EA201692249A1 - Ингибиторы фосфатидилинозитол-3-киназы - Google Patents

Ингибиторы фосфатидилинозитол-3-киназы

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Publication number
EA201692249A1
EA201692249A1 EA201692249A EA201692249A EA201692249A1 EA 201692249 A1 EA201692249 A1 EA 201692249A1 EA 201692249 A EA201692249 A EA 201692249A EA 201692249 A EA201692249 A EA 201692249A EA 201692249 A1 EA201692249 A1 EA 201692249A1
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EA
Eurasian Patent Office
Prior art keywords
phosphatidylinositol
compounds
kinase inhibitors
tautomers
isomers
Prior art date
Application number
EA201692249A
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English (en)
Inventor
Шаопэй Цай
Чжиминь Ду
Джошуа Каплан
Дженнифер А. Лойер-Дрю
Деван Надутхамби
Бартон В. Филлипс
Гэри Филлипс
Джошуа Ван Вельдхьюзен
Уильям Дж. Уотксинс
Сот Чон Ён
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.)
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Publication date
Application filed by Джилид Сайэнс, Инк. filed Critical Джилид Сайэнс, Инк.
Publication of EA201692249A1 publication Critical patent/EA201692249A1/ru

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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

В настоящей заявке предложены соединения формулы (J)или их фармацевтически приемлемые соли, изомеры, таутомеры или их смеси, где W, В, n, m, A', R, Rи Rописаны в настоящей заявке. Соединения представляют собой ингибиторы активности фосфатидилинозитол-3-киназы (PI3K) и подходят для лечения состояний, опосредованных одной или более изоформами PI3K. В настоящей заявке дополнительно предложены фармацевтические композиции, содержащие соединение формулы (I) или его фармацевтически приемлемые соли, изомеры, таутомеры или их смеси, и способы применения указанных соединений и композиций для лечения состояний, опосредованных одной или более изоформами PI3K.
EA201692249A 2014-06-13 2015-06-10 Ингибиторы фосфатидилинозитол-3-киназы EA201692249A1 (ru)

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US201462012222P 2014-06-13 2014-06-13
PCT/US2015/035157 WO2015191752A1 (en) 2014-06-13 2015-06-10 Phosphatidylinositol 3-kinase inhibitors

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EA201692249A1 true EA201692249A1 (ru) 2017-05-31

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US (1) US10092563B2 (ru)
EP (1) EP3154958B1 (ru)
JP (1) JP6454736B2 (ru)
KR (1) KR20170012557A (ru)
CN (1) CN106458932A (ru)
AR (1) AR100809A1 (ru)
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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112016028814A2 (pt) 2014-06-13 2017-08-22 Gilead Sciences Inc ?composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição de reações imunitárias ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, composto, um sal, um isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, de um sal, de um isômero, ou de uma mistura farmaceuticamente aceitável do mesmo?
SG11201610095SA (en) 2014-06-13 2016-12-29 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
CA2952012A1 (en) * 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
KR20170010063A (ko) 2014-06-13 2017-01-25 길리애드 사이언시즈, 인코포레이티드 포스파티딜이노시톨 3-키나제 억제제
NZ726055A (en) 2014-06-13 2018-04-27 Gilead Sciences Inc Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors
EP3164400A1 (en) 2014-07-04 2017-05-10 Lupin Limited Quinolizinone derivatives as pi3k inhibitors
KR20230130175A (ko) 2014-12-26 2023-09-11 에모리 유니버시티 Ｎ4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도
ES2656225T3 (es) * 2015-03-04 2018-02-26 Gilead Sciences, Inc. Receptor de tipo toll que modula compuestos de 4,6-diamino-pirido[3,2-d]pirimidina
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
KR102268448B1 (ko) 2016-09-02 2021-06-22 길리애드 사이언시즈, 인코포레이티드 톨 유사 수용체 조정제 화합물
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
US20200317660A1 (en) * 2017-11-13 2020-10-08 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Quinazolinone Compound and Application Thereof
CN111372592A (zh) 2017-12-07 2020-07-03 埃默里大学 N4-羟基胞苷及衍生物和与其相关的抗病毒用途
US10751339B2 (en) 2018-01-20 2020-08-25 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
CN108546268B (zh) * 2018-05-28 2019-04-09 西安培华学院 用于治疗动脉粥样硬化的化合物及其应用
CN109593066B (zh) * 2018-12-21 2020-06-19 上海交通大学 一种用于治疗肠道细菌感染的叶酸拮抗剂及其制备与应用
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202210480A (zh) 2019-04-17 2022-03-16 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202115056A (zh) 2019-06-28 2021-04-16 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2263501T3 (es) 1999-10-27 2006-12-16 Cytokinetics, Inc. Procedimiento y composiciones que utilizan quinazolinonas.
DK1939203T3 (en) 2000-04-25 2015-02-23 Icos Corp INHIBITORS OF HUMAN phosphatidyl-inositol 3-kinase DELTA ISOFORM
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
CN102229609A (zh) 2004-05-13 2011-11-02 艾科斯有限公司 作为人磷脂酰肌醇3-激酶δ抑制剂的喹唑啉酮
ITRM20040139U1 (it) * 2004-08-26 2004-11-26 Salice Arturo Spa Cerniera con spinta in apertura per mobili con cornice.
AU2006214190A1 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
SG10201605472WA (en) 2008-01-04 2016-09-29 Intellikine Llc Certain Chemical Entities, Compositions And Methods
US8399460B2 (en) 2009-10-27 2013-03-19 Astrazeneca Ab Chromenone derivatives
RU2573569C2 (ru) 2009-12-22 2016-01-20 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона
WO2011146882A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
AU2011302196B2 (en) 2010-09-14 2016-04-28 Exelixis, Inc. Inhibitors of PI3K-delta and methods of their use and manufacture
MX337662B (es) 2010-10-06 2016-03-14 Glaxosmithkline Llc Derivados de bencimidazol como inhibidores de cinasa pi3.
HUE030393T2 (en) 2010-12-28 2017-05-29 Sanofi Sa New pyrimidine derivatives, a process for their preparation, and their pharmaceutical use as inhibitors of AKT (PKB) phosphorylation
RU2014111823A (ru) 2011-08-29 2015-10-10 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения и их применения
SG11201501173SA (en) * 2012-08-08 2015-05-28 Kbp Biosciences Co Ltd PI3Kδ INHIBITOR
BR112015014585A2 (pt) 2012-12-21 2017-07-11 Gilead Calistoga Llc composto, composição farmacêutica, e, método de tratamento de um ser humano
WO2014100767A1 (en) 2012-12-21 2014-06-26 Gilead Calistoga Llc Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors
WO2014128612A1 (en) * 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
TWI644909B (zh) 2013-06-14 2018-12-21 基利科學股份有限公司 磷脂酸肌醇３－激酶抑制劑
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
MX2016003457A (es) 2013-09-22 2017-05-25 Calitor Sciences Llc Compuestos aminopirimidina sustituidos y metodos de uso.
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US20150148345A1 (en) 2013-11-26 2015-05-28 Gilead Sciences, Inc. Therapies for treating myeloproliferative disorders
CN103728782A (zh) * 2013-12-31 2014-04-16 深圳市华星光电技术有限公司 一种液晶显示装置及相应的制造方法
WO2015168079A1 (en) 2014-04-29 2015-11-05 Infinity Pharmaceuticals, Inc. Pyrimidine or pyridine derivatives useful as pi3k inhibitors
KR20170010063A (ko) 2014-06-13 2017-01-25 길리애드 사이언시즈, 인코포레이티드 포스파티딜이노시톨 3-키나제 억제제
SG11201610095SA (en) 2014-06-13 2016-12-29 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
BR112016028814A2 (pt) 2014-06-13 2017-08-22 Gilead Sciences Inc ?composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição de reações imunitárias ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, composto, um sal, um isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, de um sal, de um isômero, ou de uma mistura farmaceuticamente aceitável do mesmo?
NZ726055A (en) 2014-06-13 2018-04-27 Gilead Sciences Inc Quinazolinone derivatives as phosphatidylinositol 3-kinase inhibitors
CA2952012A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
SG11201610341PA (en) 2014-06-24 2017-01-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors

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