UY35464A - Inhibidores covalentes de kras g12c. - Google Patents

Inhibidores covalentes de kras g12c.

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Publication number
UY35464A
UY35464A UY0001035464A UY35464A UY35464A UY 35464 A UY35464 A UY 35464A UY 0001035464 A UY0001035464 A UY 0001035464A UY 35464 A UY35464 A UY 35464A UY 35464 A UY35464 A UY 35464A
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UY
Uruguay
Prior art keywords
kras
covalent inhibitors
mutant
ras protein
methods
Prior art date
Application number
UY0001035464A
Other languages
English (en)
Inventor
Pingda Ren
Liu Yi
Li Liansheng
Feng Jun
Wu Tao
Original Assignee
Araxes Pharma Llc
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Publication date
Application filed by Araxes Pharma Llc filed Critical Araxes Pharma Llc
Publication of UY35464A publication Critical patent/UY35464A/es

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    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D237/04Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
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    • C07D285/01Five-membered rings
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    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
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    • C07D401/04Heterocyclic 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
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    • C07D401/02Heterocyclic 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
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    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
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    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
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Abstract

Inhibidores irreversibles de la proteína K-Ras mutante G12C. También se divulgan métodos para modul ar la actividad de la proteína K-Ras mutante G12C y métodos de tratamiento de trastornos mediados p or la proteína K-Ras mutante G12C.
UY0001035464A 2013-03-15 2014-03-14 Inhibidores covalentes de kras g12c. UY35464A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361852123P 2013-03-15 2013-03-15
US201361889480P 2013-10-10 2013-10-10

Publications (1)

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UY35464A true UY35464A (es) 2014-10-31

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UY0001035464A UY35464A (es) 2013-03-15 2014-03-14 Inhibidores covalentes de kras g12c.

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US (4) US9227978B2 (es)
AR (1) AR095605A1 (es)
UY (1) UY35464A (es)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras 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
WO2016049524A1 (en) 2014-09-25 2016-03-31 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
EA201792214A1 (ru) * 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
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
CA2983927A1 (en) 2015-05-06 2016-11-10 The Regents Of The University Of California K-ras modulators
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017058902A1 (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
US10875842B2 (en) 2015-09-28 2020-12-29 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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017070256A2 (en) * 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
AU2016355433C1 (en) 2015-11-16 2021-12-16 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 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
AU2017266911B2 (en) 2016-05-18 2021-09-02 Array Biopharma, 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
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
BR112019004586A2 (pt) 2016-09-09 2019-06-11 Incyte Corp derivados de pirazolopiridina como moduladores de hpk1 e usos dos mesmos para o tratamento de câncer
TW201811799A (zh) 2016-09-09 2018-04-01 美商英塞特公司 吡唑并嘧啶化合物及其用途
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Rasの阻害剤としての複素環式化合物およびその使用方法
BR112019012976A2 (pt) 2016-12-22 2019-12-31 Amgen Inc inibidores de kras g12c e métodos de uso dos mesmos
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US20180228786A1 (en) 2017-02-15 2018-08-16 Incyte Corporation Pyrazolopyridine compounds and uses thereof
TW201900638A (zh) 2017-04-20 2019-01-01 加州大學董事會 K-ras調節劑
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
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
SG11202001499WA (en) 2017-09-08 2020-03-30 Amgen Inc Inhibitors of kras g12c and methods of using the same
UA125802C2 (uk) 2017-11-15 2022-06-08 Міраті Терапьютікс, Інк. Інгібітори kras g12c
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
SG11202007917VA (en) 2018-02-20 2020-09-29 Incyte Corp N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
US10752635B2 (en) 2018-02-20 2020-08-25 Incyte Corporation Indazole compounds and uses thereof
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
WO2019204505A2 (en) * 2018-04-18 2019-10-24 Theras, Inc. K-ras modulators with a vinyl sulfonamide moiety
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
EP3788053A1 (en) 2018-05-04 2021-03-10 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
JP7361720B2 (ja) 2018-05-10 2023-10-16 アムジエン・インコーポレーテツド がんの治療のためのkras g12c阻害剤
US11096939B2 (en) 2018-06-01 2021-08-24 Amgen Inc. KRAS G12C inhibitors and methods of using the same
IL259810A (en) 2018-06-04 2018-07-31 Yeda Res & Dev Mitogen-activated protein kinase kinase 7 inhibitors
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
MA53726A (fr) 2018-09-25 2022-05-11 Incyte Corp Composés pyrazolo[4,3-d]pyrimidine en tant que modulateurs des alk2 et/ou fgfr
EP3639820A1 (en) 2018-10-16 2020-04-22 Universitätsmedizin der Johannes Gutenberg-Universität Mainz Flavagline derivatives for inhibition of kras oncogene activation
JP2020090482A (ja) 2018-11-16 2020-06-11 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
MA55136A (fr) 2018-11-19 2022-02-23 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
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
AU2020206884A1 (en) 2019-01-09 2021-08-05 Beth Israel Deaconess Medical Center, Inc. Modulators of Pin1 activity and uses thereof
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
KR20210145787A (ko) 2019-04-02 2021-12-02 알리고스 테라퓨틱스 인코포레이티드 Prmt5를 표적으로 하는 화합물
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CR20210665A (es) 2019-05-21 2022-01-25 Amgen Inc Formas en estado sólido
EP4010338A1 (en) 2019-08-06 2022-06-15 Incyte Corporation Solid forms of an hpk1 inhibitor
EP4021444A4 (en) 2019-08-29 2023-01-04 Mirati Therapeutics, Inc. G12D KRAS INHIBITORS
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
AU2020372881A1 (en) 2019-10-28 2022-06-09 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
WO2021093758A1 (zh) * 2019-11-15 2021-05-20 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
US11702418B2 (en) 2019-12-20 2023-07-18 Mirati Therapeutics, Inc. SOS1 inhibitors
WO2022251576A1 (en) * 2021-05-28 2022-12-01 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN117164581A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 一种kras抑制剂或其盐的多晶型物及其制剂制备

Family Cites Families (215)

* 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
US4439606A (en) 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
EP0094498A3 (en) 1982-05-06 1985-04-03 American Cyanamid Company Antiatherosclerotic 1-piperazine derivatives
US4656181A (en) 1982-11-24 1987-04-07 Cermol S.A. Esters of 1,4-dihydropyridines, processes for the preparation of the new esters, and medicaments containing the same
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
JPS6143190A (ja) 1984-08-06 1986-03-01 Mitsui Petrochem Ind Ltd ピリドピリミジン誘導体およびその製法
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
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a 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
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
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
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them
CA2182517C (en) 1994-02-07 2001-08-21 Theo Nikiforov Ligase/polymerase-mediated primer extension of single nucleotide polymorphisms and its use in genetic analysis
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 ANAGONISTS
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
PT821671E (pt) 1995-04-20 2001-04-30 Pfizer Derivados do acido arilsulfonil hidroxamico como inibidores de mmp e tnf
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
ATE483733T1 (de) 1995-06-14 2010-10-15 Univ California Hochaffine humane antikörper gegen tumorantigene
DE69624081T2 (de) 1995-12-20 2003-06-12 Hoffmann La Roche Matrix-metalloprotease Inhibitoren
US6011029A (en) 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
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
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
CA2277100C (en) 1997-01-06 2005-11-22 Pfizer Inc. Cyclic sulfone derivatives
CN1113862C (zh) 1997-02-03 2003-07-09 辉瑞产品公司 芳基磺酰氨基异羟肟酸衍生物
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
NZ336836A (en) 1997-02-11 2001-02-23 Pfizer Arylsulfonyl hydroxamic acid derivatives suitable for a broad range of medicinal treatments
WO1998035951A2 (en) 1997-02-17 1998-08-20 Fujisawa Pharmaceutical Co., Ltd. New aminopiperazine derivatives
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US5919626A (en) 1997-06-06 1999-07-06 Orchid Bio Computer, Inc. Attachment of unmodified nucleic acids to silanized solid phase surfaces
EP0989979A1 (en) 1997-06-17 2000-04-05 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
ATE263147T1 (de) 1997-08-08 2004-04-15 Pfizer Prod Inc Derivate von aryloxyarylsulfonylamino hydroxyaminsäuren
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
DE19756236A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
IL136637A0 (en) 1997-12-22 2001-06-14 Du Pont Pharm Co Nitrogen containing heteroaromatics with ortho-substituted pi's as factor xa inhibitors
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
ATE423314T1 (de) 1998-06-24 2009-03-15 Illumina Inc Dekodierung von matrixartig-angeordneten sensoren durch mikropartikel
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
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6511993B1 (en) 1999-06-03 2003-01-28 Kevin Neil Dack Metalloprotease inhibitors
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
CN102586228A (zh) 1999-09-13 2012-07-18 纽亘技术公司 用于多核苷酸序列线性等温扩增的方法及组合物
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
MXPA02009312A (es) 2000-03-21 2003-03-12 Procter & Gamble Inhibidores de las metaloproteasas que contienen cadenas laterales heterociclicas.
AU5889701A (en) 2000-06-05 2001-12-17 Dong A Pharm Co Ltd Novel oxazolidinone derivatives and a process for the preparation thereof
TWI227231B (en) 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
ES2311023T3 (es) 2000-08-18 2009-02-01 Millennium Pharmaceuticals, Inc. Derivados de quinazolina como inhibidores de cinasa.
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
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
CA2443108A1 (en) 2001-04-03 2002-10-17 Merck & Co. Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
DE60227794D1 (de) 2001-04-26 2008-09-04 Eisai R&D Man Co Ltd Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon
JP2002371078A (ja) 2001-06-12 2002-12-26 Sankyo Co Ltd キノリン誘導体及びキノロン誘導体
AU2002344951A1 (en) 2001-07-02 2003-01-21 Boehringer Ingelheim International Gmbh Substituted piperazine and diazepanes as histamine h3 receptor agonists
WO2003053958A1 (en) 2001-12-20 2003-07-03 Celltech R & D Limited Quinazolinedione derivatives
EP1348434A1 (en) 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
US20050256159A1 (en) 2002-10-11 2005-11-17 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11,betahsd1 inhibitors
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
MXPA05009661A (es) 2003-03-12 2006-03-08 Kudos Pharm Ltd Derivados de ftalazinona.
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
JP4923380B2 (ja) 2003-12-22 2012-04-25 Jnc株式会社 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物
BRPI0507373A (pt) 2004-01-23 2007-07-10 Amgen Inc compostos e método de uso
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
US7368445B2 (en) 2004-03-01 2008-05-06 Eli Lilly And Company Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms
JP4775259B2 (ja) 2004-03-31 2011-09-21 味の素株式会社 アニリン誘導体
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
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
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
TW200643015A (en) 2005-03-11 2006-12-16 Akzo Nobel Nv 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives
AU2006224765B2 (en) 2005-03-16 2012-02-09 F.Hoffmann-La Roche Ag CIS-2,4,5-triaryl-imidazolines and their use as anti-cancer medicaments
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
US8232278B2 (en) 2005-06-24 2012-07-31 Gilead Sciences, Inc. Pyrido(3,2-D)pyrimidines and pharmaceutical compositions useful for treating hepatitis C
BRPI0617271A2 (pt) 2005-10-11 2011-07-19 Intermune Inc inibidores de replicação viral
CA2632030A1 (en) 2005-12-15 2007-06-21 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
US8097617B2 (en) 2006-03-31 2012-01-17 Novartis Ag Organic compounds
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
EP2038255A2 (en) 2006-06-16 2009-03-25 High Point Pharmaceuticals, LLC Pharmaceutical use of substituted piperidine carboxamides
CN101472912A (zh) 2006-06-22 2009-07-01 比奥维特罗姆上市公司 作为mnk激酶抑制剂的吡啶和吡嗪衍生物
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US9259426B2 (en) 2006-07-20 2016-02-16 Gilead Sciences, Inc. 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
WO2008033460A2 (en) 2006-09-15 2008-03-20 Schering Corporation Treating pain, diabetes, and lipid metabolism disorders
US20100144710A1 (en) 2007-03-09 2010-06-10 Astrazeneca Ab Piperazine and Piperidine MGLUR5 Potentiators
KR101511074B1 (ko) 2007-04-16 2015-04-13 애브비 인코포레이티드 7-치환된 인돌 Mcl-1 억제제
EP3425060B1 (en) 2008-03-28 2021-10-27 Pacific Biosciences of California, Inc. Compositions and methods for nucleic acid sequencing
EP2133334A1 (en) 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
US8507491B2 (en) 2008-08-25 2013-08-13 Irm Llc Compounds and compositions as hedgehog pathway inhibitors
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
PT2421826E (pt) 2009-04-20 2014-01-03 Hoffmann La Roche Derivados de prolina como inibidores de catepsina
AR076376A1 (es) 2009-04-22 2011-06-08 Janssen Pharmaceutica Nv Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
WO2010141817A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
EP2270002A1 (en) 2009-06-18 2011-01-05 Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
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
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
CA2773848A1 (en) 2009-09-09 2011-03-17 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
RU2573569C2 (ru) 2009-12-22 2016-01-20 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы фосфатидилинозитол-3-киназы на основе изоиндолинона
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
ES2521016T3 (es) 2010-01-29 2014-11-12 Otsuka Pharmaceutical Co., Ltd. Derivados de piridina di-sustituida como agentes anticancerosos
WO2011109584A2 (en) 2010-03-03 2011-09-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
WO2011113512A1 (de) 2010-03-16 2011-09-22 Merck Patent Gmbh Morpholinylchinazoline
WO2011136264A1 (ja) 2010-04-28 2011-11-03 第一三共株式会社 [5,6]複素環化合物
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
EP2580378A4 (en) 2010-06-08 2014-01-01 Nugen Technologies Inc MULTIPLEX SEQUENCING METHODS AND COMPOSITION
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
KR101826382B1 (ko) 2010-07-30 2018-02-06 온코세라피 사이언스 가부시키가이샤 퀴놀린 유도체 및 이를 함유하는 melk 억제제
CA2809991A1 (en) 2010-09-03 2012-03-08 Janssen Pharmaceutica Nv Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
PL2621923T3 (pl) 2010-09-29 2017-08-31 Intervet International B.V. Związki n-heteroarylu z mostkami cyklicznymi do leczenia chorób pasożytniczych
BR112013009858A2 (pt) 2010-10-22 2016-07-26 Janssen Pharmaceutica Nv diamidas de piperidin-4-il-azetidina como inibidores de monoacilglicerol lipase
WO2012061557A2 (en) 2010-11-05 2012-05-10 Glaxosmithkline Llc Chemical compounds
US9260484B2 (en) 2011-06-15 2016-02-16 Ohio State Innovation Foundation Small molecule composite surfaces as inhibitors of protein-protein interactions
SG195200A1 (en) 2011-06-29 2013-12-30 Otsuka Pharma Co Ltd Quinazolines as therapeutic compounds and related methods of use
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
JP2013107855A (ja) 2011-11-22 2013-06-06 Mitsubishi Tanabe Pharma Corp 医薬組成物
WO2013096455A1 (en) 2011-12-20 2013-06-27 Dana-Farber Cancer Institute, Inc. Methods for diagnosing and treating oncogenic kras-associated cancer
WO2013096151A1 (en) 2011-12-22 2013-06-27 Glaxosmithkline Llc Chemical compounds
WO2013106641A1 (en) 2012-01-13 2013-07-18 Bristol-Myers Squibb Company Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
EP2828250B1 (en) 2012-03-19 2021-03-10 Imperial College Innovations Limited Quinazoline compounds and their use in therapy
WO2013155077A1 (en) 2012-04-09 2013-10-17 Board Of Regents,The University Of Texas System Response markers for src inhibitor therapies
JP6399660B2 (ja) 2012-04-10 2018-10-03 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア 癌治療用組成物および方法
AR091004A1 (es) 2012-05-09 2014-12-30 Gradalis Inc Arn en horquilla corta bifuncional (bi-arnhc) especifico de mutaciones de nucleotidos individuales en k-ras
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
RU2019102203A (ru) 2012-07-11 2019-03-05 Блюпринт Медсинс Корпорейшн Ингибиторы рецептора фактора роста фибробластов
TW201414737A (zh) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
CA2882879A1 (en) 2012-08-24 2014-02-27 Takeda Pharmaceutical Company Limited Heterocyclic compound
LT2914296T (lt) 2012-11-01 2018-09-25 Infinity Pharmaceuticals, Inc. Vėžio gydymas, panaudojant p13 kinazės izoformos moduliatorius
AU2014244426B2 (en) 2013-03-14 2019-02-28 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
US9745319B2 (en) 2013-03-15 2017-08-29 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.
CA2904393A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
JP6518656B2 (ja) 2013-06-13 2019-05-22 バイオデシー, インコーポレイテッド 標的生体実体を標的にする生化学実体候補をスクリーニングする方法
UA120592C2 (uk) 2013-07-03 2020-01-10 Каріофарм Терапеутікс Інк. Заміщені бензофуранільні та бензоксазолільні сполуки та їхнє застосування
WO2015017502A1 (en) 2013-07-31 2015-02-05 Merck Patent Gmbh Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
EP3636639A1 (en) 2013-10-10 2020-04-15 Araxes Pharma LLC Inhibitors of kras g12c
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
JP6162904B2 (ja) 2014-02-03 2017-07-12 カディラ ヘルスケア リミティド 新規複素環式化合物
TWI683813B (zh) 2014-03-20 2020-02-01 美商卡佩拉醫療公司 苯并咪唑衍生物及其醫藥組合物及使用方法
NZ724691A (en) 2014-03-24 2018-02-23 Guangdong Zhongsheng Pharmaceutical Co Ltd Quinoline derivatives as smo inhibitors
WO2015184349A2 (en) 2014-05-30 2015-12-03 The Trustees Of Columbia University In The City Of New York Multivalent ras binding compounds
WO2015200795A1 (en) 2014-06-27 2015-12-30 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
WO2016049524A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
AU2016209046A1 (en) 2015-01-23 2017-07-20 Aclaris Therapeutics, Inc. Heterocyclic ITK inhibitors for treating inflammation and cancer
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
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
EP3325447A1 (en) 2015-07-22 2018-05-30 Araxes Pharma LLC Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
WO2017058768A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3365334A1 (en) 2015-10-21 2018-08-29 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
AU2016355433C1 (en) 2015-11-16 2021-12-16 Araxes Pharma Llc 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 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
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
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Rasの阻害剤としての複素環式化合物およびその使用方法
JP7236996B2 (ja) 2016-11-03 2023-03-10 コーバス・ファーマシューティカルズ・インコーポレイテッド インターロイキン-2誘導性t細胞キナーゼを調節する化合物及び方法
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
KR20200010306A (ko) 2017-05-25 2020-01-30 아락세스 파마 엘엘씨 Kras의 공유적 억제제
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
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2021000887A (es) 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
US20210380595A1 (en) 2018-10-24 2021-12-09 Araxes Pharma Llc 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
CA3120383A1 (en) 2018-11-29 2020-06-04 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer

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