EA201290103A1 - Гетероциклические соединения и их использование - Google Patents

Гетероциклические соединения и их использование

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Publication number
EA201290103A1
EA201290103A1 EA201290103A EA201290103A EA201290103A1 EA 201290103 A1 EA201290103 A1 EA 201290103A1 EA 201290103 A EA201290103 A EA 201290103A EA 201290103 A EA201290103 A EA 201290103A EA 201290103 A1 EA201290103 A1 EA 201290103A1
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EA
Eurasian Patent Office
Prior art keywords
heterocyclic compounds
objects
heterocyclic
kinase activity
modulate
Prior art date
Application number
EA201290103A
Other languages
English (en)
Other versions
EA026693B1 (ru
Inventor
Пингда Рен
Йи Лиу
Лианьшен Ли
Катрина Чан
Трой Эдвард Уилсон
Саймон Фрейзер Кэмпбелл
Original Assignee
ИНТЕЛЛИКАЙН, ЭлЭлСи
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43607312&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201290103(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ИНТЕЛЛИКАЙН, ЭлЭлСи filed Critical ИНТЕЛЛИКАЙН, ЭлЭлСи
Publication of EA201290103A1 publication Critical patent/EA201290103A1/ru
Publication of EA026693B1 publication Critical patent/EA026693B1/ru

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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic 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
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Abstract

Описаны гетероциклические объекты, которые модулируют PI3 киназную активность, фармацевтические композиции, содержащие данные гетероциклические объекты, и способы использования этих химических объектов для лечения болезней и состояний, которые ассоциируются с PI3 киназной активностью.
EA201290103A 2009-08-17 2010-08-17 Производные бензоксазола и бензотиазола в качестве ингибиторов pi3-киназы EA026693B1 (ru)

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Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
EA026693B1 (ru) 2009-08-17 2017-05-31 Интелликайн ЭлЭлСи Производные бензоксазола и бензотиазола в качестве ингибиторов pi3-киназы
JP5728683B2 (ja) * 2009-09-04 2015-06-03 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン
GB201008134D0 (en) * 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
WO2011149937A1 (en) * 2010-05-24 2011-12-01 Intellikine, Inc. Heterocyclic compounds and uses thereof
RU2582610C2 (ru) * 2010-07-30 2016-04-27 Онкотерапи Сайенс, Инк. Производные хинолина и содержащие их ингибиторы melk
CN103298474B (zh) * 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
WO2012065297A1 (en) * 2010-11-16 2012-05-24 Impact Therapeutics, Inc. 3-ARYL-6-ARYL-[1,2,4]TRIAZOLO[4,3-a]PYRIDINES AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
AR085397A1 (es) * 2011-02-23 2013-09-25 Intellikine Inc Combinacion de inhibidores de quinasa y sus usos
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
CN102219755B (zh) * 2011-05-05 2013-04-03 南京大学 Stat3的小分子选择性抑制剂及其制备方法和应用
WO2012154610A1 (en) * 2011-05-06 2012-11-15 Intellikine, Llc Reactive pi3k kinase inhibitors and uses thereof
EP2704723A4 (en) * 2011-05-06 2014-12-24 Univ California TREATMENT OF POLYCYSTIC DISEASES
ES2907071T3 (es) 2011-05-19 2022-04-21 Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio Compuestos macrocíclicos como inhibidores de proteína quinasas
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8883819B2 (en) 2011-09-01 2014-11-11 Irm Llc Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
EP2776428A4 (en) * 2011-11-11 2015-04-22 Intellikine Llc KINASEHEMMERPOLYMORPHE
CN104204804B (zh) * 2011-11-11 2016-09-28 因特利凯有限责任公司 激酶抑制剂的组合及其用途
WO2013078441A1 (en) * 2011-11-23 2013-05-30 Intellikine, Llc Heterocyclic compounds and uses thereof
GB201205669D0 (en) * 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
US10280168B2 (en) 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
CN104244949A (zh) * 2012-03-30 2014-12-24 诺华股份有限公司 用于治疗神经母细胞瘤、尤文氏肉瘤或横纹肌肉瘤的化合物
BR112014028881A2 (pt) 2012-05-23 2017-06-27 Hoffmann La Roche populações de células, banco de células, métodos de obtenção de uma população de células, métodos de identificação de um fator, métodos de seleção, métodos de fornecimento de terapia, populações de hepatócitos e método de obtenção de células
UA117347C2 (uk) 2012-06-13 2018-07-25 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
US9309243B2 (en) 2012-07-13 2016-04-12 Ucb Biopharma Sprl Imidazopyridine derivatives as modulators of TNF activity
GB201212513D0 (en) * 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
KR20150079745A (ko) 2012-11-08 2015-07-08 리젠 파마슈티컬스 소시에떼 아노님 Pde4 억제제 및 pi3 델타 또는 이중 pi3 델타-감마 키나아제 억제제를 함유하는 약제학적 조성물
TWI574962B (zh) 2012-11-14 2017-03-21 加拓科學公司 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途
PT3808749T (pt) 2012-12-07 2023-06-07 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis como inibidores da quinase atr para o tratamento de doenças de cancro
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9040533B2 (en) 2012-12-27 2015-05-26 Purdue Pharma L.P. Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators
EP2958564B1 (en) * 2013-02-21 2018-05-09 Calitor Sciences, LLC Heteroaromatic compounds as pi3 kinase modulators
US9073921B2 (en) 2013-03-01 2015-07-07 Novartis Ag Salt forms of bicyclic heterocyclic derivatives
WO2014160177A2 (en) * 2013-03-13 2014-10-02 Exelixis, Inc. Quinazoline inhibitors of pi3k
JP2016512835A (ja) * 2013-03-15 2016-05-09 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせ及びそれらの使用
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US20160089371A1 (en) * 2013-03-15 2016-03-31 Intellikine, Llc Combination of Kinase Inhibitors and Uses Thereof
WO2014143241A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN105263931B (zh) 2013-04-19 2019-01-25 因赛特公司 作为fgfr抑制剂的双环杂环
CN104177346A (zh) * 2013-05-21 2014-12-03 苏州科捷生物医药有限公司 喹唑啉类化合物及其用途
EP3052493A4 (en) * 2013-10-03 2017-06-14 Millennium Pharmaceuticals, Inc. Enhanced treatment regimens using pi3k inhibitors
US9936700B2 (en) 2013-10-23 2018-04-10 Bayer Cropscience Aktiengesellschaft Substituted quinoxaline derivatives as pest control agent
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
US9670210B2 (en) 2014-02-13 2017-06-06 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
CR20200362A (es) 2014-02-13 2020-10-26 Incyte Corp CICLOPROPILAMINA COMO INHIBIDORES DE LA LSD1 (Divisional 2016-0395)
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
EP3110801B1 (en) * 2014-02-27 2019-01-30 Council Of Scientific & Industrial Research 6-aryl-4-phenylamino-quinazoline analogs as phosphoinositide-3-kinase inhibitors
NZ764151A (en) 2014-06-05 2023-12-22 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
RU2736219C2 (ru) 2014-06-17 2020-11-12 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации ингибиторов снк1 и atr
WO2016004272A1 (en) 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
CN105272933B (zh) * 2014-07-24 2017-09-12 张皓 5‑萘基‑2‑氨基‑苯并[d]噁唑衍生物及其制备方法和用途
WO2016040806A1 (en) 2014-09-11 2016-03-17 The Regents Of The University Of California mTORC1 INHIBITORS
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
CN115925711A (zh) 2014-11-06 2023-04-07 Bial研发投资股份有限公司 取代的吡唑并[1,5-a]嘧啶以及它们在治疗医学障碍中的用途
CA2966581A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
KR102139496B1 (ko) * 2014-12-15 2020-07-30 더 리젠츠 오브 더 유니버시티 오브 미시간 Egfr 및 pi3k의 소분자 억제제
ES2761051T3 (es) 2014-12-19 2020-05-18 Janssen Pharmaceutica Nv Derivados de imidazopiridazina como inhibidores de PI3Kbeta
ES2760507T3 (es) 2014-12-19 2020-05-14 Janssen Pharmaceutica Nv Derivados de imidazopiridazina enlazados a heterociclilo como inhibidores de PI3Kß
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
CN107660205B (zh) 2015-04-03 2021-08-27 因赛特公司 作为lsd1抑制剂的杂环化合物
EP3319602B1 (en) * 2015-07-11 2020-02-05 Advenchen Pharmaceuticals LLC Fused quinoline compounds as pi3k/mtor inhibitors
MX2018000577A (es) * 2015-07-16 2018-09-05 Array Biopharma Inc Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la ret quinasa.
EP3334709A1 (en) 2015-08-12 2018-06-20 Incyte Corporation Salts of an lsd1 inhibitor
EP3344039A4 (en) 2015-09-03 2019-08-28 Arizona Board of Regents on behalf of the University of Arizona SMALL DYRK1A INHIBITORY MOLECULES AND USES THEREOF
CN105085503A (zh) * 2015-09-20 2015-11-25 徐敬媛 一种治疗呼吸道感染的药物组合物
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
BR112018007068B1 (pt) 2015-10-09 2024-01-02 Janssen Pharmaceutica N.V. Derivados de quinoxalina e piridopirazina como inibidores de pi3kbeta, seu uso e composição farmacêutica que os compreende
CN109311887B (zh) 2016-04-06 2022-09-13 Bial研发投资股份有限公司 吡唑并[1,5-a]嘧啶基甲酰胺化合物以及它们在治疗医学病症中的用途
MX2018012208A (es) 2016-04-06 2019-03-28 Lysosomal Therapeutics Inc Compuestos a base de imidazo [1,5-a] pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos.
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
EP3452481A4 (en) 2016-05-05 2020-02-26 Lysosomal Therapeutics Inc. IMIDAZO [1,2-B] SUBSTITUTED PYRIDAZINES, IMIDAZO [1,5-B] SUBSTITUTED PYRIDAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL CONDITIONS
US11345698B2 (en) 2016-05-05 2022-05-31 Bial—R&D Investments, S.A. Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders
WO2017205801A1 (en) 2016-05-27 2017-11-30 Takeda Pharmaceutical Company Limited Combination of immunotherapy agents and spleen tyrosine kinase inhibitors
EP3472147B1 (en) 2016-06-16 2020-06-17 Janssen Pharmaceutica NV Azabenzimidazole derivatives as pi3k beta inhibitors
MX2018015707A (es) 2016-06-16 2019-03-21 Janssen Pharmaceutica Nv Derivados biciclicos de piridina, pirazina y pirimidina como inhibidores de pi3k beta.
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
WO2018013239A1 (en) 2016-07-13 2018-01-18 Takeda Pharmaceutical Company Limited Combination of spleen tyrosine kinase inhibitors and other therapeutic agents
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
CN108239067A (zh) * 2016-12-27 2018-07-03 沈阳药科大学 喹唑啉酮类衍生物及其制备方法和用途
JP6888101B2 (ja) 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物
AU2018246321B2 (en) 2017-03-29 2021-07-29 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as PI3K-beta inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
GB201710851D0 (en) * 2017-07-06 2017-08-23 Galápagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
JP7060694B2 (ja) 2018-01-18 2022-04-26 アレイ バイオファーマ インコーポレイテッド Retキナーゼ阻害剤としての置換ピロロ[2,3-d]ピリミジン化合物
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
JP7474709B2 (ja) 2018-02-27 2024-04-25 インサイト・コーポレイション A2a/a2b阻害剤としてのイミダゾピリミジン及びトリアゾロピリミジン
JP7381492B2 (ja) 2018-05-01 2023-11-15 レヴォリューション・メディスンズ,インコーポレイテッド Mtor阻害剤としてのc26-連結ラパマイシン類似体
CR20200578A (es) 2018-05-01 2021-02-22 Revolution Medicines Inc Análogos de rapamicina a c40, c28 y c32 como inhibidores de mtor
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
EP3805231A4 (en) 2018-05-30 2022-01-12 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. INHIBITOR CONTAINING A TRICYCLIC DERIVATIVE, METHOD FOR PREPARING IT AND ITS APPLICATION
CN112469707A (zh) * 2018-06-27 2021-03-09 利伯纳生物科学株式会社 脊髓性肌萎缩症的预防剂或治疗剂
GEP20237560B (en) 2018-07-05 2023-10-25 Incyte Corp Fused pyrazine derivatives as a2a / a2b inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Retキナーゼ阻害剤としての縮合複素環式化合物
CA3115088A1 (en) * 2018-10-15 2020-04-23 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
CN111434661B (zh) * 2019-01-11 2023-09-12 爱科诺生物医药(香港)有限公司 具有细胞坏死抑制活性的芳香杂环化合物及其应用
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PE20221085A1 (es) 2019-10-14 2022-07-05 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP2023503010A (ja) 2019-11-25 2023-01-26 上▲海▼翰森生物医▲薬▼科技有限公司 3種類の縮合環誘導体含有塩又は結晶形態及びその医薬組成物
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
EP4175719A1 (en) 2020-07-02 2023-05-10 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
EP4298099A1 (en) 2021-02-25 2024-01-03 Incyte Corporation Spirocyclic lactams as jak2 v617f inhibitors
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途
CN116217551A (zh) * 2023-02-21 2023-06-06 河南中医药大学 取代的吲唑或氮杂吲唑类化合物及其应用

Family Cites Families (266)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2313993A (en) * 1939-02-04 1943-03-16 Chromogen Inc Organic sulphur and selenium compounds
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
US3657744A (en) 1970-05-08 1972-04-25 Univ Minnesota Method for fixing prosthetic implants in a living body
FR2102541A5 (ru) * 1970-08-07 1972-04-07 Aquitaine Total Organico
EP0068378B1 (en) 1981-06-26 1986-03-05 Schering Corporation Novel imidazo(1,2-a)pyridines and pyrazines, processes for their preparation and pharmaceutical compositions containing them
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5040548A (en) 1989-06-01 1991-08-20 Yock Paul G Angioplasty mehtod
US5061273A (en) 1989-06-01 1991-10-29 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5350395A (en) 1986-04-15 1994-09-27 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US4748982A (en) 1987-01-06 1988-06-07 Advanced Cardiovascular Systems, Inc. Reinforced balloon dilatation catheter with slitted exchange sleeve and method
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
CA1322628C (en) 1988-10-04 1993-10-05 Richard A. Schatz Expandable intraluminal graft
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
US5292331A (en) 1989-08-24 1994-03-08 Applied Vascular Engineering, Inc. Endovascular support device
US5674278A (en) 1989-08-24 1997-10-07 Arterial Vascular Engineering, Inc. Endovascular support device
US6344053B1 (en) 1993-12-22 2002-02-05 Medtronic Ave, Inc. Endovascular support device and method
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
CZ283425B6 (cs) 1992-04-02 1998-04-15 Smithkline Beecham Corporation Fenylové deriváty a farmaceutické prostředky s jejich obsahem
WO1993019750A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating allergic or inflammatory diseases
WO1993019751A1 (en) 1992-04-02 1993-10-14 Smithkline Beecham Corporation Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor
TW225528B (ru) 1992-04-03 1994-06-21 Ciba Geigy Ag
BR9207175A (pt) 1992-10-28 1995-12-12 Genentech Inc Composição contendo antagonista de fator de crescimento de célula endotelial vascular sequência aminoácida de anticorpo monoclonal polipeptídeo e método de tratamento de tumor em mamífero
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
WO1996030347A1 (en) 1995-03-30 1996-10-03 Pfizer Inc. Quinazoline derivatives
DK0819129T3 (da) 1995-04-03 2000-10-23 Novartis Ag Pyrazolderivater og fremgangsmåde til deres fremstilling
CA2218503C (en) 1995-04-20 2001-07-24 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
CZ1598A3 (cs) 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
GB9521987D0 (en) 1995-10-26 1996-01-03 Ludwig Inst Cancer Res Phosphoinositide 3-kinase modulators
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CN100503580C (zh) 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
BR9709959A (pt) 1996-06-24 2000-05-09 Pfizer Derivados tricìclicos de fenilamino substituìdo para o tratamento de doenças hiperproliferativas
DE69712496T2 (de) 1996-07-18 2002-08-29 Pfizer Matrix metalloprotease-inhibitoren auf basis von phosphinsäuren
KR20000068248A (ko) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐아미노 하이드록삼산 유도체
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
WO1998014450A1 (en) 1996-10-02 1998-04-09 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
PT950059E (pt) 1997-01-06 2004-10-29 Pfizer Derivados de sulfona ciclicos
US6303636B1 (en) 1997-02-03 2001-10-16 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
JP3784076B2 (ja) 1997-02-07 2006-06-07 プリンストン ユニヴァーシティ 変性ヌクレオチド三燐酸基質を利用できる組み換えタンパクキナーゼ
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
BR9807678A (pt) 1997-02-11 2000-02-15 Pfizer Derivados de ácidos arilsulfonil-hidroxâmicos
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6340759B1 (en) 1997-10-02 2002-01-22 Eisai Co., Ltd. Fused pyridine derivatives
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
CO4990969A1 (es) 1998-02-14 2000-12-26 Glaxo Group Ltd Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
US6251689B1 (en) 1998-05-14 2001-06-26 Telik, Inc. Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof
EA200001224A1 (ru) 1998-06-23 2001-08-27 Глаксо Груп Лимитед Производные 2-(пурин-9-ил)-тетрагидрофуран-3,4-диола
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
CA2335094C (en) 1998-06-30 2008-12-23 The Dow Chemical Company Polymer polyols and a process for the production thereof
CN1152031C (zh) 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
BR9914526A (pt) 1998-10-16 2001-07-03 Pfizer Derivados de adenina
UA71587C2 (ru) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Translated By PlajАМИДЫ АНТРАНИЛОВОЙ КИСЛОТЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕЧЕБНЫХ СРЕДСТВ
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
HUP0105063A2 (hu) 1998-11-16 2002-04-29 Basf Ag 3-[Benz(ox/ti)azol-7-il]-1H-pirimidin-2,4-dionok
IL143596A0 (en) 1998-12-22 2002-04-21 Genentech Inc Vascular endothelial cell growth factor antagonists and uses thereof
DE60004781T2 (de) 1999-01-11 2004-07-08 Princeton University Kinase-inhibitoren mit hoher affinität zur ziel detektion und ihre verwendung
CA2366857C (en) 1999-03-30 2010-12-14 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
ES2246233T3 (es) 1999-05-04 2006-02-16 Schering Corporation Derivados de piperidina utiles como antagonistas de ccr5.
ES2244437T3 (es) 1999-05-04 2005-12-16 Schering Corporation Derivados de piperazina utiles como antagonistas de ccr5.
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
PL200923B1 (pl) 1999-08-21 2009-02-27 Nycomed Gmbh Lek zawierający inhibitor PDE w połączeniu z agonistą receptoraß₂ -adrenergicznego oraz zastosowanie połączenia roflumilastu i salmeterolu
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
IL148718A0 (en) 1999-09-17 2002-09-12 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
US6472153B1 (en) 1999-10-26 2002-10-29 Epoch Biosciences, Inc. Hybridization-triggered fluorescent detection of nucleic acids
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
ATE502941T1 (de) 2000-04-25 2011-04-15 Icos Corp Hemmer der menschlichen phosphatidyl-inositol-3- kinase delta
JP2002037787A (ja) 2000-05-16 2002-02-06 Kyowa Hakko Kogyo Co Ltd [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体の製造法
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
US6916828B2 (en) 2000-06-27 2005-07-12 Laboratorios S.A.L.V.A.T., S.A. Carbamates derivatived from arylakylamines
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
AU2001275760B2 (en) 2000-08-05 2005-03-17 Glaxo Group Limited 6.alpha., 9.alpha.-difluoro-17.alpha.-'(2-furanylcarboxyl) oxy!-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4,-diene-17-carbothioic acid S-fluoromethyl ester as an anti-inflammatory agent
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
DE60139964D1 (de) 2000-12-15 2009-10-29 Vertex Pharma Bakterielle Gyrase-Hemmer sowie deren Verwendung
PL362989A1 (en) 2000-12-22 2004-11-15 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as m3 antagonists
SK287414B6 (sk) 2000-12-28 2010-09-07 Laboratorios Almirall, S.A. Chinuklidínové deriváty a kompozície s ich obsahom
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
HUP0400070A2 (hu) 2001-04-30 2004-04-28 Glaxo Group Limited 17alfa-helyzetben ciklusos észtercsoportot tartalmazó androsztán-17béta-karbotiosav-észter-származékok mint gyulladásgátló szerek, eljárás a vegyületek előállítására és ezeket tartalmazó gyógyszerkészítmények
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
PA8546101A1 (es) 2001-05-25 2003-12-10 Pfizer Un antagonista de a2a en combinacion con un agente anticolinergico para el tratamiento de enfermedades obstructivas de las vias aereas
JP2005500290A (ja) 2001-06-12 2005-01-06 グラクソ グループ リミテッド 抗炎症性の、17β−カルボチオアートアンドロスタン誘導体である17α複素環エステル
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
EP2327767B1 (en) 2001-06-21 2015-04-29 BASF Enzymes LLC Nitrilases
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
CZ2004501A3 (cs) 2001-10-17 2004-09-15 Ucb, S.A. Chinuklidinové deriváty, způsoby jejich přípravy a jejich použití jako M2 a/nebo M3 inhibitoru muskarinového receptoru
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
MY130622A (en) 2001-11-05 2007-07-31 Novartis Ag Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors
WO2003048181A1 (en) 2001-12-01 2003-06-12 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
HUP0500107A3 (en) 2001-12-20 2011-05-30 Chiesi Farma Spa 1-alkyl-1-azoniabicyclo[2.2.2.]octane carbamate derivatives, pharmaceutical compositions comprising thereof and their use as muscarinic receptor antagonists
WO2003072592A1 (en) 2002-01-15 2003-09-04 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
AU2003201693A1 (en) 2002-01-21 2003-09-02 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
WO2003082341A1 (en) 2002-03-22 2003-10-09 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO[3,4-d] PYRIMIDINES AS KINASE MODULATORS
EP1490317A1 (en) 2002-03-26 2004-12-29 Boehringer Ingelheim Pharmaceuticals Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EA008830B1 (ru) 2002-03-26 2007-08-31 Бёрингер Ингельхайм Фармасьютиклз, Инк. Миметики глюкокортикоидов, способы их получения, фармацевтические композиции и их применение
US20090170803A1 (en) 2002-04-10 2009-07-02 Linden Joel M Adjunctive treatment of biological diseases
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
EP1517895B1 (en) 2002-06-25 2007-03-14 Merck Frosst Canada Ltd. 8-(biaryl) quinoline pde4 inhibitors
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
ES2518940T3 (es) 2002-07-08 2014-11-06 Pfizer Products Inc. Moduladores del receptor de glucocorticoides
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
PL373597A1 (en) 2002-08-10 2005-09-05 Altana Pharma Ag Piperidine-n-oxide-derivatives
EP1556049A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Piperidine-pyridazones and phthalazones as pde4 inhibitors
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
PL373146A1 (en) 2002-08-10 2005-08-22 Altana Pharma Ag Pyridazinone-derivatives as pde4 inhibitors
RS20050116A (en) 2002-08-17 2007-11-15 Altana Pharma Ag., Novel phenanthridines
CA2495603A1 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Benzonaphthyridines with pde 3/4 inhibiting activity
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
DE60231341D1 (de) 2002-08-23 2009-04-09 Ranbaxy Lab Ltd Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten
JP4587295B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Pde4インヒビターとしての3−ヒドロキシ−6−フェニルフェナントリジン
CA2495827C (en) 2002-08-29 2012-05-08 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤
CA2497903A1 (en) 2002-09-18 2004-04-01 Ono Pharmaceutical Co., Ltd. Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
WO2004031177A1 (ja) 2002-09-30 2004-04-15 Banyu Pharmaceutical Co., Ltd. 2−アミノベンズイミダゾール誘導体
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
AP2021A (en) 2002-10-23 2009-08-03 Glenmark Pharmaceuticals Ltd Novel tricyclic compounds useful for the treatmentof inflammatory and allergic disorders: Process f or their preparation and pharmaceutical compositions containing them
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
CA2532800C (en) 2003-07-23 2013-06-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
CN101906106A (zh) 2003-09-18 2010-12-08 康福玛医药公司 作为hsp90-抑制剂的新的杂环化合物
CA2545340A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
EP1687309A1 (en) 2003-11-17 2006-08-09 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
AR046845A1 (es) * 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
WO2005074603A2 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
RU2006134021A (ru) 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные гетероарил-конденсированного пиразола
KR100843526B1 (ko) 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
US7534797B2 (en) 2004-04-02 2009-05-19 Osi Pharmaceuticals, Inc. 6,6-Bicyclic ring substituted heterobicyclic protein kinase inhibitors
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
AU2005245875C1 (en) 2004-05-13 2017-08-31 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
KR100629060B1 (ko) 2004-08-11 2006-09-26 주식회사 엘지화학 새로운 벤즈이미다졸계 화합물
MX2007004051A (es) * 2004-10-07 2007-05-24 Boehringer Ingelheim Int Pi3-quinasas.
JP2006124971A (ja) * 2004-10-27 2006-05-18 Hibi:Kk Frp成形体からなる手摺部品または手摺及びその製造方法
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
JP2008520744A (ja) 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
EP1885356A2 (en) 2005-02-17 2008-02-13 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
WO2006091897A2 (en) 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Derivatives of 8-substituted xanthines
PE20061110A1 (es) 2005-03-24 2006-10-20 Glaxo Group Ltd Derivados de imidazopiridina como antagonistas de la bomba de acido (apa)
CN200942072Y (zh) * 2005-04-08 2007-09-05 Bsh博施及西门子家用器具有限公司 器皿篮、餐具篮和器皿洗涤机
EP1871754A1 (en) 2005-04-22 2008-01-02 Wyeth a Corporation of the State of Delaware Dihydrobenzofuran derivatives and uses thereof
US8859581B2 (en) 2005-04-25 2014-10-14 Merck Patent Gmbh Azaheterocyclic compounds as kinase inhibitors
CA2620254A1 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP1919914A2 (en) 2005-08-25 2008-05-14 F.Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
CN101309904A (zh) 2005-09-29 2008-11-19 惠氏公司 作为单胺再摄取调节剂用于治疗血管舒缩症状(vasomotorsymptoms,vms)的1-(1h-吲哚-1-基)-3-(甲基氨基)-1-苯基丙-2-醇衍生物和相关化合物
CA2623374A1 (en) 2005-09-30 2007-04-05 Astrazeneca Ab Imidazo [1,2-a] pyridine having anti-cell-proliferation activity
WO2007061737A2 (en) 2005-11-17 2007-05-31 Osi Pharmaceuticals, Inc. FUSED BICYCLIC mTOR INHIBITORS
AR057960A1 (es) 2005-12-02 2007-12-26 Osi Pharm Inc Inhibidores de proteina quinasa biciclicos
EP1979002A2 (en) 2005-12-19 2008-10-15 OSI Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
EP1880723A1 (en) 2006-07-14 2008-01-23 Novartis AG Combination of mTOR inhibitor and antifolate compound
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
CA2645137A1 (en) 2006-03-07 2007-09-13 James F. Blake Heterobicyclic pyrazole compounds and methods of use
US7651687B2 (en) 2006-03-13 2010-01-26 Osi Pharmaceuticals, Inc. Combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors
AU2007347115A1 (en) 2006-04-04 2008-10-23 The Regents Of The University Of California PI3 kinase antagonists
RU2437888C2 (ru) 2006-04-26 2011-12-27 Дженентек, Инк. Ингибиторы фосфоинозитид-3-киназы и содержащие их фармацевтические композиции
PT2041139E (pt) 2006-04-26 2012-01-13 Hoffmann La Roche Compostos farmacêuticos
US20080003254A1 (en) 2006-05-23 2008-01-03 Abbott Laboratories Systems and methods for delivering a rapamycin analog that do not inhibit human coronary artery endothelial cell migration
WO2008014822A1 (en) 2006-08-03 2008-02-07 Rottapharm S.P.A. 6-1h-imidazo-quinazoline and quinolines derivatives, new potent analgesics and anti-inflammatory agents
WO2008024977A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Isoquinoline, quinazoline and phthalazine derivatives
US8883820B2 (en) 2006-08-30 2014-11-11 Cellzome Ltd. Triazole derivatives as kinase inhibitors
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
US20090286779A1 (en) 2006-09-29 2009-11-19 Novartis Ag Pyrazolopyrimidines as lipid kinase inhibitors
CN101627038A (zh) * 2006-12-04 2010-01-13 阿斯利康(瑞典)有限公司 抗菌多环脲化合物
JP5442448B2 (ja) * 2006-12-22 2014-03-12 アステックス、セラピューティックス、リミテッド Fgfrインヒビターとしての二環式ヘテロ環式化合物
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
WO2008094737A2 (en) 2007-01-26 2008-08-07 Irm Llc Purine compounds and compositions as kinase inhibitors for the treatment of plasmodium related diseases
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
CN101681921B (zh) 2007-03-27 2013-03-27 桑迪士克3D公司 包括碳纳米管织物元件和转向元件的存储器单元及其形成方法
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
JP2010532756A (ja) 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド mTORC1及びmTORC2の両方の阻害剤を含む組み合わせ抗癌療法
AU2008282728B2 (en) 2007-08-02 2012-04-19 Amgen Inc. Pl3 kinase modulators and methods of use
CN101842098A (zh) * 2007-08-10 2010-09-22 基因实验室技术有限公司 用于治疗病毒感染的含氮的二环化学实体
UY31292A1 (es) 2007-08-14 2009-03-31 Imidazoles biciclicos fusionados
US20100311736A1 (en) * 2007-10-22 2010-12-09 Glaxosmithkline Llc Pyridosulfonamide derivatives as p13 kinase inhibitors
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors
US20110021541A1 (en) 2007-11-13 2011-01-27 White Stephen L Inhibitors of human phosphatidyl-inositol 3-kinase delta
AU2008328882A1 (en) * 2007-11-27 2009-06-04 Cellzome Limited Amino triazoles as PI3K inhibitors
US8153813B2 (en) 2007-12-20 2012-04-10 Abbott Laboratories Benzothiazole and benzooxazole derivatives and methods of use
KR101897881B1 (ko) 2008-01-04 2018-09-12 인텔리카인, 엘엘씨 특정 화학 물질, 조성물 및 방법
US20090192176A1 (en) * 2008-01-30 2009-07-30 Wyeth 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
CN101981037B (zh) 2008-01-30 2013-09-04 吉宁特有限公司 吡唑并嘧啶pi3k抑制剂化合物及使用方法
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
MX2010010151A (es) 2008-03-20 2010-10-25 Amgen Inc Moduladores de cinasa aurora y metodo de uso.
JP2011525535A (ja) 2008-06-24 2011-09-22 武田薬品工業株式会社 PI3K/mTOR阻害剤
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
BRPI0915231A2 (pt) 2008-07-08 2018-06-12 Intellikine Inc compostos inibidores de quinase e métodos de uso
WO2010039186A2 (en) * 2008-09-23 2010-04-08 Renovis, Inc. Compounds useful as faah modulators and uses thereof
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
EP2358720B1 (en) 2008-10-16 2016-03-02 The Regents of The University of California Fused ring heteroaryl kinase inhibitors
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
RS55055B1 (sr) * 2008-12-08 2016-12-30 Gilead Connecticut Inc Imidazopirazin syk inhibitori
CN102282147B (zh) 2009-01-28 2015-09-30 卡拉治疗学股份有限公司 二环吡唑并-杂环
EA026693B1 (ru) * 2009-08-17 2017-05-31 Интелликайн ЭлЭлСи Производные бензоксазола и бензотиазола в качестве ингибиторов pi3-киназы
WO2011149937A1 (en) 2010-05-24 2011-12-01 Intellikine, Inc. Heterocyclic compounds and uses thereof

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