SG11201909570PA - K-ras modulators - Google Patents

K-ras modulators

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Publication number
SG11201909570PA
SG11201909570PA SG11201909570PA SG11201909570PA SG 11201909570P A SG11201909570P A SG 11201909570PA SG 11201909570P A SG11201909570P A SG 11201909570PA SG 11201909570P A SG11201909570P A SG 11201909570PA
Authority
SG
Singapore
Prior art keywords
co7d
international
frederick
pct
ras
Prior art date
Application number
Inventor
Frank Mccormick
Adam Renslo
David Turner
Anna Maciag
Marcin Dyba
Elizabeth Vo
Joseph Saavedra
Vandana Kumari
Original Assignee
Univ California
Leidos Biomedical Research Inc
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Filing date
Publication date
Application filed by Univ California, Leidos Biomedical Research Inc filed Critical Univ California
Publication of SG11201909570PA publication Critical patent/SG11201909570PA/en

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  • Optical Modulation, Optical Deflection, Nonlinear Optics, Optical Demodulation, Optical Logic Elements (AREA)

Abstract

KrasbH 5C (GppNHp dose response 100 200 300 400 500 Concentration (uM) (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 25 October 2018 (25.10.2018) WIPO I PCT Iiiimmomiolollmonolomomnioomlloonomoun (10) International Publication Number WO 2018/195439 A2 (51) International Patent Classification: CO7D 405/14 (2006.01) CO7D 241/12 A61K 31/4192 (2006.01) CO7C 233/76 (2006.01) (2006.01) C07D 231/56 (2006.01) CO7D 207/40 (2006.01) CO7D 403/06 (2006.01) CO7D 213/40 (2006.01) CO7D 237/08 (2006.01) CO7D 303/36 (2006.01) CO7D 403/14 (2006.01) CO7D 305/06 (2006.01) CO7D 239/26 (2006.01) CO7D 307/28 (2006.01) CO7D 405/12 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/US2018/028593 (22) International Filing Date: 20 April 2018 (20.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/487,756 20 April 2017 (20.04.2017) US (71) Applicants: THE REGENTS OF THE UNIVERSI- TY OF CALIFORNIA [US/US]; 1111 Franklin Street, 12th Floor, Oakland, CA 94607-5200 (US). LEIDOS BIOMEDICAL RESEARCH, INC. [US/US]; P.O. Box B, 1050 Boyles Street, Frederick, MD 21702 (US). (72) Inventors: MCCORMICK, Frank; 5 Bernice St., San Francisco, CA 94103 (US). RENSLO, Adam; 5359 Shafter Avenue, Oakland, CA 94618 (US). TURNER, David; 501 Prospect Blvd., Apt. 24C, Frederick, MD 21701 (US). MACIAG, Anna, E.; 9214 Charterhouse Rd., Frederick, MD 21704 (US). DYBA, Marcin; 1930 Moran Drive, Frederick, MD 21702-6443 (US). VO, Elizabeth, D.; 391 Valencia St., Apt. 302, San Francisco, CA 94103 (US). SAAVEDRA, Joseph; 7189 Browns Ln, Thurmont, MD 21788 (US). KUMARI, Vandana; 9159 Bealls Farm Road, Frederick, MD 21704 (US). (74) Agent: TERRANOVA, Zachary, L. et al.; Mintz Levin Cohn Ferris Glovsky and Popeo, P.C., One Financial Cen- ter, Boston, MA 02111 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, = (54) Title: K-RAS MODULATORS FIG. 2 98e844 966854 917181 917105 960005 917332 916860 916929 917680 917878 957805 © (57) : Provided herein, inter alia, are methods and compounds for modulating K-Ras treating cancer. C [Continued on next page] WO 2018/195439 A2 IMIOHOIIIMIIMEIHOMOMBREIIIRIONMMIE MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: without international search report and to be republished upon receipt of that report (Rule 48.2(g)) with sequence listing part of description (Rule 5.2(a))
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Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. K-Ras modulators
JP7039489B2 (en) 2016-05-18 2022-03-22 ミラティ セラピューティクス, インコーポレイテッド KRAS G12C inhibitor
JOP20200001A1 (en) 2017-07-11 2022-10-30 Vertex Pharma Carboxamides as modulators of sodium channels
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
AU2018369759B2 (en) 2017-11-15 2022-11-24 Array Biopharma Inc. KRas G12C inhibitors
EP3790551A4 (en) 2018-05-07 2022-03-09 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN113692276A (en) * 2019-02-19 2021-11-23 加利福尼亚大学董事会 NURR1 receptor modulators
JP2022546043A (en) 2019-08-29 2022-11-02 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 inhibitor
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
CN112574174B (en) * 2019-09-27 2021-12-07 恩瑞生物医药科技(上海)有限公司 Protein degradation targeting chimera compound and preparation method and medical application thereof
TW202128675A (en) 2019-12-06 2021-08-01 美商維泰克斯製藥公司 Substituted tetrahydrofurans as modulators of sodium channels
CN115135315A (en) 2019-12-20 2022-09-30 米拉蒂治疗股份有限公司 SOS1 inhibitors
TW202210633A (en) 2020-06-05 2022-03-16 法商昂席歐公司 A dbait molecule in combination with kras inhibitor for the treatment of cancer
TW202214574A (en) * 2020-06-08 2022-04-16 加拿大商愛彼特生物製藥公司 Substituted (phthalazin-1-ylmethyl)ureas, substituted n-(phthalazin-1-ylmethyl)amides, and analogues thereof
BR112022025550A2 (en) 2020-06-18 2023-03-07 Revolution Medicines Inc METHODS TO DELAY, PREVENT, AND TREAT ACQUIRED RESISTANCE TO RAS INHIBITORS
MX2023002248A (en) 2020-09-03 2023-05-16 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations.
EP4263535A1 (en) 2020-12-17 2023-10-25 Astrazeneca AB N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)- quinoline-4-carboxamides
US20240210412A1 (en) * 2021-04-13 2024-06-27 University Of Virginia Patent Foundation Sulfonyl-triazole compounds useful as ligands and inhibitors of prostaglandin reductase 2
PE20241335A1 (en) 2021-06-04 2024-07-03 Vertex Pharma N-(HYDROXYALKYL (HETERO)ARYL) TETRAHYDROFURAN CARBOXAMIDES AS SODIUM CHANNEL MODULATORS
AR127064A1 (en) 2021-09-15 2023-12-13 Hua Medicine Shanghai Ltd PRODRUGS OF PYRROLIDONE DERIVATIVES AS A GLUCOKINASE ACTIVATOR
CA3234429A1 (en) * 2021-10-15 2023-04-20 Luc Farmer Ras inhibitors, compositions and methods of use thereof
TW202340202A (en) * 2021-12-22 2023-10-16 美國加利福尼亞大學董事會 Gtpase inhibitors and uses thereof
CN115028678B (en) * 2022-07-08 2024-09-06 杭州医学院 Bifunctional molecule based on VHL ligand-induced BCR-ABL protein degradation, and preparation method and application thereof

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3131527A1 (en) 1981-08-08 1983-02-24 Kali-Chemie Pharma Gmbh, 3000 Hannover 1-PHENYL-2-AMINOCARBONYLINDOL COMPOUNDS AND METHODS AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS
JPS61227567A (en) 1985-04-01 1986-10-09 Eisai Co Ltd 1,4-dihydropyridine derivative
DK626889A (en) 1988-12-16 1990-06-17 Roussel Uclaf INDANDER DERIVATIVES, THEIR PREPARATION AND MEDICINES WITH CONTENTS
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
WO1996006078A1 (en) 1994-08-24 1996-02-29 Pfizer Pharmaceuticals Inc. N-(2-(pyrrolidinyl-1)-1-phenylethyl)acetamides as kappa receptor antagonists
US5475109A (en) 1994-10-17 1995-12-12 Merck & Co., Inc. Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease
US5631251A (en) 1995-06-07 1997-05-20 Merck & Co., Inc. 5-cyclopropyl-1,4 benzodiazepine-2-ones
US6953855B2 (en) 1998-12-11 2005-10-11 Targacept, Inc. 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
NZ515829A (en) 1999-06-04 2003-10-31 Astrazeneca Ab Inhibitors of metalloproteinases
ES2249270T3 (en) 1999-08-12 2006-04-01 Pharmacia Italia S.P.A. DERIVATIVES OF 3 (5) -AMINOPIRAZOL, PROCEDURE FOR ITS PREPARATION AND ITS USE AS ANTITUMOR AGENTS.
WO2003004474A1 (en) 2001-07-06 2003-01-16 Syngenta Participations Ag Pesticidally active aminoacetonitriles
US20050256159A1 (en) 2002-10-11 2005-11-17 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11,betahsd1 inhibitors
PL1633724T3 (en) 2003-03-12 2011-10-31 Kudos Pharm Ltd Phthalazinone derivatives
PT1626714E (en) * 2003-05-20 2007-08-24 Bayer Pharmaceuticals Corp Diaryl ureas for diseases mediated by pdgfr
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
GB0326029D0 (en) 2003-11-07 2003-12-10 Astrazeneca Ab Chemical compounds
US20070275990A1 (en) 2003-11-13 2007-11-29 Ono Pharmaceutical Co., Ltd. Heterocyclic Spiro Compound
BRPI0417478A (en) * 2003-12-15 2007-05-08 Almirall Prodesfarma Ag 2,6-bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists
ATE443701T1 (en) 2004-01-16 2009-10-15 Wyeth Corp HETEROCYCLIC AZOLE-CONTAINING SULFONAMIDINE INHIBITORS OF BETA-AMYLOID PRODUCTION
RU2396265C2 (en) 2006-02-17 2010-08-10 Ф. Хоффманн-Ля Рош Аг Benzoylpiperidine derivatives as 5ht2 and d3 receptor modulators
WO2007109154A2 (en) 2006-03-16 2007-09-27 Renovis, Inc. Bicycloheteroaryl compounds as p2x7 modulators and uses thereof
JP2010523599A (en) * 2007-04-05 2010-07-15 シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド Development of molecular imaging probe for carbonic anhydrase-IX using click chemistry
WO2009015237A1 (en) 2007-07-23 2009-01-29 Syndax Pharmaceuticals, Inc. Novel compounds and methods of using them
SA08290475B1 (en) 2007-08-02 2013-06-22 Targacept Inc (2S,3R)-N-(2-((3-Pyridinyl)Methyl)-1-Azabicyclo[2.2.2]Oct-3-yl)Benzofuran-2-Carboxamide, Novel Salt forms, and Methods of Use Thereof
ES2395704T3 (en) 2008-12-19 2013-02-14 Novartis Ag Isoxazoline derivatives and their use as a pesticide
CA3080983C (en) * 2009-05-27 2023-02-28 Pct Therapeutics, Inc. Method of inhibiting and reducing a viral infection
AR082453A1 (en) 2010-04-21 2012-12-12 Novartis Ag FUROPIRIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND USES OF THE SAME
JP6399660B2 (en) * 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 Cancer treatment compositions and methods
EP2698367A1 (en) 2012-08-14 2014-02-19 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Benzimidazoles for the treatment of cancer
WO2014093230A2 (en) 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
EP3401314B1 (en) 2013-03-15 2023-11-08 Araxes Pharma LLC Covalent inhibitors of kras g12c
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US10196369B2 (en) 2013-09-26 2019-02-05 Sanford Burnham Prebys Medical Discovery Institute Spirocyclic EBI2 modulators
WO2016161361A1 (en) * 2015-04-03 2016-10-06 Nantbioscience, Inc. Compositions and methods of targeting mutant k-ras
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. K-Ras modulators
BR112018071093A2 (en) * 2016-04-15 2019-01-29 Epizyme Inc compound of formula, pharmaceutical composition, and method for preventing or treating a blood disorder

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