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
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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
- A61K31/4985—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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (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) | US8741911B2 (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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| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| RU2018146886A (ru) * | 2016-06-10 | 2020-07-10 | Новартис Аг | Пути терапевтического применения ингибитора c-raf |
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| WO2018200981A1 (en) * | 2017-04-28 | 2018-11-01 | Quartz Therapeutics, Inc. | Raf-degrading conjugate compounds |
| TWI870922B (zh) | 2017-12-21 | 2025-01-21 | 德商百靈佳殷格翰國際股份有限公司 | 作為sos1抑制劑之新穎芐胺基取代吡啶并嘧啶酮及衍生物 |
| 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 |
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| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras 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 |
| US20080207617A1 (en) * | 2002-10-29 | 2008-08-28 | Kirin Beer Kabushiki Kaisha | Quinoline Derivatives and Quinazoline Derivatives Inhibiting Autophosphrylation of Flt3 and Medicinal Compositions Containing the Same |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US8188113B2 (en) * | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| AR080151A1 (es) * | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| AR090151A1 (es) * | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
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