RU2146256C1 - ПРОИЗВОДНЫЕ АЗОЛА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ С АКТИВНОСТЬЮ В ОТНОШЕНИИ СЕРОТОНИНОВОГО (5-HT1Dα)РЕЦЕПТОРА - Google Patents

ПРОИЗВОДНЫЕ АЗОЛА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ С АКТИВНОСТЬЮ В ОТНОШЕНИИ СЕРОТОНИНОВОГО (5-HT1Dα)РЕЦЕПТОРА Download PDF

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RU2146256C1
RU2146256C1 RU95115522A RU95115522A RU2146256C1 RU 2146256 C1 RU2146256 C1 RU 2146256C1 RU 95115522 A RU95115522 A RU 95115522A RU 95115522 A RU95115522 A RU 95115522A RU 2146256 C1 RU2146256 C1 RU 2146256C1
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Prior art keywords
alkyl
mmol
mixture
tetrahydro
pyrido
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RU95115522A
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English (en)
Russian (ru)
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RU95115522A (ru
Inventor
Джилмор Джереми
Таддеуш Галлагер Питер
Виктор Майлз Мартин
Мартин Оутон Вилльям
Вилльям Смит Колин
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Лилли Индастриз Лимитед
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Priority claimed from GB9418326A external-priority patent/GB9418326D0/en
Priority claimed from GBGB9511166.2A external-priority patent/GB9511166D0/en
Application filed by Лилли Индастриз Лимитед filed Critical Лилли Индастриз Лимитед
Publication of RU95115522A publication Critical patent/RU95115522A/ru
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, e.g. nicotine, cocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Otolaryngology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Optical Integrated Circuits (AREA)
  • Holo Graphy (AREA)
  • Gyroscopes (AREA)
RU95115522A 1994-09-12 1995-09-11 ПРОИЗВОДНЫЕ АЗОЛА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ С АКТИВНОСТЬЮ В ОТНОШЕНИИ СЕРОТОНИНОВОГО (5-HT1Dα)РЕЦЕПТОРА RU2146256C1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB9418326.6 1994-09-12
GB9418326A GB9418326D0 (en) 1994-09-12 1994-09-12 Pharmaceutical compounds
GBGB9511166.2A GB9511166D0 (en) 1995-06-02 1995-06-02 Pharmaceutical compounds
GB9511166.2 1995-06-02

Publications (2)

Publication Number Publication Date
RU95115522A RU95115522A (ru) 1997-08-27
RU2146256C1 true RU2146256C1 (ru) 2000-03-10

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RU95115522A RU2146256C1 (ru) 1994-09-12 1995-09-11 ПРОИЗВОДНЫЕ АЗОЛА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ С АКТИВНОСТЬЮ В ОТНОШЕНИИ СЕРОТОНИНОВОГО (5-HT1Dα)РЕЦЕПТОРА

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EP (1) EP0705832B1 (OSRAM)
JP (1) JPH0881464A (OSRAM)
KR (1) KR960010635A (OSRAM)
CN (1) CN1045602C (OSRAM)
AT (1) ATE247114T1 (OSRAM)
AU (1) AU698580B2 (OSRAM)
CA (1) CA2157998A1 (OSRAM)
CZ (1) CZ286565B6 (OSRAM)
DE (1) DE69531476T2 (OSRAM)
ES (1) ES2204932T3 (OSRAM)
FI (1) FI954243A7 (OSRAM)
HU (1) HU219491B (OSRAM)
IL (1) IL115236A (OSRAM)
IN (1) IN179550B (OSRAM)
MY (1) MY132009A (OSRAM)
NO (1) NO305174B1 (OSRAM)
NZ (1) NZ272961A (OSRAM)
PE (1) PE41796A1 (OSRAM)
PH (1) PH31631A (OSRAM)
PL (1) PL310373A1 (OSRAM)
RU (1) RU2146256C1 (OSRAM)
TR (1) TR199501114A2 (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2232578C1 (ru) * 2003-04-10 2004-07-20 Ахапкина Валентина Ивановна Вещество, обладающее антидепрессивной активностью
RU2745742C1 (ru) * 2015-10-01 2021-03-31 Олема Фармасьютикалз, Инк. ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА

Families Citing this family (22)

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GB2308362A (en) * 1995-12-19 1997-06-25 Lilly Industries Ltd Pharmaceutical indole derivatives
EP0905136A1 (en) * 1997-09-08 1999-03-31 Janssen Pharmaceutica N.V. Tetrahydro gamma-carbolines
UA70334C2 (en) * 1998-10-06 2004-10-15 Janssen Pharmaceutica N V Jans BENZOTHIENO[3,2-c]PYRIDINES AS a2 ANTAGONISTS BENZOTHIENO[3,2-c]PYRIDINES AS a2 ANTAGONISTS
UA74826C2 (en) * 2000-05-17 2006-02-15 Ortho Mcneil Pharm Inc ?-carboline derivatives as phosphodiesterase inhibitors
CA2415815A1 (en) * 2000-07-06 2002-01-17 Nigel H. Greig Tetrahydrobenzothiazole analogues as neuroprotective agents
DE10040016A1 (de) * 2000-08-16 2002-02-28 Boehringer Ingelheim Pharma Neue beta-Amyloid Inhibitoren, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1322622B1 (en) * 2000-09-19 2012-10-31 Sprout Pharmaceuticals, Inc. New n, n'-disubstituted benzimidazolone derivatives with affinity at the serotonin and dopamine receptors
US6586435B2 (en) 2000-09-19 2003-07-01 Boehringer Ingelheim Pharma Kg Benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors
MXPA03002329A (es) * 2000-09-19 2003-10-15 Boehringer Ingelheim Pharma Nuevos derivados de bencimidazolona que muestran afinidad por los receptores de serotonina y dopamina.
US7183410B2 (en) 2001-08-02 2007-02-27 Bidachem S.P.A. Stable polymorph of flibanserin
MXPA04001203A (es) * 2001-08-08 2004-05-20 Pharmacia & Upjhon Company 1-h-pirido[4,3-b] indoles terapeuticos.
UA78974C2 (en) 2001-10-20 2007-05-10 Boehringer Ingelheim Pharma Use of flibanserin for treating disorders of sexual desire
US10675280B2 (en) 2001-10-20 2020-06-09 Sprout Pharmaceuticals, Inc. Treating sexual desire disorders with flibanserin
EP1912650B8 (en) 2005-08-03 2017-10-18 Sprout Pharmaceuticals, Inc. Use of flibanserin in the treatment of obesity
JP2009513604A (ja) 2005-10-29 2009-04-02 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 月経前障害及び他の女性の性的障害治療用のベンゾイミダゾロン誘導体
ATE456369T1 (de) 2006-06-30 2010-02-15 Boehringer Ingelheim Int Flibanserin zur behandlung von harninkontinenz und assoziierten erkrankungen
MX2009001551A (es) 2006-08-14 2009-02-20 Boehringer Ingelheim Int Formulaciones de flibanserina y metodo para fabricarlas.
CL2007002214A1 (es) 2006-08-14 2008-03-07 Boehringer Ingelheim Int Composicion farmaceutica en la forma de comprimido, donde al menos la longitud del comprimido en el estado anterior de la aplicacion es al menos 7/12 del diametro pilorico del paciente y despues de ingerirlo en estado alimentado, la longitud del comp
CA2661613C (en) 2006-08-25 2016-01-26 Boehringer Ingelheim International Gmbh Controlled release system and method for manufacturing the same
PE20091188A1 (es) 2007-09-12 2009-08-31 Boehringer Ingelheim Int Compuesto 1-[2-(4-(3-trifluorometil-fenil)piperazin-1-il)etil]-2,3-dihidro-1h-benzimidazol-2-ona (flibanserina), sus sales de adicion y composiciones farmaceuticas que los contienen
US8829035B2 (en) 2009-05-29 2014-09-09 Sumitomo Chemical Company, Limited Agent for treatment or prevention of diseases associated with activity of neurotrophic factors
CA3144791A1 (en) 2019-07-07 2021-01-14 Olema Pharmaceuticals, Inc. Regimens of estrogen receptor antagonists

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SU1442074A3 (ru) * 1985-09-16 1988-11-30 Американ Хоум Продактс Корпорейшн (Фирма) Способ получени производных @ -карболина или их фармацевтически приемлемых солей

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US4035369A (en) 1975-10-08 1977-07-12 Janssen Pharmaceutica N.V. 1-Benzazolylalkyl-4-substituted-piperidines
IL69132A (en) * 1982-07-14 1986-02-28 Roussel Uclaf Benzo-and naphtho-thiopyranopyrimidinones,their preparation and pharmaceutical compositions containing them
FR2661177A1 (fr) * 1990-04-23 1991-10-25 Rhone Poulenc Sante Derives du naphtosultame antagonistes de la serotonine, leur preparation et les medicaments les contenant.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1442074A3 (ru) * 1985-09-16 1988-11-30 Американ Хоум Продактс Корпорейшн (Фирма) Способ получени производных @ -карболина или их фармацевтически приемлемых солей

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2232578C1 (ru) * 2003-04-10 2004-07-20 Ахапкина Валентина Ивановна Вещество, обладающее антидепрессивной активностью
RU2745742C1 (ru) * 2015-10-01 2021-03-31 Олема Фармасьютикалз, Инк. ТЕТРАГИДРО-1Н-ПИРИДО[3,4-b]ИНДОЛЬНЫЕ АНТИЭСТРОГЕННЫЕ ЛЕКАРСТВЕННЫЕ СРЕДСТВА
US11229630B2 (en) 2015-10-01 2022-01-25 Olema Pharmaceuticals, Inc. Tetrahydro-1H-pyrido [3,4-b]indole anti-estrogenic drugs
US11672785B2 (en) 2015-10-01 2023-06-13 Olema Pharmaceuticals, Inc. Tetrahydro-1H-pyrido [3,4-b]indole anti-estrogenic drugs

Also Published As

Publication number Publication date
AU698580B2 (en) 1998-11-05
PE41796A1 (es) 1996-10-21
MY132009A (en) 2007-09-28
HU9502631D0 (en) 1995-11-28
DE69531476T2 (de) 2004-06-09
HU219491B (hu) 2001-04-28
IN179550B (OSRAM) 1997-10-18
PL310373A1 (en) 1996-03-18
DE69531476D1 (de) 2003-09-18
ATE247114T1 (de) 2003-08-15
IL115236A (en) 1998-06-15
CZ286565B6 (cs) 2000-05-17
NO953575D0 (no) 1995-09-11
EP0705832A1 (en) 1996-04-10
CZ232295A3 (en) 1996-03-13
NO953575L (no) 1996-03-13
JPH0881464A (ja) 1996-03-26
PH31631A (en) 1999-01-12
CA2157998A1 (en) 1996-03-13
KR960010635A (ko) 1996-04-20
CN1045602C (zh) 1999-10-13
ES2204932T3 (es) 2004-05-01
NZ272961A (en) 1998-02-26
EP0705832B1 (en) 2003-08-13
TR199501114A2 (tr) 1996-10-21
AU3049795A (en) 1996-03-28
FI954243A7 (fi) 1996-03-13
CN1129219A (zh) 1996-08-21
HUT72593A (en) 1996-05-28
IL115236A0 (en) 1995-12-31
FI954243A0 (fi) 1995-09-11
NO305174B1 (no) 1999-04-12

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