JP4068452B2 - エンドセリン変換酵素阻害剤としてのピロリジン誘導体 - Google Patents

エンドセリン変換酵素阻害剤としてのピロリジン誘導体 Download PDF

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Publication number
JP4068452B2
JP4068452B2 JP2002512128A JP2002512128A JP4068452B2 JP 4068452 B2 JP4068452 B2 JP 4068452B2 JP 2002512128 A JP2002512128 A JP 2002512128A JP 2002512128 A JP2002512128 A JP 2002512128A JP 4068452 B2 JP4068452 B2 JP 4068452B2
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Prior art keywords
pyrrolidine
methyl
sulfonyl
naphthalene
mmol
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Expired - Fee Related
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JP2004504297A (ja
JP2004504297A5 (enExample
Inventor
エービ，ヨハネス
ブルーム，デニーゼ
ブール，ダニエル
クコロウスキー，アレキサンダー
デームロウ，ヘンリエッタ
キタス，エリック・アルギリオス
レフラー，ベルント・ミハエル
オブスト，ウルリケ
ヴァルバウム，ザビーネ
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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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    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • 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
    • A61P9/10—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
JP2002512128A 2000-07-19 2001-07-10 エンドセリン変換酵素阻害剤としてのピロリジン誘導体 Expired - Fee Related JP4068452B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00114947 2000-07-19
PCT/EP2001/007950 WO2002006222A1 (en) 2000-07-19 2001-07-10 Pyrrolidine derivatives as inhibitors of endothelin-converting enzyme

Publications (3)

Publication Number Publication Date
JP2004504297A JP2004504297A (ja) 2004-02-12
JP2004504297A5 JP2004504297A5 (enExample) 2007-01-18
JP4068452B2 true JP4068452B2 (ja) 2008-03-26

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ID=8169224

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JP2002512128A Expired - Fee Related JP4068452B2 (ja) 2000-07-19 2001-07-10 エンドセリン変換酵素阻害剤としてのピロリジン誘導体

Country Status (16)

Country Link
US (1) US6541638B2 (enExample)
EP (1) EP1303485A1 (enExample)
JP (1) JP4068452B2 (enExample)
KR (1) KR100568841B1 (enExample)
CN (1) CN1620433A (enExample)
AR (1) AR033984A1 (enExample)
AU (1) AU2001270627A1 (enExample)
BR (1) BR0112580A (enExample)
CA (1) CA2414311C (enExample)
GT (1) GT200100145A (enExample)
MX (1) MXPA03000223A (enExample)
PA (1) PA8522501A1 (enExample)
PE (1) PE20020294A1 (enExample)
UY (1) UY26847A1 (enExample)
WO (1) WO2002006222A1 (enExample)
ZA (1) ZA200300167B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0112655A (pt) * 2000-07-19 2003-06-24 Hoffmann La Roche Derivados de pirrolidino como inibidores de metaloproteases
US7157487B2 (en) * 2000-12-28 2007-01-02 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
DE60336986D1 (de) 2002-03-05 2011-06-16 Sumitomo Chemical Co Verfahren zur herstellung von biarylverbindungen
EP1613269B1 (en) 2003-04-04 2015-02-25 Incyte Corporation Compositions, methods and kits relating to her-2 cleavage
JP2006522825A (ja) 2003-04-10 2006-10-05 アムジェン インコーポレイテッド ブラジキニンレセプター親和性を有する二環式化合物およびその薬学的組成物
MXPA05010883A (es) 2003-04-10 2006-01-23 Amgen Inc Derivados de amina ciclica y su uso en el tratamiento de trastornos inflamatorios relacionados mediados por bradiquinina.
WO2005061467A2 (en) 2003-06-20 2005-07-07 Amgen Inc. Piperazine derivatives as bradykinin antagonists
KR101051842B1 (ko) 2003-07-24 2011-07-25 다이이찌 세이야꾸 가부시기가이샤 시클로헥산카르복실산류
CN1294120C (zh) * 2003-10-21 2007-01-10 山东大学 吡咯烷类基质金属蛋白酶抑制剂及其应用
JP2009533420A (ja) * 2006-04-13 2009-09-17 アクテリオン ファーマシューティカルズ リミテッド 早期特発性肺線維症の治療
ES2350548B1 (es) * 2009-06-25 2011-09-29 Institut Univ. De Ciència I Tecnologia, S.A. N-fenil-1-sulfonil-2-pirrolidinacarboxamidas para la identificacion de actividad biologica y farmacologica.
EP2730571A1 (en) * 2012-11-12 2014-05-14 Universitat De Barcelona 1-[1-(benzoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonitrile derivatives
WO2017168174A1 (en) 2016-04-02 2017-10-05 N4 Pharma Uk Limited New pharmaceutical forms of sildenafil
JP7163916B2 (ja) * 2017-07-05 2022-11-01 日産化学株式会社 ベンジル化合物
CN110078593A (zh) * 2018-11-15 2019-08-02 南通正达农化有限公司 一种苹果蠹蛾性信息素的合成方法
WO2025124698A1 (en) 2023-12-12 2025-06-19 Idorsia Pharmaceuticals Ltd Aryl sulfone and sulfanone derivatives as orexin receptor modulators
WO2025132542A1 (en) 2023-12-19 2025-06-26 Idorsia Pharmaceuticals Ltd Macrocyclic orexin agonists

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1283906C (en) * 1983-05-09 1991-05-07 Makoto Sunagawa .beta.-LACTAM COMPOUNDS AND PRODUCTION THEREOF
AU644008B2 (en) * 1990-08-10 1993-12-02 Sumitomo Pharmaceuticals Company, Limited Beta-lactam compounds, and their production and use
JP3091297B2 (ja) * 1992-01-10 2000-09-25 住友製薬株式会社 ピロリジン誘導体およびその製造方法
BR9713465A (pt) * 1996-08-28 2000-03-28 Procter & Gamble Inibidores metalotprotease de amina cìclica sibstituìda
BR9712792A (pt) * 1996-08-28 1999-12-14 Procter & Gamble Inibidores de metaloprotease bidentada.
WO1999002492A1 (en) * 1997-07-10 1999-01-21 Merck & Co., Inc. Crystalline forms of antibiotic side chain intermediates
ATE337321T1 (de) * 1998-05-01 2006-09-15 Kyoto Pharma Ind Cabapenemderivate, ihre anwendung und ihre zwischenprodukte

Also Published As

Publication number Publication date
PE20020294A1 (es) 2002-04-17
JP2004504297A (ja) 2004-02-12
AU2001270627A1 (en) 2002-01-30
PA8522501A1 (es) 2002-09-17
CN1620433A (zh) 2005-05-25
BR0112580A (pt) 2003-06-17
ZA200300167B (en) 2004-04-07
CA2414311C (en) 2008-01-08
KR100568841B1 (ko) 2006-04-10
US6541638B2 (en) 2003-04-01
US20020049243A1 (en) 2002-04-25
UY26847A1 (es) 2002-01-31
AR033984A1 (es) 2004-01-21
GT200100145A (es) 2002-05-16
KR20030016416A (ko) 2003-02-26
MXPA03000223A (es) 2003-06-06
CA2414311A1 (en) 2002-01-24
EP1303485A1 (en) 2003-04-23
WO2002006222A1 (en) 2002-01-24

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