KR101353829B1 - Ｐｉ-3 키나제 억제제로서 사용되는 피리미딘 유도체 - Google Patents

Ｐｉ-3 키나제 억제제로서 사용되는 피리미딘 유도체 Download PDF

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KR101353829B1
KR101353829B1 KR1020087020198A KR20087020198A KR101353829B1 KR 101353829 B1 KR101353829 B1 KR 101353829B1 KR 1020087020198 A KR1020087020198 A KR 1020087020198A KR 20087020198 A KR20087020198 A KR 20087020198A KR 101353829 B1 KR101353829 B1 KR 101353829B1
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substituted
unsubstituted
amine
compound
pyridin
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KR20080096776A (ko
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매튜 버거
지-지에 니
사비나 페키
고다나 아탈라
사라 바툴리스
켈리 프레지어
아론 스미스
조엘 버하겐
얀첸 장
앨런 웨그먼
사이먼 엔지
키스 피스터
대니얼 푼
알리시아 루이
테레사 피크
폴 바산티
에드윈 이바노비치
웬디 팬틀
토마스 헨드릭슨
마크 냅
한 메리트
찰스 볼리바
매리언 위즈먼
시아후아 신
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노파르티스 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020087020198A 2006-01-20 2007-01-22 Ｐｉ-3 키나제 억제제로서 사용되는 피리미딘 유도체 Expired - Fee Related KR101353829B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US76078906P 2006-01-20 2006-01-20
US60/760,789 2006-01-20
PCT/US2007/001708 WO2007084786A1 (en) 2006-01-20 2007-01-22 Pyrimidine derivatives used as pi-3 kinase inhibitors

Publications (2)

Publication Number Publication Date
KR20080096776A KR20080096776A (ko) 2008-11-03
KR101353829B1 true KR101353829B1 (ko) 2014-01-21

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KR1020087020198A Expired - Fee Related KR101353829B1 (ko) 2006-01-20 2007-01-22 Ｐｉ-3 키나제 억제제로서 사용되는 피리미딘 유도체

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US (2) US8217035B2 (enExample)
EP (2) EP1984350B1 (enExample)
JP (1) JP5161110B2 (enExample)
KR (1) KR101353829B1 (enExample)
CN (1) CN101389622B (enExample)
AR (2) AR059087A1 (enExample)
AT (1) ATE478064T1 (enExample)
AU (1) AU2007206048B2 (enExample)
BR (1) BRPI0707189B1 (enExample)
CA (1) CA2636993C (enExample)
CR (1) CR10163A (enExample)
CY (1) CY1111091T1 (enExample)
DE (1) DE602007008529D1 (enExample)
DK (2) DK1984350T3 (enExample)
EA (1) EA018083B1 (enExample)
EC (1) ECSP088630A (enExample)
ES (2) ES2351172T3 (enExample)
GE (1) GEP20115147B (enExample)
GT (1) GT200800143A (enExample)
HN (1) HN2008001144A (enExample)
HR (2) HRP20100603T1 (enExample)
IL (1) IL192763A (enExample)
JO (1) JO2660B1 (enExample)
MA (1) MA30208B1 (enExample)
ME (2) ME00012B (enExample)
MY (1) MY144233A (enExample)
NO (1) NO342183B1 (enExample)
NZ (1) NZ569771A (enExample)
PE (1) PE20071322A1 (enExample)
PL (2) PL1984350T3 (enExample)
PT (2) PT1984350E (enExample)
RS (2) RS52928B (enExample)
SI (2) SI2261223T1 (enExample)
SM (1) SMP200800048B (enExample)
SV (1) SV2008002984A (enExample)
TN (1) TNSN08305A1 (enExample)
TW (2) TWI385170B (enExample)
UA (1) UA96284C2 (enExample)
WO (1) WO2007084786A1 (enExample)
ZA (1) ZA200806017B (enExample)

Families Citing this family (367)

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Publication number Priority date Publication date Assignee Title
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
TW200808739A (en) 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
WO2008023159A1 (en) 2006-08-24 2008-02-28 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
PE20081679A1 (es) 2006-12-07 2008-12-18 Hoffmann La Roche Compuestos del inhibidor de fosfoinositida 3-cinasa y metodos de uso
CA2675558A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
JP5676249B2 (ja) * 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
WO2009007750A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
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
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
WO2009093981A1 (en) * 2008-01-23 2009-07-30 S Bio Pte Ltd Triazine compounds as kinase inhibitors
BRPI0908049A2 (pt) * 2008-03-05 2015-08-11 Novartis Ag Uso de derivados de pririmidina para o tratamento de doenças dependentes de egfr ou de doenças que possuem resistência adquirida a agentes que são direcionados aos membros da família de egfr
EP2474323A3 (en) * 2008-03-26 2012-10-10 Novartis AG Imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
AU2012203914C1 (en) * 2008-03-26 2013-11-28 Novartis Ag 5imidazoquinolines and pyrimidine derivatives as potent modulators of VEGF-driven angiogenic processes
WO2009120094A2 (en) * 2008-03-27 2009-10-01 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
WO2009157880A1 (en) * 2008-06-27 2009-12-30 S*Bio Pte Ltd Pyrazine substituted purines
KR20110028651A (ko) * 2008-07-11 2011-03-21 노파르티스 아게 (ａ) 포스포이노시타이드 3-키나제 억제제 및 (ｂ) ｒａｓ/ｒａｆ/ｍｅｋ 경로의 조절제의 조합물
WO2010012740A1 (en) * 2008-07-29 2010-02-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
US20100068204A1 (en) * 2008-09-12 2010-03-18 Wyeth 4-aryloxyquinolin-2(1h)-ones as mtor kinase and pi3 kinase inhibitors, for use as anti-cancer agents
CA2738868C (en) * 2008-10-01 2017-01-17 Novartis Ag Smoothened antagonism for the treatment of hedgehog pathway-related disorders
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
CA2736361C (en) * 2008-10-31 2017-10-10 Novartis Ag Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor
US8653098B2 (en) * 2008-11-20 2014-02-18 Genentech, Inc. Pyrazolopyridine PI3K inhibitor compounds and methods of use
ES2551557T3 (es) 2008-12-19 2015-11-19 Boehringer Ingelheim International Gmbh Pirimidin-4-carboxamidas cíclicas como antagonistas del receptor CCR2 para el tratamiento de inflamaciones, asma y EPOC
CA2754446A1 (en) 2009-03-05 2010-09-10 Daiichi Sankyo Company, Limited Pyridine derivative
CA2756067A1 (en) 2009-03-27 2010-09-30 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
US20120046333A1 (en) * 2009-04-09 2012-02-23 Oncothyreon Incorporated Methods and Compositions of PI-3 Kinase Inhibitors for Treating Fibrosis
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
CA2760179A1 (en) * 2009-05-15 2010-11-18 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and an antidiabetic compound
MX2011012520A (es) * 2009-05-27 2011-12-12 Hoffmann La Roche Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
CA2767008C (en) 2009-07-07 2018-01-30 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
US20120065166A1 (en) * 2009-08-12 2012-03-15 Virginia Espina Bone Modulators And Methods Therewith
CN101993416B (zh) * 2009-08-27 2013-09-11 中国科学院上海药物研究所 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途
KR20120063515A (ko) * 2009-09-09 2012-06-15 아빌라 테라퓨틱스, 인크. Ｐｉ３ 키나제 억제제 및 이들의 용도
JP2013508299A (ja) 2009-10-16 2013-03-07 リブ−エックス ファーマシューティカルズ，インコーポレイテッド 抗微生物性化合物および抗微生物性化合物の製造方法および使用方法
JP6274723B2 (ja) 2009-10-16 2018-02-07 メリンタ セラピューティクス，インコーポレイテッド 抗微生物性化合物および抗微生物性化合物の製造方法および使用方法
PL2513093T3 (pl) 2009-12-17 2015-03-31 Centrexion Therapeutics Corp Nowi antagoniści receptora CCR2 i ich zastosowanie
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
EP2569295B1 (en) 2010-05-12 2014-11-19 Boehringer Ingelheim International GmbH New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
WO2011141474A1 (en) 2010-05-12 2011-11-17 Boehringer Ingelheim International Gmbh Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
EP2571870B1 (en) 2010-05-17 2015-01-21 Boehringer Ingelheim International GmbH Ccr2 antagonists and uses thereof
US9018212B2 (en) 2010-05-25 2015-04-28 Boehringer Ingelheim International Gmbh Pyridazine carboxamides as CCR2 receptor antagonists
JP5721242B2 (ja) 2010-06-01 2015-05-20 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 新規ｃｃｒ２アンタゴニスト
SA111320519B1 (ar) 2010-06-11 2014-07-02 Astrazeneca Ab مركبات بيريميدينيل للاستخدام كمثبطات atr
TW201219353A (en) 2010-09-07 2012-05-16 Daiichi Sankyo Co Ltd Manufacturing method of benzoates
CN104945373A (zh) * 2010-10-01 2015-09-30 诺华有限公司 制造嘧啶衍生物的方法
KR20130139999A (ko) * 2010-10-14 2013-12-23 어리어드 파마슈티칼스, 인코포레이티드 Egfr-유도된 암의 세포 증식을 억제하는 방법
JP2014503488A (ja) * 2010-11-12 2014-02-13 バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー プロパ−２−エン−１−アミンから出発して２，２−ジフルオロエチルアミンを調製する方法
US20130310352A1 (en) * 2010-11-12 2013-11-21 Board Of Regents, The University Of Texas System Dexamethasone combination therapy
EA201390917A1 (ru) 2010-12-21 2013-12-30 Новартис Аг Дигетероарильные соединения в качестве ингибиторов vps34
CA2826387A1 (en) * 2011-02-11 2012-08-16 Dana Farber Cancer Institute, Inc. Method of inhibiting hamartoma tumor cells
CZ305457B6 (cs) * 2011-02-28 2015-09-30 Ústav organické chemie a biochemie, Akademie věd ČR v. v. i. Pyrimidinové sloučeniny inhibující tvorbu oxidu dusnatého a prostaglandinu E2, způsob výroby a použití
CN107501241B (zh) 2011-03-28 2020-10-13 梅制药公司 化合物、含有其的药物组合物以及它们在治疗增生性疾病中的用途
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US9271988B2 (en) 2011-07-01 2016-03-01 Novartis Ag Combination therapy comprising a CDK4/6 inhibitor and a P13K inhibitor for use in the treatment of cancer
JP5786258B2 (ja) 2011-07-15 2015-09-30 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 新規かつ選択的なｃｃｒ２拮抗薬
DK2734205T3 (en) 2011-07-21 2018-06-14 Tolero Pharmaceuticals Inc Heterocyclic Protein Kinase Inhibitors
CN103764144B (zh) 2011-08-31 2016-07-20 诺华股份有限公司 Pi3k抑制剂与mek抑制剂的协同组合
KR20140059786A (ko) * 2011-09-01 2014-05-16 노파르티스 아게 골암의 치료에 사용하기 위한 또는 골 내로의 원발성 암 세포의 전이성 파종을 예방하기 위한 pi3k 억제제
MX342326B (es) 2011-09-27 2016-09-26 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
US20140235630A1 (en) * 2011-09-30 2014-08-21 Beth Israel Deaconess Medical Center, Inc. Compositions and methods for the treatment of proliferative diseases
RU2014120792A (ru) * 2011-10-28 2015-12-10 Новартис Аг Способ лечения стромальных опухолей желудочно-кишечного тракта
US20140343128A1 (en) * 2011-11-15 2014-11-20 Novartis Ag Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the Janus Kinase 2 - Signal Transducer and Activator of Transcription 5 pathway
UY34632A (es) * 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
SG11201406584TA (en) 2012-04-24 2014-11-27 Vertex Pharma Dna-pk inhibitors
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
CN104349779A (zh) * 2012-05-16 2015-02-11 诺华股份有限公司 Pi-3激酶抑制剂的剂量方案
CN104350144B (zh) 2012-05-23 2017-08-04 弗·哈夫曼-拉罗切有限公司 获得和使用内胚层和肝细胞的组合物和方法
CA2872541A1 (en) 2012-06-06 2013-12-12 Novartis Ag Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease
WO2013192367A1 (en) 2012-06-22 2013-12-27 Novartis Ag Neuroendocrine tumor treatment
US20150224190A1 (en) 2012-07-06 2015-08-13 Mohamed Bentires-Alj Combination of a phosphoinositide 3-kinase inhibitor and an inhibitor of the IL-8/CXCR interaction
EP2874632B1 (en) * 2012-07-23 2020-06-17 Sphaera Pharma Pte. Ltd Triazine compound having pi3k-alpha and mtor inhibiting activity
CA2879704A1 (en) * 2012-08-16 2014-02-20 Novartis Ag Combination of pi3k inhibitor and c-met inhibitor
CN102952086B (zh) * 2012-09-28 2013-08-28 天津科创医药中间体技术生产力促进有限公司 一种2-吗啉基取代嘧啶类化合物的制备方法
EP2909181B1 (en) 2012-10-16 2017-08-09 Tolero Pharmaceuticals, Inc. Pkm2 modulators and methods for their use
ES2605638T3 (es) 2012-10-23 2017-03-15 Novartis Ag Proceso Mejorado para fabricar 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina
US9296733B2 (en) * 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
RU2661896C2 (ru) 2012-11-16 2018-07-23 Мерк Шарп И Доум Корп. Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека
WO2014093230A2 (en) * 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
EP2742940B1 (en) 2012-12-13 2017-07-26 IP Gesellschaft für Management mbH Fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-l-aza-bicyclo-[2.2.2]octane for adminstration once daily, twice daily or thrice daily
CN104245693B (zh) * 2012-12-14 2016-08-24 上海恒瑞医药有限公司 嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用
SG11201505896YA (en) 2013-02-20 2015-09-29 Novartis Ag Treatment of cancer using humanized anti-egfrviii chimeric antigen receptor
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
AU2014224238B2 (en) 2013-03-06 2016-07-14 Novartis Ag Formulations of organic compounds
RS62649B1 (sr) 2013-03-12 2021-12-31 Vertex Pharma Inhibitori dnk-pk
US9498532B2 (en) 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
PT2970205T (pt) 2013-03-14 2019-08-26 Tolero Pharmaceuticals Inc Inibidores da jak2 e da alk2 e métodos para a sua utilização
CA2903979A1 (en) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
MX366978B (es) 2013-03-15 2019-08-01 Novartis Ag Conjugados de anticuerpo - farmaco.
US9913844B2 (en) 2013-03-21 2018-03-13 Novartis Ag Combination therapy
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
RU2015147601A (ru) * 2013-05-01 2017-06-05 Ф. Хоффманн-Ля Рош Аг С-связанные гетероциклоалкилзамещенные пиримидины и их применения
TWI710558B (zh) * 2013-05-01 2020-11-21 瑞士商赫孚孟拉羅股份公司 二雜芳基化合物及其用途
AU2014264318B2 (en) 2013-05-07 2017-03-16 Novartis Ag Combination of a PI3 kinase inhibitor with paclitaxel for use in the treatment or prevention of a cancer of the head and neck
CN105283180A (zh) 2013-06-11 2016-01-27 诺华股份有限公司 Pi3k抑制剂与微管去稳定剂的药物组合
JP2016522247A (ja) 2013-06-18 2016-07-28 ノバルティス アーゲー 組合せ医薬
JP2016527305A (ja) 2013-08-08 2016-09-08 ノバルティス アーゲー Ｐｉｍキナーゼ阻害剤の組合せ
EP4772247A2 (en) 2013-08-14 2026-07-08 Novartis AG Combination therapy comprising ribociclib and fulvestrant for the treatment of cancer
WO2015022657A1 (en) 2013-08-16 2015-02-19 Novartis Ag Pharmaceutical combinations
MX2016002975A (es) 2013-09-09 2016-10-21 Melinta Therapeutics Inc Compuestos antimicrobianos y métodos de fabricación y utilización de los mismos.
US9937183B2 (en) 2013-09-09 2018-04-10 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
CN103483345B (zh) * 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
EP3049442A4 (en) 2013-09-26 2017-06-28 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
KR102411227B1 (ko) 2013-10-17 2022-06-21 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정
MX2016009226A (es) * 2014-01-15 2016-10-05 Novartis Ag Combinaciones farmaceuticas.
UA122479C2 (uk) 2014-01-24 2020-11-25 Дана-Фарбер Кенсер Інстітьют, Інк. Виділена молекула антитіла, яка зв’язується з людським білком програмованої смерті-1 (pd-1)
PL3099717T3 (pl) 2014-01-31 2019-10-31 Novartis Ag Cząsteczki przeciwciała dla TIM-3 i ich zastosowanie
US9340540B2 (en) 2014-02-28 2016-05-17 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
EA201691765A1 (ru) 2014-03-14 2016-12-30 Новартис Аг Молекулы антител против lag-3 и их применения
BR112016023811B8 (pt) 2014-04-22 2023-01-10 Piqur Therapeutics Ag Método para fabricação para derivados de triazina, pirimidina e piridina, seus intermediários e seus métodos de fabricação
WO2016001789A1 (en) * 2014-06-30 2016-01-07 Pfizer Inc. Pyrimidine derivatives as pi3k inhibitors for use in the treatment of cancer
WO2016001341A1 (en) * 2014-07-03 2016-01-07 F. Hoffmann-La Roche Ag Sulfonylaminopyridine compounds, compositions and methods of use
WO2016020791A1 (en) 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
MX2017001946A (es) 2014-08-12 2017-06-19 Novartis Ag Conjugados de farmacos con anticuerpos anti-cdh6.
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
CN104151256B (zh) * 2014-08-14 2016-08-24 西安交通大学 二取代苯甲酰胺类化合物及其合成方法和应用
EP3191126B1 (en) 2014-09-13 2020-05-13 Novartis AG Combination therapies of alk inhibitors
CN105461714B (zh) * 2014-09-29 2017-11-28 山东轩竹医药科技有限公司 并环类pi3k抑制剂
KR20170066546A (ko) 2014-10-03 2017-06-14 노파르티스 아게 조합 요법
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
SG11201702401RA (en) 2014-10-14 2017-04-27 Novartis Ag Antibody molecules to pd-l1 and uses thereof
NZ731185A (en) 2014-10-29 2024-03-22 Bicyclerd Ltd Bicyclic peptide ligands specific for mt1-mmp
MA40933A (fr) 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
UY36401A (es) 2014-11-14 2016-06-30 Novartis Ag Conjugados anticuerpos-fármacos
CN105085476B (zh) * 2014-11-24 2018-03-09 苏州晶云药物科技有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法
EP3229803B1 (en) * 2014-12-12 2020-01-29 Massachusetts General Hospital Treatment of breast cancer brain metastases
JP6397577B2 (ja) * 2014-12-17 2018-09-26 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドＳｈａｎｇｈａｉ Ｈａｉｙａｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ． ２−モルホリノ−４，６−二置換ピリミジン誘導体、その製法および医薬における使用
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
MX375970B (es) 2014-12-23 2025-03-06 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos.
CN105832741A (zh) * 2015-01-16 2016-08-10 复旦大学 Pi3k抑制剂与紫杉醇的药物组合物及其在制备抗肿瘤药物中的应用
WO2016138352A1 (en) 2015-02-27 2016-09-01 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EA039121B1 (ru) 2015-02-27 2021-12-07 Куртана Фармасьютикалс, Инк. ИНГИБИРОВАНИЕ АКТИВНОСТИ Olig2
TWI706958B (zh) 2015-03-10 2020-10-11 美商艾杜諾生物科技公司 活化「干擾素基因刺激因子」依賴性訊息傳導之組合物及方法
WO2016145417A1 (en) 2015-03-11 2016-09-15 Melinta Therapeutics, Inc. Antimicrobial compounds and methods of making and using the same
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
WO2016151501A1 (en) 2015-03-25 2016-09-29 Novartis Ag Pharmaceutical combinations
EP3274344B1 (en) 2015-03-25 2019-04-24 Novartis Ag Formylated n-heterocyclic derivatives as fgfr4 inhibitors
US20190194315A1 (en) 2015-06-17 2019-06-27 Novartis Ag Antibody drug conjugates
WO2017004134A1 (en) 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
MX383744B (es) 2015-07-02 2025-03-14 Centrexion Therapeutics Corp Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidin-1-il) (5-metil-6-(((2r, 6s)-6-(p-tolil)tetrahidro-2h-piran-2-il) metilamino) pirimidin-4-il) metanona.
WO2017009751A1 (en) * 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
US20180340025A1 (en) 2015-07-29 2018-11-29 Novartis Ag Combination therapies comprising antibody molecules to lag-3
US20180207273A1 (en) 2015-07-29 2018-07-26 Novartis Ag Combination therapies comprising antibody molecules to tim-3
ES2962460T3 (es) 2015-08-28 2024-03-19 Novartis Ag Inhibidores de mdm2 y combinaciones de estos
CN105001151B (zh) * 2015-08-28 2017-07-14 苏州明锐医药科技有限公司 布帕尼西中间体及其制备方法
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
MX389001B (es) * 2015-10-23 2025-03-20 Navitor Pharm Inc Moduladores de interacción de sestrina-gator2 y sus usos.
CR20180229A (es) 2015-10-29 2018-08-24 Novartis Ag Conjugados de anticuerpos que comprenden un agonista del receptor tipo toll
CN108472289A (zh) 2015-11-02 2018-08-31 诺华股份有限公司 磷脂酰肌醇3-激酶抑制剂的给药方案
PT3370768T (pt) 2015-11-03 2022-04-21 Janssen Biotech Inc Anticorpos que se ligam especificamente ao pd-1 e seus usos
RU2018123524A (ru) 2015-12-03 2020-01-09 Новартис Аг Фармацевтическая диагностика
WO2017106352A1 (en) 2015-12-14 2017-06-22 Raze Therapeutics, Inc. Caffeine inhibitors of mthfd2 and uses thereof
CN106883185B (zh) * 2015-12-15 2021-07-09 重庆博腾制药科技股份有限公司 一种4-氯-2-三氟甲基嘧啶的制备方法
CN108495651A (zh) 2015-12-17 2018-09-04 诺华股份有限公司 抗pd-1的抗体分子及其用途
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
EP3231799A1 (en) * 2016-04-14 2017-10-18 Universität Basel 4-(azetidin-1-yl)pyrimidine derivatives with anti-mitotic and anti-proliferative activity
US11098047B2 (en) 2016-05-06 2021-08-24 BioVersys AG Antimicrobials and methods of making and using same
LT3458067T (lt) * 2016-05-18 2021-04-26 Torqur Ag Neurologinių sutrikimų gydymas
KR102483630B1 (ko) 2016-05-18 2023-01-02 토르쿠르 아게 피부 병변의 치료
WO2017206904A1 (zh) * 2016-06-02 2017-12-07 上海海雁医药科技有限公司 Pi3k抑制剂及其药学上可接受的盐和多晶型物及其应用
US10689378B2 (en) 2016-06-20 2020-06-23 Novartis Ag Triazolopyridine compounds and uses thereof
JP7042812B2 (ja) 2016-06-20 2022-03-28 ノバルティス アーゲー トリアゾロピリミジン化合物の結晶形態
JP2019524872A (ja) 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
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
US10988465B2 (en) 2016-06-21 2021-04-27 X4 Pharmaceuticals, Inc. CXCR4 inhibitors and uses thereof
EP3808748B1 (en) 2016-06-21 2026-05-20 X4 Pharmaceuticals, Inc. Substituted piperidines as cxcr4-inhibitors
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
CN106905294A (zh) * 2016-07-08 2017-06-30 苏州科睿思制药有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法
WO2018064076A1 (en) 2016-09-27 2018-04-05 Cero Therapeutics, Inc. Chimeric engulfment receptor molecules
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
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
WO2018092064A1 (en) 2016-11-18 2018-05-24 Novartis Ag Combinations of mdm2 inhibitors and bcl-xl inhibitors
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
EP3559018A1 (en) 2016-12-23 2019-10-30 Bicyclerd Limited Peptide derivatives having novel linkage structures
ES2985986T3 (es) 2017-01-06 2024-11-08 Bicyclerd Ltd Conjugado biciclo para tratar el cáncer
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
WO2018163051A1 (en) 2017-03-06 2018-09-13 Novartis Ag Methods of treatment of cancer with reduced ubb expression
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
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
WO2018185618A1 (en) 2017-04-03 2018-10-11 Novartis Ag Anti-cdh6 antibody drug conjugates and anti-gitr antibody combinations and methods of treatment
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
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
EP3630118A4 (en) 2017-05-23 2021-03-31 MEI Pharma, Inc. COMBINATION THERAPY
US20200362058A1 (en) 2017-05-24 2020-11-19 Novartis Ag Antibody-cytokine engrafted proteins and methods of use
KR102920712B1 (ko) 2017-05-24 2026-01-30 노파르티스 아게 항체-사이토카인 생착된 단백질 및 암 치료에 있어서의 사용 방법
WO2018215937A1 (en) 2017-05-24 2018-11-29 Novartis Ag Interleukin-7 antibody cytokine engrafted proteins and methods of use in the treatment of cancer
MX2019015885A (es) 2017-06-22 2020-09-10 Novartis Ag Moleculas de anticuerpo que se unen a cd73 y usos de las mismas.
US20200172628A1 (en) 2017-06-22 2020-06-04 Novartis Ag Antibody molecules to cd73 and uses thereof
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
MX2020001727A (es) 2017-08-14 2020-03-20 Mei Pharma Inc Terapia de combinacion.
WO2019034868A1 (en) 2017-08-14 2019-02-21 Bicyclerd Limited CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF
JP7290627B2 (ja) * 2017-08-17 2023-06-13 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム Ａｔｒキナーゼの複素環式阻害剤
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP4306524A3 (en) 2017-08-29 2024-09-11 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
KR102811888B1 (ko) 2017-09-08 2025-05-27 에프. 호프만-라 로슈 아게 암의 진단 및 치료 방법
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.
DK3688032T3 (da) 2017-09-26 2025-12-15 Cero Therapeutics Holdings Inc Kimære engulfment-receptormolekyler og anvendelsesfremgangsmåder
CN109651341A (zh) * 2017-10-11 2019-04-19 上海医药工业研究院 二吗啉氰基嘧(吡)啶类衍生物及作为抗肿瘤药物应用
US11351156B2 (en) 2017-10-13 2022-06-07 Inserm Combination treatment of pancreatic cancer
WO2019101871A1 (en) 2017-11-23 2019-05-31 Inserm (Institut National De La Sante Et De La Recherche Medicale) A new marker for predicting the sensitivity to pi3k inhibitors
BR112020009855A8 (pt) 2017-11-23 2023-01-10 Piqur Therapeutics Ag Tratamento de distúrbios de pele
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
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
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
GB201721265D0 (en) 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
BR112020012651A2 (pt) 2017-12-22 2020-12-01 Ravenna Pharmaceuticals, Inc. compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
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
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
CA3089762A1 (en) 2018-01-29 2019-08-01 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
AU2019212969B2 (en) 2018-01-29 2025-01-23 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
RU2020135107A (ru) 2018-03-28 2022-04-29 Серо Терапьютикс, Инк. Клеточные иммунотерапевтические композиции и их применения
US12291557B2 (en) 2018-03-28 2025-05-06 Cero Therapeutics Holdings, Inc. Chimeric TIM4 receptors and uses thereof
MX2020010235A (es) 2018-03-28 2020-10-28 Cero Therapeutics Inc Vectores de expresion para receptores de engullimiento quimerico, celulas hospederas geneticamente modificadas y usos de los mismos.
BR112020020246A8 (pt) 2018-04-05 2022-10-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de cinase axl e uso dos mesmos
JPWO2019194220A1 (ja) * 2018-04-06 2021-05-13 日本曹達株式会社 （ヘテロ）アリールスルホンアミド化合物および有害生物防除剤
US11236079B2 (en) * 2018-04-10 2022-02-01 Neuropore Therapies, Inc. Morpholine derivates as inhibitors of Vps34
CN112189012B (zh) 2018-04-10 2024-02-13 神经孔疗法股份有限公司 作为pi3激酶和自噬途径的调节剂的三取代芳基和杂芳基衍生物
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
UY38247A (es) 2018-05-30 2019-12-31 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
WO2019232244A2 (en) 2018-05-31 2019-12-05 Novartis Ag Antibody molecules to cd73 and uses thereof
US10980784B2 (en) 2018-06-15 2021-04-20 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CN108864067B (zh) * 2018-06-20 2020-05-12 郑州大学 一种2-炔丙巯基-5-氰基嘧啶类衍生物及其制备方法和应用
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
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
KR20210038906A (ko) 2018-07-26 2021-04-08 스미토모 다이니폰 파마 온콜로지, 인크. 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제
CN112585136B (zh) 2018-08-17 2024-06-25 诺华股份有限公司 作为smarca2/brm atp酶抑制剂的脲化合物和组合物
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
EP3873532A1 (en) 2018-10-31 2021-09-08 Novartis AG Dc-sign antibody drug conjugates
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
GB201820325D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for psma
GB201820288D0 (en) 2018-12-13 2019-01-30 Bicycle Tx Ltd Bicycle peptide ligaands specific for MT1-MMP
GB201820295D0 (en) 2018-12-13 2019-01-30 Bicyclerd Ltd Bicyclic peptide ligands specific for MT1-MMP
WO2020124397A1 (en) 2018-12-19 2020-06-25 Inventisbio Shanghai Ltd. C-terminal src kinase inhibitors
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
AU2019409132B2 (en) 2018-12-21 2026-08-06 Novartis Ag Antibodies to PMEL17 and conjugates thereof
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
WO2020128527A1 (en) 2018-12-21 2020-06-25 Bicyclerd Limited Bicyclic peptide ligands specific for pd-l1
CN109705033B (zh) * 2019-01-22 2021-03-30 杭州壹瑞医药科技有限公司 N-杂芳基磺酰胺类衍生物及制备和应用
CN109651297B (zh) * 2019-01-22 2022-05-27 杭州壹瑞医药科技有限公司 一种n-苄基-n-芳基磺酰胺类衍生物及制备和应用
CA3126034A1 (en) 2019-01-23 2020-07-30 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
HUE072069T2 (hu) 2019-02-12 2025-10-28 Sumitomo Pharma America Inc 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
AU2020245437A1 (en) 2019-03-22 2021-09-30 Sumitomo Pharma Oncology, Inc. Compositions comprising PKM2 modulators and methods of treatment using the same
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
US11458149B1 (en) 2019-05-31 2022-10-04 Ikena Oncology, Inc. TEAD inhibitors and uses thereof
US12624044B2 (en) 2019-06-10 2026-05-12 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
WO2020251972A1 (en) 2019-06-10 2020-12-17 Kymera Therapeutics, Inc. Smarca degraders and uses thereof
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
US20220354452A1 (en) 2019-07-02 2022-11-10 Inserm (Institut National De La Santé Et De La Rechrche Médical) Use of ultrafast elasticity imaging for detecting pancreatic cancers
WO2021001431A1 (en) 2019-07-02 2021-01-07 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of pi3ka-selective inhibitors for treating metastatic disease in patients suffering from pancreatic cancer
US20220354863A1 (en) 2019-07-02 2022-11-10 Inserm (Institut National De La Santè Et De La Recherch Médicale) Methods for the prophylactic treatment of cancer in patients suffering from pancreatitis
AU2020300619A1 (en) 2019-07-03 2022-01-27 Sumitomo Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (TNK1) inhibitors 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
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Ｅｎｔｐｄ２抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
DK4034535T3 (da) 2019-09-26 2026-04-07 Novartis Ag Aza-quinolinforbindelser og anvendelser deraf
US20240058446A1 (en) 2019-10-03 2024-02-22 Cero Therapeutics, Inc. Chimeric tim4 receptors 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
US11679109B2 (en) 2019-12-23 2023-06-20 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
WO2021133917A1 (en) 2019-12-23 2021-07-01 Kymera Therapeutics, Inc. Smarca inhibitors 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
WO2021159993A1 (en) * 2020-02-14 2021-08-19 Pharmablock Sciences (Nanjing) , Inc. Inhibitors of interleukin-1 receptor associated kinase (irak) /fms-like receptor tyrosine kinase (flt3), pharmaceutical products thereof, and methods thereof
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
BR112022019387A2 (pt) * 2020-03-27 2022-11-16 Dong A St Co Ltd Derivados de aminopirimidina e seu uso como moduladores de receptores de aril hidrocarbonetos
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
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
KR20210158019A (ko) 2020-06-23 2021-12-30 주식회사 온코빅스 포스파티딜이노시톨 3-키나제(pi3k) 억제제로써 pten 과오종 증후군에 의한 종양 세포의 성장 또는 증식을 억제하는데 유용한 신규한 피리미딘 유도체 및 이의 약제학적으로 허용가능한 염, 및 이를 유효성분으로 함유하는 약제학적 조성물
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
AR123185A1 (es) 2020-08-10 2022-11-09 Novartis Ag Compuestos y composiciones para inhibir ezh2
WO2022036285A1 (en) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Compositions and methods for treating cancer with chimeric tim receptors in combination with inhibitors of poly (adp-ribose) polymerase
JP7868033B2 (ja) 2020-08-14 2026-06-01 セロ・セラピューティクス・ホールディングス・インコーポレイテッド キメラｔｉｍ受容体およびその使用
WO2022036287A1 (en) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Anti-cd72 chimeric receptors and uses thereof
WO2022038158A1 (en) 2020-08-17 2022-02-24 Bicycletx Limited Bicycle conjugates specific for nectin-4 and uses thereof
US20230321285A1 (en) 2020-08-31 2023-10-12 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
WO2022043558A1 (en) 2020-08-31 2022-03-03 Advanced Accelerator Applications International Sa Method of treating psma-expressing cancers
WO2022043556A1 (en) 2020-08-31 2022-03-03 Novartis Ag Stable radiopharmaceutical composition
EP4232425A4 (en) 2020-10-23 2024-07-24 Nimbus Clotho, Inc. Ctps1 inhibitors and uses thereof
TWI877433B (zh) 2020-11-30 2025-03-21 大陸商杭州阿諾生物醫藥科技有限公司 用於治療ｐｉｋ３ｃａ突變癌症的組合療法
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
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Ａｌｋ﹘５抑制劑和彼之用途
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
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.
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
CA3212006A1 (en) 2021-02-26 2022-09-01 Kelonia Therapeutics, Inc. Lymphocyte targeted lentiviral vectors
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
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
AU2022258829A1 (en) 2021-04-16 2023-10-26 Novartis Ag Antibody drug conjugates and methods for making 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
FI4376874T3 (fi) 2021-07-28 2026-04-08 Cero Therapeutics Holdings Inc Kimeerisiä tim4-reseptoreita ja niiden käyttöjä
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
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
US20250197375A1 (en) * 2021-12-08 2025-06-19 Kineta, Inc. Pyrimidines and methods of their use
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
CN114213340B (zh) 2022-02-22 2022-06-07 北京蓝晶微生物科技有限公司 2,4-二氨基嘧啶氧化物的制备方法
CN114591326B (zh) * 2022-02-28 2024-02-27 上海筛杰生物医药有限公司 Cct-251921的中间体及其制备方法
WO2023173057A1 (en) 2022-03-10 2023-09-14 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023173053A1 (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
CN117186072B (zh) * 2022-06-01 2026-03-27 安驰达生物医药技术(广州)有限公司 一种抑制磷脂酰肌醇-3-激酶γ亚型活性的化合物及其制备方法与应用
EP4565568A1 (en) 2022-08-02 2025-06-11 Liminal Biosciences Limited Heteroaryl carboxamide and related gpr84 antagonists and uses thereof
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
WO2024112894A1 (en) 2022-11-22 2024-05-30 PIC Therapeutics, Inc. Eif4e inhibitors and uses thereof
US20250059164A1 (en) 2023-06-23 2025-02-20 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CN122374300A (zh) * 2023-08-01 2026-07-10 意大利学院科技基金会 用于治疗癌症、良性肿瘤、视网膜病症、血管病症和心肌病的新rhoj/cdc42抑制剂
EP4780462A1 (en) 2023-09-21 2026-07-29 Takeda Pharmaceutical Company Limited Tyk2 inhibitors for use in the treatment of inflammatory bowel disease
PY2501648A (es) 2024-01-12 2025-10-31 Syngenta Crop Protection Ag Nuevos compuestos de carboxamida
WO2026008750A1 (en) 2024-07-05 2026-01-08 Syngenta Crop Protection Ag Novel carboxamide compounds
WO2026119962A1 (en) 2024-12-04 2026-06-11 Syngenta Crop Protection Ag Novel phenyl carboxamide compounds

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004048365A1 (en) 2002-11-21 2004-06-10 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

Family Cites Families (120)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB581334A (en) 1943-09-29 1946-10-09 Francis Henry Swinden Curd New pyrimidine compounds
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 １，２‐ジアミノシクロヘキサン異性体のシス白金（２）錯体
US4323581A (en) 1978-07-31 1982-04-06 Johnson & Johnson Method of treating carcinogenesis
US4329726A (en) * 1978-12-01 1982-05-11 Raychem Corporation Circuit protection devices comprising PTC elements
IL73534A (en) 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
WO1988007045A1 (fr) 1987-03-09 1988-09-22 Kyowa Hakko Kogyo Co., Ltd. Derives de la substance physiologiquement active k-252
US4994386A (en) 1987-07-13 1991-02-19 Pharmacia Diagnostics, Inc. Production of HBLV virus in the HSB-2 cell line
US4904768A (en) 1987-08-04 1990-02-27 Bristol-Myers Company Epipodophyllotoxin glucoside 4'-phosphate derivatives
EP0383919A4 (en) 1988-02-04 1992-08-05 Kyowa Hakko Kogyo Co., Ltd. Staurosporin derivatives
US4929726A (en) 1988-02-09 1990-05-29 Georgia State University Foundation, Inc. Novel diazines and their method of preparation
US5238944A (en) 1988-12-15 1993-08-24 Riker Laboratories, Inc. Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
US4929624A (en) 1989-03-23 1990-05-29 Minnesota Mining And Manufacturing Company Olefinic 1H-imidazo(4,5-c)quinolin-4-amines
GB9012311D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
US5389640A (en) 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
US6410010B1 (en) 1992-10-13 2002-06-25 Board Of Regents, The University Of Texas System Recombinant P53 adenovirus compositions
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
US5268376A (en) 1991-09-04 1993-12-07 Minnesota Mining And Manufacturing Company 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines
EP0540185A1 (en) 1991-10-10 1993-05-05 Schering Corporation 4'-(N-substituted-N-oxide)staurosporine derivatives
US5266575A (en) 1991-11-06 1993-11-30 Minnesota Mining And Manufacturing Company 2-ethyl 1H-imidazo[4,5-ciquinolin-4-amines
AU3064992A (en) 1991-11-08 1993-06-07 University Of Southern California Compositions containing k-252 compounds for potentiation of neurotrophin activity
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5948898A (en) 1992-03-16 1999-09-07 Isis Pharmaceuticals, Inc. Methoxyethoxy oligonucleotides for modulation of protein kinase C expression
US5621100A (en) 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5756494A (en) 1992-07-24 1998-05-26 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
ES2225824T3 (es) 1992-08-31 2005-03-16 Ludwig Institute For Cancer Research Nonapeptido aislado derivado del gen mage-3 y presentado por hla-a1, y sus usos.
DE69331228T4 (de) 1992-09-21 2002-09-05 Kyowa Hakko Kogyo Co., Ltd. Heilmittel für thrombozytopenia
KR100335584B1 (ko) 1992-10-28 2002-11-29 제넨테크, 인코포레이티드 혈관내피세포성장인자에대한길항제
US5395937A (en) 1993-01-29 1995-03-07 Minnesota Mining And Manufacturing Company Process for preparing quinoline amines
US5352784A (en) 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
DK0708772T3 (da) 1993-07-15 2000-09-18 Minnesota Mining & Mfg Imidazo[4,5,-c]pyridin-4-aminer
US5478932A (en) 1993-12-02 1995-12-26 The Board Of Trustees Of The University Of Illinois Ecteinascidins
EP1449529B1 (en) 1993-12-23 2010-01-27 Eli Lilly And Company Protein Kinase C Inhibitors
US5587459A (en) 1994-08-19 1996-12-24 Regents Of The University Of Minnesota Immunoconjugates comprising tyrosine kinase inhibitors
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5482936A (en) 1995-01-12 1996-01-09 Minnesota Mining And Manufacturing Company Imidazo[4,5-C]quinoline amines
ATE446955T1 (de) 1995-03-30 2009-11-15 Pfizer Prod Inc Chinazolinone derivate
US5786355A (en) 1995-04-13 1998-07-28 Taiho Pharmaceutical Co., Ltd. 4,6-diarylpyrimidine derivatives and salts thereof
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
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
WO1997007081A2 (en) 1995-08-11 1997-02-27 Yale University Glycosylated indolocarbazole synthesis
FR2741881B1 (fr) 1995-12-01 1999-07-30 Centre Nat Rech Scient Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques
DE69635966T2 (de) 1995-12-08 2006-11-30 Janssen Pharmaceutica N.V. (Imidazol-5-yl)Methyl-2-Chinolinonderivate als Farnesyl Protein transferase Inhibitoren
KR100447918B1 (ko) 1996-07-25 2005-09-28 동아제약주식회사 대장을포함한위장관보호작용을갖는플라본및플라바논화합물
CN1189562C (zh) 1996-08-02 2005-02-16 吉倪塞思技术公司 针对核糖核苷酸还原酶r1和r2组分的抗肿瘤反义序列
JP3734907B2 (ja) 1996-12-19 2006-01-11 富士写真フイルム株式会社 現像処理方法
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6126965A (en) 1997-03-21 2000-10-03 Georgetown University School Of Medicine Liposomes containing oligonucleotides
EP1017394B1 (en) 1997-07-12 2005-12-07 Cancer Research Technology Limited Cyclin dependent kinase inhibiting purine derivatives
ES2213286T3 (es) 1997-07-24 2004-08-16 Zenyaku Kogyo Kabushiki Kaisha Compuestos heterociclicos y agente antitumoral que los contiene como ingredientes activos.
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
US6150362A (en) 1997-12-12 2000-11-21 Henkin; Jack Triazine angiogenesis inhibitors
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
DK0930302T3 (da) 1998-01-16 2003-07-21 Hoffmann La Roche Benzosulfonderivater
KR100743287B1 (ko) 1998-05-29 2007-07-26 수젠, 인크. 피롤기로 치환된 2-인돌리논 단백질 인산화 효소 억제제
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville Glycogen synthase kinase 3 inhibitoren
US20030083242A1 (en) 1998-11-06 2003-05-01 Alphonse Galdes Methods and compositions for treating or preventing peripheral neuropathies
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
CA2359680A1 (en) 1999-01-22 2000-07-27 David M. Armistead Kinase inhibitors
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
SK286641B6 (sk) 1999-05-04 2009-03-05 Schering Corporation Piperazínové deriváty užitočné ako CCR5 antagonisty, farmaceutické prípravky s ich obsahom a ich použitie
PL203117B1 (pl) 1999-05-04 2009-08-31 Schering Corp Piperydynopiperydynowa pochodna użyteczna jako antagonista CCR5, zawierająca ją kompozycja farmaceutyczna i jej zastosowanie
AR024464A1 (es) 1999-06-25 2002-10-02 Genentech Inc Anticuerpos anti-erbb2 humanizados.
WO2001000214A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
US6329380B1 (en) 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
EP1206265B1 (en) 1999-06-30 2003-11-12 Merck & Co., Inc. Src kinase inhibitor compounds
AU6014900A (en) 1999-07-13 2001-01-30 Kyowa Hakko Kogyo Co. Ltd. Staurosporin derivatives
ATE250053T1 (de) 1999-07-15 2003-10-15 Pharmacopeia Inc Bradikinin b1 rezeptor antagonisten
PT1244647E (pt) 1999-11-05 2006-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de vegf
HRP20020751B1 (hr) 2000-02-15 2011-01-31 Sugen Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
GB2361236B (en) 2000-03-29 2002-04-24 Cyclacel Ltd Pyrimidines useful against proliferative disorders
EP1274718B1 (en) 2000-04-12 2006-10-18 Genaera Corporation A process for the preparation of 7.alpha.-hydroxy 3-aminosubstituted sterols using intermediates with an unprotected 7.alpha.-hydroxy group
AU5261001A (en) 2000-04-27 2001-11-12 Imperial Cancer Research Technology Ltd Condensed heteroaryl derivatives
KR100711042B1 (ko) 2000-04-28 2007-04-24 다나베 세이야꾸 가부시키가이샤 환상 화합물
AU2001268711A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
CA2413134C (en) 2000-06-30 2010-05-11 Glaxo Group Limited Quinazoline ditosylate salt compounds
WO2002020495A2 (en) 2000-09-06 2002-03-14 Chiron Corporation Inhibitors of glycogen synthase kinase 3
BRPI0113757B8 (pt) 2000-09-11 2017-11-07 Chiron Corp derivados de quinolinona como inibidores de tirosina quinase
AU2001290912A1 (en) 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6677450B2 (en) 2000-10-06 2004-01-13 Bristol-Myers Squibb Company Topoisomerase inhibitors
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
BR0116493A (pt) 2000-12-21 2003-09-30 Vertex Pharma Compostos de pirazol úteis como inibidores de proteìna cinase
ATE325865T1 (de) 2001-01-16 2006-06-15 Regeneron Pharma Isolierung von sezernierte proteine exprimierenden zellen
WO2002062826A1 (fr) 2001-02-07 2002-08-15 Vadim Viktorovich Novikov Procede de fabrication des peptides
EP1363890A4 (en) 2001-02-07 2009-06-10 Ore Pharmaceuticals Inc MELANOCORTIN-4-RECEPTOR BINDING COMPOUNDS AND METHOD FOR THEIR APPLICATION
MXPA03010724A (es) 2001-05-25 2004-03-02 Boehringer Ingelheim Pharma Compuestos de carbamato y oxamida como inhibidores de la produccion de citocina.
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
EP1404689A1 (en) 2001-07-02 2004-04-07 Debiopharm S.A. Oxaliplatin active substance with a very low content of oxalic acid
US6603000B2 (en) 2001-07-11 2003-08-05 Boehringer Ingelheim Pharmaceuticals, Inc. Synthesis for heteroarylamine compounds
KR100484504B1 (ko) 2001-09-18 2005-04-20 학교법인 포항공과대학교 쿠커비투릴 유도체를 주인 분자로서 포함하고 있는 내포화합물 및 이를 포함한 약제학적 조성물
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
US20030134846A1 (en) 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
US6927036B2 (en) 2002-02-19 2005-08-09 Xero Port, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
WO2003077921A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
AU2003225800A1 (en) 2002-03-15 2003-09-29 Hayley Binch Azolylaminoazine as inhibitors of protein kinases
US20040009981A1 (en) 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
US6846928B2 (en) 2002-03-15 2005-01-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
MXPA04009541A (es) 2002-03-29 2005-01-25 Chiron Corp Benzazoles sustituidos y uso de los mismos como inhibidores de cinasa raf.
US6900342B2 (en) 2002-05-10 2005-05-31 Dabur India Limited Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof
US6727272B1 (en) 2002-07-15 2004-04-27 Unitech Pharmaceuticals, Inc. Leflunomide analogs for treating rheumatoid arthritis
US7148342B2 (en) 2002-07-24 2006-12-12 The Trustees Of The University Of Pennyslvania Compositions and methods for sirna inhibition of angiogenesis
JP2006515274A (ja) 2002-10-08 2006-05-25 マサチューセッツ・インスティテュート・オブ・テクノロジー コレステロール輸送の調節のための化合物
CA2511646A1 (en) 2002-12-27 2004-07-22 Chiron Corporation Thiosemicarbazones as anti-virals and immunopotentiators
WO2004064759A2 (en) 2003-01-21 2004-08-05 Chiron Corporation Use of tryptanthrin compounds for immune potentiation
WO2004084824A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc. Biaryl substituted 6-membered heterocyles as sodium channel blockers
WO2004087153A2 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of organic compounds for immunopotentiation
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
EP1651619A1 (en) 2003-07-15 2006-05-03 Neurogen Corporation Substituted pyrimidin-4-ylamin analogues as vanilloid receptor ligands
CA2531619A1 (en) 2003-07-16 2005-01-27 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
PE20050952A1 (es) * 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
KR20080083188A (ko) 2006-01-11 2008-09-16 아스트라제네카 아베 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CA2675558A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
CA2826387A1 (en) 2011-02-11 2012-08-16 Dana Farber Cancer Institute, Inc. Method of inhibiting hamartoma tumor cells

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004048365A1 (en) 2002-11-21 2004-06-10 Chiron Corporation 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (pi) 3-kinase inhibitors and their use in the treatment of cancer

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