SG11201810171SA - Kras g12c inhibitors - Google Patents
Kras g12c inhibitorsInfo
- Publication number
- SG11201810171SA SG11201810171SA SG11201810171SA SG11201810171SA SG11201810171SA SG 11201810171S A SG11201810171S A SG 11201810171SA SG 11201810171S A SG11201810171S A SG 11201810171SA SG 11201810171S A SG11201810171S A SG 11201810171SA SG 11201810171S A SG11201810171S A SG 11201810171SA
- Authority
- SG
- Singapore
- Prior art keywords
- boulder
- walnut
- array biopharma
- array
- international
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102200006538 rs121913530 Human genes 0.000 abstract 3
- 101150105104 Kras gene Proteins 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 1
- 235000014571 nuts Nutrition 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000002023 wood Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111111111101110111111111111111111111111111111111111111110111111111111111111111110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2017/201161 Al 23 November 2017 (23.11.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every CO7D 231/56 (2006.01) A61K 31/445 (2006.01) kind of national protection available): AE, AG, AL, AM, CO7D 295/185 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (21) International Application Number: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, PCT/US2017/033099 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, (22) International Filing Date: KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, 17 May 2017 (17.05.2017) 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, (25) Filing Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 62/338,116 18 May 2016 (18.05.2016) US kind of regional protection available): ARIPO (BW, GH, 62/444,614 10 January 2017 (10.01.2017) US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (71) Applicants: MIRATI THERAPEUTICS, INC. [US/US]; TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 9393 Towne Centre Dr., Suite 200, San Diego, CA 92121 EE, ES, FL FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (US). ARRAY BIOPHARMA, INC. [US/US]; 3200 Wal- MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, nut St., Boulder, CO 80301 (US). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (72) Inventors: FISCHER, John, P.; c/o Array Biopharma, KM, ML, MR, NE, SN, TD, TG). _ Inc., 3200 Walnut St., Boulder, CO 80301 (US). FELL, Jay, Bradford; c/o Array Biopharma, Inc., 3200 Walnut Published: = St., Boulder, CO 80301 (US). BLAKE, James, F.; c/o Ar- — with international search report (Art. 2 I (3)) ray Biopharma, Inc., 3200 Walnut St., Boulder, CO 80301 = _ (US). HINKLIN, Ronald, Jay; c/o Array Biopharma, Inc., 3200 Walnut St., Boulder, CO 80301 (US). MEJIA, = Macedonio, J.; c/o Array Biopharma, Inc, 3200 Walnut = _ St., Boulder, CO 80301 (US). HICKEN, Erik, James; c/ = o Array Biopharma, Inc, 3200 Walnut St., Boulder, CO _ 80301 (US). CHICARELLI, Mark, Joseph; c/o Array Biopharma, Inc, 3200 Walnut St., Boulder, CO 80301 (US). — = GAUDINO, John, J.; c/o Array Biopharma, Inc, 3200 Wal- nut St., Boulder, CO 80301 (US). VIGERS, Guy, P.A.; c/o Array Biopharma, Inc, 3200 Walnut St., Boulder, CO = = = 80301 (US). BURGESS, Laurence, E.; c/o Array Bio- pharma, Inc, 3200 Walnut St., Boulder, CO 80301 (US). = MARX, Matthew, Arnold; c/o Mirati Therapeutics, Inc., 9393 Towne Centre Dr., Suite 200, San Diego, CA 92121 = (US). CHRISTENSEN, James, Gail; c/o Mirati Therapeu- = tics, Inc., 9393 Towne Centre Dr., Suite 200, San Diego, CA = — 92121 (US). LEE, Matthew, Randolf; c/o Mirati Thera- = peutics, Inc., 9393 Towne Centre Dr., Suite 200, San Diego, = CA 92121 (US). SAVECHENKOV, Pavel; c/o Array Bio- pharma, Inc., 3200 Walnut St., Boulder, CO 80301 (US). ZECCA, Henry, J.; c/o Array Biopharma, Inc., 3200 Wal- nut St., Boulder, CO 80301 (US). 1-1 .. (74) Agent: POLYAKOV, Mark, V. et al.; Wood, Phillips, Katz, Clark & Mortimer, 500 West Madison Street, Suite 1-1 1130, Chicago, IL 60661 (US). 1-1 1-1 0 ei IN (54) Title: KRAS G12C INHIBITORS 1-1 0 (57) : The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to ei compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods O of use therefor.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662338116P | 2016-05-18 | 2016-05-18 | |
| US201762444614P | 2017-01-10 | 2017-01-10 | |
| PCT/US2017/033099 WO2017201161A1 (en) | 2016-05-18 | 2017-05-17 | Kras g12c inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201810171SA true SG11201810171SA (en) | 2018-12-28 |
Family
ID=60326411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201810171SA SG11201810171SA (en) | 2016-05-18 | 2017-05-17 | Kras g12c inhibitors |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US11267812B2 (en) |
| EP (1) | EP3458445B1 (en) |
| JP (1) | JP7039489B2 (en) |
| KR (1) | KR102444509B1 (en) |
| CN (1) | CN109843856B (en) |
| AU (1) | AU2017266911B2 (en) |
| CA (1) | CA3024523A1 (en) |
| ES (1) | ES2863873T3 (en) |
| IL (1) | IL262867B (en) |
| MX (1) | MX382339B (en) |
| SG (1) | SG11201810171SA (en) |
| WO (1) | WO2017201161A1 (en) |
Families Citing this family (214)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201810171SA (en) | 2016-05-18 | 2018-12-28 | Mirati Therapeutics Inc | Kras g12c inhibitors |
| NZ754994A (en) | 2016-12-22 | 2022-12-23 | Amgen Inc | Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
| JOP20190272A1 (en) * | 2017-05-22 | 2019-11-21 | Amgen Inc | Kras g12c inhibitors and methods of using the same |
| ES2928576T3 (en) | 2017-09-08 | 2022-11-21 | Amgen Inc | KRAS G12C inhibitors and methods of use thereof |
| PT3710439T (en) | 2017-11-15 | 2023-05-15 | Array Biopharma Inc | Kras g12c inhibitors |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| WO2019110751A1 (en) * | 2017-12-08 | 2019-06-13 | Astrazeneca Ab | Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents |
| ES2969284T3 (en) * | 2018-01-19 | 2024-05-17 | Medshine Discovery Inc | Pyridone-pyrimidine derivative that acts as an inhibitor of mutein krasg12c |
| TW201942115A (en) * | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | Substituted quinazoline and pyridopyrimidine derivatives useful as anticancer agents |
| TW201942116A (en) * | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | Tetrahydroquinazoline derivatives useful as anticancer agents |
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| CA3099118A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
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| EP3802535B1 (en) | 2018-06-01 | 2022-12-14 | Amgen, Inc | Kras g12c inhibitors and methods of using the same |
| MA51848A (en) * | 2018-06-12 | 2021-04-21 | Amgen Inc | KRAS G12C INHIBITORS AND THEIR PROCEDURES FOR USE |
| BR112021002772A2 (en) * | 2018-08-16 | 2021-05-04 | F. Hoffmann-La Roche Ag | compounds, pharmaceutical compositions, method of treating cancer, methods of regulating the activity of a protein, for inhibiting the proliferation of a population of cells, for treating a disorder, for preparing a protein, for inhibiting tumor metastasis and for treating cancer and uses |
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| CA3111980A1 (en) * | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849537B1 (en) * | 2018-09-10 | 2024-10-23 | Mirati Therapeutics, Inc. | Combination therapies |
| IL281344B2 (en) * | 2018-09-10 | 2025-09-01 | Mirati Therapeutics Inc | Combination of cetuximab and adagrasib for cancer therapy |
| PT3849534T (en) * | 2018-09-10 | 2025-04-01 | Mirati Therapeutics Inc | Combination therapies |
| JP2022500385A (en) * | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス, インコーポレイテッド | Combination therapy |
| CN112996795B (en) | 2018-09-18 | 2024-11-12 | 尼坎治疗公司 | Fused tricyclic derivatives as SRC homolog-2 phosphatase inhibitors |
| CN114042070A (en) | 2018-09-30 | 2022-02-15 | 凯瑞康宁生物工程(武汉)有限公司 | Compounds as neuronal histamine receptor-3 antagonists and uses thereof |
| JP7451419B2 (en) | 2018-10-26 | 2024-03-18 | 大鵬薬品工業株式会社 | Novel indazole compound or salt thereof |
| RS66280B1 (en) * | 2018-11-09 | 2025-01-31 | Hoffmann La Roche | Fused ring compounds |
| JP7516029B2 (en) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Improved synthesis of key intermediates for KRAS G12C inhibitor compounds |
| US11053226B2 (en) | 2018-11-19 | 2021-07-06 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| JP7377679B2 (en) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | Combination therapy comprising a KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancer |
| CA3112129A1 (en) * | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2020165732A1 (en) | 2019-02-12 | 2020-08-20 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| CR20210504A (en) | 2019-03-05 | 2022-02-08 | Astrazeneca Ab | CONDENSED TRICYCLIC COMPOUNDS USEFUL AS ANTICANCER AGENTS |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| US20220227738A1 (en) * | 2019-05-20 | 2022-07-21 | California Institute Of Technology | Kras g12c inhibitors and uses thereof |
| WO2020236948A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| EP3972973A1 (en) | 2019-05-21 | 2022-03-30 | Amgen Inc. | Solid state forms |
| WO2020238791A1 (en) * | 2019-05-24 | 2020-12-03 | 江苏恒瑞医药股份有限公司 | Hydropyridopyrimidine derivative, preparation method therefor and medical use thereof |
| KR20220027879A (en) * | 2019-05-29 | 2022-03-08 | 상하이 한서 바이오메디컬 컴퍼니 리미티드 | Regulators of nitrogen-containing heterocyclic derivatives, preparation methods and uses thereof |
| CN112047939B (en) * | 2019-06-06 | 2023-05-02 | 江苏先声药业有限公司 | Tetrahydropyridopyrimidine compound with anti-tumor activity |
| CN114040914B (en) * | 2019-07-01 | 2024-10-22 | 江苏恒瑞医药股份有限公司 | Quinazolinone derivative, preparation method thereof and application thereof in medicine |
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| CN112390788A (en) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | Compound for inhibiting KRASG12C mutant protein and preparation method and application thereof |
| CN112390797A (en) * | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | Novel spirocyclic K-Ras G12C inhibitor |
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| CA3024523A1 (en) | 2017-11-23 |
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| US10633381B2 (en) | 2020-04-28 |
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| AU2017266911B2 (en) | 2021-09-02 |
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