CA2101356A1 - Improvements in or relating to benzothiophenes - Google Patents

Improvements in or relating to benzothiophenes

Info

Publication number
CA2101356A1
CA2101356A1 CA2101356A CA2101356A CA2101356A1 CA 2101356 A1 CA2101356 A1 CA 2101356A1 CA 2101356 A CA2101356 A CA 2101356A CA 2101356 A CA2101356 A CA 2101356A CA 2101356 A1 CA2101356 A1 CA 2101356A1
Authority
CA
Canada
Prior art keywords
benzothiophenes
relating
raloxifene
medicament
manufacture
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA2101356A
Other languages
French (fr)
Other versions
CA2101356C (en
Inventor
Larry John Black
George Joseph Cullinan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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=25444642&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2101356(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CA2101356A1 publication Critical patent/CA2101356A1/en
Application granted granted Critical
Publication of CA2101356C publication Critical patent/CA2101356C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The use of raloxifene, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for preventing or treating osteoporosis in a postmenopausal woman.
CA002101356A 1992-07-28 1993-07-27 Improvements in or relating to benzothiophenes Expired - Lifetime CA2101356C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US92093392A 1992-07-28 1992-07-28
US07/920,933 1992-07-28

Publications (2)

Publication Number Publication Date
CA2101356A1 true CA2101356A1 (en) 1994-01-29
CA2101356C CA2101356C (en) 1998-11-17

Family

ID=25444642

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002101356A Expired - Lifetime CA2101356C (en) 1992-07-28 1993-07-27 Improvements in or relating to benzothiophenes

Country Status (35)

Country Link
US (4) US5393763A (en)
EP (4) EP0781555A1 (en)
JP (2) JP2749247B2 (en)
KR (1) KR0161300B1 (en)
CN (1) CN1054742C (en)
AT (2) ATE152351T1 (en)
AU (1) AU658075B2 (en)
BG (1) BG61429B1 (en)
BR (1) BR9303013A (en)
CA (1) CA2101356C (en)
CY (2) CY2044B1 (en)
CZ (1) CZ281913B6 (en)
DE (3) DE19975012I2 (en)
DK (2) DK0584952T3 (en)
ES (2) ES2283939T3 (en)
GR (1) GR3024171T3 (en)
HK (1) HK90197A (en)
HU (1) HU219233B (en)
IL (1) IL106450A (en)
LU (1) LU90334I2 (en)
MX (1) MX9304432A (en)
MY (1) MY111188A (en)
NL (1) NL980044I2 (en)
NO (2) NO303863B1 (en)
NZ (3) NZ314686A (en)
PH (1) PH30032A (en)
PL (1) PL177348B1 (en)
PT (1) PT1438957E (en)
RO (1) RO113212B1 (en)
RU (1) RU2104697C1 (en)
SA (1) SA93140340B1 (en)
SG (1) SG45315A1 (en)
TW (1) TW366342B (en)
UA (1) UA26213C2 (en)
ZA (1) ZA935283B (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0670162A1 (en) * 1994-03-02 1995-09-06 Eli Lilly And Company Pharmaceutical formulations containing raloxifere, a surfactant and a watersoluble diluent
US5811120A (en) * 1994-03-02 1998-09-22 Eli Lilly And Company Solid orally administerable raloxifene hydrochloride pharmaceutical formulation
US5972383A (en) * 1994-03-02 1999-10-26 Eli Lilly And Company Solid orally administerable raloxifene hydrochloride pharmaceutical formulation
USRE39050E1 (en) 1994-03-02 2006-03-28 Eli Lilly And Company Methods of use for inhibiting bone loss and lowering serum cholesterol

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US6515009B1 (en) * 1991-09-27 2003-02-04 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5811447A (en) 1993-01-28 1998-09-22 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
USRE38968E1 (en) 1992-07-28 2006-02-07 Eli Lilly And Company Methods for inhibiting bone loss using 6-hydroxy-2-(4-hydroxyphenyl)-benzo[b]thien-3-yl-4-[2-(piperidin-1-yl) ethoxyphenylimethanone hydrochloride
TW366342B (en) * 1992-07-28 1999-08-11 Lilly Co Eli The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
USRE39049E1 (en) 1992-07-28 2006-03-28 Eli Lilly And Company Methods for inhibiting bone loss
US6395494B1 (en) * 1993-05-13 2002-05-28 Neorx Corporation Method to determine TGF-β
US6251920B1 (en) 1993-05-13 2001-06-26 Neorx Corporation Prevention and treatment of cardiovascular pathologies
US6306421B1 (en) 1992-09-25 2001-10-23 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5770609A (en) 1993-01-28 1998-06-23 Neorx Corporation Prevention and treatment of cardiovascular pathologies
TW383306B (en) * 1992-12-22 2000-03-01 Lilly Co Eli New use of 2-phenyl-3-aroylbenzothiophenes in lowering serum cholesterol
US5595722A (en) * 1993-01-28 1997-01-21 Neorx Corporation Method for identifying an agent which increases TGF-beta levels
US5981568A (en) 1993-01-28 1999-11-09 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US6491938B2 (en) 1993-05-13 2002-12-10 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US6663881B2 (en) 1993-01-28 2003-12-16 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
US5482949A (en) * 1993-03-19 1996-01-09 Eli Lilly And Company Sulfonate derivatives of 3-aroylbenzo[b]thiophenes
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US6417198B1 (en) * 1993-12-21 2002-07-09 Eli Lilly And Company Methods of inhibiting CNS problems in post-menopausal women
US5441966A (en) * 1993-12-21 1995-08-15 Eli Lilly And Company Methods of inhibiting Turner's syndrome
US5591753A (en) * 1994-01-28 1997-01-07 Eli Lilly And Company Combination treatment for osteoporosis
US6723739B1 (en) 1994-05-20 2004-04-20 Eli Lilly And Company Glucopyranoside benzothiophenes
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US5512296A (en) * 1994-08-22 1996-04-30 Eli Lilly And Company Methods for inhibiting neuronal damage
US5550123A (en) * 1994-08-22 1996-08-27 Eli Lilly And Company Methods for inhibiting bone prosthesis degeneration
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US5554628A (en) * 1994-09-20 1996-09-10 Eli Lilly And Company Method for minimizing the uterothrophic effect of tamoxifen and tamoxifen analogs
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
US5589482A (en) * 1994-12-14 1996-12-31 Pfizer Inc. Benzo-thiophene estrogen agonists to treat prostatic hyperplasia
US5494929A (en) * 1995-01-12 1996-02-27 Eli Lilly And Company Methods of inhibiting growth hormone effects
US5489587A (en) * 1995-01-20 1996-02-06 Eli Lilly And Company Benzofurans used to inhibit bone loss
US5512583A (en) * 1995-01-30 1996-04-30 Eli Lilly And Company Methods of decreasing serum calcium levels
US5571808A (en) * 1995-01-31 1996-11-05 Eli Lilly And Company Method for treating smoking-related bone loss
EP0724879A2 (en) * 1995-02-06 1996-08-07 Eli Lilly And Company 2-Phenyl-3-azoylbenzothiopenes for inhibiting effects of IL-6
US20030083733A1 (en) * 1997-10-10 2003-05-01 Neorx Corporation Therapeutic inhibitor of vascular smooth muscle cells
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US5843974A (en) * 1995-06-06 1998-12-01 Eli Lilly And Company Methods of inhibiting melanoma using Benzothiophenes as cytotoxic agents per se
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