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EA200201276A1 - Производные арилметиламина для использования в качестве ингибиторов триптазы - Google Patents

Производные арилметиламина для использования в качестве ингибиторов триптазы

Info

Publication number
EA200201276A1
EA200201276A1 EA200201276A EA200201276A EA200201276A1 EA 200201276 A1 EA200201276 A1 EA 200201276A1 EA 200201276 A EA200201276 A EA 200201276A EA 200201276 A EA200201276 A EA 200201276A EA 200201276 A1 EA200201276 A1 EA 200201276A1
Authority
EA
Eurasian Patent Office
Prior art keywords
arylmetylamine
triptase
inhibitors
derivatives
tryptase
Prior art date
Application number
EA200201276A
Other languages
English (en)
Other versions
EA006687B1 (ru
Inventor
Питер К. Эстлс
Пол Р. Иствуд
Оливье Уилль
Джулиан Лэвэлл
Хайнц Паулс
Марк Чекай
Гуиан Лианг
Йонг Гонг
Джеймс Прибиш
Кент Нойеншвандер
Original Assignee
Авентис Фармасьютикалз 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
Application filed by Авентис Фармасьютикалз Инк. filed Critical Авентис Фармасьютикалз Инк.
Priority claimed from PCT/US2001/013811 external-priority patent/WO2001090101A1/en
Publication of EA200201276A1 publication Critical patent/EA200201276A1/ru
Publication of EA006687B1 publication Critical patent/EA006687B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 containing two hetero rings
    • C07D401/06—Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
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    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • A61P25/28—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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
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    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • 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
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    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
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    • C07D211/06—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
    • C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/58—Nitrogen atoms attached in position 4
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    • C07D401/10—Heterocyclic 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 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D405/10—Heterocyclic 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 aromatic rings
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    • C07D405/12—Heterocyclic 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 chain containing hetero atoms as chain links
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  • Organic Chemistry (AREA)
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Abstract

Настоящее изобретение относится к соединениям формулы (I)где R, n и Ar являются такими, как определено в п.1 формулы изобретения, и к их фармацевтическим композициям. Указанные соединения представляют собой ингибиторы триптазы и могут быть использованы для лечения, например, астмы и воспалительных заболеваний.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200201276A 2000-05-22 2001-04-27 Производные арилметиламина для использования в качестве ингибиторов триптазы EA006687B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0012362.0A GB0012362D0 (en) 2000-05-22 2000-05-22 Chemical compounds
US09/843,126 US6977263B2 (en) 2000-05-22 2001-04-26 Chemical compounds
PCT/US2001/013811 WO2001090101A1 (en) 2000-05-22 2001-04-27 Arylmethylamine derivatives for use as tryptase inhibitors

Publications (2)

Publication Number Publication Date
EA200201276A1 true EA200201276A1 (ru) 2003-06-26
EA006687B1 EA006687B1 (ru) 2006-02-24

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EA200201276A EA006687B1 (ru) 2000-05-22 2001-04-27 Производные арилметиламина для использования в качестве ингибиторов триптазы

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US (1) US6977263B2 (ru)
JP (1) JP4796732B2 (ru)
CN (1) CN1740169B (ru)
AT (1) ATE452884T1 (ru)
CR (1) CR6824A (ru)
DE (1) DE60140871D1 (ru)
DK (1) DK1296972T3 (ru)
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ES (1) ES2337550T3 (ru)
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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602005017471D1 (ru) * 2004-03-02 2009-12-17 Aventis Pharma Inc
DOP2005000039A (es) * 2004-03-26 2005-10-31 Aventis Pharma Inc Hidrocloruro de [4-(5-aminometil-2-fluoro-fenil)- piperidin-1-il]-(4-bomo-3-metil-5-propoxi-tiofen-2-il)-metanona como un inhibidor de la triptasa de mastocitos
US7423176B2 (en) * 2004-04-13 2008-09-09 Cephalon, Inc. Bicyclic aromatic sulfinyl derivatives
WO2006044456A1 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
WO2006105035A2 (en) * 2005-03-28 2006-10-05 Vertex Pharmaceuticals Incorporated Muscarinic modulators
JP5019768B2 (ja) * 2006-03-23 2012-09-05 独立行政法人科学技術振興機構 新規低分子化合物およびその製造方法
RU2009130380A (ru) 2007-01-10 2011-02-20 Санофи-Авентис (Fr) Способ определения стабильности органических метиленаминов в присутствии семикарбазид-чувствительной аминоксидазы
US8703119B2 (en) * 2007-10-05 2014-04-22 Polygene Ltd. Injectable biodegradable polymer compositions for soft tissue repair and augmentation
ES2469824T3 (es) * 2007-11-21 2014-06-20 Janssen Pharmaceutica N.V. Espiropiperidinas para su uso como inhibidores de la triptasa
WO2010022196A2 (en) 2008-08-22 2010-02-25 Sanofi-Aventis [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase
FR2955324A1 (fr) 2010-01-15 2011-07-22 Sanofi Aventis [4-(5-aminomethyl-phenyl)-piperidin-1-yl]-1h-indol-3-yl]-methanones disubstituees
BR112012014860A2 (pt) 2009-12-23 2016-03-29 Sanofi Sa pró-fármacos de [4 [4-(5-aminometil-2-flúor-fenil)-piperidin-1-il]-(1h-pirrolo-piridin-il)-metanonas e sua síntese
WO2011078984A1 (en) 2009-12-23 2011-06-30 Sanofi [4[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof
AU2010333779A1 (en) * 2009-12-23 2012-07-12 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
BR112012020965A2 (pt) * 2010-02-24 2016-05-03 Sanofi Sa tratamento de condições alérgicas dermatológicas
US20140194383A1 (en) * 2011-04-07 2014-07-10 Cornell University Monomers capable of dimerizing in an aqueous solution, and methods of using same
HUE043221T2 (hu) * 2011-05-27 2019-08-28 Lexicon Pharmaceuticals Inc Notum pektinacetilészteráz 4H-tieno[3,2-C]kromén-alapú inhibitorai és alkalmazási eljárásaik
AU2013353004A1 (en) 2012-11-30 2015-07-09 Kyowa Hakko Kirin Co., Ltd. Nitrogen-containing heterocyclic compound
TW201441193A (zh) * 2012-12-06 2014-11-01 Kyowa Hakko Kirin Co Ltd 吡啶酮化合物
US9856214B2 (en) 2013-11-15 2018-01-02 The Wistar Institute Of Anatomy And Biology EBNA1 inhibitors and their method of use
AU2017311691B2 (en) 2016-08-18 2021-12-02 Vidac Pharma Ltd. Piperazine derivatives, pharmaceutical compositions and methods of use thereof
CN110357833B (zh) * 2019-06-03 2022-05-24 杭州维坦医药科技有限公司 芳杂乙酰胺类衍生物及其制备和应用
TW202115086A (zh) * 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑
IL294881A (en) * 2020-01-23 2022-09-01 Myoforte Therapeutics Inc pgdh inhibitors and methods of preparation and use
CA3180686A1 (en) * 2020-06-04 2021-12-09 Baskaran Pillai Novel small molecules for targeted degradation of untargetable kras in cancer therapy

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5221676A (en) * 1992-02-06 1993-06-22 Warner-Lambert Company 7-substituted quinolones and naphthyridones as antibacterial agents
DE4234295A1 (de) * 1992-10-12 1994-04-14 Thomae Gmbh Dr K Carbonsäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE4407139A1 (de) * 1994-03-04 1995-09-07 Thomae Gmbh Dr K Aryl-1-azacycloalkane und deren Salze, diese Verbindungen enthaltende Arzneimittel und deren Verwendung sowie Verfahren zu ihrer Herstellung
US5629321A (en) * 1994-10-27 1997-05-13 Mitsui Toatsu Chemicals, Inc. Bicyclic compound and platelet aggregation inhibitor containing the same
US6740682B2 (en) * 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
GB9912411D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
US20020045613A1 (en) * 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines

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UA74579C2 (en) 2006-01-16
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CN1740169A (zh) 2006-03-01
CR6824A (es) 2008-11-25
MEP54608A (en) 2011-05-10
IL152830A (en) 2009-11-18
ATE452884T1 (de) 2010-01-15
YU87202A (sh) 2006-05-25
GB0012362D0 (en) 2000-07-12
EA006687B1 (ru) 2006-02-24
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US20030187020A1 (en) 2003-10-02
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ZA200209484B (en) 2004-02-23
JP4796732B2 (ja) 2011-10-19

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