AR100809A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de fosfatidilinositol 3-quinasa

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Publication number
AR100809A1
AR100809A1 ARP150101859A ARP150101859A AR100809A1 AR 100809 A1 AR100809 A1 AR 100809A1 AR P150101859 A ARP150101859 A AR P150101859A AR P150101859 A ARP150101859 A AR P150101859A AR 100809 A1 AR100809 A1 AR 100809A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
carbon atoms
alkyl
substituted carbon
haloalkyl
Prior art date
Application number
ARP150101859A
Other languages
English (en)
Inventor
Chung Yeung Suet
j watkins William
Van Veldhuizen Joshua
Phillips Gary
W Phillips Barton
Naduthambi Devan
A Loyer-Drew Jennifer
Kaplan Joshua
Du Zhimin
Cai Shaopei
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR100809A1 publication Critical patent/AR100809A1/es

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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 or sparfloxacin
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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Abstract

Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), en donde: n es 0, 1, 2, ó 3; m es 0, 1, ó 2; A es un enlace sencillo o C(O); B es heterocicloalquilo de tres a diez miembros que tiene al menos un heteroátomo seleccionado de N ó O, en donde heterocicloalquilo está sustituido opcionalmente con halo, alquilo de uno a seis átomos de carbono sustituido opcionalmente, heterocicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente, C₁₋₆ haloalquilo, y cicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente; cada R¹ es seleccionado independientemente de halo, ciano, alquilo de uno a seis átomos de carbono sustituido opcionalmente, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alcoxi de uno a seis átomos de carbono sustituido opcionalmente, sulfonilo sustituido opcionalmente, arilo de tres a ocho átomos de carbono sustituido opcionalmente, heteroarilo de tres a ocho átomos de carbono sustituido opcionalmente, cicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente, y heterocicloalquilo de tres a ocho átomos de carbono sustituido opcionalmente; cada R² es independientemente halo, alquilo de uno a seis átomos de carbono sustituido opcionalmente, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, y -NH₂; R³ es hidrógeno, alquilo de uno a seis átomos de carbono sustituido opcionalmente, C₃₋₈ cicloalquilo, o C₆₋₁₀ arilo; R⁴ es un heteroarilo de seis a doce miembros que tiene al menos un grupo aromático y al menos dos heteroátomos seleccionados de N, O, o S, en donde el heteroarilo está sustituido opcionalmente con uno, dos o tres miembros seleccionados independientemente de halo, ciano, haloalquilo de uno a seis átomos de carbono sustituido opcionalmente, alquilo de uno a seis átomos de carbono sustituido opcionalmente, alquinilo de dos a cuatro átomos de carbono sustituido opcionalmente, y -NH₂; y R⁵ es hidrógeno o alquilo de uno a seis átomos de carbono sustituido opcionalmente, en donde R⁵ y R³ junto con los átomos a los cuales están enlazados forman un anillo heterocíclico de cuatro a ocho miembros; o una sal, isómero, o una mezcla de los mismos, farmacéuticamente aceptables.
ARP150101859A 2014-06-13 2015-06-11 Inhibidores de fosfatidilinositol 3-quinasa AR100809A1 (es)

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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016016538A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Derivados de quinazolinona como inhibidores de fosfatidilinositol 3-cinasa.
MX2016016516A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-cinasa.
US11021467B2 (en) 2014-06-13 2021-06-01 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2952025A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2952044C (en) 2014-06-13 2019-01-29 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
EA201692557A1 (ru) 2014-07-04 2017-05-31 Люпин Лимитед Хинолизиноновые производные в качестве ингибиторов pi3k
WO2016106050A1 (en) 2014-12-26 2016-06-30 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
SG11201606876RA (en) * 2015-03-04 2016-10-28 Gilead Sciences Inc Toll like receptor modulator compounds
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
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
SI3507276T1 (sl) 2016-09-02 2022-01-31 Gilead Sciences, Inc. Spojine modulatorja toličnih receptorjev
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
SG11202004361SA (en) * 2017-11-13 2020-06-29 Luoxin Pharmaceutical Shanghai Co Ltd Quinazolinone compound and application thereof
RU2020116571A (ru) 2017-12-07 2021-11-22 Эмори Юниверсити N4-гидроксицитидин и производные и связанные с этим противовирусные применения
EP3740468B1 (en) 2018-01-20 2025-12-31 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
TWI751517B (zh) 2019-04-17 2022-01-01 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
TWI879779B (zh) 2019-06-28 2025-04-11 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
EP1226129B1 (en) 1999-10-27 2006-05-24 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
DE60144277D1 (de) 2000-04-25 2011-05-05 Icos Corp Hemmer der menschlichen phosphatidyl-inositol-3-kinase delta
LT2612862T (lt) 2004-05-13 2017-01-25 Icos Corporation Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai
ITRM20040139U1 (it) * 2004-08-26 2004-11-26 Salice Arturo Spa Cerniera con spinta in apertura per mobili con cornice.
US20080287469A1 (en) 2005-02-17 2008-11-20 Diacovo Thomas G Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation
BRPI0906473A8 (pt) * 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
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
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ, インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Pi3k-德爾塔抑制劑以及其應用和生產方法
KR101594002B1 (ko) 2010-10-06 2016-02-15 글락소스미스클라인 엘엘씨 Pi3 키나제 억제제로서의 벤즈이미다졸 유도체
ES2612492T3 (es) 2010-12-28 2017-05-17 Sanofi Nuevos derivados de piridiminas, su preparación y su utilización farmacéutica como inhibidores de fosforilación de AKT (PKB)
PE20141371A1 (es) 2011-08-29 2014-10-13 Infinity Pharmaceuticals Inc Compuestos heterociclicos y usos de los mismos
SG10202003090VA (en) * 2012-08-08 2020-05-28 Kbp Biosciences Co Ltd PI3K δ INHIBITOR
US9029384B2 (en) 2012-12-21 2015-05-12 Gilead Calistoga, LLC. Phosphatidylinositol 3-kinase inhibitors
TW201441216A (zh) * 2012-12-21 2014-11-01 Gilead Calistoga Llc 肌醇磷酯3-激酶的抑制劑
WO2014128612A1 (en) * 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
ES2667173T3 (es) 2013-06-14 2018-05-09 Gilead Calistoga Llc Inhibidores de fosfatidilinositol 3-quinasa
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
KR20160060100A (ko) 2013-09-22 2016-05-27 칼리토르 사이언시즈, 엘엘씨 치환된 아미노피리미딘 화합물 및 이용 방법
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2015081127A2 (en) 2013-11-26 2015-06-04 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
US11021467B2 (en) 2014-06-13 2021-06-01 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
MX2016016538A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Derivados de quinazolinona como inhibidores de fosfatidilinositol 3-cinasa.
CA2952025A1 (en) 2014-06-13 2015-12-17 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2952044C (en) 2014-06-13 2019-01-29 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
MX2016016516A (es) 2014-06-13 2017-05-01 Gilead Sciences Inc Inhibidores de fosfatidilinositol 3-cinasa.
SG11201610341PA (en) 2014-06-24 2017-01-27 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors

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