JP5755220B2 - ヒト免疫不全ウイルス複製の阻害剤 - Google Patents

ヒト免疫不全ウイルス複製の阻害剤 Download PDF

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JP5755220B2
JP5755220B2 JP2012510079A JP2012510079A JP5755220B2 JP 5755220 B2 JP5755220 B2 JP 5755220B2 JP 2012510079 A JP2012510079 A JP 2012510079A JP 2012510079 A JP2012510079 A JP 2012510079A JP 5755220 B2 JP5755220 B2 JP 5755220B2
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JP2012526728A (ja
JP2012526728A5 (https=
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クリスチャン ヨアキム
クリスチャン ヨアキム
マーレイ ディー ベイリー
マーレイ ディー ベイリー
フランソワ ビロドー
フランソワ ビロドー
レベッカ ジェイ カーソン
レベッカ ジェイ カーソン
リー フェイダー
リー フェイダー
スティーブン カワイ
スティーブン カワイ
スティーヴン ラプラント
スティーヴン ラプラント
シモノー　ブルーノ
ブルーノ シモノー
シモン スルプルナン
シモン スルプルナン
カール ティボール
カール ティボール
ユーラ エス ツァントリゾス
ユーラ エス ツァントリゾス
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/04—Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • 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
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • 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
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4741—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
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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
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D401/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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Families Citing this family (215)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS53347B (sr) 2008-12-09 2014-10-31 Gilead Sciences, Inc. Modulatori toll-sličnih receptora
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
EP2588455B1 (en) 2010-07-02 2018-04-04 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
MX2012015097A (es) 2010-07-02 2013-05-28 Gilead Sciences Inc Derivados de acido naft-2-ilacetico para tratar sida.
US8633200B2 (en) 2010-09-08 2014-01-21 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
CA2830838A1 (en) * 2011-04-04 2012-11-10 Gilead Sciences, Inc. Process for the preparation of an hiv integrase inhibitor
EP2508511A1 (en) 2011-04-07 2012-10-10 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
EP2511273B8 (en) 2011-04-15 2019-06-26 Hivih Inhibitors of viral replication, their process of preparation and their therapeutical uses
UA111841C2 (uk) 2011-04-21 2016-06-24 Гіліад Сайєнсіз, Інк. Сполуки бензотіазолу та їх фармацевтичне застосування
AU2012278976B2 (en) 2011-07-06 2017-05-11 Gilead Sciences, Inc. Compounds for the treatment of HIV
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
CN102952069B (zh) * 2011-08-19 2014-12-17 中国科学技术大学 一种化合物及其制备方法和应用
JP2014528412A (ja) * 2011-09-30 2014-10-27 キネタ・インコーポレイテツド 抗ウイルス化合物
WO2013062028A1 (ja) 2011-10-25 2013-05-02 塩野義製薬株式会社 Ｈｉｖ複製阻害剤
WO2013073875A1 (ko) 2011-11-15 2013-05-23 한국화학연구원 신규한 항바이러스성 피롤로피리딘 유도체 및 이의 제조방법
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene acetic acid derivatives against HIV infection
US8629276B2 (en) 2012-02-15 2014-01-14 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
US9034882B2 (en) 2012-03-05 2015-05-19 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
US9006235B2 (en) 2012-03-06 2015-04-14 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
UY34750A (es) * 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
US8906929B2 (en) * 2012-08-16 2014-12-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
EP2716639A1 (en) 2012-10-05 2014-04-09 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
EP2716632A1 (en) 2012-10-05 2014-04-09 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
EP2719685A1 (en) 2012-10-11 2014-04-16 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
TW201443037A (zh) 2013-01-09 2014-11-16 Gilead Sciences Inc 治療用化合物
US9220710B2 (en) 2013-01-09 2015-12-29 Gilead Sciences, Inc. Therapeutic compounds
ES2642265T3 (es) 2013-01-09 2017-11-16 Gilead Sciences, Inc. Compuestos terapéuticos para el tratamiento de infecciones virales
TW201441197A (zh) * 2013-01-31 2014-11-01 Shionogi & Co Ｈｉｖ複製抑制劑
TWI694071B (zh) 2013-03-01 2020-05-21 美商基利科學股份有限公司 治療反轉錄病毒科(Retroviridae)病毒感染之治療性化合物
WO2014164467A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
WO2014164409A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
ES2619708T3 (es) 2013-03-13 2017-06-26 VIIV Healthcare UK (No.5) Limited Inhibidores de la replicación del virus de inmunodeficiencia humana
CN105008369B (zh) 2013-03-14 2017-07-11 百时美施贵宝公司 人类免疫缺陷病毒复制抑制剂
JP2016512558A (ja) * 2013-03-14 2016-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヒト免疫不全ウイルス複製の阻害剤
EP2821104A1 (en) 2013-07-05 2015-01-07 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
EP2821082A1 (en) 2013-07-05 2015-01-07 Laboratoire Biodim Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use
ES2859102T3 (es) 2013-07-12 2021-10-01 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH
NO2865735T3 (https=) 2013-07-12 2018-07-21
JP6434522B2 (ja) 2013-09-05 2018-12-05 ダウ アグロサイエンシィズ エルエルシー ホウ素化アレーンを生成する方法
EP3105236B1 (en) 2014-02-12 2017-10-18 ViiV Healthcare UK (No.5) Limited Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication
US9409922B2 (en) * 2014-02-18 2016-08-09 Bristol-Myers Squibb Company Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
PT3107913T (pt) 2014-02-19 2018-09-28 Viiv Healthcare Uk No 5 Ltd Inibidores da replicação do vírus da imunodeficiência humana
US9637501B2 (en) 2014-02-20 2017-05-02 Viiv Healthcare Uk (No. 5) Limited Pyridin-3-yl acetic acid macrocycles as inhibitors of human immunodeficiency virus replication
US9193720B2 (en) 2014-02-20 2015-11-24 Bristol-Myers Squibb Company Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US10202353B2 (en) 2014-02-28 2019-02-12 Gilead Sciences, Inc. Therapeutic compounds
US9975906B2 (en) 2014-05-16 2018-05-22 Shionogi & Co., Ltd. Tricyclic heterocycle derivatives having HIV replication inhibitory effect
TW201625354A (zh) 2014-06-16 2016-07-16 陶氏農業科學公司 用於製備氧硼基化芳烴之方法
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
NO2717902T3 (https=) 2014-06-20 2018-06-23
TR201807217T4 (tr) 2014-07-08 2018-06-21 Viiv Healthcare Uk Ltd Bir viral enfeksiyon sahasının tedavisinde kullanım için izoindolin türevleri.
JP6522732B2 (ja) 2014-07-11 2019-05-29 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖを治療するためのトール様受容体の調節因子
EP3172189A1 (en) * 2014-07-21 2017-05-31 VIIV Healthcare UK Limited Phenyl and tertbutylacetic acid substituted pyridinones having anti-hiv effects
US10065953B2 (en) * 2014-08-27 2018-09-04 VIIV Healthcare UK (No.5) Limited Imidazo[1,2-A]pyridine derivatives for use as inhibitors of human immunodeficiency virus replication
WO2016036759A1 (en) 2014-09-04 2016-03-10 Gilead Sciences, Inc. Methods of treating or preventing hiv in patients using a combination of tenofovir alafenamide and dolutegravir
SG11201701520TA (en) 2014-09-16 2017-04-27 Gilead Sciences Inc Solid forms of a toll-like receptor modulator
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
TWI699355B (zh) 2014-12-24 2020-07-21 美商基利科學股份有限公司 喹唑啉化合物
SG11201705192PA (en) 2014-12-24 2017-07-28 Gilead Sciences Inc Fused pyrimidine compounds for the treatment of hiv
BR112017013440A2 (pt) 2014-12-24 2018-01-09 Gilead Sciences, Inc. compostos de isoquinolina para o tratamento de hiv
US9670205B2 (en) 2015-03-04 2017-06-06 Gilead Sciences, Inc. Toll like receptor modulator compounds
KR20190057158A (ko) 2015-04-02 2019-05-27 길리애드 사이언시즈, 인코포레이티드 폴리시클릭-카르바모일피리돈 화합물 및 그의 제약 용도
TWI700284B (zh) * 2015-05-29 2020-08-01 日商塩野義製藥股份有限公司 具有ｈｉｖ複製抑制作用之含氮３環性衍生物
US20180170903A1 (en) * 2015-07-06 2018-06-21 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
RU2018102554A (ru) * 2015-07-08 2019-08-08 ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД Производные пиридин-3-ил уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека
RU2018103031A (ru) * 2015-07-09 2019-08-09 ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД Производные пиридин-3-ил уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека
US20180170904A1 (en) 2015-07-09 2018-06-21 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
KR20180035910A (ko) * 2015-08-07 2018-04-06 비브 헬스케어 유케이 (넘버5) 리미티드 인간 면역결핍 바이러스 복제의 억제제로서 피리딘-3-일 아세트산 유도체
WO2017025913A1 (en) 2015-08-10 2017-02-16 VIIV Healthcare UK (No.5) Limited Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
TWI657086B (zh) 2015-08-11 2019-04-21 英商Viiv醫療保健英國(No.5)有限公司 做為人類免疫缺陷病毒複製抑制劑之５－（ｎ－苯甲基四氫異喹啉－６－基）吡啶－３－基乙酸衍生物
CN108137553A (zh) 2015-08-12 2018-06-08 Viiv保健英国第五有限公司 作为人免疫缺陷病毒复制的抑制剂的5-(n-[6,5]-稠合双环芳基四氢异喹啉-6-基)吡啶-3-基乙酸衍生物
US10214516B2 (en) 2015-08-12 2019-02-26 VIIV Healthcare UK (No.5) Limited 5-(N-fused tricyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201718537A (zh) 2015-08-12 2017-06-01 Ｖｉｉｖ醫療保健英國（Ｎｏ．５）有限公司 做為人類免疫缺陷病毒複製抑制劑之吡啶－３－基乙酸衍生物
KR20180038047A (ko) 2015-08-20 2018-04-13 비브 헬스케어 유케이 (넘버5) 리미티드 인간 면역결핍 바이러스 복제의 억제제로서 피리딘-3-일 아세트산 유도체
US20210292327A1 (en) 2015-08-26 2021-09-23 Gilead Sciences, Inc. Deuterated toll-like receptor modulators
CA2997955A1 (en) 2015-09-15 2017-03-23 Gilead Sciences, Inc. Modulators of toll-like receptors for the treatment of hiv
AU2016330895A1 (en) 2015-09-30 2018-05-10 Gilead Sciences, Inc. Compounds and combinations for the treatment of HIV
WO2017070089A1 (en) * 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
JP2018536001A (ja) 2015-12-04 2018-12-06 ヴィーブ ヘルスケア ユーケー リミテッド イソインドリン誘導体
JP6732915B2 (ja) 2015-12-15 2020-07-29 ギリアード サイエンシーズ， インコーポレイテッド ヒト免疫不全ウイルス中和抗体
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
US10407410B2 (en) 2016-05-11 2019-09-10 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US20190152957A1 (en) 2016-05-11 2019-05-23 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
JP2019515000A (ja) * 2016-05-11 2019-06-06 ヴィーブ ヘルスケア ユーケー（ナンバー５）リミテッド ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−３−イル酢酸誘導体
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
HUE060256T2 (hu) 2016-06-20 2023-02-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
US10639284B2 (en) 2016-06-27 2020-05-05 Chemocentryx, Inc. Immunomodulator compounds
KR102482673B1 (ko) 2016-07-05 2022-12-30 광저우 맥시노벨 파마수티컬스 씨오., 엘티디. 방향족 아세틸렌 또는 방향족 에틸렌계 화합물, 그의 중간체, 제조 방법, 약물 조성물 및 용도
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
CN119462611A (zh) 2016-08-19 2025-02-18 吉利德科学公司 用于预防性或治疗性治疗hiv病毒感染的治疗性化合物
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018042332A1 (en) 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
WO2018042331A1 (en) 2016-08-31 2018-03-08 Glaxosmithkline Intellectual Property (No.2) Limited Combinations and uses and treatments thereof
AU2017318601B2 (en) 2016-09-02 2020-09-03 Gilead Sciences, Inc. Toll like receptor modulator compounds
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
WO2018051250A1 (en) 2016-09-14 2018-03-22 Viiv Healthcare Company Combination comprising tenofovir alafenamide, bictegravir and 3tc
EP3519409B1 (en) 2016-09-28 2024-09-18 Gilead Sciences, Inc. Benzothiazol-6-yl acetic acid derivatives and their use for treating hiv infection
ES2881949T3 (es) 2016-10-27 2021-11-30 Gilead Sciences Inc Forma cristalina de base libre de darunavir
JP7101678B2 (ja) 2016-12-22 2022-07-15 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
LT3558990T (lt) 2016-12-22 2022-12-27 Incyte Corporation Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
EP3565810A1 (en) 2017-01-03 2019-11-13 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201835068A (zh) 2017-01-03 2018-10-01 英商Viiv醫療保健英國(No.5)有限公司 作為人類免疫缺乏病毒複製之抑制劑之吡啶-3-基乙酸衍生物
TW202510891A (zh) 2017-01-31 2025-03-16 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
AR110922A1 (es) 2017-02-06 2019-05-15 Gilead Sciences Inc Compuestos inhibidores del vih
WO2018228984A1 (en) * 2017-06-14 2018-12-20 Bayer Aktiengesellschaft Process for preparing 3,4-dichloro-n-(2-cyanophenyl)-5-isothiazolecarboxamide
AR112257A1 (es) 2017-06-21 2019-10-09 Gilead Sciences Inc Anticuerpos multiespecíficos dirigidos al vih-1 gp120 y cd3 humana, composiciones que los comprende, ácido nucleico, vector y célula huésped relacionados, método para producirlos, método para detectar células que expresan gp120 y cd3, kit de anticuerpos, fragmentos de anticuerpo que se une a gp120 y método para producirlos
CN110958883A (zh) 2017-06-30 2020-04-03 Viiv保健公司 组合及其用途和疗法
US10919852B2 (en) 2017-07-28 2021-02-16 Chemocentryx, Inc. Immunomodulator compounds
SI3661937T1 (sl) 2017-08-01 2021-11-30 Gilead Sciences, Inc. Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb
US10392405B2 (en) 2017-08-08 2019-08-27 Chemocentryx, Inc. Macrocyclic immunomodulators
TWI687415B (zh) 2017-08-17 2020-03-11 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
CN111051305A (zh) 2017-08-22 2020-04-21 吉利德科学公司 治疗性杂环化合物
JOP20180092A1 (ar) 2017-10-13 2019-04-13 Gilead Sciences Inc مثبطات hiv بروتياز
EP3700573A1 (en) 2017-10-24 2020-09-02 Gilead Sciences, Inc. Methods of treating patients co-infected with a virus and tuberculosis
WO2019123339A1 (en) 2017-12-20 2019-06-27 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
EP3728283B1 (en) 2017-12-20 2023-11-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CN109988144B (zh) 2017-12-29 2024-07-05 广州再极医药科技有限公司 芳香乙烯或芳香乙基类衍生物、其制备方法、中间体、药物组合物及应用
EP3740209A1 (en) 2018-01-19 2020-11-25 Gilead Sciences, Inc. Metabolites of bictegravir
JP7083398B2 (ja) 2018-02-15 2022-06-10 ギリアード サイエンシーズ， インコーポレイテッド ピリジン誘導体およびｈｉｖ感染を処置するためのその使用
EP3752496B1 (en) 2018-02-16 2023-07-05 Gilead Sciences, Inc. Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection
US10568874B2 (en) 2018-02-22 2020-02-25 Chemocentryx, Inc. Indane-amines as PD-L1 antagonists
SMT202500157T1 (it) 2018-03-30 2025-05-12 Incyte Corp Composti eterociclici come immunomodulatori
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
US20190359645A1 (en) 2018-05-03 2019-11-28 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
WO2019244066A2 (en) 2018-06-19 2019-12-26 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2020003093A1 (en) 2018-06-25 2020-01-02 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
DK4257600T3 (da) 2018-07-03 2025-05-26 Gilead Sciences Inc Antistoffer rettet mod hiv gp120 og fremgangsmåder til at bruge dem
AU2019297362B2 (en) 2018-07-06 2022-05-26 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
US11186579B2 (en) 2018-07-06 2021-11-30 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
KR20210033492A (ko) 2018-07-16 2021-03-26 길리애드 사이언시즈, 인코포레이티드 Hiv의 치료를 위한 캡시드 억제제
TWI829205B (zh) 2018-07-30 2024-01-11 美商基利科學股份有限公司 抗hiv化合物
JP7313438B2 (ja) 2018-09-19 2023-07-24 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖの予防のためのインテグラーゼ阻害剤
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
WO2020176505A1 (en) 2019-02-25 2020-09-03 Gilead Sciences, Inc. Protein kinase c agonists
WO2020176510A1 (en) 2019-02-25 2020-09-03 Gilead Sciences, Inc. Protein kinase c agonists
EP3934757B1 (en) 2019-03-07 2023-02-22 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 2'3'-cyclic dinucleotides and prodrugs thereof
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
WO2020178770A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
MY201239A (en) 2019-03-22 2024-02-13 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
TW202104210A (zh) 2019-04-17 2021-02-01 美商基利科學股份有限公司 Hiv蛋白酶抑制劑
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
TWI751516B (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
US20200347036A1 (en) 2019-04-17 2020-11-05 Gilead Sciences, Inc. Solid forms of an hiv protease inhibitor
TW202231277A (zh) 2019-05-21 2022-08-16 美商基利科學股份有限公司 鑑別對使用gp120 v3聚醣導向之抗體的治療敏感之hiv病患的方法
TWI810456B (zh) 2019-05-22 2023-08-01 美商基利科學股份有限公司 Tlr7調節化合物及hiv疫苗之組合
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
RU2717101C1 (ru) 2019-06-03 2020-03-18 Андрей Александрович Иващенко Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения
CA3140708A1 (en) 2019-06-18 2020-12-24 Helen Horton Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
WO2020263830A1 (en) 2019-06-25 2020-12-30 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
BR112021025888A2 (pt) 2019-07-10 2022-04-26 Chemocentryx Inc Indanos como inibidores de pd-l1
KR20240137107A (ko) 2019-07-16 2024-09-19 길리애드 사이언시즈, 인코포레이티드 Hiv 백신, 및 이의 제조 및 사용 방법
US20220257619A1 (en) 2019-07-18 2022-08-18 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
CA3160131A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
CA3157275C (en) 2019-11-26 2026-02-10 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
IL294032A (en) 2019-12-24 2022-08-01 Carna Biosciences Inc Compounds that regulate diacylglycerol kinase
PE20221569A1 (es) 2020-02-24 2022-10-06 Gilead Sciences Inc Compuestos tetraciclicos para el tratamiento de infecciones por vih
WO2021188959A1 (en) 2020-03-20 2021-09-23 Gilead Sciences, Inc. Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
EP4153181A1 (en) 2020-05-21 2023-03-29 Gilead Sciences, Inc. Pharmaceutical compositions comprising bictegravir
TWI858267B (zh) 2020-06-25 2024-10-11 美商基利科學股份有限公司 用於治療hiv之蛋白殼抑制劑
EP4192474B1 (en) 2020-08-07 2025-09-10 Gilead Sciences, Inc. Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use
ES3064867T3 (en) 2020-09-30 2026-04-29 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds for a use in the treatment of hiv
TW202406932A (zh) 2020-10-22 2024-02-16 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
PL4244396T3 (pl) 2020-11-11 2025-12-22 Gilead Sciences, Inc. Sposoby identyfikacji pacjentów z hiv wrażliwych na terapię przeciwciałami skierowanymi na miejsce wiązania cd4 gp120
US11613546B2 (en) 2021-01-19 2023-03-28 Gilead Sciences, Inc. Substituted pyridotriazine compounds and uses thereof
WO2022245671A1 (en) 2021-05-18 2022-11-24 Gilead Sciences, Inc. Methods of using flt3l-fc fusion proteins
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
JP7651018B2 (ja) 2021-06-23 2025-03-25 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
MX2024003795A (es) * 2021-09-29 2024-06-03 Repare Therapeutics Inc Compuestos de n-(5-sustituido-[(1,3,4-tiadiazolil) o (tiazolil)])(sustituido)carboxamida y uso de estos para inhibir la polimerasa theta humana.
CR20240223A (es) 2021-12-03 2024-07-08 Gilead Sciences Inc Compuestos terapéuticos para la infección por el virus del vih
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
US12404262B2 (en) 2021-12-03 2025-09-02 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
TW202446773A (zh) 2022-04-06 2024-12-01 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
TWI867601B (zh) 2022-07-01 2024-12-21 美商基利科學股份有限公司 可用於ｈｉｖ病毒感染之疾病預防性或治療性治療的治療性化合物
CA3259040A1 (en) 2022-07-12 2024-01-18 Gilead Sciences, Inc. HIV Immunogenic Polypeptides and Vaccines and Their Uses
AU2023330037A1 (en) 2022-08-26 2025-03-06 Gilead Sciences, Inc. Dosing and scheduling regimen for broadly neutralizing antibodies
AU2023352129A1 (en) * 2022-09-29 2025-05-01 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
US20240226130A1 (en) 2022-10-04 2024-07-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
US20240390349A1 (en) 2023-04-19 2024-11-28 Gilead Sciences, Inc. Dosing regimen of capsid inhibitor
US20250042926A1 (en) 2023-05-31 2025-02-06 Gilead Sciences, Inc. Therapeutic compounds for hiv
US20250051375A1 (en) 2023-05-31 2025-02-13 Gilead Sciences, Inc. Anti-hiv compounds
CN121219281A (zh) 2023-05-31 2025-12-26 吉利德科学公司 用于治疗hiv的化合物的固体形式
WO2025029247A1 (en) 2023-07-28 2025-02-06 Gilead Sciences, Inc. Weekly regimen of lenacapavir for the treatment and prevention of hiv
WO2025042394A1 (en) 2023-08-23 2025-02-27 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
WO2025076542A1 (en) 2023-10-05 2025-04-10 Jones R Brad Atovaquone as an ros inducer for use in the elimination of hiv-infected t-cells
US20250122219A1 (en) 2023-10-11 2025-04-17 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
TW202515549A (zh) 2023-10-11 2025-04-16 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
US20250127801A1 (en) 2023-10-11 2025-04-24 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
US20250230163A1 (en) 2023-12-22 2025-07-17 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
US20250333424A1 (en) 2024-03-01 2025-10-30 Gilead Sciences, Inc. Antiviral compounds
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
US20250296932A1 (en) 2024-03-01 2025-09-25 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2025212814A1 (en) 2024-04-03 2025-10-09 Gilead Sciences, Inc. Anti-hiv compounds
US20260007683A1 (en) 2024-06-14 2026-01-08 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2026038155A1 (en) * 2024-08-16 2026-02-19 Pfizer Inc. Substituted pyridine compounds
WO2026076265A1 (en) 2024-10-03 2026-04-09 Gilead Sciences, Inc. Combination therapy comprising bridged tricyclic carbamoylpyridone compounds and p-glycoprotein inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW530047B (en) * 1994-06-08 2003-05-01 Pfizer Corticotropin releasing factor antagonists
PA8467401A1 (es) * 1998-02-17 2000-09-29 Pfizer Prod Inc Procedimiento para tratar la insuficiencia cardiaca
US20060106070A1 (en) * 2004-10-28 2006-05-18 Bioflexis, Llc Novel pyridine-based metal chelators as antiviral agents
US7939545B2 (en) 2006-05-16 2011-05-10 Boehringer Ingelheim International Gmbh Inhibitors of human immunodeficiency virus replication
FR2906251B1 (fr) 2006-09-22 2008-11-07 Sanofi Aventis Sa Derives de pyrrolizine, indolizine et quinolizine, leur preparation et leur application en therapeutique
KR101107896B1 (ko) * 2006-10-04 2012-01-25 에프. 호프만-라 로슈 아게 고 밀도 지단백질(ｈｄｌ)-콜레스테롤 상승제로서 3-피리딘카복스아마이드 및 2-피라진카복스아마이드 유도체
ES2402322T3 (es) 2007-11-15 2013-04-30 Gilead Sciences, Inc. Inhibidores de la replicación del virus de la inmunodeficiencia humana
EA019259B1 (ru) 2007-11-16 2014-02-28 Джилид Сайенсиз, Инк. Ингибиторы репликации вируса иммунодефицита человека
JO3067B1 (ar) 2008-10-27 2017-03-15 Glaxosmithkline Llc بيرميدينات بيرازولو امينو كمثبطات ل fak
CN102256963B (zh) 2008-12-19 2014-06-11 贝林格尔.英格海姆国际有限公司 作为ccr2受体拮抗剂用于治疗炎症、哮喘和copd的环状嘧啶-4-甲酰胺
GB0908394D0 (en) 2009-05-15 2009-06-24 Univ Leuven Kath Novel viral replication inhibitors
AR076839A1 (es) 2009-05-15 2011-07-13 Bayer Cropscience Ag Derivados fungicidas de pirazol carboxamidas
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
NZ596302A (en) 2009-05-15 2014-01-31 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors

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