EA200301120A1 - Цитрат 5,8,14-триазатетрацикло (10.3.1.0.0)-гексадека-2 (11),3,5,7,9-пентаена - Google Patents

Цитрат 5,8,14-триазатетрацикло (10.3.1.0.0)-гексадека-2 (11),3,5,7,9-пентаена

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Publication number
EA200301120A1
EA200301120A1 EA200301120A EA200301120A EA200301120A1 EA 200301120 A1 EA200301120 A1 EA 200301120A1 EA 200301120 A EA200301120 A EA 200301120A EA 200301120 A EA200301120 A EA 200301120A EA 200301120 A1 EA200301120 A1 EA 200301120A1
Authority
EA
Eurasian Patent Office
Prior art keywords
citrate
triazatetracyclo
hexadeca
relates
pentaena
Prior art date
Application number
EA200301120A
Other languages
English (en)
Other versions
EA005529B1 (ru
Inventor
Филип Джеймс Джонсон
Питер Роберт Роуз
Льюин Теофилус Уинт
Гленн Роберт Уилльямс
Original Assignee
Пфайзер Продактс Инк.
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=23117854&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200301120(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200301120A1 publication Critical patent/EA200301120A1/ru
Publication of EA005529B1 publication Critical patent/EA005529B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Toxicology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

Данное изобретение относится к цитрату 5,8,14-триазатетрацикло-[10.3.1.0.0]гексадека-2(11),3,5,7,9-пентаена (формула 1) и его фармацевтическим композициям. Данное изобретение также относится к различным формам цитрата, особенно, его гидрату и его безводному/практически безводному полиморфу. Данное изобретение также относится к способу получения указанных форм цитрата.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200301120A 2001-05-14 2002-04-26 Цитрат 5,8,14-триазатетрацикло-(10.3.1.0.0)-гексадека-2(11),3,5,7,9-пентаена EA005529B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29086301P 2001-05-14 2001-05-14
PCT/IB2002/001450 WO2002092597A1 (en) 2001-05-14 2002-04-26 The citrate salt of 5, 8, 14-triazatetracyclo(10.3.1.0?2,11.04.9¿)-hexadeca-2.(11),3,5,7,9-pentaene and pharmaceutical compositions thereof

Publications (2)

Publication Number Publication Date
EA200301120A1 true EA200301120A1 (ru) 2004-02-26
EA005529B1 EA005529B1 (ru) 2005-04-28

Family

ID=23117854

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200301120A EA005529B1 (ru) 2001-05-14 2002-04-26 Цитрат 5,8,14-триазатетрацикло-(10.3.1.0.0)-гексадека-2(11),3,5,7,9-пентаена

Country Status (37)

Country Link
US (1) US6787549B2 (ru)
EP (1) EP1390366B1 (ru)
JP (1) JP4137645B2 (ru)
KR (1) KR20040008175A (ru)
CN (1) CN1509288A (ru)
AP (1) AP1429A (ru)
AR (1) AR035889A1 (ru)
AT (1) ATE303386T1 (ru)
BG (1) BG108344A (ru)
CA (1) CA2446988A1 (ru)
CZ (1) CZ20032917A3 (ru)
DE (1) DE60205888T2 (ru)
DO (1) DOP2002000390A (ru)
DZ (1) DZ3503A1 (ru)
EA (1) EA005529B1 (ru)
EE (1) EE200300557A (ru)
ES (1) ES2245731T3 (ru)
GT (1) GT200200081A (ru)
HR (1) HRP20030911A2 (ru)
HU (1) HUP0304085A3 (ru)
IL (1) IL157874A0 (ru)
IS (1) IS6956A (ru)
MA (1) MA27021A1 (ru)
MX (1) MXPA03010365A (ru)
MY (1) MY134123A (ru)
NO (1) NO20035035L (ru)
NZ (1) NZ528209A (ru)
OA (1) OA12600A (ru)
PA (1) PA8545001A1 (ru)
PE (1) PE20021095A1 (ru)
PL (1) PL366774A1 (ru)
SK (1) SK13372003A3 (ru)
TN (1) TNSN03112A1 (ru)
UA (1) UA73421C2 (ru)
UY (1) UY27287A1 (ru)
WO (1) WO2002092597A1 (ru)
ZA (1) ZA200307234B (ru)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1324013C (zh) * 1997-12-31 2007-07-04 辉瑞产品公司 芳基稠合氮杂多环化合物
KR100892517B1 (ko) * 2001-11-30 2009-04-10 화이자 프로덕츠 인크. 5,8,14-트리아자테트라시클로[10.3.1.0(2,11).0(4,9)]-헥사데카-2(11)3,5,7,9-펜타엔의 약학 조성물
JP2006528237A (ja) * 2003-05-20 2006-12-14 ファイザー・プロダクツ・インク バレニクリンの医薬組成物
US20050043407A1 (en) * 2003-08-22 2005-02-24 Pfizer Inc Pharmaceutical composition for the prevention and treatment of addiction in a mammal
WO2008060487A2 (en) * 2006-11-09 2008-05-22 Pfizer Products Inc. Polymorphs of nicotinic intermediates
WO2009109651A1 (en) * 2008-03-06 2009-09-11 Medichem, S.A. SALTS OF A PYRAZINO[2,3-h][3]BENZAZEPINE DERIVATIVE
CA2709774C (en) 2008-05-22 2012-10-02 Teva Pharmaceutical Industries Ltd. Varenicline tosylate, an intermediate in the preparation process of varenicline l-tartrate
US20090318460A1 (en) * 2008-05-26 2009-12-24 Glenmark Amorphous varenicline tartrate and process for the preparation thereof
US20090318695A1 (en) * 2008-06-19 2009-12-24 Vinod Kumar Kansal Processes for the preparation of varenicline and intermediates thereof
WO2010005643A1 (en) * 2008-07-10 2010-01-14 Teva Pharmaceutical Industries Ltd. Processes for purifying varenicline l-tartrate salt and preparing crystalline forms of varenicline l-tartrate salt
MX2011006206A (es) * 2008-12-11 2011-07-20 S Bio Pte Ltd Sal de citrato de 11-(2-pirrolidin-1-il-etoxi)-14,19-dioxa-5,7,26- triaza-tetraciclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5 ,8,10,12(27),16,21,23-decaeno.
US20100189790A1 (en) 2009-01-23 2010-07-29 Teva Pharmaceutical Industries, Ltd. Delayed release rasagiline formulation
WO2010143070A2 (en) 2009-06-10 2010-12-16 Actavis Group Ptc Ehf Amorphous varenicline tartrate co-precipitates
WO2010151524A1 (en) 2009-06-22 2010-12-29 Teva Pharmaceutical Industries Ltd Solid states forms of varenicline salts and processes for preparation thereof
WO2011140431A1 (en) 2010-05-06 2011-11-10 Teva Pharmaceutical Industries Ltd. Varenicline salts and crystal forms thereof
US9090623B2 (en) 2012-04-13 2015-07-28 Lianyungang Jinkang Hexin Pharmaceutical Co., Ltd. Compound JK12A and preparation thereof
WO2018154395A2 (en) 2018-06-11 2018-08-30 Alvogen Malta Operations (Row) Ltd Controlled release pharmaceutical composition of varenicline
EP3756653A1 (en) 2019-06-28 2020-12-30 Alfred E. Tiefenbacher (GmbH & Co. KG) Microparticulate varenicline citrate

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1324013C (zh) * 1997-12-31 2007-07-04 辉瑞产品公司 芳基稠合氮杂多环化合物
IL137937A0 (en) * 1999-08-27 2001-10-31 Pfizer Prod Inc A pharmaceutical composition for the prevention and treatment of nicotine addiction in a mammal

Also Published As

Publication number Publication date
US20030149091A1 (en) 2003-08-07
HRP20030911A2 (en) 2004-02-29
OA12600A (en) 2006-06-09
CN1509288A (zh) 2004-06-30
NO20035035D0 (no) 2003-11-13
AR035889A1 (es) 2004-07-21
UA73421C2 (en) 2005-07-15
ATE303386T1 (de) 2005-09-15
CA2446988A1 (en) 2002-11-21
EP1390366A1 (en) 2004-02-25
SK13372003A3 (sk) 2004-08-03
DOP2002000390A (es) 2003-03-15
ZA200307234B (en) 2004-09-16
IS6956A (is) 2003-09-15
JP4137645B2 (ja) 2008-08-20
MXPA03010365A (es) 2004-03-16
ES2245731T3 (es) 2006-01-16
CZ20032917A3 (cs) 2004-07-14
PL366774A1 (en) 2005-02-07
NZ528209A (en) 2004-09-24
PE20021095A1 (es) 2002-12-14
WO2002092597A1 (en) 2002-11-21
EA005529B1 (ru) 2005-04-28
UY27287A1 (es) 2003-02-28
IL157874A0 (en) 2004-03-28
US6787549B2 (en) 2004-09-07
DZ3503A1 (ru) 2002-11-21
EP1390366B1 (en) 2005-08-31
HUP0304085A2 (en) 2004-04-28
MY134123A (en) 2007-11-30
TNSN03112A1 (fr) 2005-12-23
KR20040008175A (ko) 2004-01-28
BG108344A (bg) 2004-12-30
PA8545001A1 (es) 2003-09-05
MA27021A1 (fr) 2004-12-20
DE60205888D1 (de) 2005-10-06
GT200200081A (es) 2003-04-22
NO20035035L (no) 2003-11-13
DE60205888T2 (de) 2006-07-06
JP2004529186A (ja) 2004-09-24
HUP0304085A3 (en) 2005-09-28
AP1429A (en) 2005-06-13
EE200300557A (et) 2004-04-15
AP2002002522A0 (en) 2002-06-30

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