MX2021004624A - Derivados de 2-(2-acriloil-2,6-diazaspiro[3.4]octan-6-il)-6-(1h-in dazol-4-il)-benzonitrilo y compuestos relacionados como inhibidores de la proteina kras mutante g12c para inhibir metastasis de tumor. - Google Patents
Derivados de 2-(2-acriloil-2,6-diazaspiro[3.4]octan-6-il)-6-(1h-in dazol-4-il)-benzonitrilo y compuestos relacionados como inhibidores de la proteina kras mutante g12c para inhibir metastasis de tumor.Info
- Publication number
- MX2021004624A MX2021004624A MX2021004624A MX2021004624A MX2021004624A MX 2021004624 A MX2021004624 A MX 2021004624A MX 2021004624 A MX2021004624 A MX 2021004624A MX 2021004624 A MX2021004624 A MX 2021004624A MX 2021004624 A MX2021004624 A MX 2021004624A
- Authority
- MX
- Mexico
- Prior art keywords
- diazaspiro
- indazol
- acryloyl
- octan
- inhibitors
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D471/10—Spiro-condensed systems
Abstract
La presente invención proporciona por ejemplo 2-(2-acriloil-2,6-diazaespiro[3.4]octan-6-il)-6-(1H-indazol-4-il) -benzonitrilo y por ejemplo derivados de 2-(2-acriloil-2,6-diazaes piro[3.4]octan-6-il)-6-(1H-indazol-4-il)-benzonitrilo y compuestos de la fórmula (I) relacionados como inhibidores de proteína KRAS mutante G12C para el tratamiento de la metástasis tumoral. La presente descripción describe compuestos ejemplares (por ejemplo, páginas 53 a 90; tabla 1; compuestos I-1 a I-141), datos farmacológicos (por ejemplo, páginas 125 a 128; tabla 2; ejemplo 1) y síntesis de los mismos (por ejemplo, páginas 129 a 143; ejemplos 2 a 7). Los compuestos ejemplares son por ejemplo 2-(2-acriloil-2,6-diazaespiro[3.4]octan-6-il)-6-(5-metil-1H-indaz ol-4-il)-4- morfolinobenzonitrilo (ejemplo 2; compuesto I-1) y 6-(2-acriloil-2,7-diazaespiro[3.5]nonan-7-il)-3-metoxi-2-(5-metil -1H-indazol-4-il)-4-morfolinobenzonitrilo (ejemplo 7; compuesto I-84).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862750009P | 2018-10-24 | 2018-10-24 | |
PCT/US2019/057694 WO2020086739A1 (en) | 2018-10-24 | 2019-10-23 | 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 |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2021004624A true MX2021004624A (es) | 2021-05-27 |
Family
ID=68542837
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2021004624A MX2021004624A (es) | 2018-10-24 | 2019-10-23 | Derivados de 2-(2-acriloil-2,6-diazaspiro[3.4]octan-6-il)-6-(1h-in dazol-4-il)-benzonitrilo y compuestos relacionados como inhibidores de la proteina kras mutante g12c para inhibir metastasis de tumor. |
Country Status (10)
Country | Link |
---|---|
US (1) | US20210380595A1 (es) |
EP (1) | EP3870585A1 (es) |
JP (1) | JP2022505835A (es) |
KR (1) | KR20210083286A (es) |
CN (1) | CN113207291A (es) |
AU (1) | AU2019364417A1 (es) |
BR (1) | BR112021007726A2 (es) |
CA (1) | CA3117210A1 (es) |
MX (1) | MX2021004624A (es) |
WO (1) | WO2020086739A1 (es) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
TW201702232A (zh) | 2015-04-10 | 2017-01-16 | 亞瑞克西斯製藥公司 | 經取代之喹唑啉化合物及其使用方法 |
US10875842B2 (en) | 2015-09-28 | 2020-12-29 | 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 |
US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
TW201726656A (zh) | 2015-11-16 | 2017-08-01 | 亞瑞克西斯製藥公司 | 包含經取代雜環基團之2-經取代喹唑啉化合物及其使用方法 |
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 |
US11274093B2 (en) | 2017-01-26 | 2022-03-15 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
EP3573970A1 (en) | 2017-01-26 | 2019-12-04 | 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 |
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 |
EP3573964A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Benzothiophene and benzothiazole compounds and methods of use thereof |
BR112019024674A2 (pt) | 2017-05-25 | 2020-06-16 | Araxes Pharma Llc | Inibidores covalentes da kras |
EP3630747A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Quinazoline derivatives as modulators of mutant kras, hras or nras |
CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
CN115916194A (zh) | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
EP4185569A1 (en) | 2020-08-17 | 2023-05-31 | Aligos Therapeutics, Inc. | Methods and compositions for targeting pd-l1 |
CN116209438A (zh) | 2020-09-03 | 2023-06-02 | 锐新医药公司 | 使用sos1抑制剂治疗具有shp2突变的恶性疾病 |
AR123848A1 (es) * | 2020-10-20 | 2023-01-18 | Amgen Inc | Compuestos espiro heterocíclicos y métodos de uso |
WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5863A (en) | 1848-10-17 | Matthias p | ||
US5861A (en) | 1848-10-17 | Locking umbrella and parasol | ||
US949A (en) | 1838-09-27 | Improvement in roller cotton-gins for ginning long-staple and other kinds of cotton | ||
US510A (en) | 1837-12-07 | soeel | ||
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 |
GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
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 |
DK0780386T3 (da) | 1995-12-20 | 2003-02-03 | Hoffmann La Roche | Matrixmetalloproteaseinhibitorer |
JP3195756B2 (ja) | 1996-07-04 | 2001-08-06 | 公子 吉水 | 潤滑補助体 |
TR199900066T2 (xx) | 1996-07-18 | 1999-04-21 | Pfizer Inc. | Matriks metalloproteazlar�n fosfinat bazl� inhibit�rleri |
IL128189A0 (en) | 1996-08-23 | 1999-11-30 | Pfizer | Arylsulfonylamino hydroxamic acid derivatives |
US6077864A (en) | 1997-01-06 | 2000-06-20 | Pfizer Inc. | Cyclic sulfone derivatives |
PL335027A1 (en) | 1997-02-03 | 2000-03-27 | Pfizer Prod Inc | Derivatives of arylsulphonylamino hydroxamic acid |
CA2279863A1 (en) | 1997-02-07 | 1998-08-13 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
BR9807678A (pt) | 1997-02-11 | 2000-02-15 | Pfizer | Derivados de ácidos arilsulfonil-hidroxâmicos |
GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
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 |
SE0302811D0 (sv) * | 2003-10-23 | 2003-10-23 | Astrazeneca Ab | Novel compounds |
CA2663501A1 (en) * | 2006-09-15 | 2008-03-20 | Schering Corporation | Treating pain, diabetes, and disorders of lipid metabolism |
US20120083476A1 (en) * | 2009-06-05 | 2012-04-05 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
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 |
JP6559123B2 (ja) | 2013-10-10 | 2019-08-14 | アラクセス ファーマ エルエルシー | Krasg12cの阻害剤 |
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 |
JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
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2019
- 2019-10-23 CN CN201980084272.5A patent/CN113207291A/zh active Pending
- 2019-10-23 WO PCT/US2019/057694 patent/WO2020086739A1/en unknown
- 2019-10-23 EP EP19802439.0A patent/EP3870585A1/en active Pending
- 2019-10-23 AU AU2019364417A patent/AU2019364417A1/en not_active Abandoned
- 2019-10-23 JP JP2021522510A patent/JP2022505835A/ja active Pending
- 2019-10-23 KR KR1020217015082A patent/KR20210083286A/ko unknown
- 2019-10-23 BR BR112021007726-0A patent/BR112021007726A2/pt not_active Application Discontinuation
- 2019-10-23 MX MX2021004624A patent/MX2021004624A/es unknown
- 2019-10-23 CA CA3117210A patent/CA3117210A1/en active Pending
- 2019-10-23 US US17/287,473 patent/US20210380595A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
EP3870585A1 (en) | 2021-09-01 |
BR112021007726A2 (pt) | 2021-07-27 |
CN113207291A (zh) | 2021-08-03 |
AU2019364417A1 (en) | 2021-05-20 |
CA3117210A1 (en) | 2020-04-30 |
KR20210083286A (ko) | 2021-07-06 |
US20210380595A1 (en) | 2021-12-09 |
JP2022505835A (ja) | 2022-01-14 |
WO2020086739A1 (en) | 2020-04-30 |
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