EA027418B1 - ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ - Google Patents

ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ Download PDF

Info

Publication number
EA027418B1
EA027418B1 EA201490165A EA201490165A EA027418B1 EA 027418 B1 EA027418 B1 EA 027418B1 EA 201490165 A EA201490165 A EA 201490165A EA 201490165 A EA201490165 A EA 201490165A EA 027418 B1 EA027418 B1 EA 027418B1
Authority
EA
Eurasian Patent Office
Prior art keywords
methyl
triazolo
quinoxaline
chlorophenyl
carboxamide
Prior art date
Application number
EA201490165A
Other languages
English (en)
Russian (ru)
Other versions
EA201490165A1 (ru
Inventor
Хосе Игнасио Андрес-Хиль
Фредерик Ян Рита Ромбаутс
Андрес Авелино Трабанко-Суарес
Грета Констанция Петер Ванхоф
Мери Де Анхелис
Петер Якобус Йоханнес Антониус Бейнстерс
Жером Эмиль Жорж Гийемон
Ги Мориц Р. Борман
Софи Жанн Леопольдин Селен
Мартен Влиген
Original Assignee
Янссен Фармацевтика Нв
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
Application filed by Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201490165A1 publication Critical patent/EA201490165A1/ru
Publication of EA027418B1 publication Critical patent/EA027418B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0463—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/60—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Cell Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biotechnology (AREA)
  • Optics & Photonics (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
EA201490165A 2011-06-27 2012-06-26 ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ EA027418B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11171519 2011-06-27
PCT/EP2012/062381 WO2013000924A1 (en) 2011-06-27 2012-06-26 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES

Publications (2)

Publication Number Publication Date
EA201490165A1 EA201490165A1 (ru) 2014-04-30
EA027418B1 true EA027418B1 (ru) 2017-07-31

Family

ID=44370665

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490165A EA027418B1 (ru) 2011-06-27 2012-06-26 ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ

Country Status (11)

Country Link
US (1) US10604523B2 (https=)
EP (1) EP2723744B1 (https=)
JP (1) JP6115962B2 (https=)
CN (1) CN103619846B (https=)
AU (1) AU2012277912B2 (https=)
BR (1) BR112013033375B1 (https=)
CA (1) CA2838645C (https=)
EA (1) EA027418B1 (https=)
ES (1) ES2575092T3 (https=)
MX (1) MX344600B (https=)
WO (1) WO2013000924A1 (https=)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9540379B2 (en) 2011-01-31 2017-01-10 Boehringer Ingelheim International Gmbh (1,2,4)triazolo[4,3-A]quinoxaline derivatives as inhibitors of phosphodiesterases
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
JP2014526453A (ja) * 2011-09-09 2014-10-06 ハー・ルンドベック・アクチエゼルスカベット ピリジン化合物およびそれらの使用
HK1206250A1 (en) 2012-06-26 2016-01-08 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
BR112015017674A2 (pt) * 2013-01-31 2017-07-11 Hoffmann La Roche compostos rádio marcados
WO2014139983A1 (en) 2013-03-13 2014-09-18 H. Lundbeck A/S [1,2,4]triazolo[4,3-a]quinoxalines as dual pde2/pde10 inhibitors
EP3091983B1 (en) 2014-01-08 2019-10-02 Intra-Cellular Therapies, Inc. Pharmaceutical compositions comprising a pde-1 inhibitor and a pde-2 inhibitor
DK3134413T3 (da) 2014-04-23 2019-10-14 Dart Neuroscience Cayman Ltd Substituerede [1,2,4]triazolo[1,5-a]pyrimidin-7-yl-forbindelser som pde2-inhibitorer
US10239882B2 (en) 2014-11-05 2019-03-26 Dart Neuroscience (Cayman) Ltd. Substituted 5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine compounds as PDE2 inhibitors
CN107205993B (zh) 2014-12-06 2021-03-09 细胞内治疗公司 有机化合物
US10300064B2 (en) 2014-12-06 2019-05-28 Intra-Cellular Therapies, Inc. Organic compounds
WO2016145614A1 (en) 2015-03-17 2016-09-22 Merck Sharp & Dohme Corp. Triazolyl pyrimidinone compounds as pde2 inhibitors
WO2016154081A1 (en) 2015-03-26 2016-09-29 Merck Sharp & Dohme Corp. Pyrazolyl pyrimidinone compounds as pde2 inhibitors
WO2016179059A1 (en) 2015-05-05 2016-11-10 Merck Sharp & Dohme Corp. Heteroaryl-pyrimidinone compounds as pde2 inhibitors
WO2016183741A1 (en) 2015-05-15 2016-11-24 Merck Sharp & Dohme Corp. Pyrimidinone amide compounds as pde2 inhibitors
WO2016191935A1 (en) 2015-05-29 2016-12-08 Merck Sharp & Dohme Corp. 6-alkyl dihydropyrazolopyrimidinone compounds as pde2 inhibitors
WO2016192083A1 (en) 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Dihydropyrazolopyrimidinone compounds as pde2 inhibitors
US10647727B2 (en) 2015-06-25 2020-05-12 Merck Sharp & Dohme Corp. Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors
WO2017000277A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Substituted triazolo bicycliccompounds as pde2 inhibitors
WO2017000276A1 (en) 2015-07-01 2017-01-05 Merck Sharp & Dohme Corp. Bicyclic heterocyclic compounds as pde2 inhibitors
EP3156405A1 (en) 2015-10-13 2017-04-19 Boehringer Ingelheim International GmbH Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxamide
CN108349979B (zh) 2015-11-02 2021-04-09 詹森药业有限公司 [1,2,4]三唑并[1,5-a]嘧啶-7-基化合物
WO2017165311A1 (en) * 2016-03-21 2017-09-28 Perlstein Lab Pbc Fused heterocyclic organic compounds and uses thereof
MY193511A (en) 2016-11-02 2022-10-17 Janssen Pharmaceutica Nv [1,2,4]triazolo[1,5-a]pyrimidine derivatives as pde2 inhibitors
CN109890824B (zh) 2016-11-02 2022-05-24 詹森药业有限公司 作为pde2抑制剂的[1,2,4]三唑并[1,5-a]嘧啶化合物
EA039102B1 (ru) * 2016-11-02 2021-12-03 Янссен Фармацевтика Нв Соединения [1,2,4]триазоло[1,5-a]пиримидина в качестве ингибиторов pde2
CN107827828B (zh) * 2017-11-21 2021-03-30 南京华漫新材料科技有限公司 含苯酰肼骨架的喹喔啉衍生物及其制备方法和在制备抗肿瘤药物中的应用
AU2018371216B2 (en) 2017-11-23 2024-09-19 Oslo University Hospital Hf Treatment of tachycardia

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010138833A1 (en) * 2009-05-29 2010-12-02 Wyeth SUBSTITUTED IMIDAZO[1,5-a]QUINOXALINES AS INHIBITORS OF PHOSPHODIESTERASE 10

Family Cites Families (213)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5584421A (en) 1978-12-21 1980-06-25 Mitsui Cokes Kogyo Kk Method of making fibrous carbon
US4242513A (en) 1979-03-05 1980-12-30 Appleton Papers Inc. Lactone compounds containing a heterocyclic radical
DE3666434D1 (de) 1985-05-25 1989-11-23 Yoshitomi Pharmaceutical Oxodiazine compounds
KR920702621A (ko) 1989-06-13 1992-10-06 스튜어트 알. 슈터 단핵세포 및/또는 마크로파지에 의한 인터루킨-1 또는 종양회사인자 생성의 억제
KR920702606A (ko) 1989-06-13 1992-10-06 스튜어트 알. 슈터 모노킨(Monokine)의 활성저해
AU622330B2 (en) 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
KR910011852A (ko) 1989-12-04 1991-08-07 폴 디. 매튜카이티스 신경독 장해 치료용 이미다조[1,2-a]피리디닐알킬 화합물
KR930700104A (ko) 1990-06-12 1993-03-13 원본미기재 5-리프옥시게나제 및 사이클로옥시게나제 경로 개재된 질병의 억제
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
IE914327A1 (en) 1990-12-13 1992-06-17 Smithkline Beecham Corp Novel csaids
JPH06504779A (ja) 1990-12-13 1994-06-02 スミスクライン・ビーチャム・コーポレイション 新規ｃｓａｉｄｓ
US5683998A (en) 1991-04-23 1997-11-04 Toray Industries, Inc. Tricyclic triazolo derivatives, processes for producing the same and the uses of the same
CN1033327C (zh) 1991-04-23 1996-11-20 东丽株式会社 三环三唑并衍生物的制造方法
DK31093D0 (https=) 1993-03-19 1993-03-19 Novo Nordisk As
US5486525A (en) 1993-12-16 1996-01-23 Abbott Laboratories Platelet activating factor antagonists: imidazopyridine indoles
US5869486A (en) 1995-02-24 1999-02-09 Ono Pharmaceutical Co., Ltd. Fused pyrimidines and pyriazines as pharmaceutical compounds
AU5348396A (en) 1995-05-01 1996-11-21 Fujisawa Pharmaceutical Co., Ltd. Imidazo 1,2-a pyridine and imidazo 1,2-a pyridezine derivati ves and their use as bone resorption inhibitors
US6992188B1 (en) 1995-12-08 2006-01-31 Pfizer, Inc. Substituted heterocyclic derivatives
US20010007867A1 (en) 1999-12-13 2001-07-12 Yuhpyng L. Chen Substituted 6,5-hetero-bicyclic derivatives
JP2001511813A (ja) 1997-02-18 2001-08-14 ニューロクライン バイオサイエンシーズ，インコーポレイテッド Ｃｒｆレセプターアンタゴニストおよびそれらに関連する方法
US6054587A (en) 1997-03-07 2000-04-25 Metabasis Therapeutics, Inc. Indole and azaindole inhibitors of fructose-1,6-bisphosphatase
EP1012151B1 (en) 1997-09-02 2002-08-07 Bristol-Myers Squibb Pharma Company Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders
JP2002519373A (ja) 1998-07-02 2002-07-02 エーザイ株式会社 製薬組成物及びそれらの使用
US6248755B1 (en) 1999-04-06 2001-06-19 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
JP4032566B2 (ja) 1999-06-21 2008-01-16 東レ株式会社 発光素子
JP2001057292A (ja) 1999-08-20 2001-02-27 Toray Ind Inc 発光素子
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
CO5271670A1 (es) 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
CA2398956A1 (en) 2000-02-14 2001-08-16 Japan Tobacco Inc. A pharmaceutical composition for prophylaxis or therapy of a postoperative stress
EP1149583A3 (en) 2000-04-13 2001-11-14 Pfizer Products Inc. Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
WO2002006286A2 (en) 2000-07-14 2002-01-24 Bristol-Myers Squibb Pharma Company IMIDAZO[1,2-a]PYRAZINES FOR THE TREATMENT OF NEUROLOGICAL DISORDERS
WO2002034748A1 (fr) 2000-10-24 2002-05-02 Sankyo Company, Limited Derives d'imidazopyridine
AU2002224927A1 (en) 2000-12-13 2002-06-24 Basf Aktiengesellschaft Use of substituted imidazoazines, novel imidazoazines, methods for the production thereof, and agents containing these compounds
WO2002057425A2 (en) 2001-01-22 2002-07-25 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
SE0100568D0 (sv) 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
EP1423388B1 (en) 2001-02-20 2008-12-03 AstraZeneca AB 2-arylamino-pyrimidines for the treatment of gsk3-related disorders
EP1373240B1 (en) 2001-03-14 2005-06-15 Eli Lilly And Company Retinoid x receptor modulators
US7074801B1 (en) 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
CA2448306A1 (en) 2001-05-30 2002-12-05 Alteon Inc. Method for treating fibrotic diseases or other indications
US6806268B2 (en) 2001-05-30 2004-10-19 Alteon, Inc. Method for treating glaucoma V
WO2003000689A1 (en) 2001-06-21 2003-01-03 Smithkline Beecham Corporation Imidazo`1,2-a!pyridine derivatives for the prophylaxis and treatment of herpes viral infections
CA2450555A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
ES2262893T3 (es) 2001-10-05 2006-12-01 Smithkline Beecham Corporation Derivados de imidazo-piridina para su uso en el tratamiento de infeccion virica por herpes.
JP2005529067A (ja) 2002-01-22 2005-09-29 メルク　エンド　カムパニー　インコーポレーテッド ケモカイン受容体ｃｃｒ５モジュレータによるストレス応答の治療
DK1483265T3 (da) 2002-03-05 2007-03-19 Lilly Co Eli Purinderivater som kinaseinhibitorer
JP2003313126A (ja) 2002-04-23 2003-11-06 Sankyo Co Ltd イミダゾピリジン誘導体を有効成分とする医薬
JP2004002826A (ja) 2002-04-24 2004-01-08 Sankyo Co Ltd 高分子イミダゾピリジン誘導体
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
US20040014957A1 (en) 2002-05-24 2004-01-22 Anne Eldrup Oligonucleotides having modified nucleoside units
WO2004013135A1 (en) 2002-07-31 2004-02-12 Smithkline Beecham Corporation 2-phenylpyridin-4-yl derivatives as alk5 inhibitors
GB0217783D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Compounds
WO2004014900A1 (en) 2002-08-09 2004-02-19 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
US7312341B2 (en) 2002-09-09 2007-12-25 Cgi Pharmaceuticals, Inc. 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof
EP1539749A4 (en) 2002-09-13 2007-06-13 Merck & Co Inc BY CONDENSED HETEROBICYCLOGRUPPEN SUBSTITUTED PHENYL COMPOUNDS AS METOBOTROPE GLUTAMATE-5 MODULATORS
ATE378336T1 (de) 2002-09-19 2007-11-15 Schering Corp Imidazopyridine als hemmstoffe cyclin abhängiger kinasen
TW200413378A (en) 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
US7186740B2 (en) 2002-09-23 2007-03-06 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
US7576085B2 (en) 2002-09-23 2009-08-18 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
WO2004035579A1 (ja) 2002-10-15 2004-04-29 Takeda Pharmaceutical Company Limited イミダゾピリジン誘導体、その製造法および用途
HUE033832T2 (en) 2002-11-15 2018-01-29 Idenix Pharmaceuticals Llc 2'-methyl nucleosides in combination with interferon and Flaviviridae mutation
AU2003284596A1 (en) 2002-11-22 2004-06-18 Takeda Pharmaceutical Company Limited Imidazole derivative, process for producing the same, and use
WO2004063159A1 (ja) 2003-01-10 2004-07-29 Idemitsu Kosan Co., Ltd. 含窒素複素環誘導体及びそれを用いた有機エレクトロルミネッセンス素子
WO2004072081A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
WO2004075846A2 (en) 2003-02-25 2004-09-10 Bristol-Myers Squibb Company Pyrazolopurine-based tricyclic compounds and pharmaceutical compositions comprising same
PA8595001A1 (es) 2003-03-04 2004-09-28 Pfizer Prod Inc Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf)
US7041671B2 (en) 2003-04-02 2006-05-09 Pfizer Inc Pyrrolo[1,2-b]pyridazine compounds and their uses
US20060094699A1 (en) 2003-04-11 2006-05-04 Kampen Gita Camilla T Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy
JP2006522750A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ 代謝性症候群ならびに関連の疾患および障害を治療するために、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤および抗高血圧剤を使用する併用療法
US20060100235A1 (en) 2003-04-11 2006-05-11 Novo Nordisk A/S Pharmaceutical use of substituted 1,2,4-triazoles
WO2004103991A1 (en) 2003-05-20 2004-12-02 'chemical Diversity Research Institute', Ltd. 2-substituted piperidines, focused library and a pharmaceutical compound
WO2005020885A2 (en) 2003-05-21 2005-03-10 Isis Pharmaceuticals, Inc. Compositions and methods for the treatment of severe acute respiratory syndrome (sars)
EP1630152A4 (en) 2003-05-30 2009-09-23 Takeda Pharmaceutical CONDENSED CYCLIC COMPOUND
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7259164B2 (en) 2003-08-11 2007-08-21 Cgi Pharmaceuticals, Inc. Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
KR100553752B1 (ko) 2003-10-13 2006-02-20 삼성에스디아이 주식회사 이미다졸 고리 함유 화합물 및 이를 이용한 유기 전계발광 소자
JP2007509960A (ja) 2003-10-28 2007-04-19 セプラコア インコーポレーテッド イミダゾ［１，２−ａ］ピリジン抗不安薬
US20050288295A1 (en) 2003-11-11 2005-12-29 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
US20090023737A1 (en) 2004-02-12 2009-01-22 Neurogen Corporation Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
JP2005343889A (ja) 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
WO2005120513A1 (en) 2004-06-09 2005-12-22 Oncalis Ag Protein kinase inhibitors
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
US7718801B2 (en) 2004-08-31 2010-05-18 Banyu Pharmaceutical Co., Ltd. Substituted imidazole derivative
EP1804801A2 (en) 2004-10-15 2007-07-11 Biogen Idec MA, Inc. Methods of treating vascular injuries
CN101083996A (zh) 2004-10-28 2007-12-05 Irm责任有限公司 作为hedgehog途径调节剂的化合物和组合物
EP1813613B1 (en) 2004-11-08 2012-12-19 Msd K.K. Novel fused imidazole derivative
CA2587192A1 (en) 2004-11-10 2006-05-18 Cgi Pharmaceuticals, Inc. Imidazo[1 , 2-a] pyrazin-8-ylamines useful as modulators of kinase activity
JP2008524255A (ja) 2004-12-17 2008-07-10 スミスクライン ビーチャム コーポレーション 化学物質
US20080167314A1 (en) 2004-12-28 2008-07-10 Osamu Uchikawa Condensed Imidazole Compound And Use Thereof
AU2006218403A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
US7666880B2 (en) 2005-03-21 2010-02-23 S*Bio Pte Ltd. Imidazo[1,2-A]pyridine derivatives: preparation and pharmaceutical applications
AU2006227300B2 (en) 2005-03-21 2012-02-02 Eli Lilly And Company Imidazopyridazine compounds
PE20061110A1 (es) 2005-03-24 2006-10-20 Glaxo Group Ltd Derivados de imidazopiridina como antagonistas de la bomba de acido (apa)
WO2006107784A1 (en) 2005-04-05 2006-10-12 Eli Lilly And Company Imidazopyridazine compounds
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
GB0513423D0 (en) 2005-06-30 2005-08-03 Glaxo Group Ltd Novel compounds
AU2006268908A1 (en) 2005-07-11 2007-01-18 Novartis Ag Indolylmaleimide derivatives
JP2009502734A (ja) 2005-07-29 2009-01-29 アステラス製薬株式会社 Ｌｃｋ阻害剤としての縮合複素環
US20070185063A1 (en) 2005-08-23 2007-08-09 Idenix Pharmaceuticals, Inc. Seven-membered ring nucleosides
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
US7709468B2 (en) 2005-09-02 2010-05-04 Abbott Laboratories Imidazo based heterocycles
US7723336B2 (en) 2005-09-22 2010-05-25 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
AU2006298829B2 (en) 2005-09-27 2011-03-03 F. Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mGluR2 antagonists
WO2007036732A1 (en) 2005-09-30 2007-04-05 Astrazeneca Ab Imidazo [1,2-a] pyridine having anti-cell-proliferation activity
JO2769B1 (en) 2005-10-26 2014-03-15 جانسين فارماسوتيكا ان. في Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor
EP1945216A1 (en) 2005-11-10 2008-07-23 Schering Corporation Methods for inhibiting protein kinases
TW200804386A (en) 2005-11-10 2008-01-16 Schering Corp Imidazopyrazines as protein kinase inhibitors
EP1959962A2 (en) 2005-12-16 2008-08-27 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
AU2007208358A1 (en) 2006-01-23 2007-08-02 Vertex Pharmaceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
JP2009524689A (ja) 2006-01-25 2009-07-02 スミスクライン ビーチャム コーポレーション 化合物
EP1993539A4 (en) 2006-03-02 2010-05-19 Glaxosmithkline Llc THIAZOLONE AS A PI3 KINASE INHIBITOR
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
AR061229A1 (es) 2006-06-06 2008-08-13 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa
ITVA20060041A1 (it) 2006-07-05 2008-01-06 Dialectica Srl Uso di composti derivati amminotiazolici, di loro composizioni farmaceutiche, nel trattamento di malattie caratterizzate dalla anormale repressione della trascrizione genica, particolarmente il morbo di huntington
EP2044061A2 (en) 2006-07-20 2009-04-08 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
WO2008014219A2 (en) 2006-07-24 2008-01-31 Smithkline Beecham Corporation Thiozolidinedione derivatives as p13 kinase inhibitors
WO2008027812A2 (en) 2006-08-28 2008-03-06 Forest Laboratories Holdings Limited Imidazopyridine and imidazopyrimidine derivatives
US8268809B2 (en) 2006-09-05 2012-09-18 Emory University Kinase inhibitors for preventing or treating pathogen infection and method of use thereof
WO2008030795A2 (en) 2006-09-05 2008-03-13 Boards Of Regents, The University Of Texas System Compositions and methods for inhibition of tyrosine kinases
CA2663091A1 (en) 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
WO2008063287A2 (en) 2006-10-06 2008-05-29 Abbott Laboratories Novel imidazothiazoles and imidazoxazoles
WO2008053285A1 (en) 2006-10-30 2008-05-08 Draximage Limited Methods for preparing 2-methoxyisobutylisonitrile and tetrakis(2-methoxyisobutylisonitrile)copper(i) tetrafluoroborate
WO2008057402A2 (en) 2006-11-02 2008-05-15 Cytovia, Inc. N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof
PE20080931A1 (es) 2006-11-08 2008-07-19 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
AU2007321923A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
US7622584B2 (en) 2006-11-24 2009-11-24 Samsung Mobile Display Co., Ltd. Imidazopyridine-based compound and organic light emitting diode including organic layer comprising the imidazopyridine-based compound
ATE507225T1 (de) 2006-12-04 2011-05-15 Astrazeneca Ab Antibakterielle polycyclische harnstoffverbindungen
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
WO2008088692A2 (en) 2007-01-12 2008-07-24 Merck & Co., Inc. Spirochromanon derivatives
US20080242862A1 (en) 2007-03-27 2008-10-02 Calderwood David J Novel imidazo based heterocycles
US20100144751A1 (en) 2007-03-28 2010-06-10 Array Biopharma Inc. IMIDAZO[1,2-a]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
EP2137184B1 (en) 2007-04-03 2013-05-08 Array Biopharma, Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
BRPI0809567A2 (pt) 2007-04-10 2014-09-23 Lundbeck & Co As H Composto, composição farmacêutica, método para modular a atividade de um receptor de p2x7, para tratar uma condição responsiva à modulação do receptor de p2x7 em um paciente, para inibir a morte de células do gânglio retinal em um paciente, e para determinar a presença ou ausência do receptor de p2x7 em uma amostra, preparação farmacêutica acondiciaonada, e, uso de um composto
WO2008133192A1 (ja) 2007-04-19 2008-11-06 Takeda Pharmaceutical Company Limited 縮合イミダゾール化合物およびその用途
WO2008134553A1 (en) 2007-04-26 2008-11-06 Xenon Pharmaceuticals Inc. Methods of using bicyclic compounds in treating sodium channel-mediated diseases
CA2684932A1 (en) 2007-05-09 2008-11-20 Novartis Ag Substituted imidazopyridazines as pi3k lipid kinase inhibitors
CA2685520A1 (en) 2007-05-10 2008-11-20 Biocryst Pharmaceuticals, Inc. Tetrahydrofuro [3 4-d] dioxolane compounds for use in the treatment of viral infections and cancer
US20100216779A1 (en) 2007-06-01 2010-08-26 Glaxosmithkline Llc Imidazopyridine Kinase Inhibitors
MX2009013729A (es) 2007-06-14 2010-01-25 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa.
KR101030007B1 (ko) 2007-06-15 2011-04-20 삼성모바일디스플레이주식회사 헤테로방향환 함유 화합물, 이의 제조 방법 및 이를 이용한유기 발광 소자
EP2170882A1 (en) 2007-06-26 2010-04-07 Gilead Colorado, Inc. Imidazopyridinyl thiazolyl histone deacetylase inhibitors
FR2918061B1 (fr) 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
WO2009005675A1 (en) 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
FR2918986B1 (fr) 2007-07-19 2009-09-04 Sanofi Aventis Sa Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique
CA2693817A1 (en) 2007-07-27 2009-02-05 Actelion Pharmaceuticals Ltd Trans-3-aza-bicyclo[3.1.0]hexane derivatives
KR20100042287A (ko) 2007-07-31 2010-04-23 쉐링 코포레이션 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물
WO2009023179A2 (en) 2007-08-10 2009-02-19 Genelabs Technologies, Inc. Nitrogen containing bicyclic chemical entities for treating viral infections
UY31292A1 (es) 2007-08-14 2009-03-31 Imidazoles biciclicos fusionados
WO2009023253A2 (en) 2007-08-15 2009-02-19 Arena Pharmaceuticals Inc. IMIDAZO[L,2-α]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
GB0716292D0 (en) 2007-08-21 2007-09-26 Biofocus Dpi Ltd Imidazopyrazine compounds
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
EP2217069A4 (en) 2007-11-09 2012-03-14 Salk Inst For Biological Studi INHIBITORS OF NON-NUCLEOSIDE INHIBITORS OF THE REVERSE TRANSCRIPTASE
KR20100110804A (ko) * 2007-11-30 2010-10-13 와이어쓰 엘엘씨 포스포디에스테라제 10의 저해물질로서의 아릴 및 헤테로아릴 융합된 이미다조[1,5-ａ]피라진
CA2708361C (en) 2007-12-14 2016-06-07 F. Hoffmann-La Roche Ag Novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives
AU2008345681A1 (en) 2007-12-21 2009-07-09 Wyeth Llc Imidazo [1,2-a] pyridine compounds
JP5355421B2 (ja) 2007-12-21 2013-11-27 出光興産株式会社 有機エレクトロルミネッセンス素子
US20100331333A1 (en) 2007-12-21 2010-12-30 Wyeth Llc Imidazo [1,2-B] Pyridazine Compounds
FR2926556B1 (fr) 2008-01-22 2010-02-19 Sanofi Aventis Derives de carboxamides n-azabicycliques, leur preparation et leur application en therapeutique
CA2710929A1 (en) 2008-01-28 2009-08-06 Schering Corporation Imidazopyrazines as protein kinase inhibitors
WO2009108546A1 (en) 2008-02-26 2009-09-03 Merck & Co., Inc. Ahcy hydrolase inhibitors for treatment of hyper homocysteinemia
ES2413806T3 (es) 2008-03-20 2013-07-17 Amgen Inc. Moduladores de la aurora cinasa y método de uso
DE102008017853A1 (de) 2008-04-09 2009-10-15 Merck Patent Gmbh Thienopyrimidine
TW201000107A (en) 2008-04-09 2010-01-01 Infinity Pharmaceuticals Inc Inhibitors of fatty acid amide hydrolase
ES2398684T3 (es) 2008-04-23 2013-03-21 Gilead Sciences, Inc. Análogos de carbanucleósido para el tratamiento antiviral
WO2010036407A2 (en) 2008-05-15 2010-04-01 Biocryst Pharmaceuticals, Inc. Antiviral nucleoside analogs
CA2724842A1 (en) 2008-05-19 2009-11-26 Sunovion Pharmaceuticals Inc. Imidazo[1,2-a]pyridine compounds
CN102112475A (zh) 2008-05-29 2011-06-29 西特里斯药业公司 作为沉默调节蛋白调节剂的咪唑并吡啶和相关的类似物
AR072008A1 (es) 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
ES2605815T3 (es) 2008-07-01 2017-03-16 Ptc Therapeutics, Inc. Moduladores de la expresión de la proteína Bmi-1
NZ602832A (en) 2008-07-14 2014-04-30 Gilead Sciences Inc Fused heterocyclic hdac inhibitor compounds
US8476430B2 (en) 2008-07-24 2013-07-02 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
ES2378513T3 (es) 2008-08-06 2012-04-13 Pfizer Inc. Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1
FR2934994B1 (fr) 2008-08-12 2010-09-17 Sanofi Aventis Derives de 2-alkyl-6cycloamino-3-(pyridin-4-yl)imidaz°1,2-b! pyridazine, leur preparation et leur application en therapeutique
US8198449B2 (en) 2008-09-11 2012-06-12 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2010033906A2 (en) 2008-09-19 2010-03-25 President And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
JP5416944B2 (ja) 2008-10-23 2014-02-12 ユー・ディー・シー アイルランド リミテッド 有機電界発光素子
US20100120762A1 (en) 2008-11-07 2010-05-13 Wyeth Triazine derivatives as inhibitors of phosphodiesterases
WO2010059838A2 (en) 2008-11-20 2010-05-27 Decode Genetics Ehf Pde4 inhibitors selective for the long form of pde4 for treating inflammation and avoiding side effects
WO2010059836A1 (en) 2008-11-20 2010-05-27 Decode Genetics Ehf Substituted aza-bridged bicyclics for cardiovascular and cns disease
GB0822981D0 (en) 2008-12-17 2009-01-21 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
ES2397934T3 (es) * 2008-12-17 2013-03-12 Amgen Inc. Compuestos de aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10
JP5210187B2 (ja) 2009-01-22 2013-06-12 ユー・ディー・シー アイルランド リミテッド 有機電界発光素子
EP2210891A1 (en) 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
WO2010088518A2 (en) 2009-01-31 2010-08-05 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US20110305637A1 (en) 2009-02-24 2011-12-15 Janssen Pharmaceutica N.V. Radiolabelled pde10 ligands
US8367222B2 (en) 2009-02-27 2013-02-05 Idemitsu Kosan Co., Ltd. Organic electroluminescent device
WO2010101230A1 (ja) 2009-03-05 2010-09-10 アステラス製薬株式会社 キノキサリン化合物
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
US8604466B2 (en) 2009-03-24 2013-12-10 Idemitsu Kosan Co., Ltd. Organic electroluminescent element
SG175195A1 (en) 2009-04-16 2011-11-28 Ct Nac Investigaciones Oncologicas Cnio Imidazopyrazines for use as kinase inhibitors
TW201107329A (en) 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
KR101732289B1 (ko) 2009-08-19 2017-05-02 이데미쓰 고산 가부시키가이샤 방향족 아민 유도체 및 그것을 이용한 유기 전기발광 소자
PH12012500778A1 (en) 2009-10-30 2012-11-26 Janssen Pharmaceutica Nv IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
JP5739815B2 (ja) 2009-11-16 2015-06-24 出光興産株式会社 芳香族アミン誘導体及びそれを用いた有機エレクトロルミネッセンス素子
EP2526102B1 (en) 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III Inhibitors of PI3 kinase
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
US9540379B2 (en) 2011-01-31 2017-01-10 Boehringer Ingelheim International Gmbh (1,2,4)triazolo[4,3-A]quinoxaline derivatives as inhibitors of phosphodiesterases
WO2012146644A1 (en) 2011-04-28 2012-11-01 Janssen Pharmaceutica Nv Salt of an inhibitor of phosphodiesterase 10 enzyme
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
JP2014526453A (ja) 2011-09-09 2014-10-06 ハー・ルンドベック・アクチエゼルスカベット ピリジン化合物およびそれらの使用
WO2013034755A1 (en) 2011-09-09 2013-03-14 H. Lundbeck A/S Triazolopyrazine derivatives and their use for treating neurological and psychiatric disorders
WO2014009305A1 (en) 2012-07-09 2014-01-16 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010138833A1 (en) * 2009-05-29 2010-12-02 Wyeth SUBSTITUTED IMIDAZO[1,5-a]QUINOXALINES AS INHIBITORS OF PHOSPHODIESTERASE 10

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DALIP KUMAR, KONDAPALLI V G CHANDRA SEKHAR, HARMEET DHILLON, VAJJA S RAO AND RAJENDER S VARMA: "An expeditious synthesis of 1-aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines under solvent-free conditions using iodobenzene diacetate", GREEN CHEMISTRY, ROYAL SOCIETY OF CHEMISTRY, GB, vol. 6, no. 3, 1 January 2004 (2004-01-01), GB, pages 156 - 157, XP002657376, ISSN: 1463-9262, DOI: 10.1039/B315031C *
RANJANA AGGARWAL AND GARIMA SUMRAN: "Hypervalent Iodine-Mediated Synthesis of 1-Aryl-4-methyl-1,2,4-triazolo[4,3-a]quinoxalines by Oxidative Cyclization of Arene Carbaldehyde-3-methylquinoxalin-2-yl Hydrazones", SYNTHETIC COMMUNICATIONS, TAYLOR & FRANCIS INC., PHILADELPHIA, PA; US, vol. 36, no. 13, 1 January 2006 (2006-01-01), PHILADELPHIA, PA; US, pages 1873 - 1878, XP002657377, ISSN: 0039-7911, DOI: 10.1080/00397910600602586 *

Also Published As

Publication number Publication date
CN103619846B (zh) 2016-08-17
US20140147386A1 (en) 2014-05-29
MX344600B (es) 2016-12-20
AU2012277912B2 (en) 2017-03-23
ES2575092T3 (es) 2016-06-24
US10604523B2 (en) 2020-03-31
JP6115962B2 (ja) 2017-04-19
CA2838645C (en) 2020-03-10
BR112013033375A2 (pt) 2016-09-06
EP2723744A1 (en) 2014-04-30
AU2012277912A1 (en) 2013-12-19
EP2723744B1 (en) 2016-03-23
JP2014518234A (ja) 2014-07-28
MX2013015201A (es) 2014-02-17
CA2838645A1 (en) 2013-01-03
EA201490165A1 (ru) 2014-04-30
BR112013033375B1 (pt) 2022-05-10
CN103619846A (zh) 2014-03-05
WO2013000924A1 (en) 2013-01-03

Similar Documents

Publication Publication Date Title
EA027418B1 (ru) ПРОИЗВОДНЫЕ 1-АРИЛ-4-МЕТИЛ[1,2,4]ТРИАЗОЛО[4,3-a]ХИНОКСАЛИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, СПОСОБЫ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ ИХ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ
EP2300481B1 (en) Novel substituted azabenzoxazoles
RU2655172C2 (ru) Пиридинилпиразолохинолиновые соединения
JP6076370B2 (ja) ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（トランス）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オンの薬剤組成物、その固体形態、およびその使用方法
JP2023516291A (ja) エストロゲン受容体関連疾患の治療方法
EA011033B1 (ru) 3-замещенные-2(арилалкил)-1-азабициклоалканы и способы их применения
CN102918031A (zh) 放射标记的化合物及其方法
EA020564B1 (ru) Замещенные n-фенил-1-(4-пиридинил)-1н-пиразол-3-амины
CA3129516A1 (en) Low affinity poly(ad-ribose) polymerase 1 dependent cytotoxic agents
JP2023512762A (ja) ムスカリン性受容体４アンタゴニストおよび使用方法
JP7742517B2 (ja) Ｍｙｔ１阻害活性を有する含窒素複素環化合物
RU2657540C2 (ru) Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств
JP7773233B2 (ja) Ｐｅｔ放射性トレーサとしての［１８ｆ］標識イミダゾピリジン誘導体
CA2749261A1 (en) Combination therapies for neoplastic disorders
WO2025064492A1 (en) Trpm8 antagonist for treating cancer
JP2020526532A (ja) ２−オキソ−１，３−オキサゾリジニルイミダゾチアジアゾール誘導体

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM