PE20151248A1 - Derivados de ciclopentano como inhibidores de catepsinas - Google Patents

Derivados de ciclopentano como inhibidores de catepsinas

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Publication number
PE20151248A1
PE20151248A1 PE2015000673A PE2015000673A PE20151248A1 PE 20151248 A1 PE20151248 A1 PE 20151248A1 PE 2015000673 A PE2015000673 A PE 2015000673A PE 2015000673 A PE2015000673 A PE 2015000673A PE 20151248 A1 PE20151248 A1 PE 20151248A1
Authority
PE
Peru
Prior art keywords
catepsin
cyclopentan
inhibitors
derivatives
compound
Prior art date
Application number
PE2015000673A
Other languages
English (en)
Inventor
Sanchez Ruben Alvarez
David Banner
Simona M Ceccarelli
Uwe Grether
Wolfgang Haap
Hans Hilpert
Holger Kuehne
Harald Mauser
Jean-Marc Plancher
Original Assignee
Hoffmann La Roche
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=42342001&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20151248(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20151248A1 publication Critical patent/PE20151248A1/es

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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
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    • 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
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    • A61P17/00—Drugs for dermatological disorders
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
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    • A61P35/00—Antineoplastic agents
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    • 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
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    • 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
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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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    • C07D211/36—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
    • C07D211/40—Oxygen atoms
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    • 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
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  • Diabetes (AREA)
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Abstract

La invencion se refiere a un compuesto de la formula (I), en la que A1 y R1 a R5 tienen los significados definidos en la descripcion y en las reivindicaciones. El compuesto (I) tiene actividad como inhibidor de la cisteina proteasa catepsina, en particular de la cisteina proteasa catepsina S o L, por lo que son utiles en el tratamiento de diabetes, ateroesclerosis, aneurismo aortico abdominal, entre otros
PE2015000673A 2009-06-11 2010-06-08 Derivados de ciclopentano como inhibidores de catepsinas PE20151248A1 (es)

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EP2812322B1 (en) * 2012-02-07 2017-12-06 F. Hoffmann-La Roche AG Novel azetidine derivatives
BR112014019220A8 (pt) * 2012-02-17 2017-07-11 Hoffmann La Roche Novos derivados de pirrolidina
EP3055314B1 (en) * 2013-10-08 2018-09-12 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
KR102553613B1 (ko) 2017-01-24 2023-07-07 아스테라스 세이야쿠 가부시키가이샤 페닐디플루오로메틸 치환 프롤린아미드 화합물
TWI830733B (zh) * 2018-05-11 2024-02-01 中國大陸商迪哲（江蘇）醫藥有限公司 環戊烷化合物

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ES2270898T3 (es) * 1999-12-24 2007-04-16 F. Hoffmann-La Roche Ag Derivados de nitrilo como inhibidores de catepsina k.
US6462076B2 (en) * 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
US6982263B2 (en) * 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
JP4343690B2 (ja) * 2001-11-13 2009-10-14 メルク フロスト カナダ リミテツド プロテアーゼ阻害薬としてのシアノアルキルアミノ誘導体
SE0201977D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
CA2530068A1 (en) * 2003-06-30 2005-01-06 Merck Frosst Canada Ltd. Cyanoalklamino derivatives useful as cathepsin cysteine protease inhibitors
CA2547591C (en) * 2003-10-24 2010-08-17 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
CA2602112A1 (en) * 2005-03-22 2006-09-28 Celera Genomics Sulfonyl containing compounds as cysteine protease inhibitors
WO2007103719A2 (en) * 2006-03-03 2007-09-13 Incyte Corporation MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
WO2009001129A1 (en) * 2007-06-26 2008-12-31 Astrazeneca Ab 1-cyanocyclopropyl-derivatives as cathepsin k inhibitors

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WO2010142650A1 (en) 2010-12-16
RU2572555C2 (ru) 2016-01-20
BRPI1010740A2 (pt) 2016-03-15
ES2466720T3 (es) 2014-06-11
IL216448A0 (en) 2012-02-29
KR20120034727A (ko) 2012-04-12
EP2440521A1 (en) 2012-04-18
MX2011012778A (es) 2011-12-16
CN102459162B (zh) 2014-01-08
IL216448A (en) 2014-06-30
CN102459162A (zh) 2012-05-16
TWI496575B (zh) 2015-08-21
JP5766691B2 (ja) 2015-08-19
US20100317647A1 (en) 2010-12-16
CA2762619A1 (en) 2010-12-16
PE20120537A1 (es) 2012-05-26
AU2010257586A1 (en) 2011-12-01
CL2011003123A1 (es) 2012-07-20
AU2010257586B2 (en) 2015-06-11
HK1166307A1 (en) 2012-10-26
ZA201109041B (en) 2012-08-29
JP2012529460A (ja) 2012-11-22
TW201103543A (en) 2011-02-01
AR077051A1 (es) 2011-07-27
KR101726896B1 (ko) 2017-04-13
US7893099B2 (en) 2011-02-22
CA2762619C (en) 2017-07-11
EP2440521B1 (en) 2014-04-30

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