EA201690094A1 - Ингибиторы syk - Google Patents

Ингибиторы syk

Info

Publication number
EA201690094A1
EA201690094A1 EA201690094A EA201690094A EA201690094A1 EA 201690094 A1 EA201690094 A1 EA 201690094A1 EA 201690094 A EA201690094 A EA 201690094A EA 201690094 A EA201690094 A EA 201690094A EA 201690094 A1 EA201690094 A1 EA 201690094A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
syk
formula
present
syk inhibitors
Prior art date
Application number
EA201690094A
Other languages
English (en)
Other versions
EA031601B1 (ru
Inventor
Кевин С. Карри
Чжиминь Ду
Джули Фаранд
Хуан А. Герреро
Эшли А. Катана
Деррил Катто
Скотт Е. Лазервит
Цзяяо Ли
Джон О. Линк
Николас Май
Грегори Нотт
Хьюн-Цзюн Пюнь
Майкл Санджи
Аарон К. Шмитт
Адам Дж. Шриер
Кирк Л. Стивенс
Чандрасекар Венкатарамани
Уильям Дж. Уоткинс
Чжэн-Юй Ян
Джефф Заблоцки
Шейла Зипфел
Дженнифер Ло
Сёнг Х. Ли
Чжундун Чжао
Джеффри Кропф
Цзяньцзюнь Сюй
Питер Бломгрен
Скотт А. Митчелл
Цзиньмин Сюн
Джаяраман Чандрасекхар
Original Assignee
Джилид Сайэнс, Инк.
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 Джилид Сайэнс, Инк. filed Critical Джилид Сайэнс, Инк.
Publication of EA201690094A1 publication Critical patent/EA201690094A1/ru
Publication of EA031601B1 publication Critical patent/EA031601B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Настоящее изобретение относится к соединениям, которые представляют собой ингибиторы Syk, и к их применению для лечения различных болезненных состояний, в том числе раковых заболеваний и воспалительных состояний. Согласно конкретным вариантам реализации структура соединений представлена формулой Iгде X, X, X, R, R, R, Rи Y такие, как описано в настоящем документе. В настоящем изобретении также предложены фармацевтические композиции, которые включают соединение формулы I или его фармацевтически приемлемые соли, и способы применения указанных соединений и композиций для лечения состояний, опосредованных Syk.
EA201690094A 2013-07-31 2014-07-31 Ингибиторы syk EA031601B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361860870P 2013-07-31 2013-07-31
US201462025304P 2014-07-16 2014-07-16
PCT/US2014/049032 WO2015017610A1 (en) 2013-07-31 2014-07-31 Syk inhibitors

Publications (2)

Publication Number Publication Date
EA201690094A1 true EA201690094A1 (ru) 2016-08-31
EA031601B1 EA031601B1 (ru) 2019-01-31

Family

ID=51359434

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690094A EA031601B1 (ru) 2013-07-31 2014-07-31 Ингибиторы syk

Country Status (16)

Country Link
US (2) US9376441B2 (ru)
EP (1) EP3027601B1 (ru)
JP (1) JP6159028B2 (ru)
KR (1) KR101750667B1 (ru)
CN (1) CN105555780B (ru)
AU (1) AU2014296184B2 (ru)
BR (1) BR112016001954A2 (ru)
CA (1) CA2919479C (ru)
EA (1) EA031601B1 (ru)
ES (1) ES2656192T3 (ru)
IL (1) IL243578A0 (ru)
MX (1) MX2016001427A (ru)
NZ (1) NZ715747A (ru)
PT (1) PT3027601T (ru)
SG (1) SG11201600373YA (ru)
WO (1) WO2015017610A1 (ru)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ593460A (en) 2008-12-08 2013-11-29 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
NZ602362A (en) 2010-03-11 2014-11-28 Gilead Connecticut Inc Imidazopyridines syk inhibitors
AP2016009007A0 (en) 2013-07-30 2016-01-31 Gilead Connecticut Inc Formulation of syk inhibitors
KR101810798B1 (ko) 2013-07-30 2017-12-19 질레드 코네티컷 인코포레이티드 Syk 억제제의 다형체
JP6159028B2 (ja) 2013-07-31 2017-07-05 ギリアード サイエンシーズ, インコーポレイテッド Syk阻害剤
EA201690608A1 (ru) 2013-12-04 2016-12-30 Джилид Сайэнс, Инк. Способы лечения раковых заболеваний
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
UY35898A (es) 2013-12-23 2015-07-31 Gilead Sciences Inc ?compuestos inhibidores de syk y composiciones que los comprenden?.
MX2016011784A (es) * 2014-03-19 2016-12-02 Boehringer Ingelheim Int Nuevos heteroarilos y su uso como medicamentos.
JP6177456B2 (ja) 2014-04-04 2017-08-09 ファイザー・インク 二環式縮合ヘテロアリールまたはアリール化合物およびirak4阻害剤としてのそれらの使用
KR20170029580A (ko) 2014-07-14 2017-03-15 길리애드 사이언시즈, 인코포레이티드 암을 치료하기 위한 조합물
CA2998250A1 (en) * 2015-09-11 2017-03-16 Boehringer Ingelheim International Gmbh Pyrazolyl-substituted heteroaryls and their use as medicaments
CO2018008799A2 (es) 2016-02-24 2018-09-20 Pfizer Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak
CN105646476B (zh) * 2016-03-07 2018-09-04 暨南大学 联苯并[1,2,5]硒二唑衍生物及其制备方法和应用
DK3500568T3 (da) 2016-08-16 2020-12-14 Bayer Cropscience Ag Fremgangsmåde til fremstilling af 2-(3,6-dihalopyridin-2-yl)-3h-imidazol[4,5-c]pyridinderivater og beslægtede forbindelser ved hjælp af omsætning af 3h-imidazol[4,5-c]pyridinderivatet med en metalorganisk zink-amin base
AU2017325844A1 (en) 2016-09-14 2019-03-07 Gilead Sciences, Inc. SYK inhibitors
KR102471278B1 (ko) 2016-09-14 2022-11-25 바이엘 크롭사이언스 악티엔게젤샤프트 할로겐화 바이사이클릭 화합물의 제조 방법
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
WO2018195471A1 (en) 2017-04-21 2018-10-25 Gilead Sciences, Inc. Syk inhibitors in combination with hypomethylating agents
EP3668858A1 (en) 2017-08-14 2020-06-24 Pfizer Inc Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives
CA3073871A1 (en) 2017-08-25 2019-02-28 Gilead Sciences, Inc. Polymorphs of syk inhibitors
EP3636645A1 (de) 2018-10-11 2020-04-15 Bayer Aktiengesellschaft Verfahren zur herstellung schwefel-substituierter pyridinderivate
ES2951539T3 (es) 2018-10-11 2023-10-23 Bayer Ag Procedimiento para la preparación de derivados de imidazol
CA3116347A1 (en) * 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
JP7460644B2 (ja) 2018-10-31 2024-04-02 ギリアード サイエンシーズ, インコーポレイテッド Hpk1阻害剤としての置換6-アザベンゾイミダゾール化合物
KR20210131372A (ko) 2019-02-22 2021-11-02 크로노스 바이오, 인코포레이티드 Syk 억제제로서의 축합된 피라진의 고체 형태
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN113121524B (zh) 2019-12-31 2023-04-25 南京创济生物医药有限公司 杂环亚砜亚胺化合物及其中间体、制备方法和应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021226262A1 (en) * 2020-05-06 2021-11-11 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
AR125588A1 (es) 2021-03-04 2023-08-02 Lilly Co Eli Compuestos inhibidores de fgfr3
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
WO2022271612A1 (en) 2021-06-22 2022-12-29 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
CN113788741B (zh) * 2021-09-28 2023-12-29 大连九信精细化工有限公司 一种制备2-环丙基苯酚衍生物的方法
CN113816889B (zh) * 2021-10-11 2023-08-22 中国药科大学 一类4-磺酰亚胺-1H-吡咯类Mcl-1抑制剂及其抗肿瘤医药用途
WO2024015425A1 (en) 2022-07-14 2024-01-18 Fmc Corporation Herbicidal benzoxazines
CN115197115A (zh) * 2022-08-25 2022-10-18 成都金博汇康医药科技有限公司 一种手性5-氧代吡咯烷-3-甲酸的制备方法与应用

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
CL2007002617A1 (es) * 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
WO2009079011A1 (en) 2007-12-19 2009-06-25 The Scripps Research Institute Benzimidazoles and analogs as rho kinase inhibitors
WO2009102468A1 (en) * 2008-02-13 2009-08-20 Cgi Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 2-a] pyrazine derivatives, method of making, and method of use thereof
EP2324022A1 (de) * 2008-08-05 2011-05-25 Boehringer Ingelheim International GmbH Substituierte naphthyridine und ihre verwendung als arzneimittel
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶,其組合物及使用其之治療方法
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
NZ593460A (en) 2008-12-08 2013-11-29 Gilead Connecticut Inc Imidazopyrazine syk inhibitors
RS55055B1 (sr) 2008-12-08 2016-12-30 Gilead Connecticut Inc Imidazopirazin syk inhibitori
UA107100C2 (xx) 2009-12-23 2014-11-25 Конденсовані гетероароматичні піролідинони як інгібітори syk
NZ602362A (en) 2010-03-11 2014-11-28 Gilead Connecticut Inc Imidazopyridines syk inhibitors
GB201007203D0 (en) * 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
KR20130130729A (ko) * 2010-10-28 2013-12-02 니뽄 신야쿠 가부시키가이샤 피리딘 유도체 및 의약
US20140135319A1 (en) * 2010-12-17 2014-05-15 Bayer Intellectual Property Gmbh 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
AU2012253885A1 (en) * 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
BR112014001898A2 (pt) * 2011-07-26 2017-02-21 Boehringer Ingelheim Int quinolinas substituídas e seu uso como medicamentos
JP6159028B2 (ja) * 2013-07-31 2017-07-05 ギリアード サイエンシーズ, インコーポレイテッド Syk阻害剤
EA201690608A1 (ru) 2013-12-04 2016-12-30 Джилид Сайэнс, Инк. Способы лечения раковых заболеваний
UY35898A (es) 2013-12-23 2015-07-31 Gilead Sciences Inc ?compuestos inhibidores de syk y composiciones que los comprenden?.
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
TW201639573A (zh) 2015-02-03 2016-11-16 吉李德科學股份有限公司 有關治療癌症之合併治療
BR112017022323A2 (pt) 2015-04-21 2018-07-03 Gilead Sciences, Inc. método para tratar doença do enxerto contra hospedeiro, uso de um composto, e, kit.

Also Published As

Publication number Publication date
CA2919479C (en) 2017-08-22
EP3027601B1 (en) 2017-10-25
JP2016529244A (ja) 2016-09-23
AU2014296184A1 (en) 2016-01-28
MX2016001427A (es) 2016-08-03
US9376441B2 (en) 2016-06-28
CN105555780A (zh) 2016-05-04
SG11201600373YA (en) 2016-02-26
US20150038488A1 (en) 2015-02-05
ES2656192T3 (es) 2018-02-26
US20160368918A1 (en) 2016-12-22
WO2015017610A1 (en) 2015-02-05
PT3027601T (pt) 2018-01-08
KR101750667B1 (ko) 2017-07-04
EA031601B1 (ru) 2019-01-31
US10005774B2 (en) 2018-06-26
AU2014296184B2 (en) 2017-04-27
EP3027601A1 (en) 2016-06-08
BR112016001954A2 (pt) 2017-08-01
NZ715747A (en) 2017-03-31
IL243578A0 (en) 2016-02-29
CA2919479A1 (en) 2015-02-05
KR20160037198A (ko) 2016-04-05
CN105555780B (zh) 2018-01-23
JP6159028B2 (ja) 2017-07-05

Similar Documents

Publication Publication Date Title
EA201690094A1 (ru) Ингибиторы syk
EA201891553A1 (ru) Ингибиторы syk
EA201690268A1 (ru) Замещенные производные хиназолин-4-она
EA201790088A1 (ru) Ингибиторы syk
EA201691803A1 (ru) Ингибиторы калликреина плазмы человека
EA201690153A1 (ru) Замещенные бензофуранильные и бензоксазолильные соединения и их применения
EA201691840A1 (ru) Замещенные спироциклические ингибиторы аутотаксина
EA201591296A1 (ru) Фталазиноны и изохинолиноны в качестве ингибиторов rock
EA201790599A1 (ru) Соединения и композиции в качестве ингибиторов киназ
EA201690752A1 (ru) Ингибиторы g12c kras
EA201592199A1 (ru) Производные бипиразола в качестве ингибиторов jak
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA201491012A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201591301A1 (ru) Новые пиримидиновые и пиридиновые соединения и их применение
EA201592255A1 (ru) Производные пиразолопирролидин-4-она в качестве ингибиторов вет и их применение при лечении заболевания
EA201690247A1 (ru) Аминометилбиарильные производные-ингибиторы фактора d комплемента и их применения
EA201491247A1 (ru) Производные дигидробензооксазина и дигидропиридооксазина
EA201491747A1 (ru) Замещенные пиридопиримидиновые соединения и их применение в качестве flt3 ингибиторов
EA201690844A1 (ru) Ингибиторы gsk-3
EA201600636A1 (ru) 2-амино-6-метил-4,4а,5,6-тетрагидропирано[3,4-d][1,3]тиазин-8а(8н)-ил-1,3-тиазол-4-ил амиды
EA201591628A1 (ru) Дейтерированный палбоциклиб
EA201600434A1 (ru) Применение производных бензимидазолпролина
EA201790830A1 (ru) Ингибиторы альдостеронсинтазы
EA201790253A1 (ru) Ингибиторы альдостеронсинтазы
EA201792425A1 (ru) Трициклические соединения и их применение в качестве ингибиторов фосфодиэстераз

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 RU