MY158843A - Quinoline derivatives as p13 kinase inhibitors - Google Patents

Quinoline derivatives as p13 kinase inhibitors

Info

Publication number
MY158843A
MY158843A MYPI20094867A MYPI20094867A MY158843A MY 158843 A MY158843 A MY 158843A MY PI20094867 A MYPI20094867 A MY PI20094867A MY PI20094867 A MYPI20094867 A MY PI20094867A MY 158843 A MY158843 A MY 158843A
Authority
MY
Malaysia
Prior art keywords
quinoline derivatives
diseases
kinase inhibitors
invented
pancreatitis
Prior art date
Application number
MYPI20094867A
Other languages
English (en)
Inventor
Nicholas D Adams
Joelle Lorraine Burgess
Michael Gerard Darcy
Carla A Donatelli
Steven David Knight
Kenneth Allen Newlander
Lance Ridgers
Martha Sarpong
Stanley J Schmidt
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of MY158843A publication Critical patent/MY158843A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
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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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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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    • C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
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MYPI20094867A 2007-05-18 2008-05-16 Quinoline derivatives as p13 kinase inhibitors MY158843A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US93876107P 2007-05-18 2007-05-18

Publications (1)

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MY158843A true MY158843A (en) 2016-11-15

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MYPI20094867A MY158843A (en) 2007-05-18 2008-05-16 Quinoline derivatives as p13 kinase inhibitors

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US (6) US8138347B2 (enExample)
EP (3) EP2192902A4 (enExample)
JP (3) JP4814396B2 (enExample)
KR (1) KR101458660B1 (enExample)
CN (1) CN101754759B (enExample)
AR (1) AR066614A1 (enExample)
AU (1) AU2008254915B2 (enExample)
BR (1) BRPI0811761A2 (enExample)
CA (1) CA2686016C (enExample)
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Families Citing this family (270)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
US7928140B2 (en) 2007-08-02 2011-04-19 Amgen Inc. Benzothiazole PI3 kinase modulators for cancer treatment
JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
JP5599783B2 (ja) 2008-05-30 2014-10-01 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
EP2298731A4 (en) * 2008-06-25 2011-09-21 Takeda Pharmaceutical AMIDE COMPOUND
JP5564045B2 (ja) * 2008-09-02 2014-07-30 ノバルティス アーゲー 二環式キナーゼ阻害剤
KR101712576B1 (ko) 2008-11-10 2017-03-06 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
WO2010059549A1 (en) * 2008-11-18 2010-05-27 Glaxosmithkline Llc Prolyl hydroxylase inhibitors
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
RU2505539C2 (ru) 2008-12-23 2014-01-27 Эбботт Лэборетриз Антивирусные соединения
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
CA2751892A1 (en) 2009-01-15 2010-07-22 Rutgers, The State University Of New Jersey Benzo [c] phenanthridines as antimicrobial agents
AU2010231162B2 (en) 2009-04-02 2014-12-11 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Imidazo [2, 1-b] [ 1, 3, 4 ] thiadiazole derivatives
WO2010120935A1 (en) 2009-04-15 2010-10-21 Abbott Laboratories Anti-viral compounds
CA2760526A1 (en) 2009-04-30 2010-11-04 Rutgers, The State University Of New Jersey Antimicrobial agents
ES2459468T3 (es) 2009-05-15 2014-05-09 Novartis Ag Arilpiridinas como inhibidores de aldosterona sintasa
WO2010135568A1 (en) 2009-05-22 2010-11-25 Exelixis, Inc. Benzoxazepines as inhibitors of mtor and their use to treat cancer
EP2445902A2 (en) * 2009-06-25 2012-05-02 Amgen, Inc Heterocyclic compounds and their uses as inhibitors of pi3k activity
UA111579C2 (uk) 2009-08-17 2016-05-25 Інтеллікіне Ллк ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
WO2011021678A1 (ja) * 2009-08-21 2011-02-24 武田薬品工業株式会社 縮合複素環化合物
EP2473487B1 (en) * 2009-09-03 2016-10-26 Bristol-Myers Squibb Company Quinazolines as potassium ion channel inhibitors
KR20120063515A (ko) * 2009-09-09 2012-06-15 아빌라 테라퓨틱스, 인크. Ｐｉ３ 키나제 억제제 및 이들의 용도
CN102713618B (zh) 2009-09-16 2015-07-15 新基阿维罗米克斯研究公司 蛋白激酶复合物和抑制剂
WO2011038380A2 (en) * 2009-09-28 2011-03-31 Glaxosmithkline Llc Combination
EP2488184A4 (en) * 2009-10-12 2013-04-24 Glaxosmithkline Llc COMBINATION
WO2011051958A1 (en) 2009-10-30 2011-05-05 E.I. Du Pont De Nemours And Company Fungicidal pyrazolones
WO2011082285A1 (en) 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP5836367B2 (ja) 2010-05-12 2015-12-24 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キナーゼ阻害剤として有用な化合物
JP2013526540A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
JP2013526538A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
US9096584B2 (en) 2010-05-12 2015-08-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8933096B2 (en) 2010-06-09 2015-01-13 Rugers, The State University of New Jersey Antimicrobial agents
JP2013529643A (ja) 2010-06-23 2013-07-22 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 Ａｔｒキナーゼ阻害剤として有用なピロロピラジン誘導体
WO2011163610A2 (en) * 2010-06-25 2011-12-29 Rutgers, The State University Of New Jersey Antimicrobial agents
US9120749B2 (en) * 2010-07-30 2015-09-01 Oncotherapy Science, Inc. Quinoline derivatives and MELK inhibitors containing the same
EP2603078A4 (en) * 2010-08-09 2014-01-01 Glaxosmithkline Llc COMBINATION
EP2640366A2 (en) 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
WO2012068106A2 (en) 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
US20130317037A1 (en) * 2010-11-16 2013-11-28 Glaxosmithkline Intellectual Property Development Limited Method of administration and treatment
CN104689318A (zh) * 2010-11-19 2015-06-10 葛兰素史密斯克莱知识产权（第2号）有限公司 使用braf抑制剂的治疗方法
EP2643316A2 (en) 2010-11-24 2013-10-02 Exelixis, Inc. Benzoxazepines as inhibitors of p13k/mtor and methods of their use and manufacture
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
JP6026441B2 (ja) 2011-03-04 2016-11-16 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としてのアミノキノリン
WO2012122370A2 (en) * 2011-03-08 2012-09-13 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
CN102718745A (zh) * 2011-03-30 2012-10-10 中国科学院上海药物研究所 新型胺基吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
MX2013012486A (es) * 2011-04-29 2014-05-28 Exelixis Inc Metodo para tratar linfoma usando inhibidores de piridopirimidinona de fosfonio sitol 3-cinasa/diana de rapalamina en celulas de mamifero (pi3k/mtor).
JP2014522818A (ja) 2011-06-22 2014-09-08 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 Ａｔｒキナーゼ阻害剤として有用な化合物
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
TWI547494B (zh) 2011-08-18 2016-09-01 葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之胺基喹唑啉類
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
RU2018147217A (ru) 2011-09-30 2019-01-18 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
AU2012315384B2 (en) 2011-09-30 2017-08-10 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with ATR inhibitors
IN2014KN00943A (enExample) 2011-09-30 2015-08-21 Vertex Pharma
SG11201401937YA (en) 2011-11-04 2014-05-29 Hoffmann La Roche New aryl-quinoline derivatives
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2661510T3 (es) 2011-12-15 2018-04-02 Novartis Ag Uso de inhibidores de la actividad o función de PI3K
WO2013106756A2 (en) 2012-01-13 2013-07-18 Rutgers, The State University Of New Jersey Antimicrobial agents
CA2861521A1 (en) * 2012-02-06 2013-08-15 Glaxosmithkline Intellectual Property (No.2) Limited Novel use
WO2013117504A1 (en) 2012-02-06 2013-08-15 Glaxosmithkline Intellectual Property (No.2) Limited Pi3k inhibitors for treating cough
EP2828245A1 (en) 2012-03-21 2015-01-28 Rutgers, The State University of New Jersey Antimicrobial agents
CN104582795B (zh) 2012-04-05 2018-04-20 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物及其组合疗法
EP2863920B1 (en) 2012-06-20 2023-03-22 Eutropics Pharmaceuticals, Inc. Quinoline derivatives for use in the tratment of breast cancer
AR092530A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
AR092529A1 (es) 2012-09-13 2015-04-22 Glaxosmithkline Llc Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento
CN103497177B (zh) * 2012-09-29 2017-03-22 天津滨江药物研发有限公司 作为c‑Met抑制剂的氨基芳香杂环类化合物及其制备方法
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN103788071A (zh) * 2012-11-01 2014-05-14 中国人民解放军第二军医大学 N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途
EP2922544B1 (en) 2012-11-21 2018-08-01 Eutropics Pharmaceuticals, Inc. Methods and compositions useful for treating diseases involving bcl-2 family proteins with quinoline derivatives
LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
CN105143208B (zh) 2013-02-21 2017-09-26 葛兰素史密斯克莱知识产权发展有限公司 作为激酶抑制剂的喹唑啉
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
CN104098542A (zh) * 2013-04-11 2014-10-15 苏州朗信医药科技有限公司 一种6-溴代-4-(4-吡嗪基)喹啉的制备方法
US10732182B2 (en) 2013-08-01 2020-08-04 Eutropics Pharmaceuticals, Inc. Method for predicting cancer sensitivity
CN104418858B (zh) 2013-08-30 2018-12-11 浙江医药股份有限公司新昌制药厂 2,6-二含氮取代的嘌呤衍生物及其制备方法和其药物组合物与应用
KR20160060100A (ko) 2013-09-22 2016-05-27 칼리토르 사이언시즈, 엘엘씨 치환된 아미노피리미딘 화합물 및 이용 방법
CN104557955B (zh) * 2013-10-23 2017-05-03 上海汇伦生命科技有限公司 作为PI3K/mTOR抑制剂的三环类化合物，其制备方法和用途
AU2014342269B2 (en) 2013-10-30 2020-02-27 Eutropics Pharmaceuticals, Inc. Methods for determining chemosensitivity and chemotoxicity
US9458150B2 (en) 2013-11-08 2016-10-04 Rutgers, The State University Of New Jersey Antimicrobial agents
JP6496731B2 (ja) * 2013-11-27 2019-04-03 シグナルケム・ライフサイエンシーズ・コーポレイションＳｉｇｎａｌｃｈｅｍ Ｌｉｆｅｓｃｉｅｎｃｅｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍファミリーキナーゼ阻害剤としてのアミノピリジン誘導体
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
US9340540B2 (en) 2014-02-28 2016-05-17 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
CN104922116B (zh) * 2014-03-23 2020-08-11 上海诗丹德生物技术有限公司 甲基丙烯酰基苯并咪唑酮衍生物的用途
NO2714752T3 (enExample) * 2014-05-08 2018-04-21
ES2777608T3 (es) 2014-06-05 2020-08-05 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
WO2015192761A1 (zh) 2014-06-17 2015-12-23 辰欣药业股份有限公司 作为mTOR/PI3K抑制剂的吡啶并[1,2-a]嘧啶酮类似物
US11179394B2 (en) 2014-06-17 2021-11-23 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
CN117164657A (zh) 2014-08-12 2023-12-05 莫纳什大学 定向淋巴的前药
CN105330699B (zh) * 2014-08-13 2018-12-04 山东汇睿迪生物技术有限公司 一种含磷吡啶并[2,3-d]嘧啶-7-酮类化合物或其药学上可接受的盐、药物组合物及其应用
PT3180315T (pt) 2014-08-15 2020-05-27 Janssen Pharmaceuticals Inc Pirazoles
EP3180329B1 (en) 2014-08-15 2020-03-18 Janssen Pharmaceuticals, Inc. Triazoles as nr2b receptor inhibitors
NZ731185A (en) 2014-10-29 2024-03-22 Bicyclerd Ltd Bicyclic peptide ligands specific for mt1-mmp
WO2016138352A1 (en) 2015-02-27 2016-09-01 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
FR3033499A1 (fr) 2015-03-11 2016-09-16 Centre Leon-Berard Composition pour le traitement des tumeurs neuroendocrines pancreatiques
CN104961725B (zh) * 2015-06-18 2017-04-19 浙江大学 4‑α,β不饱和酰胺基喹啉类化合物及制备和应用
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
MX2018000352A (es) 2015-07-09 2018-08-15 Janssen Pharmaceutica Nv 4-azaindoles sustituidos y su uso como moduladores del receptor glun2b.
EP3328839A1 (en) * 2015-07-30 2018-06-06 Bristol-Myers Squibb Company Aryl substituted bicyclic heteroaryl compounds
US10329257B2 (en) * 2015-08-13 2019-06-25 The Broad Institute, Inc. Compositions and methods for treating tuberculosis
EP4327809A3 (en) 2015-09-02 2024-04-17 Takeda Pharmaceutical Company Limited Tyk2 inhibitors and uses thereof
CN118063537A (zh) 2015-09-08 2024-05-24 莫纳什大学 定向淋巴的前药
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
MX389001B (es) 2015-10-23 2025-03-20 Navitor Pharm Inc Moduladores de interacción de sestrina-gator2 y sus usos.
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
TWI713655B (zh) * 2015-12-16 2020-12-21 大陸商上海嘉坦醫藥科技有限公司 吡啶並[1,2-a]嘧啶酮類似物的晶型及其製備方法和中間體
KR20180108822A (ko) 2016-02-10 2018-10-04 얀센 파마슈티카 엔.브이. Nr2b-선택적 nmda 조절제로서 치환된 1,2,3-트라이아졸
WO2017147316A1 (en) 2016-02-25 2017-08-31 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
EP4234552A3 (en) 2016-03-09 2023-10-18 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
PT3426243T (pt) 2016-03-09 2021-08-19 Raze Therapeutics Inc Inibidores de 3-fosfoglicerato desidrogenase e utilizações dos mesmos
US11337969B2 (en) 2016-04-08 2022-05-24 X4 Pharmaceuticals, Inc. Methods for treating cancer
JP6994767B2 (ja) 2016-06-21 2022-01-14 エックス４ ファーマシューティカルズ， インコーポレイテッド Ｃｘｃｒ４阻害剤およびその使用
EP3808748B1 (en) 2016-06-21 2026-05-20 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
US10154992B2 (en) * 2016-07-12 2018-12-18 The Regents Of The University Of California Compounds and methods for treating HIV infection
AU2017312970B2 (en) * 2016-08-16 2021-08-12 Merck Patent Gmbh 2-oxo-imidazopyridines as reversible BTK inhibitors and uses thereof
TW201819376A (zh) 2016-10-06 2018-06-01 比利時商健生藥品公司 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途
TWI763722B (zh) 2016-10-14 2022-05-11 美商林伯士拉克許米公司 Tyk2抑制劑及其用途
CN110300590A (zh) 2016-10-21 2019-10-01 林伯士拉克许米公司 Tyk2抑制剂及其用途
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
CN106580986B (zh) * 2016-11-28 2017-09-15 王保亮 一种治疗少弱精子症的药物组合物
US20180193270A1 (en) 2016-11-29 2018-07-12 PureTech Health LLC Exosomes for delivery of therapeutic agents
US11091451B2 (en) 2016-12-05 2021-08-17 Raze Therapeutics, Inc. SHMT inhibitors and uses thereof
US20180153922A1 (en) 2016-12-06 2018-06-07 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Inhibition of expansion and function of pathogenic age-associated b cells and use for the prevention and treatment of autoimmune disease
EP3559018A1 (en) 2016-12-23 2019-10-30 Bicyclerd Limited Peptide derivatives having novel linkage structures
EP4169918B8 (en) 2016-12-26 2025-09-24 Institute of Materia Medica, Chinese Academy of Medical Sciences Quinazoline derivatives as inhibitors of pi3k for the treatment of cancer
ES2985986T3 (es) 2017-01-06 2024-11-08 Bicyclerd Ltd Conjugado biciclo para tratar el cáncer
AU2018230737B2 (en) 2017-03-08 2022-09-22 Takeda Pharmaceutical Company Limited Tyk2 inhibitors, uses, and methods for production thereof
EP3375778A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aryl-piperidine derivatives
EP3375784A1 (en) 2017-03-14 2018-09-19 Artax Biopharma Inc. Aza-dihydro-acridone derivatives
CN110891566B (zh) 2017-03-30 2023-12-19 塔克西斯医药股份有限公司 合成方法和合成中间体
WO2018191146A1 (en) 2017-04-10 2018-10-18 Navitor Pharmaceuticals, Inc. Heteroaryl rheb inhibitors and uses thereof
ES3040534T3 (en) 2017-04-26 2025-11-03 Navitor Pharm Inc Modulator of sestrin-gator2 interaction for use in the treatment of treatment-resistant depression
EP3615550A1 (en) 2017-04-27 2020-03-04 BicycleTx Limited Bicyclic peptide ligands and uses thereof
JP7352284B2 (ja) * 2017-05-15 2023-09-28 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン ＬＳＤ－１インヒビターとしてのピロロ〔２，３－ｃ〕ピリジン及び関連類似体
WO2019002842A1 (en) 2017-06-26 2019-01-03 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF
IL317854A (en) 2017-07-28 2025-02-01 Takeda Pharmaceuticals Co TYK2 inhibitors and their uses
JP7670481B2 (ja) 2017-08-04 2025-04-30 バイスクルテクス・リミテッド Ｃｄ１３７に対して特異的な二環式ペプチドリガンド
WO2019034866A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited BICYCLIC PEPTIDE LIGANDS CONJUGATES AND USES THEREOF
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
EP4306524A3 (en) 2017-08-29 2024-09-11 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
CN107793404A (zh) * 2017-11-07 2018-03-13 全椒先奇医药科技有限公司 一种治疗缺血性脑损伤药物组合物及其应用
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
TWI825046B (zh) 2017-12-19 2023-12-11 英商拜西可泰克斯有限公司 Epha2特用之雙環胜肽配位基
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
AU2019212969B2 (en) 2018-01-29 2025-01-23 Merck Patent Gmbh GCN2 inhibitors and uses thereof
CA3089762A1 (en) 2018-01-29 2019-08-01 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
CA3091775A1 (en) 2018-02-23 2019-08-29 Bicycletx Limited Multimeric bicyclic peptide ligands
KR20260028873A (ko) 2018-02-27 2026-03-04 아텍스 바이오파마 인코포레이티드 Tcr-nck 상호 작용의 억제제로서의 크로멘 유도체
CR20200464A (es) * 2018-03-08 2021-04-14 Incyte Corp Compuestos diólicos de aminopirazina como inhibidores de pi3k-y
EP3774732A4 (en) 2018-04-04 2022-02-09 Janssen Pharmaceutica NV PYRIDINE AND SUBSTITUTED PYRIMIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
IL301501B2 (en) 2018-04-24 2024-10-01 Vertex Pharma Antiproliferation compounds and uses thereof
EP3784669B1 (en) 2018-04-24 2023-10-25 Vertex Pharmaceuticals Incorporated Pteridinone compounds and uses thereof
WO2019229765A1 (en) * 2018-05-29 2019-12-05 Council Of Scientific & Industrial Research, India Bicycle topoisomerase i inhibiting compounds, process for preparation and use thereof
EP3575305A1 (fr) * 2018-05-31 2019-12-04 Biocidal Alternative Solutions Procédé de fabrication de composés comprenant un groupe fonctionnel oxazolopyridinones
EP3801069A4 (en) 2018-06-01 2022-03-16 Cornell University COMBINATION THERAPY FOR A PI3K-ASSOCIATED DISEASE OR DISORDER
US10980784B2 (en) 2018-06-15 2021-04-20 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
US11180531B2 (en) 2018-06-22 2021-11-23 Bicycletx Limited Bicyclic peptide ligands specific for Nectin-4
GB201810316D0 (en) 2018-06-22 2018-08-08 Bicyclerd Ltd Peptide ligands for binding to EphA2
KR102595520B1 (ko) * 2018-07-05 2023-10-30 엘지디스플레이 주식회사 헤테로아릴기를 가진 벤즈아졸 유도체 및 이를 포함하는 유기전계발광소자
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US10548889B1 (en) 2018-08-31 2020-02-04 X4 Pharmaceuticals, Inc. Compositions of CXCR4 inhibitors and methods of preparation and use
EP3846793B1 (en) 2018-09-07 2024-01-24 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
JP7619951B2 (ja) 2018-10-15 2025-01-22 武田薬品工業株式会社 Ｔｙｋ２阻害剤およびその使用
WO2020084305A1 (en) 2018-10-23 2020-04-30 Bicycletx Limited Bicyclic peptide ligands and uses thereof
WO2020086816A1 (en) 2018-10-24 2020-04-30 Navitor Pharmaceuticals, Inc. Polymorphic compounds and uses thereof
WO2020112937A1 (en) 2018-11-30 2020-06-04 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
AU2019389174A1 (en) 2018-11-30 2021-07-01 Kymera Therapeutics, Inc. Irak degraders and uses thereof
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
EP3670659A1 (en) 2018-12-20 2020-06-24 Abivax Biomarkers, and uses in treatment of viral infections, inflammations, or cancer
EP3897849A1 (en) 2018-12-21 2021-10-27 BicycleTx Limited Bicyclic peptide ligands specific for pd-l1
WO2020128527A1 (en) 2018-12-21 2020-06-25 Bicyclerd Limited Bicyclic peptide ligands specific for pd-l1
CA3126034A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
US20220184222A1 (en) 2019-04-02 2022-06-16 Bicycletx Limited Bicycle toxin conjugates and uses thereof
KR102980990B1 (ko) 2019-04-05 2026-06-25 카이메라 쎄라퓨틱스 인코포레이티드 Stat 분해제 및 이의 용도
EP3976027B1 (en) 2019-05-30 2025-11-05 Merck Sharp & Dohme LLC Quinoline derivatives as factor xi activation inhibitors
US11458149B1 (en) 2019-05-31 2022-10-04 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
US12624044B2 (en) 2019-06-10 2026-05-12 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
AU2020290772A1 (en) 2019-06-14 2022-01-06 Janssen Pharmaceutica Nv Pyrazine carbamates and their use as GluN2B receptor modulators
EP3983413A1 (en) 2019-06-14 2022-04-20 Janssen Pharmaceutica NV Substituted pyrazolo-pyrazines and their use as glun2b receptor modulators
SG11202112407PA (en) 2019-06-14 2021-12-30 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators
BR112021025132A2 (pt) 2019-06-14 2022-01-25 Janssen Pharmaceutica Nv Carbamatos de piridina e seu uso como moduladores do receptor glun2b
US20220324860A1 (en) 2019-06-14 2022-10-13 Janssen Pharmaceutica Nv SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
JP7667097B2 (ja) 2019-06-14 2025-04-22 ヤンセン ファーマシューティカ エヌ．ベー． 置換ピラゾロ－ピリジンアミド及びｇｌｕｎ２ｂ受容体調節因子としてのその使用
AU2020291188A1 (en) 2019-06-14 2022-01-20 Janssen Pharmaceutica Nv Substituted heteroaromatic Pyrazolo-pyridines and their use as GluN2B receptor modulators
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
US12558427B2 (en) 2019-07-17 2026-02-24 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
TWI860386B (zh) 2019-07-30 2024-11-01 英商拜西可泰克斯有限公司 異質雙環肽複合物
CA3150492A1 (en) 2019-09-11 2021-03-18 Donna L. Romero Usp30 inhibitors and uses thereof
US12215105B2 (en) 2019-09-13 2025-02-04 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
AU2020376950B2 (en) 2019-11-01 2026-06-11 Supernus Pharmaceuticals, Inc. Methods of treatment using an mTORC1 modulator
EP4069223A4 (en) 2019-12-05 2023-12-20 Janssen Pharmaceutica NV RAPAMYCIN ANALOGS AND THEIR USES
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3161878A1 (en) 2019-12-17 2021-06-24 Matthew M. Weiss Irak degraders and uses thereof
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors and uses thereof
US11679109B2 (en) 2019-12-23 2023-06-20 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
JP7810970B2 (ja) 2020-02-05 2026-02-04 シーポート・セラピューティクス・インコーポレイテッド 神経ステロイドの脂質プロドラッグ
AR121506A1 (es) 2020-03-03 2022-06-08 Pic Therapeutics Inc Inhibidores del eif4e y sus usos
WO2021188948A1 (en) 2020-03-19 2021-09-23 Kymera Therapeutics, Inc. Mdm2 degraders and uses thereof
TWI904146B (zh) * 2020-03-31 2025-11-11 美商卡默森屈有限公司 使用ｃｃｒ９抑制劑及抗ｉｌ-２３阻斷抗體治療發炎性腸道疾病的組成物及方法
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
CN116348476A (zh) 2020-08-03 2023-06-27 拜斯科技术开发有限公司 基于肽的接头
WO2022038158A1 (en) 2020-08-17 2022-02-24 Bicycletx Limited Bicycle conjugates specific for nectin-4 and uses thereof
EP4232425A4 (en) 2020-10-23 2024-07-24 Nimbus Clotho, Inc. Ctps1 inhibitors and uses thereof
WO2022120353A1 (en) 2020-12-02 2022-06-09 Ikena Oncology, Inc. Tead inhibitors and uses thereof
EP4255895A1 (en) 2020-12-02 2023-10-11 Ikena Oncology, Inc. Tead inhibitors and uses thereof
US12606568B2 (en) 2020-12-09 2026-04-21 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
AR124547A1 (es) 2020-12-30 2023-04-05 Kymera Therapeutics Inc Degradadores de irak y sus usos
KR20230153387A (ko) 2021-02-02 2023-11-06 리미널 바이오사이언시스 리미티드 Gpr84 길항제 및 이의 용도
JP2024506858A (ja) 2021-02-02 2024-02-15 リミナル・バイオサイエンシーズ・リミテッド Ｇｐｒ８４アンタゴニストおよびその使用
WO2022174253A1 (en) 2021-02-12 2022-08-18 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
MX2023009178A (es) 2021-02-15 2023-08-21 Kymera Therapeutics Inc Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos.
EP4295849A4 (en) 2021-02-16 2025-02-19 Ribotech Co., Ltd. COMPOUND FOR SUPPRESSION OF DEGRADATION OF MRNA CARRYING NONSENSE CODONS
CN117295737A (zh) 2021-03-05 2023-12-26 林伯士萨顿公司 Hpk1拮抗剂和其用途
EP4310081A4 (en) * 2021-03-18 2025-06-04 Suzhou Guokuang Pharmtech. Co., Ltd. Ctla-4 small molecule degradation agent and application thereof
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
US12325697B2 (en) 2021-04-09 2025-06-10 Nimbus Clio, Inc. CBL-B modulators and uses thereof
AU2022258968A1 (en) 2021-04-16 2023-10-19 Ikena Oncology, Inc. Mek inhibitors and uses thereof
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
CN115353512B (zh) * 2021-07-30 2025-07-08 上海翊石医药科技有限公司 一种杂环脲类化合物及其制备方法和用途
CN113416181B (zh) * 2021-08-02 2022-05-03 四川大学 喹唑啉类衍生物及其用途
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
IL310924A (en) 2021-08-25 2024-04-01 Pic Therapeutics Inc Eif4e inhibitors and uses thereof
CN115869320A (zh) * 2021-09-27 2023-03-31 广州嘉越医药科技有限公司 一种吡啶并[1,2-a]嘧啶酮类化合物的应用
JP2024540080A (ja) 2021-10-29 2024-10-31 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその合成
WO2023114984A1 (en) 2021-12-17 2023-06-22 Ikena Oncology, Inc. Tead inhibitors and uses thereof
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
WO2023173053A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023211889A1 (en) 2022-04-25 2023-11-02 Ikena Oncology, Inc. Polymorphic compounds and uses thereof
CN119768393A (zh) 2022-05-25 2025-04-04 医肯纳肿瘤学公司 Mek抑制剂和其用途
WO2023250082A2 (en) * 2022-06-22 2023-12-28 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of dyrk/clk and uses thereof
WO2024012534A1 (zh) * 2022-07-13 2024-01-18 武汉人福创新药物研发中心有限公司 杂环并苯环类化合物及其制备方法和用途
EP4565569A1 (en) 2022-08-02 2025-06-11 Liminal Biosciences Limited Aryl-triazolyl and related gpr84 antagonists and uses thereof
WO2024028365A1 (en) 2022-08-02 2024-02-08 Liminal Biosciences Limited Substituted pyridone gpr84 antagonists and uses thereof
EP4565568A1 (en) 2022-08-02 2025-06-11 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
EP4605089A1 (en) * 2022-10-20 2025-08-27 Mekanistic Therapeutics LLC Compounds useful in modulating egfr and pi3k
WO2024112894A1 (en) 2022-11-22 2024-05-30 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
CN116239594B (zh) * 2023-03-05 2023-09-22 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) 6-(咪唑并[1,2-a]吡啶-6-基)喹唑啉衍生物及用途
US20250059164A1 (en) 2023-06-23 2025-02-20 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2025045915A1 (en) * 2023-08-29 2025-03-06 Institut National de la Santé et de la Recherche Médicale Methods for inducing muscle hypertrophy
EP4780462A1 (en) 2023-09-21 2026-07-29 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
CN118126038B (zh) * 2024-05-08 2024-07-12 烟台大学 吡唑并吡啶类衍生物及其制备方法和应用

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE533691C (de) * 1929-06-10 1931-09-23 I G Farbenindustrie Akt Ges Verfahren zur Darstellung von Chinolin- und Acridinverbindungen, die im Kern eine Benzthiazolyl-, Benzoxazolyl- oder Benzimidazolylgruppe und eine primaere, sekundaere oder tertiaere Aminogruppe enthalten
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
WO1996005186A1 (en) * 1994-08-10 1996-02-22 Takeda Chemical Industries, Ltd. Thiazolidinedione derivatives, their production and use
US5925656A (en) 1995-04-10 1999-07-20 Dr. Reddy's Research Foundation Compounds having antidiabetic, hypolipidemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
EP0801063B1 (en) 1996-04-09 2003-01-15 Dr. Reddy's Laboratories Ltd. Thiazolidinedione derivatives having antidiabetic, hypolipidaemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
ID24175A (id) 1997-11-28 2000-07-13 Lg Chemical Ltd Turunan-turunan imidazol yang mempunyai aktivitas penghambatan untuk farnesil transferase dan proses pembuatannya
AU4005299A (en) 1998-05-19 1999-12-06 Regents Of The University Of California, The Thiazolidine and oxazolidine derivatives for the treatment of acute myocardial infarction and inhibition of cardiomyocyte apoptosis
AU5261001A (en) 2000-04-27 2001-11-12 Imperial Cancer Research Technology Ltd Condensed heteroaryl derivatives
US7343348B2 (en) * 2000-05-19 2008-03-11 First American Residential Group, Inc. System for performing real-estate transactions over a computer network using participant templates
US6900226B2 (en) * 2000-09-06 2005-05-31 Hoffman-La Roche Inc. Neuropeptide Y antagonists
US6452014B1 (en) * 2000-12-22 2002-09-17 Geron Corporation Telomerase inhibitors and methods of their use
BR0207846A (pt) * 2001-03-07 2005-09-13 Incyte San Diego Inc Derivados heterocìclicos para o tratamento de câncer e outras doenças proliferativas
EP1377976A2 (de) * 2001-03-28 2004-01-07 Bayer Chemicals AG Optischer datenträger enthaltend in der informationsschicht einen merocyaninfarbstoff als lichtabsorbierende verbindung
EP1392283A4 (en) 2001-05-16 2004-10-20 Cytovia Inc SUBSTITUTED CUMARINE AND CHINOLINE AS CASPASE ACTIVATORS
SI1397364T1 (sl) * 2001-05-24 2007-12-31 Lilly Co Eli Novi pirolni derivati kot farmacevtske uäśinkovine
AUPR688101A0 (en) 2001-08-08 2001-08-30 Luminis Pty Limited Protein domains and their ligands
CA2473740A1 (en) 2002-01-18 2003-07-31 David Solow-Cordero Methods of treating conditions associated with an edg receptor
AR038703A1 (es) * 2002-02-28 2005-01-26 Novartis Ag Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
US20050019825A9 (en) * 2002-03-15 2005-01-27 Qing Dong Common ligand mimics: pseudothiohydantoins
AU2003291613B2 (en) 2002-04-30 2007-09-27 Merck & Co., Inc. Aryl-link-aryl substituted thiazolidine-dione and oxazolidine-dione as sodium channel blockers
MXPA05000453A (es) 2002-07-10 2005-03-23 Applied Research Systems Derivados de benceno fusionados a azolidinona-vinilo.
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
EP1531813A1 (en) 2002-07-10 2005-05-25 Applied Research Systems ARS Holding N.V. Use of compounds for increasing spermatozoa motility
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
EP1597255A1 (en) * 2002-11-13 2005-11-23 Rigel Pharmaceuticals, Inc. Rhodanine derivatives and pharmaceutical compositions containing them
HUP0203985A3 (en) 2002-11-18 2005-04-28 Gene Res Lab Inc New York N Use of a pharmaceutical composition for alleviating side effect
GB0302882D0 (en) 2003-02-07 2003-03-12 Univ Cardiff Improvements in or relating to agents for the treatment of cardiovascular dysfunction and weight loss
MXPA05009722A (es) * 2003-03-10 2006-03-09 Schering Corp Inhibidores heterociclicos de cinasa: metodos de uso y sintesis.
EP1617844A4 (en) 2003-04-03 2009-07-22 Prana Biotechnology Ltd TREATMENT OF NEUROLOGICAL DISEASES
WO2004089925A1 (en) * 2003-04-03 2004-10-21 Semafore Pharmaceuticals, Inc. Pi-3 kinase inhibitor prodrugs
US20060106077A1 (en) 2003-07-18 2006-05-18 Pintex Pharmaceuticals, Inc. Pin1-Modulating compounds and methods of use thereof
CA2531140C (en) 2003-07-28 2013-06-18 Applied Research Systems Ars Holding N.V. 2-imino-4-(thio) oxo-5-polycyclovinylazolines for use as pi3 kinase inhibitors
EP1654380A4 (en) 2003-08-14 2009-09-09 Insight Biopharmaceuticals Ltd METHODS AND PHARMACEUTICAL COMPOSITIONS FOR MODULATING HEPARANASE ACTIVATION AND USES THEREOF
CN1930128A (zh) 2004-01-16 2007-03-14 惠氏公司 受体酪氨酸激酶抑制剂的喹啉中间体及其合成
WO2005085277A1 (en) * 2004-02-06 2005-09-15 Concepcion Gisela P Cyclic hexapeptides, process and use thereof
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
ES2317238T3 (es) 2004-07-01 2009-04-16 F. Hoffmann-La Roche Ag Quinolina-tiazolinonas con actividad antiproliferante cdk-1.
US7452993B2 (en) 2004-07-27 2008-11-18 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US20060249289A1 (en) 2005-05-05 2006-11-09 Halliburton Energy Services, Inc. Set-delayed cement compositions comprising hydrated lime and silica and methods of cementing in subterranean formations
GB0509224D0 (en) 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Inhibitors of intracellular enzymatic activity
US20070004763A1 (en) 2005-06-10 2007-01-04 Nand Baindur Aminoquinoline and aminoquinazoline kinase modulators
US7449571B2 (en) 2005-06-14 2008-11-11 Board Of Regents Of The University Of Nebraska Halogenated aminoquinolines and oligonucleotides containing the same
EP1896461A2 (en) * 2005-06-30 2008-03-12 Amgen Inc. Bis-aryl kinase inhibitors and their use in the treatment of inflammation, angiogenesis and cancer
CA2619706A1 (en) 2005-08-17 2007-02-22 Schering Corporation Novel high affinity quinoline-based kinase ligands
US20090170848A1 (en) * 2006-03-02 2009-07-02 Smithkline Beecham Corporation Thiazolones for use as pi3 kinase inhibitors
US7667043B2 (en) * 2006-03-20 2010-02-23 E.I. Du Pont De Nemours And Company Molecular structures with controllable electron conducting properties
AR060391A1 (es) * 2006-04-11 2008-06-11 Smithkline Beecham Corp Compuestos de quinolin tiazolidinadiona, sustituidos con heterociclos, composiciones farmaceuticas que los contienen y usos para preparar medicamentos que inhiben la actividad de pi3 quinasas.
WO2007139496A1 (en) 2006-05-30 2007-12-06 Clanotech Ab Quinoline derivatives acting as tyrosine kinase inhibitors
PT2049502E (pt) * 2006-07-28 2012-04-02 Novartis Ag Quinazolinas 2,4-substituídas como inibidores da lípido cinase
TW200902008A (en) * 2007-05-10 2009-01-16 Smithkline Beecham Corp Quinoxaline derivatives as PI3 kinase inhibitors
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa

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