KR100823889B1 - 치환된 피페라진 및 피페리딘 칼슘 채널 차단제 및 이를 포함하는 약제학적 조성물 - Google Patents

치환된 피페라진 및 피페리딘 칼슘 채널 차단제 및 이를 포함하는 약제학적 조성물 Download PDF

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KR100823889B1
KR100823889B1 KR1020027007951A KR20027007951A KR100823889B1 KR 100823889 B1 KR100823889 B1 KR 100823889B1 KR 1020027007951 A KR1020027007951 A KR 1020027007951A KR 20027007951 A KR20027007951 A KR 20027007951A KR 100823889 B1 KR100823889 B1 KR 100823889B1
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테란스 피. 스너치
제랄드 더블유. 잼포니
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뉴로메드 파머큐티칼즈 리미티드
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    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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KR1020027007951A 1999-12-20 2000-12-20 치환된 피페라진 및 피페리딘 칼슘 채널 차단제 및 이를 포함하는 약제학적 조성물 Expired - Fee Related KR100823889B1 (ko)

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Application Number Priority Date Filing Date Title
US17283199P 1999-12-20 1999-12-20
US60/172,831 1999-12-20
US09/476,927 US6387897B1 (en) 1998-06-30 1999-12-30 Preferentially substituted calcium channel blockers
US09/476,927 1999-12-30

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KR20020075874A KR20020075874A (ko) 2002-10-07
KR100823889B1 true KR100823889B1 (ko) 2008-04-22

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Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040259866A1 (en) * 1998-06-30 2004-12-23 Snutch Terrance P. Calcium channel blockers comprising two benzhydril moieties
US6943168B2 (en) * 1998-06-30 2005-09-13 Neuromed Technologies Inc. Calcium channel inhibitors comprising benzhydril spaced from piperazine
US20060084660A1 (en) * 1998-06-30 2006-04-20 Neuromed Technologies Inc. Calcium channel blockers comprising two benzhydril moieties
WO2004089922A2 (en) * 1998-06-30 2004-10-21 Neuromed Technologies, Inc. Calcium channel inhibitors comprising benzhydril spaced from piperazine
US20040266784A1 (en) * 1998-06-30 2004-12-30 Snutch Terrance P. Calcium channel inhibitors comprising benzhydril spaced from piperazine
US6387897B1 (en) * 1998-06-30 2002-05-14 Neuromed Technologies, Inc. Preferentially substituted calcium channel blockers
US6951862B2 (en) * 1998-06-30 2005-10-04 Neuromed Technologies, Inc. Calcium channel blockers comprising two benzhydril moieties
US7186726B2 (en) * 1998-06-30 2007-03-06 Neuromed Pharmaceuticals Ltd. Preferentially substituted calcium channel blockers
US7151102B2 (en) * 2000-10-30 2006-12-19 Kudos Pharmaceuticals Limited Phthalazinone derivatives
WO2003066040A1 (en) 2002-02-05 2003-08-14 Ajinomoto Co.,Inc. Medicinal compositions containing gabapentin or pregabalin and n-type calcium channel antagonist
US20030199523A1 (en) * 2002-02-28 2003-10-23 Snutch Terrance P. Heterocyclic calcium in channel blockers
US20040204404A1 (en) * 2002-09-30 2004-10-14 Robert Zelle Human N-type calcium channel blockers
JP2006522742A (ja) * 2003-04-08 2006-10-05 ニューロームド テクノロジーズ、インク． ピペラジンから距離をおいて配置したベンズヒドリル基から成る一群のカルシウムチャンネル阻害剤
WO2004093813A2 (en) * 2003-04-22 2004-11-04 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a calcium modulating agent for the treatment of pain, inflammation or inflammation mediated disorders
WO2004093816A2 (en) * 2003-04-22 2004-11-04 Pharmacia Corporation Compositions comprising a selective cox-2 inhibitor and a calcium modulating agent
EP1633343A1 (en) * 2003-05-30 2006-03-15 Neuromed Technologies, Inc. 3-aminomethyl-pyrrolidines as n-type calcium channel blockers
WO2005015159A2 (en) * 2003-08-08 2005-02-17 The Regents Of The University Of California. Methods for modulating a drug-related effect or behavior
US7524846B2 (en) 2003-10-14 2009-04-28 Wyeth Arylalkyl- and cycloalkylalkyl-piperazine derivatives and methods of their use
US7507760B2 (en) * 2004-01-22 2009-03-24 Neuromed Pharmaceuticals Ltd. N-type calcium channel blockers
AU2005231872A1 (en) * 2004-04-09 2005-10-20 Neuromed Pharmaceuticals Ltd. Diarylamine derivatives as calcium channel blockers
US20050227999A1 (en) * 2004-04-09 2005-10-13 Neuromed Technologies Inc. Diarylamine derivatives as calcium channel blockers
GB0419072D0 (en) * 2004-08-26 2004-09-29 Kudos Pharm Ltd Phthalazinone derivatives
KR20070063526A (ko) 2004-08-30 2007-06-19 뉴로메드 파머큐티칼즈 리미티드 칼슘 채널 차단제인 우레아 유도체
TW200630337A (en) 2004-10-14 2006-09-01 Euro Celtique Sa Piperidinyl compounds and the use thereof
US7511077B2 (en) 2005-02-09 2009-03-31 Neuromed Pharmaceuticals Ltd. Diamine calcium channel blockers
JP2008534630A (ja) * 2005-04-08 2008-08-28 ニューロメッド ファーマシューティカルズ リミテッド 疼痛の軽減のためのｎ型カルシウムチャネルブロッカーを含む組み合わせ治療の方法
WO2007018459A1 (en) * 2005-08-08 2007-02-15 Astrazeneca Ab Therapeutic agents
US8022177B2 (en) * 2005-09-30 2011-09-20 The Board Of Trustees Of The University Of Illinois Peptides and calcium regulation in mammalian cells
US8299211B2 (en) * 2005-09-30 2012-10-30 The Board Of Trustees Of The University Of Illinois Peptides and regulation of calcium channels
WO2007110449A1 (en) * 2006-03-29 2007-10-04 Euro-Celtique S.A. Benzenesulfonamide compounds and their use
US8791264B2 (en) * 2006-04-13 2014-07-29 Purdue Pharma L.P. Benzenesulfonamide compounds and their use as blockers of calcium channels
TW200812963A (en) * 2006-04-13 2008-03-16 Euro Celtique Sa Benzenesulfonamide compounds and the use thereof
CA2651811A1 (en) * 2006-05-11 2007-11-22 Neuromed Pharmaceuticals Ltd. Method for increasing the bioavailability of benzhydryl piperazine containing compounds
WO2008031227A1 (en) * 2006-09-14 2008-03-20 Neuromed Pharmaceuticals Ltd. Diaryl piperidine compounds as calcium channel blockers
US20100105682A1 (en) * 2006-10-13 2010-04-29 Hassan Pajouhesh Cyclopropyl-piperazine compounds as calcium channel blockers
TWI404716B (zh) * 2006-10-17 2013-08-11 Kudos Pharm Ltd 酞嗪酮（ｐｈｔｈａｌａｚｉｎｏｎｅ）衍生物
WO2008124118A1 (en) * 2007-04-09 2008-10-16 Purdue Pharma L.P. Benzenesulfonyl compounds and the use therof
US8765736B2 (en) * 2007-09-28 2014-07-01 Purdue Pharma L.P. Benzenesulfonamide compounds and the use thereof
ES2428326T3 (es) * 2007-10-04 2013-11-07 Merck Sharp & Dohme Corp. Derivados de aril sulfona sustituida como bloqueadores de canales de calcio
KR101598231B1 (ko) * 2007-10-17 2016-02-26 쿠도스 파마슈티칼스 리미티드 4-[3-(4-시클로프로판카르보닐-피페라진-1-카르보닐)-4-플루오로-벤질]-2ｈ-프탈라진-1-온
WO2009132454A1 (en) * 2008-04-28 2009-11-05 Neuromed Pharmaceuticals Ltd. Di-t-butylphenyl piperazines as calcium channel blockers
EP2344450A1 (en) * 2008-09-29 2011-07-20 Merck Sharp & Dohme Corp. Substituted aryl sulfone derivatives as calcium channel blockers
CA2737400C (en) * 2008-10-07 2016-11-22 Astrazeneca Uk Limited Pharmaceutical formulation 514
EP2352501B1 (en) * 2008-11-03 2014-01-01 ChemoCentryx, Inc. Compounds for use in the treatment of osteoporosis
WO2011026240A1 (en) 2009-09-04 2011-03-10 Zalicus Pharmaceuticals Ltd. Oxopiperazine derivatives for the treatment of pain and epilepsy
AU2011305610A1 (en) 2010-09-20 2013-03-14 Kareus Therapeutics, Sa Methods and compositions for treatment of diabetes and dyslipidemia
US8409560B2 (en) 2011-03-08 2013-04-02 Zalicus Pharmaceuticals Ltd. Solid dispersion formulations and methods of use thereof
US8591944B2 (en) 2011-03-08 2013-11-26 Zalicus Pharmaceuticals Ltd. Solid dispersion formulations and methods of use thereof
EP2961403A4 (en) 2013-03-01 2016-11-30 Zalicus Pharmaceuticals Ltd HETEROCYCLIC INHIBITORS OF SODIUM CHANNEL
US10168144B2 (en) 2016-03-25 2019-01-01 Sony Corporation Optical apparatus for 3D data collection

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000018402A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Method for treating androgen-related conditions
WO2000037059A2 (en) * 1998-12-18 2000-06-29 Neuromed Technologies, Inc. Compositions and methods to inactivate n-type calcium channels

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1051527A (enExample) 1964-07-31
US3997539A (en) 1974-05-31 1976-12-14 American Hoechst Corporation 3-(4-Acylaminopiperazin-1-yl alkyl)indoles, precursors and processes for the preparation thereof
US4188485A (en) 1978-06-16 1980-02-12 G. D. Searle & Co. 1-[(10,11-Dihydro-5H-dibenzo[a,d]-cyclohepten-5-yl)methyl]-4-substituted piperidines and related compounds
JPS61155358A (ja) 1984-12-21 1986-07-15 Suntory Ltd ジアリール酪酸誘導体
FR2584723B1 (fr) 1985-07-09 1988-02-12 Adir Nouveaux derives du dihydro-2,3 benzofuranne, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent
DE3600390A1 (de) 1986-01-09 1987-07-16 Hoechst Ag Diarylalkyl-substituierte alkylamine, verfahren zu ihrer herstellung, ihre verwendung sowie sie enthaltende arzneimittel
US5386025A (en) 1990-02-20 1995-01-31 The Salk Institute Biotechnology/Industrial Associates Calcium channel compositions and methods
IE73232B1 (en) 1990-05-25 1997-05-21 Akzo Nv Isochromane derivatives
US5703071A (en) 1990-08-29 1997-12-30 Pharmacia & Upjohn Company Tropolone derivatives and pharmaceutical composition thereof for preventing and treating ischemic diseases
DE4111861A1 (de) 1991-04-11 1992-10-15 Schwabe Willmar Gmbh & Co Benzopyranone, verfahren zu ihrer herstellung und verwendung
KR950704284A (ko) 1992-12-22 1995-11-17 데이비드 로버츠 칼슘 채널 길항제로서의 피페리딘 유도체(Piperidine Derivatives as Calcium Channel Antagonists)
BR9406080A (pt) 1993-12-08 1996-02-06 Alcon Lab Inc Compostos que tem tanto antividade de anaonista potente de calcio como de antioxidante e uso dos mesmos como agentes citoprotetores
US5623051A (en) 1994-11-10 1997-04-22 University Of Washington Methods and compositions for screening for presynaptic calcium channel blockers
CA2304503A1 (en) 1997-09-23 1999-04-01 Graham Johnson Selective cpla2 inhibitors
ID24475A (id) 1997-11-18 2000-07-20 Teijin Limeted Cs Turunan-turunan amina siklik dan penggunaannya sebagai obat
US6011035A (en) 1998-06-30 2000-01-04 Neuromed Technologies Inc. Calcium channel blockers
US6387897B1 (en) * 1998-06-30 2002-05-14 Neuromed Technologies, Inc. Preferentially substituted calcium channel blockers

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000018402A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Method for treating androgen-related conditions
WO2000037059A2 (en) * 1998-12-18 2000-06-29 Neuromed Technologies, Inc. Compositions and methods to inactivate n-type calcium channels

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ATE333878T1 (de) 2006-08-15
CA2394327C (en) 2012-01-24
KR20020075874A (ko) 2002-10-07
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IL150117A0 (en) 2002-12-01
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