EA021424B1 - Тиазолопиридиновые соединения, регулирующие сиртуин - Google Patents

Тиазолопиридиновые соединения, регулирующие сиртуин Download PDF

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Publication number
EA021424B1
EA021424B1 EA201170847A EA201170847A EA021424B1 EA 021424 B1 EA021424 B1 EA 021424B1 EA 201170847 A EA201170847 A EA 201170847A EA 201170847 A EA201170847 A EA 201170847A EA 021424 B1 EA021424 B1 EA 021424B1
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EA
Eurasian Patent Office
Prior art keywords
sirtuin
phenyl
compound
thiazolo
protein
Prior art date
Application number
EA201170847A
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English (en)
Russian (ru)
Other versions
EA201170847A1 (ru
Inventor
Кристофер Оулманн
Джереми С. Диш
Пуи Йее Нг
Роберт Б. Перни
Original Assignee
Сертрис Фармасьютикалз, Инк.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42269132&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA021424(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Сертрис Фармасьютикалз, Инк. filed Critical Сертрис Фармасьютикалз, Инк.
Publication of EA201170847A1 publication Critical patent/EA201170847A1/ru
Publication of EA021424B1 publication Critical patent/EA021424B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201170847A 2008-12-19 2009-12-18 Тиазолопиридиновые соединения, регулирующие сиртуин EA021424B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20315608P 2008-12-19 2008-12-19
PCT/US2009/068865 WO2010071853A1 (en) 2008-12-19 2009-12-18 Thiazolopyridine sirtuin modulating compounds

Publications (2)

Publication Number Publication Date
EA201170847A1 EA201170847A1 (ru) 2011-12-30
EA021424B1 true EA021424B1 (ru) 2015-06-30

Family

ID=42269132

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170847A EA021424B1 (ru) 2008-12-19 2009-12-18 Тиазолопиридиновые соединения, регулирующие сиртуин

Country Status (22)

Country Link
US (2) US8343997B2 (enExample)
EP (1) EP2376502B1 (enExample)
JP (1) JP5628828B2 (enExample)
KR (1) KR20110110194A (enExample)
CN (1) CN102388054B (enExample)
BR (1) BRPI0922435A2 (enExample)
CA (1) CA2747715A1 (enExample)
CO (1) CO6400181A2 (enExample)
CR (1) CR20110353A (enExample)
DO (1) DOP2011000188A (enExample)
EA (1) EA021424B1 (enExample)
ES (1) ES2544258T3 (enExample)
IL (1) IL213217A0 (enExample)
MA (1) MA32909B1 (enExample)
MX (1) MX2011006555A (enExample)
MY (1) MY160006A (enExample)
NZ (1) NZ594122A (enExample)
PE (1) PE20120057A1 (enExample)
SG (1) SG171835A1 (enExample)
UA (1) UA104447C2 (enExample)
WO (1) WO2010071853A1 (enExample)
ZA (1) ZA201104060B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070014833A1 (en) * 2005-03-30 2007-01-18 Sirtris Pharmaceuticals, Inc. Treatment of eye disorders with sirtuin modulators
AU2009243006B2 (en) 2008-05-01 2013-03-21 Sirtris Pharmaceuticals, Inc. Quinolines and related analogs as sirtuin modulators
BRPI0914006A2 (pt) * 2008-07-03 2015-10-27 Sirtris Pharmaceuticals Inc benzimidazóis e análogos relacionados como moduladores de sirtuína
CA2738794C (en) 2008-09-29 2016-01-05 Sirtris Pharmaceuticals, Inc. Chromenone analogs as sirtuin modulators
WO2011059839A1 (en) 2009-10-29 2011-05-19 Sirtris Pharmaceuticals, Inc. Bicyclic pyridines and analogs as sirtuin modulators
WO2013142817A2 (en) 2012-03-23 2013-09-26 Dennis Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
EP2847198B1 (en) 2012-05-08 2016-12-14 Lycera Corporation Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of ror-gamma and the treatment of disease
BR112014030412A2 (pt) 2012-06-14 2017-06-27 Basf Se método para combater ou controlar pragas, método para proteger culturas, compostos, processo para a preparação de compostos, uso de um composto, composição agrícola ou veterinária e semente.
WO2016081692A2 (en) * 2014-11-19 2016-05-26 Glaxosmithkline Llc Substituted bridged urea analogs as sirtuin modulators
JP6376707B2 (ja) 2013-05-13 2018-08-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC サーチュイン調節剤としての置換架橋尿素類似体
US10172915B2 (en) 2013-10-20 2019-01-08 Duke University Methods and compositions for activation of sirtuins with Annexin A1 peptides
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095792A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease
WO2015095788A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
AU2015222917A1 (en) 2014-02-27 2016-09-15 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods
EP3140291A4 (en) 2014-05-05 2018-01-10 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease
WO2015171558A2 (en) 2014-05-05 2015-11-12 Lycera Corporation BENZENESULFONAMIDO AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORγ AND THE TREATEMENT OF DISEASE
US10316054B2 (en) 2014-06-02 2019-06-11 Glaxosmithkline Intellectual Property (No. 2) Limited Preparation and use of crystalline beta-D-nicotinamide riboside
RU2016149767A (ru) 2014-06-06 2018-07-16 Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед Аналоги никотинамидрибозида и фармацевтические композиции и их применение
CA2975997A1 (en) 2015-02-11 2016-08-18 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as rorgammat inhibitors and uses thereof
WO2016179343A1 (en) 2015-05-05 2016-11-10 Lycera Corporation DIHYDRO-2H-BENZO[b][1,4]OXAZINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORy AND THE TREATMENT OF DISEASE
CN107980042B (zh) 2015-06-11 2021-10-08 莱斯拉公司 用作RORγ激动剂和用于治疗疾病的芳基二氢-2H-苯并[b][1,4]噁嗪磺酰胺和相关化合物
US9782859B2 (en) * 2015-07-16 2017-10-10 Siemens Energy, Inc. Slag free flux for additive manufacturing
EP3368516B1 (en) 2015-10-27 2020-07-15 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
JP2018531958A (ja) 2015-10-27 2018-11-01 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. RORγT阻害薬としてのヘテロアリール置換安息香酸及びその使用
JP2019509272A (ja) 2016-02-23 2019-04-04 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation 脊髄性筋萎縮症の治療のための併用療法
US20220304958A1 (en) * 2019-06-04 2022-09-29 The Regents Of The University Of California Small molecule inhibitors of a protein complex
CA3213068A1 (en) 2021-03-25 2022-09-29 Ramot At Tel-Aviv University Ltd. Compositions and articles comprising an adnf polypeptide

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007019346A1 (en) * 2005-08-04 2007-02-15 Sirtris Pharmaceuticals, Inc. Benzothiazoles and thiazolopyridines as sirtuin modulators
WO2008156869A2 (en) * 2007-06-20 2008-12-24 Sirtris Pharmaceuticals, Inc. Sirtuin modulating thiazolopyridine compounds
WO2009061453A1 (en) * 2007-11-08 2009-05-14 Sirtris Pharmaceuticals, Inc. Solubilized thiazolopyridines

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3164603A (en) 1965-01-05 xnhcox
DE1108698B (de) 1959-09-03 1961-06-15 Hoechst Ag Verfahren zur Herstellung von 2-(2'-Aminoaryl)-4, 5-arylen-1, 2, 3-triazolen
FR1439129A (fr) 1965-04-02 1966-05-20 Chimetron Nouveaux sulfonylbenzimidazoles
FR1476529A (fr) 1965-04-24 1967-04-14 Chimetron Sarl Nouveaux dérivés benzimidazole-sulfoniques et sulfamides correspondants
US3503929A (en) 1965-10-21 1970-03-31 Minnesota Mining & Mfg Polyimidazoquinazolines and polyamidobenzimidazoles
US3517007A (en) 1968-04-05 1970-06-23 American Home Prod 5 - acetamido - 4 - pyrimidinecarboxamides,5 - acetamido - 4 - pyrimidinecarboxylic acid hydrazides and related compounds
US3928228A (en) 1969-04-28 1975-12-23 Sterling Drug Inc 4,4{40 -Stilbenebis-pyridooxazoles and related optical brighteners and polymeric compositions brightened thereby
US3712888A (en) 1970-12-14 1973-01-23 American Cyanamid Co Bis-pyridoxazole-stilbene derivatives for optical brightening
CA1006165A (en) 1971-04-06 1977-03-01 Eastman Kodak Company Ballasted color photographic couplers
AR208500A1 (es) 1972-06-14 1977-02-15 Merck & Co Inc Procedimiento para la preparacion de derivados de oxazolo(4,5-b)-piridinas
US4038396A (en) 1975-02-24 1977-07-26 Merck & Co., Inc. Anti-inflammatory oxazole[4,5-b]pyridines
PL96241B1 (pl) 1975-06-30 1977-12-31 Sposob wytwarzania 2-/2-podstawionych-4-tiazolilo/-benzimidazoli
JPS6040016B2 (ja) 1977-08-31 1985-09-09 コニカ株式会社 マゼンタ色素画像の形成方法
US4471040A (en) 1980-09-10 1984-09-11 Canon Kabushiki Kaisha Electrophotographic disazo photosensitive member
US4727064A (en) 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
US4939133A (en) 1985-10-01 1990-07-03 Warner-Lambert Company N-substituted-2-hydroxy-α-oxo-benzeneacetamides and pharmaceutical compositions having activity as modulators of the arachidonic acid cascade
DE3807084A1 (de) 1988-03-04 1989-09-14 Knoll Ag Neue benzimidazo(1,2-c)chinazoline, ihre herstellung und verwendung
JPH04190232A (ja) 1990-11-26 1992-07-08 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
US5814651A (en) 1992-12-02 1998-09-29 Pfizer Inc. Catechol diethers as selective PDEIV inhibitors
JPH06247969A (ja) 1992-12-28 1994-09-06 Takeda Chem Ind Ltd 縮合複素環化合物及びそれを含む農園芸用殺虫剤
US5852011A (en) 1994-05-31 1998-12-22 Mitsui Chemicals, Inc. Benzimidazole derivatives
AUPN449295A0 (en) 1995-07-28 1995-08-24 Inner And Eastern Health Care Network, The Radioprotectors
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5808087A (en) 1995-11-29 1998-09-15 Mitsui Chemicals, Inc. Sulfonium salts of pyrrolylbenzimidazoles
CN1299358A (zh) 1997-12-31 2001-06-13 新泽西州州立大学(拉特格斯) 杂环拓扑异构酶毒性剂
US6653309B1 (en) 1999-04-26 2003-11-25 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme technical field of the invention
EP1177188B1 (en) 1999-05-12 2005-10-12 Ortho-McNeil Pharmaceutical, Inc. Pyrazole carboxamides useful for the treatment of obesity and other disorders
HK1047582B (zh) 1999-06-23 2005-03-04 萨诺费-阿文蒂斯德国有限公司 取代的苯並咪唑
AU7314200A (en) 1999-09-17 2001-04-24 Yamanouchi Pharmaceutical Co., Ltd. Benzimidazole derivatives
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
MXPA02010763A (es) 2000-06-14 2003-03-10 Warner Lambert Co Heterociclicos biciclos-6,5 fusionados.
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
JP2002161084A (ja) 2000-11-28 2002-06-04 Sumitomo Pharmaceut Co Ltd 複素環誘導体
US20040010033A1 (en) 2001-02-20 2004-01-15 Pfizer Inc. Non-peptide GnRH agents, methods and intermediates for their preparation
WO2002066454A1 (fr) 2001-02-21 2002-08-29 Sankyo Company, Limited Derives de chromene
US7081454B2 (en) 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
CA2442428A1 (en) 2001-03-28 2002-10-10 Mark D. Wittman Novel tyrosine kinase inhibitors
WO2003007959A1 (en) 2001-07-16 2003-01-30 Fujisawa Pharmaceutical Co., Ltd. Quinoxaline derivatives which have parp inhibitory action
EA007339B1 (ru) 2001-07-27 2006-08-25 Кьюэрис, Инк. Медиаторы путей передачи сигналов генами hedgehog, содержащие их композиции и способы применения указанных веществ
AU2002368274A1 (en) 2001-09-13 2004-06-03 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
WO2003045929A1 (en) 2001-11-26 2003-06-05 Takeda Chemical Industries, Ltd. Bicyclic derivative, process for producing the same, and use
WO2003048140A1 (en) 2001-12-03 2003-06-12 Japan Tobacco Inc. Azole compound and medicinal use thereof
KR20040084896A (ko) 2002-02-06 2004-10-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 헤테로아릴 화합물
GB0205256D0 (en) 2002-03-06 2002-04-17 Oxford Glycosciences Uk Ltd Novel compounds
ATE432261T1 (de) 2002-03-18 2009-06-15 Merck Frosst Canada Ltd Pde4-inhibitoren mit heterobrückensubstituiertem 8-arylchinolin
MXPA04009040A (es) 2002-03-20 2005-01-25 Metabolex Inc Acidos fenilaceticos sustituidos.
TW200304820A (en) 2002-03-25 2003-10-16 Avanir Pharmaceuticals Use of benzimidazole analogs in the treatment of cell proliferation
JP4239463B2 (ja) 2002-04-09 2009-03-18 大正製薬株式会社 3−トリフルオロメチルアニリド誘導体
JP4224979B2 (ja) 2002-04-09 2009-02-18 大正製薬株式会社 インターロイキン12抑制剤
CN100360130C (zh) 2002-04-18 2008-01-09 先灵公司 用作组胺h3拮抗剂的1-(4-哌啶基)苯并咪唑酮
JP2003313176A (ja) 2002-04-24 2003-11-06 Sankyo Co Ltd アミノアゾール誘導体
AU2003249937A1 (en) 2002-07-12 2004-02-02 Sanofi-Aventis Deutschland Gmbh Heterocyclically substituted benzoylureas, method for their production and their use as medicaments
SE0202429D0 (sv) 2002-08-14 2002-08-14 Astrazeneca Ab Novel Compounds
DE10237722A1 (de) 2002-08-17 2004-08-19 Aventis Pharma Deutschland Gmbh Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase
JP2004075614A (ja) 2002-08-20 2004-03-11 Sankyo Co Ltd クロメン誘導体を含有する医薬
TW200501960A (en) 2002-10-02 2005-01-16 Bristol Myers Squibb Co Synergistic kits and compositions for treating cancer
JP2006515274A (ja) 2002-10-08 2006-05-25 マサチューセッツ・インスティテュート・オブ・テクノロジー コレステロール輸送の調節のための化合物
JP2006504725A (ja) 2002-10-09 2006-02-09 ファイザー・プロダクツ・インク 神経変性障害治療用ピラゾール化合物
AU2003299378A1 (en) 2002-10-11 2004-05-04 Board Of Regents, The University Of Texas System Method and compounds for inhibiting hec1 activity for the treatment of proliferative diseases
AU2003285958A1 (en) 2002-10-25 2004-05-25 Genesoft Pharmaceuticals, Inc. Anti-infective biaryl compounds
WO2004041277A1 (en) 2002-11-01 2004-05-21 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
WO2004050833A2 (en) 2002-11-27 2004-06-17 University Of North Carolina At Chapel Hill Glyceraldehyde 3-phosphate dehydrogenase-s(gapds), a glycolytic enzyme expressed only in male germ cells,is a target for male contraception
DE10300398A1 (de) 2003-01-09 2004-07-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von substituierten 2-Phenylbenzimidazolen als Arzneimittel
WO2004069160A2 (en) 2003-01-28 2004-08-19 Smithkline Beecham Corporation Chemical compounds
WO2004072068A1 (en) 2003-02-10 2004-08-26 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
PT2476667E (pt) 2003-02-26 2014-09-18 Sugen Inc Compostos de aminoheteroarilo como inibidores da proteína quinase
DE602004015429D1 (de) 2003-03-11 2008-09-11 Pfizer Prod Inc Pyrazinverbindungen als inhibitoren des transforming growth factor (tgf)
WO2004084813A2 (en) 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
GB2405793A (en) 2003-09-12 2005-03-16 4 Aza Bioscience Nv Pteridine derivatives for treating TNF-alpha related disorders
PL1663244T3 (pl) 2003-09-12 2008-01-31 4 Aza Ip Nv Pochodne pterydyny do leczenia chorób związanych z TNF-alfa
WO2005028484A1 (en) 2003-09-19 2005-03-31 F. Hoffmann-La Roche Ag Thiazolopyridine derivatives as adenosine receptor ligands
JP4795634B2 (ja) 2003-10-31 2011-10-19 出光興産株式会社 有機薄膜トランジスタ
JP2005162855A (ja) 2003-12-02 2005-06-23 Konica Minolta Holdings Inc 着色組成物、インクジェット記録用インク、カラートナー、光記録媒体、感熱転写記録材料用インクシート、カラーフィルター、及び該インクジェット記録用インクを用いたインクジェット記録方法
EP1723138B1 (en) 2004-02-11 2010-07-14 Basilea Pharmaceutica AG Substituted benzimidazoles and their use for inducing apoptosis
WO2005100342A1 (en) 2004-03-26 2005-10-27 Vertex Pharmaceuticals, Incorporated Pyridine inhibitors of erk2 and uses thereof
DE102004021716A1 (de) 2004-04-30 2005-12-01 Grünenthal GmbH Substituierte Imidazo[1,2-a]pyridin-Verbindungen und Arzneimittel enthaltend substituierte Imidazo[1,2-a]pyridin-Verbindungen
TW200600492A (en) 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
CA2881078C (en) 2004-06-24 2018-10-02 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
BRPI0515012A (pt) 2004-08-13 2008-07-01 Genentech Inc substáncia quìmica, composição e formulação farmacêutica, método de tratamento, método de inibição de pelo menos uma enzima que utiliza atp e uso
DE102004039789A1 (de) 2004-08-16 2006-03-02 Sanofi-Aventis Deutschland Gmbh Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
GB0421525D0 (en) 2004-09-28 2004-10-27 Novartis Ag Inhibitors of protein kineses
CA2587489C (en) 2004-11-03 2013-12-31 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
JP2008519850A (ja) 2004-11-10 2008-06-12 シンタ ファーマシューティカルズ コーポレーション Il−12調節化合物
US20090163476A1 (en) * 2005-03-03 2009-06-25 Sirtris Pharmaceuticals, Inc. N-Phenyl Benzamide Derivatives as Sirtuin Modulators
CA2599992A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Acridine and quinoline dervatives as sirtuin modulators
US20060235037A1 (en) 2005-04-15 2006-10-19 Purandare Ashok V Heterocyclic inhibitors of protein arginine methyl transferases
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
CN101316853B (zh) * 2005-08-04 2014-09-24 西特里斯药业公司 作为sirtuin调节剂的苯并噻唑和噻唑并吡啶
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
CN101490128B (zh) 2006-07-14 2011-11-30 东洋油墨制造株式会社 聚酯分散剂及其制备方法、以及使用该分散剂的颜料组合物
WO2008073451A2 (en) 2006-12-11 2008-06-19 Sirtris Pharmaceuticals, Inc. Benzoimidazole derivatives as sirtuin (sir) modulating compounds
CN101679266B (zh) 2007-03-01 2015-05-06 诺华股份有限公司 Pim激酶抑制剂及其应用方法
TW200918542A (en) 2007-06-20 2009-05-01 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
EP2215066A1 (en) 2007-11-01 2010-08-11 Sirtris Pharmaceuticals, Inc. Amide derivatives as sirtuin modulators
US20100168084A1 (en) 2008-05-08 2010-07-01 Huber L Julie Therapeutic compounds and related methods of use
WO2010019606A1 (en) 2008-08-12 2010-02-18 Sirtris Pharmaceuticals, Inc. Benzoxazoles, benzthiazoles and related analogs as sirtuin modulators

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007019346A1 (en) * 2005-08-04 2007-02-15 Sirtris Pharmaceuticals, Inc. Benzothiazoles and thiazolopyridines as sirtuin modulators
WO2008156869A2 (en) * 2007-06-20 2008-12-24 Sirtris Pharmaceuticals, Inc. Sirtuin modulating thiazolopyridine compounds
WO2009061453A1 (en) * 2007-11-08 2009-05-14 Sirtris Pharmaceuticals, Inc. Solubilized thiazolopyridines

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