ME02423B - 1-(3,3-DIMETILBUTIL)-3-(2-FLUOR-4-METIL-5-(7-METIL-2-(METILAMINO)PIRIDO[2,3-d]PIRIMIDIN-6-IL)FENIL)UREA KAO INHIBITOR Raf KINAZE U LIJEČENJU RAKA - Google Patents
1-(3,3-DIMETILBUTIL)-3-(2-FLUOR-4-METIL-5-(7-METIL-2-(METILAMINO)PIRIDO[2,3-d]PIRIMIDIN-6-IL)FENIL)UREA KAO INHIBITOR Raf KINAZE U LIJEČENJU RAKAInfo
- Publication number
- ME02423B ME02423B MEP-2016-124A MEP2016124A ME02423B ME 02423 B ME02423 B ME 02423B ME P2016124 A MEP2016124 A ME P2016124A ME 02423 B ME02423 B ME 02423B
- Authority
- ME
- Montenegro
- Prior art keywords
- compound
- salt
- cancer
- methyl
- phenyl
- Prior art date
Links
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical compound NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 159000000018 pyrido[2,3-d]pyrimidines Chemical class 0.000 title 1
- 102000009929 raf Kinases Human genes 0.000 title 1
- 108010077182 raf Kinases Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- HHCBMISMPSAZBF-UHFFFAOYSA-N LY3009120 Chemical compound CC1=NC2=NC(NC)=NC=C2C=C1C1=CC(NC(=O)NCCC(C)(C)C)=C(F)C=C1C HHCBMISMPSAZBF-UHFFFAOYSA-N 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 229920003083 Kollidon® VA64 Polymers 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 229940117958 vinyl acetate Drugs 0.000 claims 1
Classifications
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- 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
- C07D471/12—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 three hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Claims (12)
1. Spoj, naznačen time što je 1-(3,3-dimetilbutil)-3-(2-fluor-4-metil-5-(7-metil-2-(metilamino)pirido[2,3-d]pirimidin-6-il)fenil)urea, ili njezina farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je 1-(3,3-dimetilbutil)-3-(2-fluor-4-metil-5-(7-metil-2-(metilamino)pirido[2,3-d]pirimidin-6-il)fenil)urea.
3. Spoj u skladu s patentnim zahtjevom 2, koji je 1-(3,3-dimetilbutil)-3-(2-fluor-4-metil-5-(7-metil-2-(metilamino)pirido[2,3-d]pirimidin-6-il)fenil)urea u kristalnom obliku, naznačenom time što ima uzorak difrakcije rendgenskih zraka na prahu s karakterističnim signalima, u 2θ ± 0,2, koji se nalaze na 16,0 i jednom ili više od 6,9, 7,0, 18,2, te 23,2.
4. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1, ili njegovu farmaceutski prihvatljivu sol, uz farmaceutski prihvatljivu podlogu.
5. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, kao i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
6. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, kao i polivinilpirolidon–vinil-acetat (PVP-VA).
7. Farmaceutski pripravak u skladu s patentnim zahtjevom 6, naznačen time što je PVP-VA Kollidon® VA 64.
8. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačeni time što su namijenjeni upotrebi u terapiji.
9. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačeni time što su namijenjeni upotrebi u liječenju raka.
10. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 9, naznačeni time što se rak bira iz skupine koju čine rak štitnjače, rak jajnika, melanom, akuta mijelogena leukemija (AML) i kolorektalni rak.
11. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 10, naznačeni time što je rak melanom.
12. Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 10, naznačeni time što je rak kolorektalni rak.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261607702P | 2012-03-07 | 2012-03-07 | |
| PCT/US2013/029084 WO2013134243A1 (en) | 2012-03-07 | 2013-03-05 | 2-amino, 6-phenyl substituted pyrido [2, 3 - d] pyrimidine derivatives useful as raf kinase inhibitors |
| EP13712005.1A EP2850082B1 (en) | 2012-03-07 | 2013-03-05 | 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido(2,3-d)pyrimidin-6-yl)phenyl)urea as Raf kinase inhibitor for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02423B true ME02423B (me) | 2016-09-20 |
Family
ID=47884613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-124A ME02423B (me) | 2012-03-07 | 2013-03-05 | 1-(3,3-DIMETILBUTIL)-3-(2-FLUOR-4-METIL-5-(7-METIL-2-(METILAMINO)PIRIDO[2,3-d]PIRIMIDIN-6-IL)FENIL)UREA KAO INHIBITOR Raf KINAZE U LIJEČENJU RAKA |
Country Status (39)
| Country | Link |
|---|---|
| US (2) | US9334267B2 (me) |
| EP (1) | EP2850082B1 (me) |
| JP (1) | JP2015509536A (me) |
| KR (1) | KR20140129087A (me) |
| CN (1) | CN104302646B (me) |
| AP (1) | AP2014007899A0 (me) |
| AR (1) | AR090151A1 (me) |
| AU (1) | AU2013230146B2 (me) |
| BR (1) | BR112014018528A8 (me) |
| CA (1) | CA2863673A1 (me) |
| CL (1) | CL2014002220A1 (me) |
| CO (1) | CO7010837A2 (me) |
| CR (1) | CR20140378A (me) |
| CY (1) | CY1117846T1 (me) |
| DK (1) | DK2850082T3 (me) |
| DO (1) | DOP2014000200A (me) |
| EA (1) | EA024824B1 (me) |
| EC (1) | ECSP14017584A (me) |
| ES (1) | ES2584387T3 (me) |
| HK (1) | HK1202541A1 (me) |
| HR (1) | HRP20160654T1 (me) |
| HU (1) | HUE028095T2 (me) |
| IL (1) | IL234052A (me) |
| IN (1) | IN2014MN01575A (me) |
| LT (1) | LT2850082T (me) |
| MA (1) | MA37316B1 (me) |
| ME (1) | ME02423B (me) |
| MX (1) | MX2014010701A (me) |
| NZ (1) | NZ627454A (me) |
| PE (1) | PE20142338A1 (me) |
| PH (1) | PH12014501986A1 (me) |
| PT (1) | PT2850082T (me) |
| RS (1) | RS54840B1 (me) |
| SG (1) | SG11201404969YA (me) |
| SI (1) | SI2850082T1 (me) |
| TN (1) | TN2014000375A1 (me) |
| TW (1) | TW201348233A (me) |
| UA (1) | UA112340C2 (me) |
| WO (2) | WO2013134243A1 (me) |
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| AR090151A1 (es) * | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| JP2019517549A (ja) * | 2016-06-10 | 2019-06-24 | ノバルティス アーゲー | Ｃ−ｒａｆ阻害薬の治療的使用 |
| EP3878850A1 (en) | 2016-12-22 | 2021-09-15 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| WO2018200981A1 (en) * | 2017-04-28 | 2018-11-01 | Quartz Therapeutics, Inc. | Raf-degrading conjugate compounds |
| DK3728254T3 (da) | 2017-12-21 | 2023-06-06 | Boehringer Ingelheim Int | Benzylamin-substituerede pyridopyrimidinoner og derivater som sos1-inhibitorer |
| JP7161849B2 (ja) * | 2018-01-24 | 2022-10-27 | 株式会社クラレ | 第一級アミンの製造方法 |
| EP3746060A1 (en) | 2018-01-31 | 2020-12-09 | Deciphera Pharmaceuticals, LLC | Combination therapy for the treatment of mastocytosis |
| BR112020015581A2 (pt) | 2018-01-31 | 2021-02-02 | Deciphera Pharmaceuticals, Llc | terapia de combinação para o tratamento de tumores estromais gastrointestinais |
| WO2020055760A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| BR112021012812A2 (pt) | 2018-12-28 | 2021-12-07 | Deciphera Pharmaceuticals Llc | Csf1r inhibitors para uso e tratamento de câncer |
| AU2020218180B2 (en) | 2019-02-06 | 2025-09-04 | Eli Lilly And Company | 1-((2-(2,2,2-trifluoroethoxy)pyridin-4-yl)methyl)urea derivatives as KCNQ potentiators |
| TWI756636B (zh) * | 2019-02-18 | 2022-03-01 | 美商建南德克公司 | 嘧啶并嘧啶化合物及使用方法 |
| CA3138300A1 (en) | 2019-05-03 | 2020-11-12 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
| IL287795B2 (en) | 2019-05-10 | 2025-05-01 | Deciphera Pharmaceuticals Llc | Heteroarylaminopyrimidine amides as autophagy inhibitors and methods of using them |
| CN118878519A (zh) | 2019-05-10 | 2024-11-01 | 德西费拉制药有限责任公司 | 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
| WO2020257180A1 (en) | 2019-06-17 | 2020-12-24 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| KR20220045189A (ko) | 2019-08-12 | 2022-04-12 | 데시페라 파마슈티칼스, 엘엘씨. | 위장관 기질 종양을 치료하는 방법 |
| WO2021030405A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
| PH12022550976A1 (en) | 2019-10-24 | 2023-09-25 | Kinnate Biopharma Inc | Inhibitors of raf kinases |
| SMT202300467T1 (it) | 2019-12-30 | 2024-01-10 | Deciphera Pharmaceuticals Llc | Formulazioni di inibitori di chinasi amorfi e loro procedimenti d’uso |
| CN118948773A (zh) | 2019-12-30 | 2024-11-15 | 德西费拉制药有限责任公司 | 1-(4溴-5-(1乙基-7-(甲氨基)-2侧氧基-1,2-二氢-1,6-萘啶-3基)-2氟苯基)-3-苯基脲的组合物 |
| US20230212164A1 (en) | 2020-06-02 | 2023-07-06 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US11407737B2 (en) | 2020-09-18 | 2022-08-09 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| US11377431B2 (en) | 2020-10-12 | 2022-07-05 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
| WO2022090481A1 (en) | 2020-11-02 | 2022-05-05 | Boehringer Ingelheim International Gmbh | Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors |
| EP4247795A1 (en) | 2020-11-18 | 2023-09-27 | Deciphera Pharmaceuticals, LLC | Gcn2 and perk kinase inhibitors and methods of use thereof |
| CA3203111A1 (en) | 2020-12-22 | 2022-06-30 | Kailiang Wang | Sos1 inhibitors and uses thereof |
| IL307908A (en) | 2021-04-23 | 2023-12-01 | Kinnate Biopharma Inc | Cancer treatment with a RAF inhibitor |
| US12065427B2 (en) | 2021-04-29 | 2024-08-20 | Boehringer Ingelheim International Gmbh | Heterocyclic compounds capable of activating STING |
| JP2024543967A (ja) | 2021-12-01 | 2024-11-26 | 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 | ガン処置のための環化２－アミノ－３－シアノチオフェン及び誘導体 |
| EP4441050A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023099620A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| TW202340209A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| EP4441054A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| CN118613485A (zh) | 2021-12-01 | 2024-09-06 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物 |
| CN119585242A (zh) | 2021-12-09 | 2025-03-07 | 德西费拉制药有限责任公司 | Raf激酶抑制剂及其使用方法 |
| MX2024007042A (es) | 2021-12-09 | 2024-09-04 | Deciphera Pharmaceuticals Llc | Inhibidores de raf quinasa y metodos de uso de los mismos. |
| CN118434735A (zh) | 2021-12-23 | 2024-08-02 | 勃林格殷格翰国际有限公司 | 8-氮杂喹唑啉作为脑渗透sos1抑制剂 |
| WO2023173017A1 (en) * | 2022-03-09 | 2023-09-14 | Blossomhill Therapeutics, Inc. | Kras inhibitors for treating disease |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
| EP4608820A1 (en) | 2022-10-26 | 2025-09-03 | Boehringer Ingelheim International GmbH | Heterocyclic compounds capable of activating sting |
| CN120091996A (zh) | 2022-10-26 | 2025-06-03 | 勃林格殷格翰国际公司 | 能够激活sting的杂环化合物 |
| CR20250088A (es) | 2022-10-26 | 2025-05-21 | Boehringer Ingelheim Int | Compuestos heterocíclicos con capacidad para activar el receptor sting |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024246099A1 (en) | 2023-05-30 | 2024-12-05 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| GB2631397A (en) | 2023-06-28 | 2025-01-08 | Sevenless Therapeutics Ltd | New treatments for pain |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| GB2633813A (en) | 2023-09-21 | 2025-03-26 | Sevenless Therapeutics Ltd | New treatments for pain |
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| WO2025210041A1 (en) | 2024-04-03 | 2025-10-09 | Boehringer Ingelheim International Gmbh | Bicyclic benzylamido pyridine derivatives as sos1 inhibitors |
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| WO2003033472A1 (en) * | 2001-10-17 | 2003-04-24 | Kirin Beer Kabushiki Kaisha | Quinoline or quinazoline derivatives inhibiting auto- phosphorylation of fibroblast growth factor receptors |
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-
2013
- 2013-02-26 AR ARP130100576A patent/AR090151A1/es unknown
- 2013-02-27 TW TW102107122A patent/TW201348233A/zh unknown
- 2013-03-05 PE PE2014001381A patent/PE20142338A1/es not_active Application Discontinuation
- 2013-03-05 SG SG11201404969YA patent/SG11201404969YA/en unknown
- 2013-03-05 MA MA37316A patent/MA37316B1/fr unknown
- 2013-03-05 IN IN1575MUN2014 patent/IN2014MN01575A/en unknown
- 2013-03-05 DK DK13712005.1T patent/DK2850082T3/en active
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