CA2608890C - Heterobicyclic metalloprotease inhibitors - Google Patents

Heterobicyclic metalloprotease inhibitors Download PDF

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Publication number
CA2608890C
CA2608890C CA2608890A CA2608890A CA2608890C CA 2608890 C CA2608890 C CA 2608890C CA 2608890 A CA2608890 A CA 2608890A CA 2608890 A CA2608890 A CA 2608890A CA 2608890 C CA2608890 C CA 2608890C
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Canada
Prior art keywords
alkyl
nr10r11
group
aryl
heteroaryl
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Expired - Fee Related
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CA2608890A
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English (en)
French (fr)
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CA2608890A1 (en
Inventor
Christoph Steeneck
Christian Gege
Frank Richter
Matthias Hochguertel
Tim Feurstein
Harald Bluhm
Irving Sucholeiki
Jurgen Boer
Xinyuan Wu
Matthias Schneider
Bert Nolte
Brian Gallagher
Joshua Van Veldhuizen
Hongbo Deng
Michael Essers
Heiko Kroth
Andrew Kiely
Timothy Powers
Arthur G. Taveras
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Alantos Pharmaceuticals Holding Inc
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Alantos Pharmaceuticals Holding Inc
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Publication of CA2608890A1 publication Critical patent/CA2608890A1/en
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Publication of CA2608890C publication Critical patent/CA2608890C/en
Expired - Fee Related legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
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    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
CA2608890A 2005-05-20 2006-05-22 Heterobicyclic metalloprotease inhibitors Expired - Fee Related CA2608890C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US68347005P 2005-05-20 2005-05-20
US60/683,470 2005-05-20
US70646505P 2005-08-08 2005-08-08
US60/706,465 2005-08-08
US73499105P 2005-11-09 2005-11-09
US60/734,991 2005-11-09
PCT/US2006/020970 WO2006128184A2 (en) 2005-05-20 2006-05-22 Pyrimidine or triazine fused bicyclic metalloprotease inhibitors

Publications (2)

Publication Number Publication Date
CA2608890A1 CA2608890A1 (en) 2006-11-30
CA2608890C true CA2608890C (en) 2011-08-02

Family

ID=37239216

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2608890A Expired - Fee Related CA2608890C (en) 2005-05-20 2006-05-22 Heterobicyclic metalloprotease inhibitors

Country Status (13)

Country Link
US (2) US20060293345A1 (enExample)
EP (1) EP1910367A2 (enExample)
JP (3) JP5463034B2 (enExample)
KR (1) KR20080087070A (enExample)
CN (1) CN101238127A (enExample)
AU (1) AU2006251989B2 (enExample)
BR (1) BRPI0609802A2 (enExample)
CA (1) CA2608890C (enExample)
CR (1) CR9614A (enExample)
EA (1) EA013525B1 (enExample)
IL (1) IL187495A0 (enExample)
NO (1) NO20076554L (enExample)
WO (1) WO2006128184A2 (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070155737A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20090221703A1 (en) 2006-07-09 2009-09-03 Chongxi Yu High penetration composition and uses thereof
US20090238763A1 (en) 2006-07-09 2009-09-24 Chongxi Yu High penetration compositions and uses thereof
CA2670044A1 (en) * 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
US20080176870A1 (en) * 2006-11-20 2008-07-24 Bert Nolte Heterobicyclic metalloprotease inhibitors
US20080221093A1 (en) * 2007-03-07 2008-09-11 Christian Gege Metalloprotease inhibitors containing a heterocyclic moiety
KR20220107078A (ko) 2007-06-04 2022-08-01 테크필즈 인크 매우 높은 피부 및 막 침투율을 가지는 비스테로이드성 소염제(nsaia) 약물전구체 및 이들의 새로운 의약적 용도
WO2009075790A1 (en) * 2007-12-07 2009-06-18 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors for intra-articular application
CA2723302C (en) 2008-05-05 2013-08-20 Sanofi-Aventis Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
MX379054B (es) 2008-12-04 2025-03-11 Chongxi Yu Composiciones de alta penetracion y sus aplicaciones.
AR079022A1 (es) 2009-11-02 2011-12-21 Sanofi Aventis Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion
CN101709034B (zh) * 2009-12-14 2017-05-31 大连九信精细化工有限公司 双环[2.2.2]辛烷‑1,4‑二羧酸单甲酯的合成方法
US8343977B2 (en) 2009-12-30 2013-01-01 Arqule, Inc. Substituted triazolo-pyrimidine compounds
BR112013014242B1 (pt) 2010-12-08 2022-02-22 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Composição farmacêutica e composto ou seu sal farmaceuticamente aceitável
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
KR101935868B1 (ko) 2011-12-30 2019-04-03 에스케이이노베이션 주식회사 폴리프로필렌 카보네이트 발포체 조성물 제조방법 및 이로부터 제조된 성형품
CN107929743B (zh) 2012-01-18 2023-09-01 苏州泰飞尔医药有限公司 治疗肺部疾病的高穿透力前药组合物和医药组合物
PL3808749T3 (pl) 2012-12-07 2023-07-10 Vertex Pharmaceuticals Incorporated Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych
WO2014100779A1 (en) 2012-12-21 2014-06-26 Advanced Cell Technology, Inc. Methods ofr production of platelets from pluripotent stem cells and compositions thereof
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
JP2016512239A (ja) 2013-03-15 2016-04-25 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な化合物
PL3077397T3 (pl) 2013-12-06 2020-04-30 Vertex Pharmaceuticals Inc. Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne
SG10201902206QA (en) 2014-06-05 2019-04-29 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
PT3157566T (pt) 2014-06-17 2019-07-11 Vertex Pharma Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr
CN104326914A (zh) * 2014-11-18 2015-02-04 江苏恒祥化工有限责任公司 一种反式-4-甲酸甲酯环己烷甲酸的制备方法
CN104560997B (zh) * 2014-12-25 2018-05-04 中国科学院广州生物医药与健康研究院 抑制ADAMTS-5和ADAM17基因的siRNA组合物及其应用
WO2016103042A1 (en) 2014-12-25 2016-06-30 Guangzhou Ribobio Co., Ltd. Compositions and methods for inhibiting expression of adamts-5 and adam17
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
EP3529230B1 (en) 2016-10-19 2020-09-30 Eastman Chemical Company Synthesis of bicyclo(2.2.2)octanes
EP3694831A1 (en) 2017-10-11 2020-08-19 Eastman Chemical Company Synthesis of bicyclo[2.2.2]octane derivatives
TWI835770B (zh) * 2018-01-19 2024-03-21 美商胞質動力學公司 心肌節抑制劑
CN108558672B (zh) * 2018-06-21 2021-04-30 利尔化学股份有限公司 2-硝基-4-三氟甲基苯甲酸及其异构体的制备方法
CN110950868B (zh) * 2018-09-27 2022-05-13 苏州锐明新药研发有限公司 吡唑并嘧啶化合物及制备方法与制备抗癌症药物的应用
US10836899B2 (en) 2018-12-13 2020-11-17 Eastman Chemical Company Polyesters with specified crystallization half-times
CN116283995B (zh) * 2022-09-08 2023-12-29 华中科技大学同济医学院附属同济医院 一种脂酰辅酶a合成酶短链家族成员3的激动剂及其应用
CN116969831B (zh) * 2023-08-01 2025-09-23 菏泽皓元医药科技有限公司 一种莫奈太尔的中间体及其制备方法

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4497814A (en) * 1982-08-16 1985-02-05 Schering Corporation 2-(Pyridinyl)-1,2,4-triazolo[1,5-a]pyrimidines and derivatives useful in increasing cardiac contractility
JPH0750322B2 (ja) * 1986-06-25 1995-05-31 富士写真フイルム株式会社 ハロゲン化銀カラ−写真感光材料の処理方
DE3704203A1 (de) * 1987-02-11 1988-08-25 Boehringer Ingelheim Kg Verwendung von oxochinazolinderivaten bei der behandlung der hyperurikaemie
FI883320L (fi) * 1987-08-07 1989-02-08 Sankei Yakuhin Kk --laktam, dess framstaellning och mellanprodukter foer dess framstaellning.
US5236917A (en) * 1989-05-04 1993-08-17 Sterling Winthrop Inc. Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof
KR910011852A (ko) * 1989-12-04 1991-08-07 폴 디. 매튜카이티스 신경독 장해 치료용 이미다조[1,2-a]피리디닐알킬 화합물
US5716964A (en) * 1989-12-04 1998-02-10 G.D. Searle & Co. Tetrazolyl substituted imidazo 1,2-a!pyridinylalkyl compounds for treatment of neurotoxic injury
DE3942357A1 (de) * 1989-12-21 1991-06-27 Boehringer Mannheim Gmbh 3-aminopyrazolo-heterocyclen, deren verwendung zur bestimmung von wasserstoffperoxid, wasserstoffperoxid-bildenden systemen, peroxidase, peroxidatisch wirksamen substanzen oder von elektronenreichen aromatischen verbindungen, entsprechende bestimmungsverfahren und hierfuer geeignete mittel
US5955470A (en) * 1991-06-11 1999-09-21 Merrell Pharmaceuticals, Inc. Derivatives of amide analogs of certain methano bridged quinolizines
CZ281628B6 (cs) * 1991-07-29 1996-11-13 Warner-Lambert Company Deriváty chinazolinu a farmaceutické přípravky na jejich bázi
US5435991A (en) * 1991-08-09 1995-07-25 Nycomed Innovation Ab Use of persistent heterocyclic free-radicals in magnetic resonance imaging
US5302586A (en) * 1991-12-19 1994-04-12 G. D. Searle & Co. Phosphonomethyl-imidazo[1,2-a]pyrimidine-2-carboxylic acid compounds for treatment of neurotoxic injury
FR2687675B1 (fr) * 1992-01-31 1997-04-18 Roussel Uclaf Nouveaux derives bicycliques de la pyridine, leur procede de preparation, les nouveaux intermediaires obtenus, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant.
JP2794510B2 (ja) * 1992-03-27 1998-09-10 富士写真フイルム株式会社 ハロゲン化銀写真感光材料
US5464843A (en) * 1992-06-23 1995-11-07 G.D. Searle & Co. Imidazo[1,2-a]pyridinyldiacid compounds for cognitive enhancement and for treatment of cognitive disorders and neutrotoxic injury
MX9304801A (es) * 1992-08-06 1997-06-28 Warner Lambert Co 2-toindoles (selenoidoles) disulfuros (seleniduros) relacinados, los cuales inhiben a las proteinas tirosina cinasas y los cuales tienen propiedades anti-tumorales.
DE4327027A1 (de) * 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
DE4311464A1 (de) * 1993-04-08 1994-10-13 Boehringer Mannheim Gmbh Verfahren zur kolorimetrischen Bestimmung eines Analyten mit einer PQQ-abhängigen Dehydrogenase
DE4311460A1 (de) * 1993-04-08 1994-10-13 Boehringer Mannheim Gmbh Verfahren zur kolorimetrischen Bestimmung eines Analyten mittels Benzylalkoholdehydrogenase und einem chromogenen Redoxindikator
WO1996025414A1 (en) * 1995-02-15 1996-08-22 Pharmacia & Upjohn Company Imidazo[1,2-a]pyridines for the treatment of cns and cardiac diseases
JPH11506428A (ja) * 1995-05-09 1999-06-08 ビーエーエスエフ アクチェンゲゼルシャフト ピラゾロ[1,5a]ピリミジン、その製造方法およびその用途
US5760028A (en) * 1995-12-22 1998-06-02 The Dupont Merck Pharmaceutical Company Integrin receptor antagonists
IT1286545B1 (it) * 1996-02-09 1998-07-15 Antonio Guarna Derivati benzo(c) chinolizinici,loro preparazione ed uso come inibitori delle 5-alfa-riduttasi
AR015104A1 (es) * 1996-11-13 2001-04-18 Dowelanco Compuestos de n-arilsulfilimina sustituidos, utiles como catalizadores en la preparacion de compuestos de n-arilarilsulfonamida; proceso para preparar dichos compuestos y su uso para catalizar dicha preparacion.
AU6691798A (en) * 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase
US6110944A (en) * 1997-03-12 2000-08-29 G. D. Searle & Co. LTA4, hydrolase inhibitors
WO1998043962A1 (en) * 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Heterocyclic integrin inhibitor prodrugs
ITFI970193A1 (it) * 1997-08-01 1999-02-01 Applied Research Systems Uso di derivati benzo(c) chinolizinici come regolatori della crescita delle piante e composizioni ad uso agricolo che contengono tali
US6013654A (en) * 1997-08-14 2000-01-11 Pharmacia & Upjohn Company Imidazo[1,2-A]pyridines for the treatment of CNS and cardiac diseases
JP3773227B2 (ja) * 1997-10-16 2006-05-10 東京応化工業株式会社 レジスト用剥離液組成物およびこれを用いたレジスト剥離方法
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
AUPP278498A0 (en) * 1998-04-03 1998-04-30 Australian Nuclear Science & Technology Organisation Peripheral benzodiazepine receptor binding agents
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
US6319660B1 (en) * 1998-12-28 2001-11-20 Eastman Kodak Company Color photographic element containing speed improving compound
US6190848B1 (en) * 1999-07-21 2001-02-20 Eastman Kodak Company Color photographic element containing ballasted triazole derivative and inhibitor releasing coupler
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
FR2801308B1 (fr) * 1999-11-19 2003-05-09 Oreal COMPOSITIONS DE TEINTURE DE FIBRES KERATINIQUES CONTENANT DE DES 3-AMINO PYRAZOLO-[1,(-a]-PYRIDINES, PROCEDE DE TEINTURE, NOUVELLES 3-AMINO PYRAZOLO-[1,5-a]-PYRIDINES
US6461538B2 (en) * 1999-12-16 2002-10-08 Fuji Photo Film Co., Ltd. Production process for indolizine compounds and their use in organic light-emitting devices
US6770666B2 (en) * 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
FR2805539B1 (fr) * 2000-02-25 2005-06-10 Oreal Compositions de teinture des fibres keratiniques contenant des derives d'indolizine et procede de teinture
JP2001348520A (ja) * 2000-04-03 2001-12-18 Fuji Photo Film Co Ltd メチン化合物、固体微粒子分散物、インクジェット用記録液、およびインクジェット記録方法
US6403588B1 (en) * 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
EE200200607A (et) * 2000-04-28 2004-04-15 Baxter Healthcare Sa 2-atsüülindoolderivaadid ja nende kasutamine kasvajavastaste ravimitena
CA2413802A1 (en) * 2000-06-30 2002-01-10 Mark R. Schmitt Substituted-triazolopyrimidines as anticancer agents
US20020041880A1 (en) * 2000-07-05 2002-04-11 Defeo-Jones Deborah Method of treating cancer
AUPQ969800A0 (en) * 2000-08-28 2000-09-21 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
TWI243019B (en) * 2000-08-31 2005-11-11 Basf Ag Process for the preparation of a solid herbicidal formulation
JP2002205992A (ja) * 2000-11-08 2002-07-23 Takeda Chem Ind Ltd 二環式トリアゾロン誘導体およびそれを含有する除草剤
AU2002239344A1 (en) * 2000-12-15 2002-06-24 Glaxo Group Limited Pyrazolopyridines
DOP2002000328A (es) * 2001-02-14 2003-08-30 Warner Lambert Co Pirimidinas inhibidoras de metaloproteinasas de matriz
PA8539501A1 (es) * 2001-02-14 2002-09-30 Warner Lambert Co Compuestos triazolo como inhibidores de mmp
DE60230160D1 (de) * 2001-02-20 2009-01-15 Astrazeneca Ab 2-arylaminopyrimidine zur behandlung von mit gsk3 in zusammenhang stehenden erkrankungen
EP1372643A1 (en) * 2001-03-30 2004-01-02 Smithkline Beecham Corporation Pyrazolopyridines, process for their preparation and use as therapeutic compounds
US6756498B2 (en) * 2001-04-27 2004-06-29 Smithkline Beecham Corporation Process for the preparation of chemical compounds
CA2448306A1 (en) * 2001-05-30 2002-12-05 Alteon Inc. Method for treating fibrotic diseases or other indications
AR035543A1 (es) * 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
US20040116462A1 (en) * 2002-12-12 2004-06-17 Mitsunori Ono Indolizine compounds
PT1432709E (pt) * 2001-09-13 2005-10-31 Synta Pharmaceuticals Corp Indolizinas de 1-glioxilamida para o trtamento do cancro
EP1427408A4 (en) * 2001-09-17 2005-10-26 Bristol Myers Squibb Co CYCLIC HYDROXAMINE ACIDS AS INHIBITORS OF MATRIX METALLOPROTEINASES AND / OR TNF-a-CONVERTASE (TACE TNF-a-CONVERTING ENZYM)
DE10160357A1 (de) * 2001-12-08 2003-06-18 Aventis Pharma Gmbh Verwendung von Pyridin-2,4-dicarbonsäurediamiden und Pyrimidin-4,6-dicarbonsäurediamiden zur selektiven Inhibierung von Kollagenasen
CN1633434A (zh) * 2002-01-31 2005-06-29 第一制药株式会社 咪唑并[1,2-a]吡啶衍生物
JP2005530788A (ja) * 2002-05-13 2005-10-13 メルク エンド カムパニー インコーポレーテッド フェニル置換イミダゾピリジン類およびフェニル置換ベンズイミダゾール類
EP1511751B1 (en) * 2002-06-04 2008-03-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidine compounds as antiviral agents
WO2004014354A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc 1,6-fused uracil derivatives as matrix metalloproteinase inhibitors
AU2003253165A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidine fused bicyclic metalloproteinase inhibitors
RU2344129C2 (ru) * 2002-11-02 2009-01-20 Санофи-Авентис Дойчланд Гмбх Новые диамиды пиримидин-4,6-дикарбоновой кислоты для селективного ингибирования коллагеназ
CN1849142A (zh) * 2002-11-15 2006-10-18 埃迪尼克斯(开曼)有限公司 2′-支链核苷和黄病毒突变
US7550470B2 (en) * 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
JP2006520385A (ja) * 2003-03-13 2006-09-07 シンタ ファーマスーティカルズ コーポレイション 縮合ピロール化合物
US7893096B2 (en) * 2003-03-28 2011-02-22 Novartis Vaccines And Diagnostics, Inc. Use of small molecule compounds for immunopotentiation
US7235569B2 (en) * 2003-05-02 2007-06-26 Wyeth Piperidinyl indole and tetrohydropyridinyl indole derivatives and method of their use
WO2005002672A2 (en) * 2003-07-01 2005-01-13 President And Fellows Of Harvard College Sirt1 modulators for manipulating cells/organism lifespan/stress response
EP1653968A4 (en) * 2003-07-23 2006-09-06 Synta Pharmaceuticals Corp METHOD FOR MODULATING CALCIUMION RELIEF ACTIVATED CALCIUMION CHANNELS
FR2857966A1 (fr) * 2003-07-24 2005-01-28 Aventis Pharma Sa Produits aryl-heteroaromatiques, compositions les contenant et utilisation
US7144907B2 (en) * 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US20060173183A1 (en) * 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155737A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP2009522295A (ja) * 2005-12-30 2009-06-11 アラントス・フアーマシユーテイカルズ・ホールデイング・インコーポレイテツド 置換ビス−アミドメタロプロテアーゼ阻害剤

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