SG10202113146UA - Covalent inhibitors of kras - Google Patents

Covalent inhibitors of kras

Info

Publication number
SG10202113146UA
SG10202113146UA SG10202113146UA SG10202113146UA SG10202113146UA SG 10202113146U A SG10202113146U A SG 10202113146UA SG 10202113146U A SG10202113146U A SG 10202113146UA SG 10202113146U A SG10202113146U A SG 10202113146UA SG 10202113146U A SG10202113146U A SG 10202113146UA
Authority
SG
Singapore
Prior art keywords
kras
covalent inhibitors
covalent
inhibitors
Prior art date
Application number
SG10202113146UA
Inventor
Liansheng Li
Jun Feng
Tao Wu
Yuan Liu
Yi Wang
Pingda Ren
Yi Liu
Original Assignee
Araxes Pharma Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Araxes Pharma Llc filed Critical Araxes Pharma Llc
Publication of SG10202113146UA publication Critical patent/SG10202113146UA/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
SG10202113146UA 2017-05-25 2018-05-24 Covalent inhibitors of kras SG10202113146UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762511163P 2017-05-25 2017-05-25
US201862625889P 2018-02-02 2018-02-02

Publications (1)

Publication Number Publication Date
SG10202113146UA true SG10202113146UA (en) 2021-12-30

Family

ID=63586845

Family Applications (1)

Application Number Title Priority Date Filing Date
SG10202113146UA SG10202113146UA (en) 2017-05-25 2018-05-24 Covalent inhibitors of kras

Country Status (14)

Country Link
US (3) US10745385B2 (en)
EP (1) EP3630745A2 (en)
JP (1) JP2020521742A (en)
KR (1) KR20200010306A (en)
CN (1) CN110869358A (en)
AU (1) AU2018271990A1 (en)
BR (1) BR112019024674A2 (en)
CA (1) CA3063440A1 (en)
MX (1) MX2019013954A (en)
PH (1) PH12019550248A1 (en)
SG (1) SG10202113146UA (en)
TW (1) TW201900633A (en)
WO (1) WO2018218070A2 (en)
ZA (1) ZA202101138B (en)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (en) 2013-10-10 2021-01-31 Araxes Pharma Llc Inhibitors of kras g12c
EA201792214A1 (en) 2015-04-10 2018-01-31 Араксис Фарма Ллк COMPOUNDS OF SUBSTITUTE QUINAZOLINE
ES2856880T3 (en) 2015-04-15 2021-09-28 Araxes Pharma Llc KRAS Condensed Tricyclic Inhibitors and Methods of Using Them
WO2017058728A1 (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
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 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
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
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
WO2017172979A1 (en) 2016-03-30 2017-10-05 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
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
JP2019534260A (en) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Heterocyclic compounds as inhibitors of RAS and methods of use thereof
CN110382482A (en) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 Condensed miscellaneous-Heterobicyclic compounds and its application method
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
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
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
BR112019024674A2 (en) 2017-05-25 2020-06-16 Araxes Pharma Llc COVALENT KRAS INHIBITORS
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
TW201906832A (en) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 Compounds for cancer treatment and methods of use thereof
CA3095494C (en) 2018-04-04 2023-11-07 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
AU2019255310B2 (en) 2018-04-18 2022-11-24 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TW202012415A (en) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 Chemical compounds
US11919912B2 (en) 2018-05-21 2024-03-05 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP6941241B2 (en) 2018-11-09 2021-09-29 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Condensation ring compound
EP3908283A4 (en) * 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP4249000A3 (en) 2019-02-12 2023-12-27 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
CN114096544A (en) * 2019-05-20 2022-02-25 加州理工学院 KRAS G12C inhibitors and uses thereof
CN113423703A (en) * 2019-05-29 2021-09-21 上海翰森生物医药科技有限公司 Nitrogen-containing heterocyclic derivative regulator, and preparation method and application thereof
CN112047948B (en) * 2019-06-06 2022-08-16 山东轩竹医药科技有限公司 Kras mutant inhibitors
US20220372036A1 (en) * 2019-06-25 2022-11-24 Medshine Discovery Inc. Seven-membered heterocyclic derivative acting as kras g12c mutant protein inhibitor
WO2021063346A1 (en) * 2019-09-30 2021-04-08 上海迪诺医药科技有限公司 Kras g12c inhibitor and application thereof
CN112707846B (en) * 2019-10-25 2023-04-21 成都伊诺达博医药科技有限公司 Preparation method of dacatinib key intermediate
MX2022005053A (en) 2019-10-28 2022-05-18 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12c mutant.
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
JP2022553858A (en) 2019-11-04 2022-12-26 レボリューション メディシンズ インコーポレイテッド RAS inhibitor
CA3159559A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
TWI760919B (en) * 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 A kind of pyrimidocyclic derivative and its application in medicine
JP2023505100A (en) 2019-11-27 2023-02-08 レボリューション メディシンズ インコーポレイテッド Covalent RAS inhibitors and uses thereof
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
WO2021216770A1 (en) * 2020-04-22 2021-10-28 Accutar Biotechnology Inc. Substituted tetrahydroquinazoline compounds as kras inhibitors
EP4144732A4 (en) * 2020-04-29 2024-05-01 Shanghai Ringene Biopharma Co Ltd Benzothiazolyl biaryl compound, and preparation method and use
EP4168002A1 (en) 2020-06-18 2023-04-26 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2021259331A1 (en) * 2020-06-24 2021-12-30 南京明德新药研发有限公司 Eight-membered n-containing heterocyclic compound
CN115836055A (en) * 2020-06-30 2023-03-21 益方生物科技(上海)股份有限公司 Quinazoline compounds, preparation method and application thereof
MX2023002248A (en) 2020-09-03 2023-05-16 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations.
CR20230165A (en) 2020-09-15 2023-06-02 Revolution Medicines Inc Indole derivatives as ras inhibitors in the treatment of cancer
WO2022068921A1 (en) * 2020-09-30 2022-04-07 上海医药集团股份有限公司 Quinazoline compound and application thereof
WO2022087624A1 (en) * 2020-10-21 2022-04-28 Bioardis Llc Compounds as ras inhibitors and uses thereof
WO2022098625A1 (en) * 2020-11-03 2022-05-12 Mirati Therapeutics, Inc. Kras g12d inhibitors
US20230406849A1 (en) * 2020-11-06 2023-12-21 Tyligand Bioscience (Shanghai) Limited Kras inhibitors for treatment of cancers
WO2022105855A1 (en) * 2020-11-20 2022-05-27 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
US20240025918A1 (en) * 2020-11-20 2024-01-25 Jacobio Pharmaceuticals Co., Ltd KRAS G12D Inhibitors
WO2022133345A1 (en) 2020-12-18 2022-06-23 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
CN113999226B (en) * 2020-12-22 2023-01-06 上海科州药物研发有限公司 Heterocyclic compounds as KRAS inhibitors and methods of use thereof
TW202241869A (en) * 2020-12-22 2022-11-01 大陸商上海科州藥物研發有限公司 Preparation and application method of heterocyclic compound as KRAS inhibitor
WO2022148422A1 (en) * 2021-01-08 2022-07-14 Beigene, Ltd. Bridged compounds as kras g12d inhibitor and degrader and the use thereof
WO2022152233A1 (en) * 2021-01-15 2022-07-21 Beigene, Ltd. Kras g12c inhibitors
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
AU2022232523A1 (en) * 2021-03-12 2023-11-16 Bristol-Myers Squibb Company Kras g12d inhibitors
WO2022194191A1 (en) * 2021-03-16 2022-09-22 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12d
WO2022228568A1 (en) * 2021-04-30 2022-11-03 劲方医药科技(上海)有限公司 Pyridino- or pyrimido-cyclic compound, preparation method therefor and medical use thereof
CN117616031A (en) 2021-05-05 2024-02-27 锐新医药公司 RAS inhibitors for the treatment of cancer
BR112023022819A2 (en) 2021-05-05 2024-01-16 Revolution Medicines Inc COMPOUNDS, PHARMACEUTICAL COMPOSITION, CONJUGATES AND METHODS FOR TREATING CANCER IN A SUBJECT, FOR TREATING A DISORDER AND FOR INHIBITING A RAS PROTEIN IN A CELL
WO2022247760A1 (en) * 2021-05-22 2022-12-01 上海科州药物研发有限公司 Heterocyclic compounds as kras inhibitor, and preparation therefor and use thereof in treatment
KR20240021197A (en) * 2021-06-10 2024-02-16 레드엑스 파마 피엘씨 Quinazoline derivatives useful as RAS inhibitors
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
KR20240024903A (en) * 2021-06-21 2024-02-26 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 Fused tetracyclic compounds, methods for their preparation and their applications in medicine
TW202317100A (en) 2021-06-23 2023-05-01 瑞士商諾華公司 Pharmaceutical combinations comprising a kras g12c inhibitor and uses thereof for the treatment of cancers
WO2023278600A1 (en) * 2021-06-30 2023-01-05 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of kras g12d mutant
WO2023280026A1 (en) * 2021-07-05 2023-01-12 四川科伦博泰生物医药股份有限公司 Heteroaromatic ring compound, preparation method therefor and use thereof
AU2022315228A1 (en) * 2021-07-23 2024-02-08 Lawrence Livermore National Security, Llc Compositions and methods for inhibition of ras
CN117858878A (en) * 2021-08-18 2024-04-09 北京加科思新药研发有限公司 N-cyclopropyl pyrido [4,3-d ] pyrimidine-4-amine derivatives and uses thereof
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
AR127308A1 (en) 2021-10-08 2024-01-10 Revolution Medicines Inc RAS INHIBITORS
CA3234429A1 (en) * 2021-10-15 2023-04-20 Luc Farmer Ras inhibitors, compositions and methods of use thereof
CN116217591A (en) * 2021-12-02 2023-06-06 思路迪生物医药(上海)有限公司 Pyridopyrimidine derivatives serving as KRAS G12D mutation inhibitors
WO2023103523A1 (en) * 2021-12-09 2023-06-15 苏州浦合医药科技有限公司 Substituted bicyclic heteroaryl compound as kras g12d inhibitor
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023173016A1 (en) * 2022-03-09 2023-09-14 Blossomhill Therapeutics, Inc. Kras inhibitors for treating disease
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2023244604A1 (en) * 2022-06-14 2023-12-21 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2023244615A1 (en) * 2022-06-15 2023-12-21 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds

Family Cites Families (232)

* 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
US4436748A (en) 1980-10-20 1984-03-13 Hoechst-Roussel Pharmaceuticals Inc. Benzo[b]thiophenes
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 (en) 1983-03-09 1984-09-14 Showa Denko Kk Pyrazole derivative, its preparation and herbicide
JPS60193955A (en) 1984-03-13 1985-10-02 Mitsui Toatsu Chem Inc Cyclic unsaturated amide-substituted ether compound and its preparation
JPS6143190A (en) 1984-08-06 1986-03-01 Mitsui Petrochem Ind Ltd Pyridopyrimidine derivative and preparation thereof
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (en) 1985-10-03 1988-12-02 Merck Sharp & Dohme LIQUID-GEL PHASE TRANSITION PHARMACEUTICAL COMPOSITION
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
JP2594486B2 (en) 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 Topical ophthalmic composition
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 the preparation thereof and pharmaceutical compositions containing the same
AU694187B2 (en) 1994-02-07 1998-07-16 Beckman Coulter, Inc. Ligase/polymerase-mediated genetic bit analysis TM 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
WO1996013262A1 (en) 1994-10-27 1996-05-09 Merck & Co., Inc. Muscarine antagonists
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
CA2218503C (en) 1995-04-20 2001-07-24 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
FR2734816B1 (en) 1995-05-31 1997-07-04 Adir NOVEL ARYL (ALKYL) PROPYLAMIDES, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
DE69638269D1 (en) 1995-06-14 2010-11-18 Univ California HIGH-AFFINE HUMAN ANTIBODY AGAINST TUMORANTIGENE
ATE225343T1 (en) 1995-12-20 2002-10-15 Hoffmann La Roche MATRIX METALLOPROTEASE INHIBITORS
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
DE69712496T2 (en) 1996-07-18 2002-08-29 Pfizer MATRIX METALLOPROTEASE INHIBITORS BASED ON PHOSPHINIC ACIDS
KR20000068248A (en) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 Arylsulfonylamino Hydroxamic Acid Derivatives
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
PT950059E (en) 1997-01-06 2004-10-29 Pfizer CYCLIC SULFONA DERIVATIVES
US6303636B1 (en) 1997-02-03 2001-10-16 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
BR9807678A (en) 1997-02-11 2000-02-15 Pfizer Derivatives of arylsulfonyl hydroxamic acids
WO1998035951A2 (en) 1997-02-17 1998-08-20 Fujisawa Pharmaceutical Co., Ltd. New aminopiperazine derivatives
UA73073C2 (en) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Substituted 3-cyan chinolines
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
WO1998057948A1 (en) 1997-06-17 1998-12-23 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
CA2299355C (en) 1997-08-08 2005-09-27 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
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 (en) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Novel piperazinyl-substituted pyridylalkane, alkene and alkyarboxylic acid amides
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
PA8469501A1 (en) 1998-04-10 2000-09-29 Pfizer Prod Inc HYDROXAMIDES OF THE ACID (4-ARILSULFONILAMINO) -TETRAHIDROPIRAN-4-CARBOXILICO
PA8469401A1 (en) 1998-04-10 2000-05-24 Pfizer Prod Inc BICYCLE DERIVATIVES OF HYDROXAMIC ACID
AU754952B2 (en) 1998-06-24 2002-11-28 Illumina, Inc. Decoding of array sensors with microspheres
EP1004578B1 (en) 1998-11-05 2004-02-25 Pfizer Products Inc. 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
US6586447B1 (en) 1999-04-01 2003-07-01 Pfizer Inc 3,3-disubstituted-oxindole derivatives useful as anticancer agents
US6511993B1 (en) 1999-06-03 2003-01-28 Kevin Neil Dack Metalloprotease inhibitors
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
KR100527265B1 (en) 1999-09-13 2005-11-09 뉴젠 테크놀로지스 인코포레이티드 Methods and compositions for linear isothermal amplification of polynucleotide sequences
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
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
KR20080009294A (en) 2000-03-13 2008-01-28 와이어쓰 홀딩스 코포레이션 Pharmaceutical composition for treating or inhibiting colonic polyps comprising cyanoquinolines
MXPA02009312A (en) 2000-03-21 2003-03-12 Procter & Gamble Heterocyclic side chain containing metalloprotease inhibitors.
HUP0301562A2 (en) 2000-06-05 2003-12-29 Dong A Pharm. Co., Ltd. Novel oxazolidinone derivatives and a process for the preparation thereof and pharmaceutical compositions containing them
TWI227231B (en) 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
BR0113356A (en) 2000-08-18 2004-04-20 Millennium Pharm Inc Quinazoline derivatives as kinase inhibitors
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
JP2005511478A (en) 2001-04-03 2005-04-28 メルク エンド カムパニー インコーポレーテッド N-substituted non-aryl heterocyclic amidyl NMDA / NR2B antagonist
EP1382603B1 (en) 2001-04-26 2008-07-23 Eisai R&D Management Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
JP2002371078A (en) 2001-06-12 2002-12-26 Sankyo Co Ltd Quinoline derivative and quinolone derivative
EP1421071B1 (en) 2001-07-02 2009-11-18 High Point Pharmaceuticals, LLC Substituted piperazine and diazepane derivaives as histamine h3 receptor modulators
AU2002352444A1 (en) 2001-12-20 2003-07-09 Celltech R And D Limited Quinazolinedione derivatives
EP1348434A1 (en) 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
AU2003269242A1 (en) 2002-10-11 2004-05-04 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors
JP4608852B2 (en) 2002-10-15 2011-01-12 チッソ株式会社 Liquid crystalline vinyl ketone derivatives and polymers thereof
JP2004250329A (en) 2002-12-26 2004-09-09 Dainippon Pharmaceut Co Ltd Isatin derivative
CA2516234A1 (en) 2003-02-21 2004-09-02 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
AU2004220321B2 (en) 2003-03-12 2010-02-25 Kudos Pharmaceuticals Ltd Phthalazinone derivatives
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
SE0302811D0 (en) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
JP4923380B2 (en) 2003-12-22 2012-04-25 Jnc株式会社 Low refractive index anisotropic compounds, compositions and polymers or polymer compositions thereof
JP4932495B2 (en) 2004-01-23 2012-05-16 アムゲン インコーポレイテッド Compound and method 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
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
GB0405628D0 (en) 2004-03-12 2004-04-21 Glaxo Group Ltd Novel compounds
JP4775259B2 (en) 2004-03-31 2011-09-21 味の素株式会社 Aniline derivative
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
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 (en) 2005-06-10 2007-01-25 Nippon Soda Co Ltd New nitrogen-containing heterocyclic compound having antioxidative activity and antioxidative agent containing the compound
CA2612788A1 (en) 2005-06-24 2006-12-28 Steven Cesar Alfons De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c
US20090099186A1 (en) 2005-10-11 2009-04-16 Leonid Beigelman Inhibitors of viral replication
TW200800201A (en) 2005-11-18 2008-01-01 Lilly Co Eli Pyrimidinyl benzothiophene compounds
JP2009519349A (en) 2005-12-15 2009-05-14 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 Compounds that modulate the CB2 receptor
RU2008132333A (en) 2006-02-07 2010-03-20 Вайет (Us) 11-BETA HSD1 INHIBITORS
PE20070978A1 (en) 2006-02-14 2007-11-15 Novartis Ag HETEROCICLIC COMPOUNDS AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASES (PI3Ks)
BRPI0710110A2 (en) 2006-03-31 2011-08-02 Novartis Ag organic compounds
CA2647448A1 (en) 2006-04-12 2007-10-18 Pfizer Limited Pyrrolidine derivatives as modulators of chemokine ccr5 receptors
WO2007144394A2 (en) 2006-06-16 2007-12-21 High Point Pharmaceuticals, Llc. Pharmaceutical use of substituted piperidine carboxamides
ES2340093T3 (en) 2006-06-22 2010-05-28 Biovitrum Ab (Publ) PIRAZINE AND PIRIDINE DERIVATIVES AS INHIBITORS OF CINASA MNK.
FR2903101B1 (en) 2006-06-30 2008-09-26 Servier Lab NOVEL NAPHTHALENIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
US20080021026A1 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
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
EP1903038A1 (en) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-hetaryl-piperidin-4-yl)-(het)arylamide as EP2 receptor modulators
EP2061462A2 (en) 2006-09-15 2009-05-27 Schering Corporation Treating pain, diabetes and lipid metabolism disorders
WO2008112440A1 (en) 2007-03-09 2008-09-18 Astrazeneca Ab Piperazine and piperidine mglur5 potentiators
JP5496877B2 (en) 2007-04-16 2014-05-21 アッヴィ・インコーポレイテッド 7-substituted indole Mcl-1 inhibitors
BRPI0909212A2 (en) 2008-03-28 2015-08-18 Pacific Biosciences California Compositions and method 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
CA2743134A1 (en) 2008-11-10 2010-05-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2010087399A1 (en) 2009-01-30 2010-08-05 第一三共株式会社 Urotensin-ii receptor antagonists
ES2436550T3 (en) 2009-04-20 2014-01-02 F. Hoffmann-La Roche Ag New proline derivatives as cathepsin inhibitors
AR076376A1 (en) 2009-04-22 2011-06-08 Janssen Pharmaceutica Nv AZETIDINIL DIAMIDS AS INHIBITORS OF MONOACILGLICEROL LIPASA
US20120083476A1 (en) 2009-06-05 2012-04-05 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
ES2618630T3 (en) 2009-06-29 2017-06-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011016559A1 (en) 2009-08-07 2011-02-10 武田薬品工業株式会社 Heterocyclic compound and use thereof
KR101256018B1 (en) 2009-08-20 2013-04-18 한국과학기술연구원 1,3,6-Substituted indole derivatives having inhibitory activity for protein kinase
US20110230476A1 (en) 2009-09-09 2011-09-22 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
AU2010341573B2 (en) 2009-12-22 2016-10-13 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
CN102812167A (en) 2009-12-30 2012-12-05 阿维拉制药公司 Ligand-directed Covalent Modification Of Protein
US8722663B2 (en) 2010-01-29 2014-05-13 Otsuka Pharmaceutical Co., Ltd. Di-substituted pyridine derivatives as anticancers
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
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
EP2547664B1 (en) 2010-03-16 2016-05-04 Merck Patent GmbH Morpholinylquinazolines
RU2012136643A (en) 2010-04-28 2014-06-10 Дайити Санкио Компани, Лимитед [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
EP2580378A4 (en) 2010-06-08 2014-01-01 Nugen Technologies Inc Methods and composition for multiplex sequencing
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
RU2582610C2 (en) 2010-07-30 2016-04-27 Онкотерапи Сайенс, Инк. Quinoline derivatives and melk inhibitors containing same
CN103068798A (en) 2010-09-03 2013-04-24 詹森药业有限公司 Di-azetidinyl diamide as monoacylglycerol lipase inhibitors
AR083199A1 (en) 2010-09-29 2013-02-06 Intervet Internationale B V N-HETEROARILO COMPOUNDS WITH CYCLE BRIDGE UNIT
JP2013540159A (en) 2010-10-22 2013-10-31 ヤンセン ファーマシューティカ エヌ.ベー. Piperidin-4-yl-azetidine diamide as monoacylglycerol lipase inhibitor
EP2635279A4 (en) 2010-11-05 2014-10-29 Glaxosmithkline Ip No 2 Ltd Chemical compounds
US9260484B2 (en) 2011-06-15 2016-02-16 Ohio State Innovation Foundation Small molecule composite surfaces as inhibitors of protein-protein interactions
CA2840627A1 (en) 2011-06-29 2013-01-03 Otsuka Pharmaceutical Co., Ltd. Quinazolines as therapeutic compounds and related methods of use
CN103087077B (en) 2011-11-03 2016-05-18 上海希迈医药科技有限公司 Thienopyrimidine and furans miazines derivative, its preparation method and in application pharmaceutically
JP2013107855A (en) 2011-11-22 2013-06-06 Mitsubishi Tanabe Pharma Corp Pharmaceutical composition
US9745631B2 (en) 2011-12-20 2017-08-29 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
ES2575604T3 (en) 2012-01-13 2016-06-29 Bristol-Myers Squibb Company Thiazolyl or thiadiazolyl substituted pyridyl compounds useful as kinase inhibitors
WO2013140148A1 (en) 2012-03-19 2013-09-26 Imperial 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
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
AR091004A1 (en) 2012-05-09 2014-12-30 Gradalis Inc RNA IN SHORT BIFUNCTIONAL FORK (BI-ARNHC) SPECIFIC OF INDIVIDUAL NUCLEOTID MUTATIONS IN K-RAS
JO3300B1 (en) 2012-06-06 2018-09-16 Novartis Ag Compounds and compositions for modulating egfr activity
CN109627239B (en) 2012-07-11 2021-10-12 缆图药品公司 Inhibitors of fibroblast growth factor receptors
TW201414737A (en) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 Imidazotriazinecarbonitriles useful as kinase inhibitors
CA2882879A1 (en) 2012-08-24 2014-02-27 Takeda Pharmaceutical Company Limited Heterocyclic compound
US20150283142A1 (en) 2013-03-15 2015-10-08 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
MX2015006152A (en) 2012-11-20 2016-01-20 Genentech Inc Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants.
JP6464139B2 (en) 2013-03-14 2019-02-06 コンバージーン・リミテッド・ライアビリティ・カンパニー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
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
MX364438B (en) 2013-03-15 2019-04-26 Araxes Pharma Llc Covalent inhibitors of kras g12c.
KR20160003647A (en) 2013-03-15 2016-01-11 에피자임, 인코포레이티드 Carm1 inhibitors and uses thereof
JP6518656B2 (en) 2013-06-13 2019-05-22 バイオデシー, インコーポレイテッド Method of screening candidate biochemical entities targeting a target biological entity
US20150005277A1 (en) 2013-06-28 2015-01-01 Beigene, Ltd. Protein Kinase Inhibitors and Uses Thereof
KR102325247B1 (en) 2013-07-03 2021-11-11 카리오팜 쎄라퓨틱스, 인코포레이티드 Substituted benzofuranyl and benzoxazolyl compounds and uses thereof
ES2706150T3 (en) 2013-07-31 2019-03-27 Merck Patent Gmbh Pyridines, pyrimidines and pyrazines, as inhibitors of BTK and their uses
CN104418860B (en) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 Pyrimido heterocycle compound and Pharmaceutical composition thereof and application
BR112016008016B8 (en) 2013-10-10 2023-09-26 Araxes Pharma Llc kras g12c inhibitory compounds, pharmaceutical composition comprising said compounds, methods for regulating the activity and for preparing a kras, hras or nras g12c mutant protein, method for inhibiting the proliferation of a population of cells and therapeutic uses of said compounds
JO3805B1 (en) 2013-10-10 2021-01-31 Araxes Pharma Llc Inhibitors of kras g12c
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
MX2016009403A (en) 2014-02-03 2016-09-16 Cadila Healthcare Ltd Heterocyclic compounds.
AU2015231202B9 (en) 2014-03-20 2019-10-24 Capella Therapeutics, Inc. Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer
BR112016021730B1 (en) 2014-03-24 2022-09-06 Guangdong Zhongsheng Pharmaceutical Co., Ltd QUINOLINE DERIVATIVES AS SMO INHIBITORS
EP3148981A4 (en) 2014-05-30 2017-11-08 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
US20170305922A1 (en) 2014-09-17 2017-10-26 Epizyme, Inc. Carm1 inhibitors and uses thereof
JO3556B1 (en) 2014-09-18 2020-07-05 Araxes Pharma Llc Combination therapies for treatment of cancer
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
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
CN106852142B (en) 2014-10-08 2020-08-21 豪夫迈·罗氏有限公司 Spirodiamine derivatives as aldosterone synthase inhibitors
CN107278202A (en) 2015-01-23 2017-10-20 融合生命科学公司 Heterocycle ITK inhibitor for treating inflammation and cancer
EA201792214A1 (en) * 2015-04-10 2018-01-31 Араксис Фарма Ллк COMPOUNDS OF SUBSTITUTE QUINAZOLINE
ES2856880T3 (en) 2015-04-15 2021-09-28 Araxes Pharma Llc KRAS Condensed Tricyclic Inhibitors and Methods of Using Them
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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 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
EP3356349A1 (en) 2015-09-28 2018-08-08 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
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 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
MX2018004643A (en) 2015-10-21 2018-08-01 Otsuka Pharma 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
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (en) 2016-03-30 2017-10-05 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
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
JP2019534260A (en) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Heterocyclic compounds as inhibitors of RAS and methods of use thereof
DK3534899T3 (en) 2016-11-03 2022-06-20 Corvus Pharmaceuticals Inc CONNECTIONS AND METHODS OF MODULATING INTERLEUKIN-2 INDUCERABLE T-CELL KINKASE
CN110382482A (en) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 Condensed miscellaneous-Heterobicyclic compounds and its application method
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
JP2020505395A (en) 2017-01-26 2020-02-20 アラクセス ファーマ エルエルシー Fused N-heterocyclic compounds and methods of use
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
EP3573954A1 (en) 2017-01-26 2019-12-04 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
JOP20190186A1 (en) 2017-02-02 2019-08-01 Astellas Pharma Inc Quinazoline compound
TW201906832A (en) 2017-05-25 2019-02-16 美商亞瑞克西斯製藥公司 Compounds for cancer treatment and methods of use thereof
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
BR112019024674A2 (en) 2017-05-25 2020-06-16 Araxes Pharma Llc COVALENT KRAS INHIBITORS
JP7266043B2 (en) 2018-05-04 2023-04-27 アムジエン・インコーポレーテツド KRas G12C inhibitors and methods of using them
CN112584833A (en) 2018-08-01 2021-03-30 亚瑞克西斯制药公司 Heterocyclic spiro compounds and methods of use thereof for treating cancer
MX2021004624A (en) 2018-10-24 2021-05-27 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.
WO2020113071A1 (en) 2018-11-29 2020-06-04 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer

Also Published As

Publication number Publication date
CA3063440A1 (en) 2018-11-29
AU2018271990A1 (en) 2019-12-12
PH12019550248A1 (en) 2021-01-11
CN110869358A (en) 2020-03-06
MX2019013954A (en) 2020-08-31
EP3630745A2 (en) 2020-04-08
WO2018218070A3 (en) 2019-02-07
US20230203018A1 (en) 2023-06-29
ZA202101138B (en) 2022-09-28
US11377441B2 (en) 2022-07-05
WO2018218070A2 (en) 2018-11-29
JP2020521742A (en) 2020-07-27
US10745385B2 (en) 2020-08-18
TW201900633A (en) 2019-01-01
US20190062313A1 (en) 2019-02-28
US20210024501A1 (en) 2021-01-28
BR112019024674A2 (en) 2020-06-16
KR20200010306A (en) 2020-01-30

Similar Documents

Publication Publication Date Title
ZA202101138B (en) Covalent inhibitors of kras
HK1249513A1 (en) Fused-tricyclic inhibitors of kras and methods of use thereof
IL274601A (en) Kras g12c inhibitors
HK1259232A1 (en) Substituted inhibitors of menin-mll and methods of use
HK1255699A1 (en) Modulators of kras expression
IL262867B (en) Kras g12c inhibitors
EP3541932A4 (en) Inhibitors of crispr-cas9
EP3600318A4 (en) Methods of using ehmt2 inhibitors
HK1215029A1 (en) Covalent inhibitors of kras g12c kras g12c
RS64271B1 (en) Inhibitors of trpc6
IL279949A (en) Heterocyclic inhibitors of mct4
IL257061A (en) Inhibitors of ezh2
EP3405477C0 (en) Inhibitors of transglutaminases
GB201521059D0 (en) Inhibitors of metallo-beta-lactamases
IL259796A (en) Aza-benzimidazole inhibitors of pad4
PT3458448T (en) Methods of using fasn inhibitors
GB201708457D0 (en) Inhibitors of metallo-beta-lactamases
IL270703A (en) Derivatives of resiquimod
GB201708451D0 (en) Inhibitors of metallo-beta-lactamases
AU2017904351A0 (en) Inhibitors of necroptosis
GB201614783D0 (en) Kinases inhibitors