PE20020294A1 - Derivados de pirrolidina como inhibidores de la enzima conversor de endotelina - Google Patents

Derivados de pirrolidina como inhibidores de la enzima conversor de endotelina

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Publication number
PE20020294A1
PE20020294A1 PE2001000711A PE2001000711A PE20020294A1 PE 20020294 A1 PE20020294 A1 PE 20020294A1 PE 2001000711 A PE2001000711 A PE 2001000711A PE 2001000711 A PE2001000711 A PE 2001000711A PE 20020294 A1 PE20020294 A1 PE 20020294A1
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PE
Peru
Prior art keywords
alkyl
aryl
arylalkyl
endothelin
sulfonil
Prior art date
Application number
PE2001000711A
Other languages
English (en)
Inventor
Daniel Bur
Sabine Wallbaum
Alexander Chucholowski
Johannes Aebi
Eric Argirios Kitas
Bernd Michael Loeffler
Denise Blum
Henrietta Dehmlow
Ulrike Obst
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20020294A1 publication Critical patent/PE20020294A1/es

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    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
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    • 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
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P39/00—General protective or antinoxious agents
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
    • C07D207/12—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
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    • 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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  • Organic Chemistry (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
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Abstract

SE REFIERE A DERIVADOS DE PIRROLIDINA DE FORMULA I DONDE R1 ES H, ALQUILCARBONILO, ARILCARBONILO; R2 ES ALQUILO, ALQUILCICLOALQUILO, ALQUILCICLOALQUILALQUILO, CICLOALQUILO, ENTRE OTROS; A ES CO-R3, CH(OH)R4, CONR5R6; R3 Y R4 SON ALQUILO, ARILO, ARILALQUINILO, ARILALQUILO, ENTRE OTROS; R5 ES H, ALQUILO, CICLOALQUILO, CICLOALQUILALQUILO, ENTRE OTROS; R6 ES ALQUILO, ALQUILCARBONILALQUILO, CIANOALQUILO, -CHR7-COR8, CH2CH2COR8, GRUPO IIc, ENTRE OTROS, R7 ES H, ALQUILO, ALQUENILO, ALQUILTIOALQUILO, ENTRE OTROS; R7A Y R10 SON H, ALQUILO; R8 ES OR9, NR10R11; R9 ES H, ALQUILO, ARILALQUILO; R11 ES ALQUILO, ARILO, HETEROARILO, ENTRE OTROS; R12 ES ALQUILO, ARILO, ARILALQUILO; Y ES O, O-S(O2), OCO; m ES 0-2; X ES SO2, CO, COO, SO2NH, CONR13; R13 ES H, ALQUILO, ARILO, CARBOXIALQUILO. SON COMPUESTOS PREFERIDOS ACIDO (2S,4S)-1-[4-MERCAPTO-1-(NAFTALEN-2-SULFONIL)-PIRROLIDIN-2-CARBONIL]PIPERIDIN-4-CARBOXILICO ETIL ESTER; ACIDO (2S,4R)-4-MERCAPTO-1-(NAFTALEN-2-SULFONIL)-PIRROLIDIN-2-CARBOXILICO BENCIL METIL AMIDA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES INHIBIDOR DE ZINC HIDROLASA ESPECIALMENTE DE ENZIMA CONVERSORA DE ENDOTELINA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE ISQUEMIA DE MIOCARDIO, INSUFICIENCIA CARDIACA CONGESTIVA, ARRITMIA, HIPERTENSION, HIPERTENSION PULMONAR, ASMA, VASOESPASMO CEREBRAL
PE2001000711A 2000-07-19 2001-07-16 Derivados de pirrolidina como inhibidores de la enzima conversor de endotelina PE20020294A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP00114947 2000-07-19

Publications (1)

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PE20020294A1 true PE20020294A1 (es) 2002-04-17

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ID=8169224

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Country Status (16)

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

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KR100613196B1 (ko) * 2000-07-19 2006-08-18 에프. 호프만-라 로슈 아게 메탈로프로테아제 억제제로서의 피롤리딘 유도체
WO2002053534A1 (fr) 2000-12-28 2002-07-11 Daiichi Pharmaceutical Co., Ltd. Inhibiteurs de vla-4
EP1481967B1 (en) 2002-03-05 2011-05-04 Sumitomo Chemical Company, Limited Process for the preparation of biaryl compounds
ES2537514T3 (es) 2003-04-04 2015-06-09 Incyte Corporation Composiciones, métodos y kits relacionados con la escisión de HER-2
CA2521937A1 (en) 2003-04-10 2004-10-28 Amgen, Inc. Bicyclic compounds having bradykinin receptors affinity and pharmaceutical compositions thereof
WO2004092164A1 (en) 2003-04-10 2004-10-28 Amgen, Inc. Cyclic amine derivatives and their use in the treatment of inflammation-related disorders mediated by bradykinin
KR20060036399A (ko) 2003-06-20 2006-04-28 암젠 인코포레이티드 피페라진 유도체 및 사용 방법
ES2382806T3 (es) 2003-07-24 2012-06-13 Daiichi Sankyo Company, Limited Compuesto ácido ciclohexanocarboxílico
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
EP2010167A2 (en) * 2006-04-13 2009-01-07 Actelion Pharmaceuticals Ltd. Endothelin receptor antagonists for early stage idiopathic pulmonary fibrosis
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

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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
DK0927161T3 (da) * 1996-08-28 2003-02-17 Procter & Gamble Substitueret cyklisk amin-metalloproteaseinhibitorer
BR9712792A (pt) * 1996-08-28 1999-12-14 Procter & Gamble Inibidores de metaloprotease bidentada.
AU736136B2 (en) * 1997-07-10 2001-07-26 Merck Sharp & Dohme Corp. Crystalline forms of antibiotic side chain intermediates
BR9910098A (pt) * 1998-05-01 2000-12-26 Kyoto Pharma Ind Derivados de carbapenem, utilização dos mesmos e compostos intermediários dos mesmos

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US6541638B2 (en) 2003-04-01
MXPA03000223A (es) 2003-06-06
CA2414311C (en) 2008-01-08
CN1620433A (zh) 2005-05-25
AR033984A1 (es) 2004-01-21
UY26847A1 (es) 2002-01-31
EP1303485A1 (en) 2003-04-23
AU2001270627A1 (en) 2002-01-30
GT200100145A (es) 2002-05-16
KR20030016416A (ko) 2003-02-26
ZA200300167B (en) 2004-04-07
JP2004504297A (ja) 2004-02-12
PA8522501A1 (es) 2002-09-17
WO2002006222A1 (en) 2002-01-24
KR100568841B1 (ko) 2006-04-10
US20020049243A1 (en) 2002-04-25
CA2414311A1 (en) 2002-01-24
JP4068452B2 (ja) 2008-03-26
BR0112580A (pt) 2003-06-17

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