JP2017528498A5 - - Google Patents

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JP2017528498A5
JP2017528498A5 JP2017516106A JP2017516106A JP2017528498A5 JP 2017528498 A5 JP2017528498 A5 JP 2017528498A5 JP 2017516106 A JP2017516106 A JP 2017516106A JP 2017516106 A JP2017516106 A JP 2017516106A JP 2017528498 A5 JP2017528498 A5 JP 2017528498A5
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Priority claimed from PCT/US2015/052349 external-priority patent/WO2016049524A1/en
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JP2017516106A 2014-09-25 2015-09-25 Kras g12c変異体タンパク質のインヒビター Pending JP2017528498A (ja)

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US201462055188P 2014-09-25 2014-09-25
US62/055,188 2014-09-25
PCT/US2015/052349 WO2016049524A1 (en) 2014-09-25 2015-09-25 Inhibitors of kras g12c mutant proteins

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JP2017528498A JP2017528498A (ja) 2017-09-28
JP2017528498A5 true JP2017528498A5 (enExample) 2018-11-01

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US (2) US9862701B2 (enExample)
EP (1) EP3197870B1 (enExample)
JP (1) JP2017528498A (enExample)
AR (1) AR102094A1 (enExample)
ES (1) ES2826443T3 (enExample)
WO (1) WO2016049524A1 (enExample)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
EP3197870B1 (en) 2014-09-25 2020-08-19 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) * 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) * 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
EA038635B9 (ru) 2015-11-16 2021-10-26 Араксис Фарма Ллк 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
JP2019516700A (ja) * 2016-05-12 2019-06-20 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Ash1l阻害剤及びそれを用いた治療方法
EP3458445B1 (en) 2016-05-18 2021-02-17 Mirati Therapeutics, Inc. Kras g12c inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
TW201815766A (zh) * 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ido及tdo調節之化合物及方法以及其適應症
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
WO2018098352A2 (en) 2016-11-22 2018-05-31 Jun Oishi Targeting kras induced immune checkpoint expression
MY196830A (en) 2016-12-22 2023-05-03 Amgen Inc Kras g12c inhibitors and methods of using the same
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
JP7161760B2 (ja) 2017-02-03 2022-10-27 国立大学法人東北大学 複素環化合物
WO2018206539A1 (en) * 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
CA3063440A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Covalent inhibitors of kras
AR112797A1 (es) 2017-09-08 2019-12-11 Amgen Inc Inhibidores de kras g12c y métodos para utilizarlos
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
EP3710439B1 (en) 2017-11-15 2023-02-15 Mirati Therapeutics, Inc. Kras g12c inhibitors
US10597405B2 (en) 2017-12-08 2020-03-24 Astrazeneca Ab Chemical compounds
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
EP3768666A1 (en) 2018-03-20 2021-01-27 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
AU2019262599B2 (en) 2018-05-04 2023-10-12 Amgen Inc. KRAS G12C inhibitors and methods of using the same
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. Kras g12c inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
ES2986917T3 (es) 2018-05-10 2024-11-13 Amgen Inc Inhibidores de KRAS G12C para el tratamiento del cáncer
CA3098885A1 (en) 2018-06-01 2019-12-05 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7369719B2 (ja) 2018-06-12 2023-10-26 アムジエン・インコーポレーテツド KRas G12C阻害剤及びそれを使用する方法
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP3829580A1 (en) 2018-08-01 2021-06-09 Araxes Pharma LLC Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
EP3849538A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
ES3004338T3 (en) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
EP3849536A4 (en) * 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
HUE071715T2 (hu) 2018-09-10 2025-09-28 Mirati Therapeutics Inc Dasatinib és adagrasib kombinációja felhasználásra nem-kissejtes tüdõrák kezelésében
US12065430B2 (en) 2018-10-26 2024-08-20 Taiho Pharmaceutical Co., Ltd. Indazole compound or salt thereof
AR117194A1 (es) 2018-11-09 2021-07-21 Hoffmann La Roche Compuestos de anillos fusionados
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
WO2020118066A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3911640A4 (en) 2019-01-18 2022-10-26 Astrazeneca AB PCSK9 INHIBITORS AND METHODS OF USE THEREOF
CN113382774A (zh) 2019-02-12 2021-09-10 诺华股份有限公司 包含tno155和krasg12c抑制剂的药物组合
US12281099B2 (en) 2019-02-26 2025-04-22 Boehringer Ingelheim International Gmbh Isoindolinone substituted indoles and derivatives as RAS inhibitors
WO2020178282A1 (en) 2019-03-05 2020-09-10 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
US11198699B2 (en) 2019-04-02 2021-12-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CA3225293A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
JP7622043B2 (ja) 2019-08-29 2025-01-27 ミラティ セラピューティクス, インコーポレイテッド Kras g12d阻害剤
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN114761012B (zh) * 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
PE20221253A1 (es) 2019-10-28 2022-08-16 Merck Sharp & Dohme Inhibidores de pequenas moleculas de mutante g12c de kras
CN115894606A (zh) 2019-11-04 2023-04-04 锐新医药公司 Ras抑制剂
CA3160142A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091967A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
EP4065112A4 (en) * 2019-11-22 2023-12-27 The Regents of the University of California Taspase1 inhibitors and uses thereof
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
WO2021121371A1 (zh) * 2019-12-19 2021-06-24 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
IL294048A (en) 2019-12-20 2022-08-01 Mirati Therapeutics Inc sos1 inhibitors
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
EP4110464A1 (en) * 2020-02-28 2023-01-04 Remix Therapeutics Inc. Compounds and methods for modulating splicing
TW202210633A (zh) 2020-06-05 2022-03-16 法商昂席歐公司 用於治療癌症之dbait分子與kras抑制劑的組合
JP2023530351A (ja) 2020-06-18 2023-07-14 レヴォリューション・メディスンズ,インコーポレイテッド Ras阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法
KR20230081726A (ko) 2020-09-03 2023-06-07 레볼루션 메디슨즈, 인크. Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도
KR20230137286A (ko) 2020-09-11 2023-10-04 미라티 테라퓨틱스, 인크. Kras g12c 억제제의 결정 형태
KR20230067635A (ko) 2020-09-15 2023-05-16 레볼루션 메디슨즈, 인크. 암의 치료에서 ras 억제제로서 인돌 유도체
KR20230094198A (ko) 2020-09-23 2023-06-27 에라스카, 아이엔씨. 3환식 피리돈 및 피리미돈
CR20230185A (es) 2020-09-30 2023-06-27 Astrazeneca Ab Compuestos y su uso en el tratamiento del cáncer
EP4262807A4 (en) 2020-12-15 2025-04-23 Mirati Therapeutics, Inc. Azachinazoline pan-KRAS inhibitors
US11999753B2 (en) 2020-12-16 2024-06-04 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
CN118852330A (zh) 2021-05-05 2024-10-29 锐新医药公司 用于治疗癌症的ras抑制剂
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
EP4395769A1 (en) 2021-09-01 2024-07-10 Novartis AG Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
US20250154170A1 (en) 2022-02-10 2025-05-15 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
AU2023285116A1 (en) 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250116016A (ko) 2022-11-09 2025-07-31 레볼루션 메디슨즈, 인크. 화합물, 복합체 및 이들의 제조 및 사용 방법
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
TW202446388A (zh) 2023-04-14 2024-12-01 美商銳新醫藥公司 Ras抑制劑之結晶形式、含有其之組合物及其使用方法
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
CN120981456A (zh) 2023-05-24 2025-11-18 金橘生物科技公司 杂环化合物及其用途
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025016899A1 (en) 2023-07-19 2025-01-23 Bayer Aktiengesellschaft Spirocyclic compounds for the treatment of cancer
WO2025026903A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft Imidazo pyrimidine compounds for the treatment of cancer
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
US12466840B2 (en) 2023-10-20 2025-11-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS proteins
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217247A1 (en) * 2024-04-10 2025-10-16 Amgen Inc. Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB939516A (en) 1961-05-29 1963-10-16 British Drug Houses Ltd Sulphonyl ureas
US3702849A (en) 1967-10-26 1972-11-14 Pfizer 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters
US3752660A (en) 1971-03-15 1973-08-14 Allied Chem Chlorophenoxyacetyloxazolidone herbicides and preparation thereof
JPS59163372A (ja) 1983-03-09 1984-09-14 Showa Denko Kk ピラゾ−ル誘導体とその製造法及び除草剤
JPS60193955A (ja) 1984-03-13 1985-10-02 Mitsui Toatsu Chem Inc 環式不飽和アミド置換エ−テル化合物及びその製造方法
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5925525A (en) 1989-06-07 1999-07-20 Affymetrix, Inc. Method of identifying nucleotide differences
IE66205B1 (en) 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5650489A (en) 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
DE69212850T2 (de) 1991-01-15 1997-03-06 Alcon Lab Inc Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6051380A (en) 1993-11-01 2000-04-18 Nanogen, Inc. Methods and procedures for molecular biological analysis and diagnostics
US6017696A (en) 1993-11-01 2000-01-25 Nanogen, Inc. Methods for electronic stringency control for molecular biological analysis and diagnostics
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5605798A (en) 1993-01-07 1997-02-25 Sequenom, Inc. DNA diagnostic based on mass spectrometry
US5858659A (en) 1995-11-29 1999-01-12 Affymetrix, Inc. Polymorphism detection
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US6068818A (en) 1993-11-01 2000-05-30 Nanogen, Inc. Multicomponent devices for molecular biological analysis and diagnostics
US5538848A (en) 1994-11-16 1996-07-23 Applied Biosystems Division, Perkin-Elmer Corp. Method for detecting nucleic acid amplification using self-quenching fluorescence probe
DE69531542T2 (de) 1994-02-07 2004-06-24 Beckman Coulter, Inc., Fullerton Ligase/polymerase-vermittelte analyse genetischer elemente von einzelnukleotid-polymorphismen und ihre verwendung in der genetischen analyse
US5593853A (en) 1994-02-09 1997-01-14 Martek Corporation Generation and screening of synthetic drug libraries
US5539083A (en) 1994-02-23 1996-07-23 Isis Pharmaceuticals, Inc. Peptide nucleic acid combinatorial libraries and improved methods of synthesis
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
EP0786997A4 (en) 1994-10-27 1998-03-11 Merck & Co Inc MUSCARINE ANTAGONISTS
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
FI973974A7 (fi) 1995-04-20 1997-10-16 Pfizer Aryylisulfonyylihydroksaamihappojohdannaisia MMP- ja TNF-inhibiittorei na
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2258726A1 (en) 1995-06-14 2010-12-08 The Regents of the University of California High affinity human antibodies to c-erbB-2
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
HUP9903014A3 (en) 1996-07-18 2000-08-28 Pfizer Phosphinate derivatives having matrix metalloprotease inhibitor effect and medicaments containing the same
IL128189A0 (en) 1996-08-23 1999-11-30 Pfizer Arylsulfonylamino hydroxamic acid derivatives
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
ES2224277T3 (es) 1997-01-06 2005-03-01 Pfizer Inc. Derivados de sulfonas ciclicas.
PT977733E (pt) 1997-02-03 2003-12-31 Pfizer Prod Inc Derivados de acido arilsulfonilamino-hidroxamico
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
IL131123A0 (en) 1997-02-11 2001-01-28 Pfizer Arylsulfonyl hydroxamic acid derivatives
US5919626A (en) 1997-06-06 1999-07-06 Orchid Bio Computer, Inc. Attachment of unmodified nucleic acids to silanized solid phase surfaces
WO1998057948A1 (en) 1997-06-17 1998-12-23 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
ES2216293T3 (es) 1997-08-08 2004-10-16 Pfizer Products Inc. Derivados de acido ariloxiarilsulfonilamino-hidroxamico.
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
DE19756236A1 (de) * 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
US6903118B1 (en) * 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
JP3662850B2 (ja) 1998-06-24 2005-06-22 イルミナ インコーポレイテッド 微小球を有するアレイセンサーのデコード
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
JP3929775B2 (ja) 1999-09-13 2007-06-13 ニューゲン テクノロジーズ, インコーポレイテッド ポリヌクレオチド配列の線形等温増幅のための方法および組成物
MXPA02012045A (es) 2000-06-05 2003-10-15 Dong A Pharm Co Ltd Nuevos derivados de oxazolidinona y proceso para su preparacion.
BR0113356A (pt) 2000-08-18 2004-04-20 Millennium Pharm Inc Derivados de quinazolina como inibidores de quinase
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US20020169300A1 (en) 2001-01-30 2002-11-14 Waterman Marian L. Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1
ATE449090T1 (de) 2001-07-02 2009-12-15 High Point Pharmaceuticals Llc Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
JP4608852B2 (ja) 2002-10-15 2011-01-12 チッソ株式会社 液晶性ビニルケトン誘導体およびその重合体
BRPI0407618A (pt) 2003-02-21 2006-02-21 Pfizer derivados de tiazole amino substituidos com cicloalquilo contendo n e composições farmacêuticas para inibição da proliferação celular e métodos para a sua utilização
WO2005070891A2 (en) 2004-01-23 2005-08-04 Amgen Inc Compounds and methods of use
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
JP2007016011A (ja) 2005-06-10 2007-01-25 Nippon Soda Co Ltd 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬
EP1899332A1 (en) 2005-06-24 2008-03-19 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c.
WO2007070760A2 (en) * 2005-12-15 2007-06-21 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
AU2007233709A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
EP2059515A2 (en) 2006-04-12 2009-05-20 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
EP2038255A2 (en) 2006-06-16 2009-03-25 High Point Pharmaceuticals, LLC Pharmaceutical use of substituted piperidine carboxamides
ATE456565T1 (de) 2006-06-22 2010-02-15 Biovitrum Ab Publ Pyridin- und pyrazinderivate als mnk- kinaseinhibitoren
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
US8445679B2 (en) 2007-04-16 2013-05-21 Abbvie Inc. 7-substituted indole MCL-1 inhibitors
CA2719747C (en) 2008-03-28 2018-02-20 Pacific Biosciences Of California, Inc. Compositions and methods for nucleic acid sequencing
EP2328871B1 (en) 2008-08-25 2020-04-01 Novartis AG Hedgehog pathway modulators
WO2010087399A1 (ja) 2009-01-30 2010-08-05 第一三共株式会社 ウロテンシンii受容体拮抗薬
PL2421826T3 (pl) 2009-04-20 2014-03-31 Hoffmann La Roche Pochodne proliny jako inhibitory katepsyn
EP2421848A1 (en) 2009-04-22 2012-02-29 Janssen Pharmaceutica N.V. Azetidinyl diamides as monoacylglycerol lipase inhibitors
SE533816C2 (sv) 2009-05-06 2011-01-25 Tetra Laval Holdings & Finance Förfarande för framställning av kartongflaskor
WO2011016559A1 (ja) * 2009-08-07 2011-02-10 武田薬品工業株式会社 複素環化合物およびその用途
SG179085A1 (en) * 2009-09-09 2012-04-27 Avila Therapeutics Inc Pi3 kinase inhibitors and uses thereof
KR20130067487A (ko) 2009-12-30 2013-06-25 아빌라 테라퓨틱스, 인크. 단백질의 리간드-지정 공유 변형
US8722663B2 (en) * 2010-01-29 2014-05-13 Otsuka Pharmaceutical Co., Ltd. Di-substituted pyridine derivatives as anticancers
AU2011246067A1 (en) 2010-04-28 2012-09-27 Daiichi Sankyo Company, Limited [5,6] heterocyclic compound
TW201202230A (en) 2010-05-24 2012-01-16 Mitsubishi Tanabe Pharma Corp Novel quinazoline compound
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CN103119439A (zh) 2010-06-08 2013-05-22 纽亘技术公司 用于多重测序的方法和组合物
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
SG10201505951VA (en) 2010-07-30 2015-08-28 Oncotherapy Science Inc Quinoline derivatives and melk inhibitors containing the same
RU2013114771A (ru) 2010-09-03 2014-10-10 Янссен Фармацевтика Нв Диамиды азетидинила как ингибиторы моноацилглицерол липазы
WO2012041872A1 (en) 2010-09-29 2012-04-05 Intervet International B.V. N-heteroaryl compounds with cyclic bridging unit for the treatment of parasitic diseases
BR112013009858A2 (pt) 2010-10-22 2016-07-26 Janssen Pharmaceutica Nv diamidas de piperidin-4-il-azetidina como inibidores de monoacilglicerol lipase
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
CN103087077B (zh) 2011-11-03 2016-05-18 上海希迈医药科技有限公司 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用
US9932317B2 (en) 2012-03-19 2018-04-03 Imperial Innovations Limited Quinazoline compounds and their use in therapy
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
TW201402813A (zh) 2012-05-09 2014-01-16 Gradalis Inc 對單核苷酸kras突變具專一性之雙功能性短髮夾rna(bi-shrna)
WO2014071109A1 (en) * 2012-11-01 2014-05-08 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
EP2968360B1 (en) 2013-03-14 2021-01-20 ConverGene LLC Quinolinone derivatives for the inhibition of bromodomain-containing proteins
TW201524952A (zh) * 2013-03-15 2015-07-01 Araxes Pharma Llc Kras g12c之共價抑制劑
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
WO2014143659A1 (en) * 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
GB2538216A (en) 2013-06-13 2016-11-16 Biodesy Inc Method of screening candidate biochemical entities targeting a target biochemical entity
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
CN106488910B (zh) 2013-10-10 2020-07-31 亚瑞克西斯制药公司 Kras g12c的抑制剂
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
EP3148981A4 (en) 2014-05-30 2017-11-08 The Trustees of Columbia University in the City of New York Multivalent ras binding compounds
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
EP3197870B1 (en) 2014-09-25 2020-08-19 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3280708B1 (en) 2015-04-10 2021-09-01 Araxes Pharma LLC Substituted quinazoline compounds and methods of use thereof
JP6789239B2 (ja) 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
CA2993013A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS

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