WO2007001975A8 - Piperidine derivatives useful as histamine h3 antagonists - Google Patents

Piperidine derivatives useful as histamine h3 antagonists

Info

Publication number
WO2007001975A8
WO2007001975A8 PCT/US2006/023800 US2006023800W WO2007001975A8 WO 2007001975 A8 WO2007001975 A8 WO 2007001975A8 US 2006023800 W US2006023800 W US 2006023800W WO 2007001975 A8 WO2007001975 A8 WO 2007001975A8
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
heteroaryl
heterocycloalkyl
cycloalkyl
aryl
Prior art date
Application number
PCT/US2006/023800
Other languages
French (fr)
Other versions
WO2007001975A1 (en
Inventor
Robert G Aslanian
Michael Y Berlin
Christopher W Boyce
Jianhua Chao
Lera Ruiz Manuel De
Pietro Mangiaracina
Kevin D Mccormick
Mwangi W Mutahi
Stuart B Rosenblum
Neng-Yang Shih
Daniel M Solomon
Wing C Tom
Henry A Vaccaro
Junying Zheng
Xiaohong Zhu
Original Assignee
Schering Corp
Robert G Aslanian
Michael Y Berlin
Christopher W Boyce
Jianhua Chao
Lera Ruiz Manuel De
Pietro Mangiaracina
Kevin D Mccormick
Mwangi W Mutahi
Stuart B Rosenblum
Neng-Yang Shih
Daniel M Solomon
Wing C Tom
Henry A Vaccaro
Junying Zheng
Xiaohong Zhu
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
Application filed by Schering Corp, Robert G Aslanian, Michael Y Berlin, Christopher W Boyce, Jianhua Chao, Lera Ruiz Manuel De, Pietro Mangiaracina, Kevin D Mccormick, Mwangi W Mutahi, Stuart B Rosenblum, Neng-Yang Shih, Daniel M Solomon, Wing C Tom, Henry A Vaccaro, Junying Zheng, Xiaohong Zhu filed Critical Schering Corp
Priority to EP06773528A priority Critical patent/EP1902046B1/en
Priority to AU2006262441A priority patent/AU2006262441A1/en
Priority to CA002610959A priority patent/CA2610959A1/en
Priority to JP2008518276A priority patent/JP2008546784A/en
Priority to MX2008000115A priority patent/MX2008000115A/en
Priority to AT06773528T priority patent/ATE450526T1/en
Priority to DE602006010870T priority patent/DE602006010870D1/en
Publication of WO2007001975A1 publication Critical patent/WO2007001975A1/en
Priority to IL187984A priority patent/IL187984A0/en
Publication of WO2007001975A8 publication Critical patent/WO2007001975A8/en
Priority to HK08110560.1A priority patent/HK1121737A1/en

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    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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Abstract

Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- or -SO1-2-; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, -C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
PCT/US2006/023800 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine h3 antagonists WO2007001975A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
EP06773528A EP1902046B1 (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine h3 antagonists
AU2006262441A AU2006262441A1 (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine H3 antagonists
CA002610959A CA2610959A1 (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine h3 antagonists
JP2008518276A JP2008546784A (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine H3 antagonists
MX2008000115A MX2008000115A (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine h3 antagonists.
AT06773528T ATE450526T1 (en) 2005-06-20 2006-06-19 PIPERIDINE DERIVATIVES SUITABLE AS ANTAGONISTS OF HISTAMINE H3
DE602006010870T DE602006010870D1 (en) 2005-06-20 2006-06-19 PIPERIDINE DERIVATIVES SUITED AS ANTAGONISTS OF HISTAMINE H3
IL187984A IL187984A0 (en) 2005-06-20 2007-12-06 Piperidine derivatives useful as histamine h3 antagonists
HK08110560.1A HK1121737A1 (en) 2005-06-20 2008-09-23 Piperidine derivatives useful as histamine h3 antagonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US69211005P 2005-06-20 2005-06-20
US60/692,110 2005-06-20

Publications (2)

Publication Number Publication Date
WO2007001975A1 WO2007001975A1 (en) 2007-01-04
WO2007001975A8 true WO2007001975A8 (en) 2008-01-24

Family

ID=36968725

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/023800 WO2007001975A1 (en) 2005-06-20 2006-06-19 Piperidine derivatives useful as histamine h3 antagonists

Country Status (17)

Country Link
US (2) US7635705B2 (en)
EP (1) EP1902046B1 (en)
JP (1) JP2008546784A (en)
KR (1) KR20080021082A (en)
CN (1) CN101243072A (en)
AR (1) AR054787A1 (en)
AT (1) ATE450526T1 (en)
AU (1) AU2006262441A1 (en)
CA (1) CA2610959A1 (en)
DE (1) DE602006010870D1 (en)
ES (1) ES2337727T3 (en)
HK (1) HK1121737A1 (en)
IL (1) IL187984A0 (en)
MX (1) MX2008000115A (en)
TW (1) TW200738676A (en)
WO (1) WO2007001975A1 (en)
ZA (1) ZA200710968B (en)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Fast Dissociting Dopamine 2 Receptor Antagonists
WO2007075555A2 (en) * 2005-12-21 2007-07-05 Schering Corporation Combination of an h3 antagonist/inverse agonist and an appetite suppressant
BRPI0717742A2 (en) * 2006-10-20 2013-11-26 Arete Therapeutics Inc SOLID SOLID EPOXIDE HYDROLASE INHIBITORS
JO2642B1 (en) 2006-12-08 2012-06-17 جانسين فارماسوتيكا ان. في Fast Dissociating Dopamine 2 Receptor Antagonists
CA2675450A1 (en) * 2007-01-29 2008-08-07 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors for treatment of metabolic syndrome and related disorders
JO2849B1 (en) 2007-02-13 2015-03-15 جانسين فارماسوتيكا ان. في Fast -Dissociating Dopamine 2 Receptor Antagonists
MX2009009417A (en) * 2007-03-02 2009-09-11 Schering Corp Piperidinyl-piperidine and piperazinyl-piperidine for use in the treatment of diabetes or pain.
WO2008112022A1 (en) * 2007-03-13 2008-09-18 Arete Therapeutics, Inc. 4 -pi peridinylurea compounds as soluble epoxide hydrolase inhibitors
US8906921B2 (en) 2007-04-23 2014-12-09 Janssen Pharmaceutica Nv 4-alkoxypyridazine derivatives as fast dissociating dopamine 2 receptor antagonists
CN101663299A (en) 2007-04-23 2010-03-03 詹森药业有限公司 Thiophene (two) azole compounds as fast dissociating dopamine 2 receptor antagonists
JP2010527915A (en) * 2007-04-26 2010-08-19 アバロン ファーマシューティカルズ,インコーポレイテッド Multiple ring compounds and uses thereof
GB0713686D0 (en) 2007-07-13 2007-08-22 Addex Pharmaceuticals Sa New compounds 2
MX2011000043A (en) 2008-07-03 2011-02-22 Janssen Pharmaceutica Nv Substituted 6- (1-piperazinyl) -pyridazines as 5-ht6 receptor antagonists.
WO2010027567A2 (en) 2008-07-23 2010-03-11 Schering Corporation Tricyclic spirocycle derivatives and methods of use thereof
ES2622161T3 (en) 2008-07-31 2017-07-05 Janssen Pharmaceutica, N.V. Piperazin-1-yl-trifluoromethyl substituted pyridines as fast dissociation dopamine 2 receptor antagonists
US8889674B2 (en) 2009-03-05 2014-11-18 Shionogi & Co., Ltd. Piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonism
US8337835B2 (en) * 2009-04-10 2012-12-25 Washington University Use of an endogenous ligand for peroxisome proliferator activated receptor alpha to treat liver disorders
PL2527340T3 (en) * 2010-01-22 2017-01-31 Taiho Pharmaceutical Co., Ltd. Piperazine compound having a pgds inhibitory effect
US9045445B2 (en) 2010-06-04 2015-06-02 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US20140288169A1 (en) * 2011-01-07 2014-09-25 Targacept, Inc. Nicotinic receptor non-competitive antagonists
US8865641B2 (en) * 2011-06-16 2014-10-21 The Feinstein Institute For Medical Research Methods of treatment of fatty liver disease by pharmacological activation of cholinergic pathways
MX360979B (en) 2011-09-16 2018-11-22 Galectin Therapeutics Inc Galacto-rhamnogalacturonate compositions for the treatment of non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.
WO2013151982A1 (en) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Methods and compounds useful in treating pruritus, and methods for identifying such compounds
CN102657868A (en) * 2012-05-30 2012-09-12 中国药科大学 5-hydroxy tryptamine 2 receptor antagonist or transporter inhibitor for treating fatty liver or hyperlipemia
KR102071739B1 (en) 2012-06-06 2020-01-30 갈렉틴 테라퓨틱스, 인크. Galacto-rhamnogalacturonate compositions for the treatment of diseases associated with elevated inducible nitric oxide synthase
US8652527B1 (en) 2013-03-13 2014-02-18 Upsher-Smith Laboratories, Inc Extended-release topiramate capsules
US9101545B2 (en) 2013-03-15 2015-08-11 Upsher-Smith Laboratories, Inc. Extended-release topiramate capsules
CN109082465A (en) * 2018-08-20 2018-12-25 苏州市广济医院 The molecular marker and application thereof of Olanzapine induction carbohydrate metabolism disturbance related disease
BR112021019465A8 (en) 2019-04-02 2022-06-07 Aligos Therapeutics Inc Compounds that target prmt5
WO2021187605A1 (en) * 2020-03-19 2021-09-23 田辺三菱製薬株式会社 NITROGEN-CONTAINING HETEROCYCLIC α-CYANO CARBONYL COMPOUND

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US661145A (en) * 1900-08-06 1900-11-06 Otto Hausmann Attachment for bicycles.
US856473A (en) * 1906-05-21 1907-06-11 Daniel E Krause Drilling-machine.
US4983567A (en) * 1987-03-16 1991-01-08 Biomeasure, Inc. Immunomodulators and methods of making same
US4983597A (en) 1989-08-31 1991-01-08 Merck & Co., Inc. Beta-lactams as anticholesterolemic agents
US5688787A (en) * 1991-07-23 1997-11-18 Schering Corporation Substituted β-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof
ATE158789T1 (en) * 1991-07-23 1997-10-15 Schering Corp SUBSTITUTED BETA-LACTAM COMPOUNDS AS HYPOCHOLESTEROLEMIC AGENTS AND METHOD FOR THE PRODUCTION THEREOF
US5561227A (en) * 1991-07-23 1996-10-01 Schering Corporation Process for the stereospecific synthesis of azetidinones
US5688785A (en) * 1991-07-23 1997-11-18 Schering Corporation Substituted azetidinone compounds useful as hypocholesterolemic agents
LT3300B (en) 1992-12-23 1995-06-26 Schering Corp Combination of a cholesterol biosynhtesis inhibitor and a beta- lactam cholesterol absorbtion inhibitor
LT3595B (en) * 1993-01-21 1995-12-27 Schering Corp Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents
KR0176001B1 (en) * 1993-07-09 1999-03-20 에릭 에스. 딕커 Process for the synthesis of azetidinones
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
US5627176A (en) * 1994-03-25 1997-05-06 Schering Corporation Substituted azetidinone compounds useful as hypocholesterolemic agents
US5633246A (en) * 1994-11-18 1997-05-27 Schering Corporation Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US5624920A (en) * 1994-11-18 1997-04-29 Schering Corporation Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
US5656624A (en) * 1994-12-21 1997-08-12 Schering Corporation 4-[(heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinones useful as hypolipidemic agents
US5618707A (en) * 1996-01-04 1997-04-08 Schering Corporation Stereoselective microbial reduction of 5-fluorophenyl-5-oxo-pentanoic acid and a phenyloxazolidinone condensation product thereof
WO1997016424A1 (en) 1995-11-02 1997-05-09 Schering Corporation Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-([phenyl or 4-fluorophenyl])-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinone
US5739321A (en) * 1996-05-31 1998-04-14 Schering Corporation 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
BR9711149A (en) 1996-08-16 1999-08-17 Schering Corp Treatment of allergic responses of the upper respiratory tract with a combination of histamine receptor antagonists
US5756470A (en) * 1996-10-29 1998-05-26 Schering Corporation Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents
US5869479A (en) * 1997-08-14 1999-02-09 Schering Corporation Treatment of upper airway allergic responses
US6133001A (en) * 1998-02-23 2000-10-17 Schering Corporation Stereoselective microbial reduction for the preparation of 1-(4-fluorophenyl)-3(R)-[3(S)-Hydroxy-3-(4-fluorophenyl)propyl)]-4(S)-(4 -hydroxyphenyl)-2-azetidinone
WO1999065867A1 (en) * 1998-06-17 1999-12-23 Du Pont Pharmaceuticals Company Cyclic hydroxamic acids as metalloproteinase inhibitors
US5919672A (en) * 1998-10-02 1999-07-06 Schering Corporation Resolution of trans-2-(alkoxycarbonylethyl)-lactams useful in the synthesis of 1-(4-fluoro-phenyl)-3(R)- (S)-hydroxy-3-(4-fluorophenyl)-propyl!-4(S)-(4-hydroxyphenyl)-2-azetidinone
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
AU4343500A (en) * 1999-04-16 2000-11-02 Schering Corporation Use of azetidinone compounds
IL150849A0 (en) * 2000-02-11 2003-02-12 Vertex Pharma Piperzine and piperidine derivatives and pharmaceutical compositions containg the same
US20020045686A1 (en) * 2000-08-24 2002-04-18 The Yokohama Rubber Co., Ltd Rubber composition having improved wet skid resistance and rolling resistance
DE10042447A1 (en) * 2000-08-29 2002-03-28 Aventis Pharma Gmbh Vertebrate intestinal protein that absorbs cholesterol and use of this protein to identify inhibitors of intestinal cholesterol transport
PE20020507A1 (en) 2000-10-17 2002-06-25 Schering Corp NON-IMIDAZOLE COMPOUNDS AS ANTAGONISTS OF THE HISTAMINE H3 RECEPTOR
US6982251B2 (en) * 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
IL156552A0 (en) * 2000-12-21 2004-01-04 Aventis Pharma Gmbh Diphenyl azetidinone derivatives, method for the production thereof, medicaments containing these compounds, and their use
EP1345924B1 (en) * 2000-12-21 2006-08-30 Sanofi-Aventis Deutschland GmbH Diphenyl azetidinone derivatives, method for the production thereof, medicaments containing these compounds, and their use
WO2002050027A1 (en) * 2000-12-21 2002-06-27 Aventis Pharma Deutschland Gmbh Novel 1,2-diphenzylazetidinones, method for producing the same, medicaments containing said compounds, and the use thereof for treating disorders of the lipid metabolism
TWI291957B (en) 2001-02-23 2008-01-01 Kotobuki Pharmaceutical Co Ltd Beta-lactam compounds, process for repoducing the same and serum cholesterol-lowering agents containing the same
MXPA03008356A (en) * 2001-03-13 2003-12-11 Schering Corp Novel non-imidazole compounds.
ATE305459T1 (en) * 2001-03-28 2005-10-15 Schering Corp METHOD FOR THE ENANTIOSELECTIVE SYNTHESIS OF AZETIDINONE INTERMEDIATE PRODUCTS
US20030137689A1 (en) * 2002-01-18 2003-07-24 General Instrument Corporation. Remote printer driver server
US7105505B2 (en) * 2002-04-18 2006-09-12 Schering Corporation Benzimidazole derivatives useful as histamine H3 antagonists
MY132566A (en) * 2002-04-18 2007-10-31 Schering Corp Benzimidazolone histamine h3 antagonists
EP1499316B1 (en) 2002-04-18 2008-03-19 Schering Corporation (1-4-piperidinyl)benzimidazole derivatives useful as histamine h3 antagonists
DE10227508A1 (en) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Acid group-substituted diphenylazetidinones, processes for their preparation, pharmaceutical compositions containing them and their use
DE10227507A1 (en) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Cationically substituted diphenylazetidinones, processes for their preparation, medicaments containing these compounds and their use
DE10227506A1 (en) 2002-06-19 2004-01-08 Aventis Pharma Deutschland Gmbh Ring-substituted diphenylazetidinones, processes for their preparation, pharmaceutical compositions containing them and their use
MXPA05000193A (en) 2002-06-24 2005-04-08 Schering Corp Indole derivatives useful as histamine h3 antagonists.
GB0215579D0 (en) 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
WO2004014947A1 (en) 2002-08-06 2004-02-19 Aventis Pharma Deutschland Gmbh Method for isolating an intestinal cholesterol binding protein
US20040198743A1 (en) * 2003-01-31 2004-10-07 Schering Corporation Methods for treating allergic skin and allergic ocular conditions using combinations of histamine receptor antagonists
ATE418551T1 (en) * 2003-03-07 2009-01-15 Schering Corp SUBSTITUTED AZETIDINONE DERIVATIVES, THEIR PHARMACEUTICAL FORMULATIONS AND THEIR USE IN THE TREATMENT OF HYPERCHOLESTEROLEMIA
US7235543B2 (en) * 2003-03-07 2007-06-26 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
CA2517573C (en) * 2003-03-07 2011-12-06 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
DE10314610A1 (en) 2003-04-01 2004-11-04 Aventis Pharma Deutschland Gmbh New diphenylazetidinone with improved physiological properties, process for its preparation, medicaments containing these compounds and its use
GB0308333D0 (en) 2003-04-10 2003-05-14 Glaxo Group Ltd Novel compounds
RU2005136368A (en) 2003-04-23 2006-06-10 Глэксо Груп Лимитед (GB) PIPERASIN DERIVATIVES AND THEIR APPLICATION FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISEASES
US20040224952A1 (en) * 2003-05-07 2004-11-11 Cowart Marlon D. Fused bicyclic-substituted amines as histamine-3 receptor ligands
JP2005015434A (en) 2003-06-27 2005-01-20 Kotobuki Seiyaku Kk Serum cholesterol-lowering agent or prophylactic or therapeutic agent for atherosclerosis
GB0315360D0 (en) 2003-07-01 2003-08-06 Burns Robert N Anti-theft device
AU2003259547A1 (en) 2003-07-31 2005-02-14 Hetero Drugs Limited Ezetimibe polymorphs
EP1660456A2 (en) 2003-08-25 2006-05-31 Microbia Inc. Quaternary salt derivatives of 1,4-diphenylazetidin-2-ones
EP1660446A2 (en) 2003-08-28 2006-05-31 Microbia, Inc. Tethered dimers and trimers of 1,4-diphenylazetidn-2-ones
GB0321228D0 (en) 2003-09-10 2003-10-08 Inpharmatica Ltd Modulating cell activity
JP2007524651A (en) 2003-09-26 2007-08-30 フォーブス メディ−テック インコーポレーテッド A method of suppressing the expression of a multi-drug resistance gene to suppress the production of a protein caused by the expression of the gene, thereby increasing the effectiveness of a chemotherapeutic agent for cancer treatment.
EP1522541A1 (en) 2003-10-07 2005-04-13 Lipideon Biotechnology AG Novel hypocholesterolemic compounds
EP1682117A1 (en) 2003-10-30 2006-07-26 Merck & Co., Inc. 2-azetidinones as anti-hypercholesterolemic agents
WO2005042692A2 (en) 2003-10-31 2005-05-12 Forbes Medi-Tech Inc. A method of inhibiting the expression of genes which mediate cellular cholesterol influx in animal cells and inhibiting the production of proteins resulting from the expression of such genes using cholesterol absorption inhibitors
JP4839221B2 (en) 2003-11-07 2011-12-21 ジェイ ジェイ ファーマ,インコーポレイテッド Combination therapy combination to increase HDL
CA2545058A1 (en) 2003-11-10 2005-05-26 Microbia, Inc. 4-biarylyl-1-phenylazetidin-2-ones
SA04250427A (en) 2003-12-23 2005-12-03 استرازينيكا ايه بي Diphenylazetidone derivates
GB0329778D0 (en) 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
CN100471835C (en) 2003-12-23 2009-03-25 默克公司 Anti-hypercholesterolemic compounds

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