-26 2001-11-28 Warner Lambert Co Cyclic amino acid derivatives useful as pharmaceutical agents
IL152770A0 (en) 2000-06-26 2003-06-24 Warner Lambert Co Gabapentin analogues for sleep disorders
ATE321052T1 (en) * 2000-07-07 2006-04-15 Novo Nordisk As MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPASES)
AU2001268951A1 (en) * 2000-07-07 2002-01-21 Novo-Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
GB0018528D0 (en) * 2000-07-27 2000-09-13 Photocure Asa Compounds
DZ3415A1 (en) * 2000-08-31 2002-03-07 Chiron Corp GUANIDINOBENZAMIDES AS MC4-R AGONISTS.
EP1361847A2 (en) * 2000-10-06 2003-11-19 Xenoport, Inc. Bile-acid conjugates for providing sustained systemic concentrations of drugs
US7144877B2 (en) * 2000-10-06 2006-12-05 Xenoport, Inc. Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
US6992076B2 (en) * 2000-10-06 2006-01-31 Xenoport, Inc. Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
DK1383731T3 (en) * 2000-10-20 2009-12-07 Biocryst Pharm Inc Biaryl compounds as serine protease inhibitors
US6683112B2 (en) * 2000-10-24 2004-01-27 Andrx Corporation Gabapentin prodrugs and formulations
GB2368579A (en) * 2000-10-31 2002-05-08 Parke Davis & Co Ltd Azole pharmaceutical agents
AU2002239257A1 (en) * 2000-11-17 2002-06-03 Xenoport, Inc. Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
WO2002062766A2 (en) * 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
US20030031711A1 (en) * 2001-05-29 2003-02-13 Fara John W. Method of treating gastroesophageal reflux disease and nocturnal acid breakthrough
US6818787B2 (en) * 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
ATE540678T1 (en) * 2001-06-11 2012-01-15 Xenoport Inc GABA ANALOG PRODRUGS, COMPOSITIONS AND USES THEREOF
GB0115517D0 (en) * 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
AU2002355686B2 (en) * 2001-07-04 2007-11-29 Sun Pharmaceutical Industries Limited Gastric retention controlled drug delivery system
EP2332547A1 (en) * 2001-07-13 2011-06-15 Paratek Pharmaceuticals, Inc. Tetracyclines for the treatment of inflammatory bowel disease
US7053076B2 (en) * 2001-08-29 2006-05-30 Xenoport, Inc. Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
US6723340B2 (en) * 2001-10-25 2004-04-20 Depomed, Inc. Optimal polymer mixtures for gastric retentive tablets
TWI312285B (en) * 2001-10-25 2009-07-21 Depomed Inc Methods of treatment using a gastric retained gabapentin dosage
US20030158254A1 (en) * 2002-01-24 2003-08-21 Xenoport, Inc. Engineering absorption of therapeutic compounds via colonic transporters
WO2003077902A1 (en) * 2002-02-19 2003-09-25 Xenoport, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
WO2005098444A2 (en) * 2003-07-03 2005-10-20 Xenoport, Inc. Monocarboxylate transporters expressed in cancer cells
US20060003920A1 (en) * 2004-06-04 2006-01-05 Xenoport, Inc. LAT1 transporters expressed in cancer cells
TW200616604A (en) * 2004-08-26 2006-06-01 Nicholas Piramal India Ltd Nitric oxide releasing prodrugs containing bio-cleavable linker

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1178034A1 (en) * 2000-08-01 2002-02-06 Warner-Lambert Company Alkyl amino acid derivatives useful as pharmaceutical agents

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