EA201301301A1 - Производные тиазола - Google Patents

Производные тиазола

Info

Publication number
EA201301301A1
EA201301301A1 EA201301301A EA201301301A EA201301301A1 EA 201301301 A1 EA201301301 A1 EA 201301301A1 EA 201301301 A EA201301301 A EA 201301301A EA 201301301 A EA201301301 A EA 201301301A EA 201301301 A1 EA201301301 A1 EA 201301301A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tiazole
derivatives
tiazole derivatives
ikkε
tbk1
Prior art date
Application number
EA201301301A
Other languages
English (en)
Other versions
EA026654B1 (ru
Inventor
Сриниваса Р. Карра
Вольфганг Штеле
Айке Штауб
Маргарита Вухерер-Плиткер
Original Assignee
Мерк Патент Гмбх
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 Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of EA201301301A1 publication Critical patent/EA201301301A1/ru
Publication of EA026654B1 publication Critical patent/EA026654B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pathology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)

Abstract

Соединения формулы Iв которой R, R, X и Y имеют значения, указанные в п.1, являются ингибиторами ТBK1 и IKKε и могут быть использованы, в частности, для лечения злокачественного новообразования и воспалительных заболеваний.
EA201301301A 2011-05-23 2012-04-12 Производные тиазола EA026654B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161489007P 2011-05-23 2011-05-23
PCT/US2012/033200 WO2012161879A1 (en) 2011-05-23 2012-04-12 Thiazole derivatives

Publications (2)

Publication Number Publication Date
EA201301301A1 true EA201301301A1 (ru) 2014-04-30
EA026654B1 EA026654B1 (ru) 2017-05-31

Family

ID=46026922

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201301301A EA026654B1 (ru) 2011-05-23 2012-04-12 Производные тиазола

Country Status (22)

Country Link
US (1) US9249114B2 (ru)
EP (1) EP2714668B9 (ru)
JP (1) JP6050335B2 (ru)
KR (1) KR101893627B1 (ru)
CN (1) CN103596938B (ru)
AU (1) AU2012259335B2 (ru)
BR (1) BR112013029999B1 (ru)
CA (1) CA2831966C (ru)
DK (1) DK2714668T3 (ru)
EA (1) EA026654B1 (ru)
ES (1) ES2622526T3 (ru)
HR (1) HRP20170499T1 (ru)
IL (1) IL229544A (ru)
LT (1) LT2714668T (ru)
MX (1) MX345127B (ru)
PL (1) PL2714668T3 (ru)
PT (1) PT2714668T (ru)
RS (1) RS56084B1 (ru)
SG (1) SG194107A1 (ru)
SI (1) SI2714668T1 (ru)
WO (1) WO2012161879A1 (ru)
ZA (1) ZA201307428B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014060381A1 (de) * 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
CA2924141C (en) 2013-08-22 2022-06-07 The General Hospital Corporation 5-amino 4-cyano substituted oxazole and thiazole derivatives as inhibitors of human 12/15-lipoxygenase
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CN106715419A (zh) 2014-09-26 2017-05-24 吉利德科学公司 用作tank‑结合激酶抑制剂化合物的氨基三嗪衍生物
WO2016161361A1 (en) * 2015-04-03 2016-10-06 Nantbioscience, Inc. Compositions and methods of targeting mutant k-ras
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CA3006772A1 (en) 2015-12-17 2017-06-22 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
WO2017102091A1 (en) 2015-12-18 2017-06-22 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazole compounds
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
DE102016113714A1 (de) 2016-07-26 2018-02-01 Rosa Karl Transfektionsverfahren mit nicht-viralen Genliefersystemen
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
EP3853225B1 (en) 2018-09-17 2023-11-29 Yungjin Pharm. Co., Ltd. N-(5-(3-(1-((thiazol-2-yl)amino)-1-oxopropan-2-yl)phenyl)pyridin-2-yl)acrylamide derivatives as cdk7 inhibitors for the treatment of cancer

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD261153A1 (de) * 1987-03-19 1988-10-19 Bitterfeld Chemie Verfahren zur herstellung von neuen 2-heteroaryl-5-acylamino-thiazolen
CA2336848A1 (en) * 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
AR030154A1 (es) * 1999-07-05 2003-08-13 Nihon Nohyaku Co Ltd Derivado de ftalamida, derivado de amina heterociclico util como intermediario para la produccion del mismo, insecticida agrohorticola y metodo para utilizar dicho insecticida
WO2003103658A1 (ja) * 2002-06-05 2003-12-18 株式会社医薬分子設計研究所 免疫関連プロテインキナーゼ阻害剤
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
FR2889190A1 (fr) * 2005-08-01 2007-02-02 Merck Sante Soc Par Actions Si Nouveaux derives d'imidazoles carboxamides comme inhibiteurs de fructose -1,6-biphosphatase et compositions pharmaceutiques les contenant
CN101484452A (zh) 2006-05-03 2009-07-15 阿斯利康(瑞典)有限公司 噻唑衍生物及其作为抗肿瘤药物的用途
GB0701426D0 (en) * 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
WO2009030890A1 (en) 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
AU2008315746A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
US20100056524A1 (en) 2008-04-02 2010-03-04 Mciver Edward Giles Compound
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CA2809830C (en) 2010-08-27 2019-09-10 Calcimedica, Inc. Compounds comprising n-acyl-2-amino-1,3-thiazole for modulating intracellular calcium

Also Published As

Publication number Publication date
CN103596938B (zh) 2016-12-28
EP2714668B9 (en) 2017-06-14
ES2622526T3 (es) 2017-07-06
IL229544A (en) 2016-10-31
AU2012259335A1 (en) 2013-10-24
AU2012259335B2 (en) 2017-03-16
EP2714668B1 (en) 2017-01-18
SI2714668T1 (sl) 2017-06-30
BR112013029999B1 (pt) 2021-03-02
JP2014518885A (ja) 2014-08-07
PL2714668T3 (pl) 2017-06-30
PT2714668T (pt) 2017-04-26
KR20140027296A (ko) 2014-03-06
HRP20170499T1 (hr) 2017-06-02
CA2831966C (en) 2016-07-19
DK2714668T3 (en) 2017-03-20
CN103596938A (zh) 2014-02-19
CA2831966A1 (en) 2012-11-29
MX345127B (es) 2017-01-18
RS56084B1 (sr) 2017-10-31
SG194107A1 (en) 2013-11-29
EP2714668A1 (en) 2014-04-09
IL229544A0 (en) 2014-01-30
WO2012161879A1 (en) 2012-11-29
KR101893627B1 (ko) 2018-08-30
EA026654B1 (ru) 2017-05-31
MX2013012977A (es) 2013-12-06
US9249114B2 (en) 2016-02-02
LT2714668T (lt) 2017-04-10
BR112013029999A2 (pt) 2017-01-31
JP6050335B2 (ja) 2016-12-21
US20140148457A1 (en) 2014-05-29
ZA201307428B (en) 2014-12-23

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