CN101389335A - 噻二唑化合物和使用方法 - Google Patents

噻二唑化合物和使用方法 Download PDF

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Publication number
CN101389335A
CN101389335A CNA2005800356937A CN200580035693A CN101389335A CN 101389335 A CN101389335 A CN 101389335A CN A2005800356937 A CNA2005800356937 A CN A2005800356937A CN 200580035693 A CN200580035693 A CN 200580035693A CN 101389335 A CN101389335 A CN 101389335A
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CN
China
Prior art keywords
amine
thiadiazoles
amino
indazole
propyl group
Prior art date
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Pending
Application number
CNA2005800356937A
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English (en)
Chinese (zh)
Inventor
曾庆平
姚国民
G·E·沃尔希特
V·N·维斯瓦纳汉
A·塔斯克
J·T·赖德
H·莫宁谢恩
C·多明格斯
M·P·波尔博
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Amgen Inc
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Amgen Inc
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Application filed by Amgen Inc filed Critical Amgen Inc
Publication of CN101389335A publication Critical patent/CN101389335A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/13—Oxygen atoms
    • 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
    • A61K31/433—Thidiazoles
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA2005800356937A 2004-10-18 2005-10-18 噻二唑化合物和使用方法 Pending CN101389335A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61901004P 2004-10-18 2004-10-18
US60/619,010 2004-10-18

Publications (1)

Publication Number Publication Date
CN101389335A true CN101389335A (zh) 2009-03-18

Family

ID=36203652

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2005800356937A Pending CN101389335A (zh) 2004-10-18 2005-10-18 噻二唑化合物和使用方法

Country Status (15)

Country Link
US (3) US7354944B2 (https=)
EP (1) EP1809282B1 (https=)
JP (1) JP4931823B2 (https=)
KR (1) KR20070073791A (https=)
CN (1) CN101389335A (https=)
AU (1) AU2005295441B2 (https=)
BR (1) BRPI0516609A (https=)
CA (1) CA2583217C (https=)
EA (1) EA012181B1 (https=)
ES (1) ES2400689T3 (https=)
IL (1) IL182203A0 (https=)
MA (1) MA29029B1 (https=)
MX (1) MX2007004551A (https=)
WO (1) WO2006044860A2 (https=)
ZA (1) ZA200703975B (https=)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA012181B1 (ru) 2004-10-18 2009-08-28 Амген, Инк. Соединения тиадиазола и их применение
WO2007007054A1 (en) * 2005-07-08 2007-01-18 Cancer Research Technology Limited Phthalamides, succinimides and related compounds and their use as pharmaceuticals
MY149143A (en) * 2006-01-18 2013-07-15 Amgen Inc Thiazole compounds as protien kinase b (pkb) inhibitors
DE102006030479A1 (de) * 2006-07-01 2008-03-20 Merck Patent Gmbh Indazolderivate
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
DE102007002717A1 (de) 2007-01-18 2008-07-24 Merck Patent Gmbh Heterocyclische Indazolderivate
DE102007022565A1 (de) 2007-05-14 2008-11-20 Merck Patent Gmbh Heterocyclische Indazolderivate
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
US7897619B2 (en) 2007-07-17 2011-03-01 Amgen Inc. Heterocyclic modulators of PKB
AU2008276512A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of PKB
DE102008038221A1 (de) 2008-08-18 2010-02-25 Merck Patent Gmbh 7-Azaindolderivate
DE102008038222A1 (de) 2008-08-18 2010-02-25 Merck Patent Gmbh Indazol-5-carbonsäurehydrazid-derivate
DE102008038220A1 (de) 2008-08-18 2010-02-25 Merck Patent Gmbh Oxadiazolderivate
WO2010083246A1 (en) * 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
MX352672B (es) 2011-09-27 2017-12-04 Amgen Inc Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer.
US8729263B2 (en) 2012-08-13 2014-05-20 Novartis Ag 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions
US9040712B2 (en) 2013-01-23 2015-05-26 Novartis Ag Thiadiazole analogs thereof and methods for treating SMN-deficiency-related-conditions
US20160002185A1 (en) 2013-02-19 2016-01-07 Amgen Inc. Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer
AU2014236812B2 (en) 2013-03-14 2018-03-01 Amgen Inc. Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
CN105358530A (zh) 2013-06-10 2016-02-24 美国安进公司 制备mdm2抑制剂的方法及其结晶形式
EP4105208A1 (en) 2013-07-31 2022-12-21 Novartis AG 1,4-disubstituted pyridazine derivatives and their use for treating smn-deficiency-related conditions
HRP20220718T1 (hr) 2013-11-11 2022-09-30 Amgen Inc. Kombinacijska terapija uključujući inhibitor mdm2 i jedan ili više dodatnih farmaceutski aktivnih sredstava za liječenje raka
AU2014368619B2 (en) 2013-12-19 2018-11-22 Idorsia Pharmaceuticals Ltd Antibacterial 1H-indazole and 1H-indole derivatives
RU2624857C1 (ru) * 2016-01-26 2017-07-07 федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургская государственная химико-фармацевтическая академия" Министерства здравоохранения Российской Федерации (ФГБОУ ВО СПХФА Минздрава России) Фармацевтическая композиция с противогрибковой активностью и способ ее получения
WO2017151409A1 (en) 2016-02-29 2017-09-08 University Of Florida Research Foundation, Incorporated Chemotherapeutic methods
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
EA201992781A1 (ru) 2017-05-22 2020-04-01 Эмджен Инк. Ингибиторы g12c kras и способы их применения
JP7312749B2 (ja) 2017-08-04 2023-07-21 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングをモジュレートする方法および組成物
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES3060664T3 (en) 2018-06-12 2026-03-27 Amgen Inc Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
IL315550A (en) 2018-08-31 2024-11-01 Amgen Inc A process for preparing an MDM2 inhibitor
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
WO2020163405A1 (en) 2019-02-05 2020-08-13 Skyhawk Therapeutics, Inc. Methods and compositions for modulating splicing
JP7551629B2 (ja) 2019-02-05 2024-09-17 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
JP7603595B2 (ja) 2019-02-06 2024-12-20 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
JP7603594B2 (ja) 2019-02-06 2024-12-20 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3452035A (en) * 1966-12-23 1969-06-24 American Cyanamid Co 2 - amino - 5 - (5 - nitro - 1 - substituted-2 - imidazolyl) - 1,3,4 - thiadiazoles and oxadiazoles
US3904756A (en) * 1966-12-23 1975-09-09 American Cyanamid Co Substituted nitroimidazolyl thiadiazoles and oxadiazoles as antibacterial agents and growth promoting compounds
US3991200A (en) * 1974-04-25 1976-11-09 American Cyanamid Company Substituted nitroimidazolyl thiadiazoles and oxadiazoles as antibacterial agents and growth promoting compounds
US3666860A (en) 1966-12-23 1972-05-30 Gerald Berkelhammer Substituted nitroimidazolylthiadiazoles and oxadiazoles as antiprotozoal agents
US3830924A (en) * 1966-12-23 1974-08-20 American Cyanamid Co Substituted nitroimidazolyl-thiadiazoles as growth promoting agents
US3740434A (en) * 1966-12-23 1973-06-19 American Cyanamid Co Substituted nitroimidazolylthiadiazoles and oxadiazoles as antiprotozoal agents
US3842174A (en) * 1966-12-23 1974-10-15 American Cyanamid Co Substituted nitroimidazolylthiadiazoles and oxadiazoles as antiprotozoal agents
US3666830A (en) * 1971-01-21 1972-05-30 Gen Electric Lead compound catalyzed siloxane resin system
US4086238A (en) * 1976-06-21 1978-04-25 Velsicol Chemical Corporation 1-Thiadiazolyl-4-methoxymethyl-5-hydroxyimidazolidinones
DE2640601C2 (de) * 1976-09-09 1985-11-28 Agfa-Gevaert Ag, 5090 Leverkusen Farbphotographisches Material mit 2-Äquivalent-Gelbkupplern
DE3407505A1 (de) 1984-03-01 1985-09-05 A. Nattermann & Cie GmbH, 5000 Köln Neue benzothiazin-carbonsaeureamide mit antiarthritischer wirksamkeit
FR2572074B1 (fr) * 1984-10-18 1987-07-17 Sanofi Sa Derives du thiadiazole actifs sur le systeme nerveux central, procede d'obtention et compositions pharmaceutiques les contenant
FR2636628B1 (fr) * 1988-08-25 1990-12-28 Sanofi Sa Derives du thiadiazole-1,3,4, leur procede d'obtention et compositions pharmaceutiques en contenant
WO1993019054A1 (en) 1992-03-26 1993-09-30 Dowelanco N-heterocyclic nitro anilines as fungicides
JPH08151364A (ja) * 1994-02-18 1996-06-11 Nissan Chem Ind Ltd 含窒素環状化合物および除草剤
WO1996038419A1 (en) 1995-05-31 1996-12-05 Nissan Chemical Industries, Ltd. 5-pyrazolecarboxamide derivatives and plant disease control agent
US20050053594A1 (en) * 1995-11-16 2005-03-10 Dario Alessi RAC-PK as a therapeutic agent or in diagnostics, screening method for agents and process for activating RAC-PK
EP0868195A2 (en) 1995-12-20 1998-10-07 Medical Research Council Control of protein synthesis, and screening method for agents
AU1924099A (en) 1997-12-18 1999-07-05 Lyonnaise Industrielle Pharmaceutique (Lipha) Piperazine derivatives useful as hypoglycemic agents
WO1999035164A1 (en) * 1998-01-09 1999-07-15 Arizona Board Of Regents, A Body Corporate, Acting On Behalf Of Arizona State University Anti-cryptococcal peptides
US6323315B1 (en) * 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
US6852752B2 (en) * 1999-12-17 2005-02-08 Vicuron Pharmaceuticals Inc. Urea compounds, compositions and methods of use and preparation
US6797820B2 (en) * 1999-12-17 2004-09-28 Vicuron Pharmaceuticals Inc. Succinate compounds, compositions and methods of use and preparation
EP1237862A1 (en) 1999-12-17 2002-09-11 Versicor, Inc. Succinate compounds, compositions and methods of use and preparation
US6420400B1 (en) * 2000-04-07 2002-07-16 Kinetek Pharmaceuticals, Inc. Antiproliferative 1,2,3-thiadiazole compounds
AR032653A1 (es) * 2001-02-09 2003-11-19 Telik Inc Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos.
US20040106540A1 (en) * 2001-04-10 2004-06-03 Barnett Stanley F Method of treating cancer
FR2832713B1 (fr) * 2001-11-23 2004-02-13 Sanofi Synthelabo Derives de 4-(1,3,4-thiadiazol-2-yl)-1,4-diazabicyclo[3.2.2] nonane, leur preparation et leur application en therapeutique
EP1496981A2 (en) 2002-04-08 2005-01-19 Merck & Co., Inc. Method of treating cancer
EP1501829B1 (en) * 2002-05-06 2010-11-24 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase
DE60310548T2 (de) 2002-05-07 2007-05-10 Neurosearch A/S Diazabicyclische biarylderivate
GB0218625D0 (en) 2002-08-10 2002-09-18 Astex Technology Ltd Pharmaceutical compounds
US7220741B2 (en) * 2002-09-30 2007-05-22 Neurosearch A/S 1,4-diazabicycloalkane derivatives, their preparation and use
EP1410844A1 (en) * 2002-10-15 2004-04-21 Centre National De La Recherche Scientifique (Cnrs) Silicon-based porous catalytic system for oligomerising light olefins
US20040102360A1 (en) * 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
EP1558607B1 (en) * 2002-10-30 2010-05-05 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of rock and other protein kinases
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
US20050004186A1 (en) * 2002-12-20 2005-01-06 Pfizer Inc MEK inhibiting compounds
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
WO2005014554A1 (en) 2003-08-08 2005-02-17 Astex Therapeutics Limited 1h-indazole-3-carboxamide compounds as mapkap kinase modulators
AU2004267094A1 (en) 2003-08-20 2005-03-03 Vertex Pharmaceuticals Incorporated (4 -amino -1,2, 5-oxadiazol-4-yl) -hetxiroaromatic compounds useful as protein kinase inhibitors
JP2007502828A (ja) * 2003-08-21 2007-02-15 ファイザー・プロダクツ・インク 神経変性性疾患の治療のための化合物
US20050143384A1 (en) * 2003-10-30 2005-06-30 Eric Sartori Amide thiadiazole inhibitors of plasminogen activator inhibitor-1
JP2007510667A (ja) 2003-11-07 2007-04-26 スミスクライン ビーチャム （コーク） リミテッド 癌の治療法
BRPI0508970A (pt) 2004-03-19 2007-08-21 Penn State Res Found método combinatórios e composições para o tratamento de melanoma
US7232820B2 (en) * 2004-04-01 2007-06-19 Pfizer Inc Thiadiazole-amine compounds for the treatment of neurodegenerative disorders
WO2005113762A1 (en) 2004-05-18 2005-12-01 Pfizer Products Inc. CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF
WO2005113579A1 (en) * 2004-05-21 2005-12-01 Mpex Pharmaceuticals, Inc. Bacterial efflux pump inhibitors and methods of treating bacterial infections
JP2008506669A (ja) * 2004-07-16 2008-03-06 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 神経変性疾患の処置に適するピペリジン、ピペラジンもしくはモルホリンの二量体化合物またはそれらの７−員同族体
EA012181B1 (ru) 2004-10-18 2009-08-28 Амген, Инк. Соединения тиадиазола и их применение
EP1805183B1 (en) 2004-10-20 2010-12-29 NeuroSearch A/S Novel diazabicyclic aryl derivatives and their medical use
MY149143A (en) * 2006-01-18 2013-07-15 Amgen Inc Thiazole compounds as protien kinase b (pkb) inhibitors
US20080242694A1 (en) 2006-09-18 2008-10-02 D Sidocky Neil R Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith

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WO2006044860A2 (en) 2006-04-27
WO2006044860A3 (en) 2007-07-05
AU2005295441A1 (en) 2006-04-27
ZA200703975B (en) 2009-01-28
MA29029B1 (fr) 2007-11-01
US7700636B2 (en) 2010-04-20
EP1809282A4 (en) 2009-11-25
JP4931823B2 (ja) 2012-05-16
JP2008516986A (ja) 2008-05-22
ES2400689T3 (es) 2013-04-11
KR20070073791A (ko) 2007-07-10
EA200700886A1 (ru) 2008-02-28
CA2583217A1 (en) 2006-04-27
EA012181B1 (ru) 2009-08-28
CA2583217C (en) 2011-05-31
US7354944B2 (en) 2008-04-08
EP1809282B1 (en) 2013-01-09
IL182203A0 (en) 2007-07-24
AU2005295441B2 (en) 2009-04-23
US20060154961A1 (en) 2006-07-13
BRPI0516609A (pt) 2008-04-29
MX2007004551A (es) 2007-05-23
US20080255145A1 (en) 2008-10-16
US7919514B2 (en) 2011-04-05

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