HRP20161498T1 - Inhibitori kinaza i njihova upotreba u liječenju raka - Google Patents
Inhibitori kinaza i njihova upotreba u liječenju raka Download PDFInfo
- Publication number
- HRP20161498T1 HRP20161498T1 HRP20161498TT HRP20161498T HRP20161498T1 HR P20161498 T1 HRP20161498 T1 HR P20161498T1 HR P20161498T T HRP20161498T T HR P20161498TT HR P20161498 T HRP20161498 T HR P20161498T HR P20161498 T1 HRP20161498 T1 HR P20161498T1
- Authority
- HR
- Croatia
- Prior art keywords
- cancer
- compound
- salt
- pharmaceutically acceptable
- acceptable salt
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims 8
- 201000011510 cancer Diseases 0.000 title claims 8
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 13
- 206010006187 Breast cancer Diseases 0.000 claims 7
- 208000026310 Breast neoplasm Diseases 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 206010039491 Sarcoma Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000032383 Soft tissue cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 206010024627 liposarcoma Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- -1 methoxy, methyl Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010073135 Dedifferentiated liposarcoma Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 101000582914 Homo sapiens Serine/threonine-protein kinase PLK4 Proteins 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 201000010395 Pleomorphic liposarcoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 102100030267 Serine/threonine-protein kinase PLK4 Human genes 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000026534 luminal B breast carcinoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 206010042863 synovial sarcoma Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/535—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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Claims (13)
1. Spoj, naznačen time što ga predstavlja sljedeća strukturna formula:
[image]
;
ili njegova farmaceutski prihvatljiva sol, gdje:
Ra je -F, metoksi, metil ili etil;
R4 je -H ili metil; i
R6 je -CH=CH-(izborno supstituirani fenil), gdje je fenil u -CH=CH-(fenil) izborno supstituiran s jednim ili više supstituenata, koje se neovisno bira iz skupine koju čine halogen, C1-6 alkil, C1-6 halogenalkil, (C1-6 aminoalkil), (C1-6 alkilamino)C1-6 alkil, (fenil)C1-6 alkil, amino, C1-6 alkilamino, C1-6 dialkilamino, -(CH2)0-3-N-piperidinil, -(CH2)0-3-N-morfolinil, -(CH2)0-3-N-pirolidinil, -(CH2)0-3-N-piperazinil i -(CH2)0-3-N-oksazepanil, gdje je N-piperazinil izborno N′-supstituiran s C1-6 alkilom ili C1-6 acilom.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što spoj predstavlja sljedeća strukturna formula:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što spoj predstavlja sljedeća strukturna formula:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
4. Spoj, naznačen time što ga predstavlja sljedeća strukturna formula:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
5. Spoj, naznačen time što ga predstavlja sljedeća strukturna formula:
[image]
;
ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi kao medikament.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju raka.
8. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 7, naznačen time što se rak bira iz skupine koju čine rak pluća, rak dojke, rak debelog crijeva, rak na mozgu, neuroblastom, rak prostate, melanom, multiformni glioblastom, rak jajnika, limfom, leukemija, melanom, sarkom, paraneoplazije, osteosarkom, germinom, gliom i mezoteliom.
9. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 8, naznačen time što se rak bira iz skupine koju čine rak pluća, rak dojke ili rak debelog crijeva.
10. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 9, naznačen time što je rak bazalni podtip raka dojke ili luminalni B podtip raka dojke.
11. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je rak bazalni podtip raka dojke koji hipereksprimira PLK4.
12. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 9, naznačen time što je rak bazalni podtip raka dojke koji je ER, HER2 i PR negativan rak dojke.
13. Spoj, ili njegova sol, namijenjen upotrebi u skladu s patentnim zahtjevom 7, naznačen time što je rak rak mekog tkiva, gdje je rak mekog tkiva sarkom, kojeg se po mogućnosti bira iz skupine koju čine fibrosarkom, gastrointestinalni sarkom, lejomiosarkom, dediferencirani liposarkom, pleomorfni liposarkom, zloćudni fibrozni histiocitom, sarkom okruglih stanica, te sinovijski sarkom.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32132910P | 2010-04-06 | 2010-04-06 | |
| US32133210P | 2010-04-06 | 2010-04-06 | |
| PCT/CA2010/000518 WO2010115279A1 (en) | 2009-04-06 | 2010-04-06 | Kinase inhibitors and method of treating cancer with same |
| PCT/CA2011/000386 WO2011123946A1 (en) | 2010-04-06 | 2011-04-06 | Kinase inhibitors and method of treating cancer with same |
| EP11764988.9A EP2556071B1 (en) | 2010-04-06 | 2011-04-06 | Kinase inhibitors and their use in treating cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161498T1 true HRP20161498T1 (hr) | 2016-12-16 |
Family
ID=44761967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161498TT HRP20161498T1 (hr) | 2010-04-06 | 2016-11-14 | Inhibitori kinaza i njihova upotreba u liječenju raka |
Country Status (25)
| Country | Link |
|---|---|
| US (9) | US8921545B2 (hr) |
| EP (2) | EP2556070B1 (hr) |
| JP (1) | JP5442906B2 (hr) |
| KR (1) | KR101782668B1 (hr) |
| CN (1) | CN102892766B (hr) |
| AU (1) | AU2011238384B2 (hr) |
| BR (1) | BR112012025496B1 (hr) |
| CY (1) | CY1118610T1 (hr) |
| DK (1) | DK2556071T3 (hr) |
| EA (1) | EA023173B1 (hr) |
| ES (2) | ES2639757T3 (hr) |
| HR (1) | HRP20161498T1 (hr) |
| HU (1) | HUE030651T2 (hr) |
| IL (1) | IL221556A (hr) |
| LT (1) | LT2556071T (hr) |
| ME (1) | ME02545B (hr) |
| MX (1) | MX2012011516A (hr) |
| NZ (1) | NZ602350A (hr) |
| PL (1) | PL2556071T3 (hr) |
| PT (1) | PT2556071T (hr) |
| SG (1) | SG183875A1 (hr) |
| SI (1) | SI2556071T1 (hr) |
| SM (1) | SMT201600430B (hr) |
| TW (1) | TWI516262B (hr) |
| WO (2) | WO2011123947A1 (hr) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2235004A4 (en) | 2007-12-21 | 2011-05-04 | Univ Health Network | INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL-SUBSTITUTED INDOLUND DERIVATIVES AS A KINASE-HEMMER FOR CANCER TREATMENT |
| WO2010115279A1 (en) | 2009-04-06 | 2010-10-14 | University Health Network | Kinase inhibitors and method of treating cancer with same |
| US8921545B2 (en) | 2010-04-06 | 2014-12-30 | University Health Network | Synthesis of chiral 2-(1H-indazol-6-yl)-spiro[cyclopropane-1,3′-indolin]-2′-ones |
| US8933070B2 (en) | 2010-07-02 | 2015-01-13 | University Health Network | Methods of targeting PTEN mutant diseases and compositions therefor |
| WO2012048411A1 (en) * | 2010-10-13 | 2012-04-19 | University Health Network | Plk-4 inhibitors and method of treating cancer with same |
| KR102226489B1 (ko) * | 2012-07-27 | 2021-03-11 | 사토 파머슈티컬 가부시키가이샤 | 디플루오로메틸렌 화합물 |
| HUE043194T2 (hu) | 2013-10-18 | 2019-08-28 | Univ Health Network | PLK-4 inhibitor sója és kristályformái |
| KR102195494B1 (ko) | 2013-10-18 | 2020-12-28 | 유니버시티 헬스 네트워크 | 췌장암 치료 |
| CN104130175A (zh) * | 2014-06-13 | 2014-11-05 | 天津科技大学 | 不同位置取代吲哚酮类衍生物及其应用 |
| WO2018145525A1 (zh) | 2017-02-08 | 2018-08-16 | 中国医药研究开发中心有限公司 | 吡咯并芳杂环类化合物及其制备方法和医药用途 |
| CN108947970B (zh) * | 2017-05-18 | 2022-04-05 | 四川大学 | 吲唑类衍生物及其制备方法和用途 |
| CA3074876A1 (en) * | 2017-09-08 | 2019-03-14 | University Health Network | Combination therapies for inhibition of polo-like kinase 4 |
| CA3137191A1 (en) | 2019-04-24 | 2020-10-29 | University Health Network | Crystal form s4 of the plk4 inhibitor (ir,2s)-(e)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)- 1 h-imidazol-6-yl)-5'-methoxyspiro[cyclopropane-l,3'-indolin]-2'-one fumarate |
| WO2021226261A1 (en) | 2020-05-06 | 2021-11-11 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CN112250614B (zh) * | 2020-10-20 | 2022-02-01 | 苏州大学 | 3-螺三元环吲哚酮衍生物的合成方法 |
| TW202300485A (zh) * | 2021-03-02 | 2023-01-01 | 大陸商上海齊魯製藥研究中心有限公司 | Plk4抑制劑及其用途 |
| EP4337198A1 (en) | 2021-05-11 | 2024-03-20 | Oric Pharmaceuticals, Inc. | Polo like kinase 4 inhibitors |
| CN115677682B (zh) * | 2021-07-30 | 2023-07-18 | 上海齐鲁制药研究中心有限公司 | 螺环类plk4抑制剂及其用途 |
| AU2022388555A1 (en) | 2021-11-09 | 2024-05-02 | Ajax Therapeutics, Inc. | 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| WO2024006379A1 (en) * | 2022-06-30 | 2024-01-04 | Axonis Therapeutics, Inc. | Methods and compounds for inhibiting mkk7 enzymes |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3310891A1 (de) | 1983-03-25 | 1984-09-27 | Boehringer Mannheim Gmbh, 6800 Mannheim | Neue indolinon-(2)-derivate, verfahren zu ihrer herstellung, diese verbindungen enthaltende arzneimittel und zwischenprodukte |
| US5182397A (en) * | 1990-05-31 | 1993-01-26 | American Cyanamid Company | Aryloxyspiroalkylindolinone herbicides |
| GB9507298D0 (en) | 1995-04-07 | 1995-05-31 | Pharmacia Spa | Substituted indolylmethylene-oxindale analogues as tyrosine kinase inhibitors |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| WO1998007695A1 (en) | 1996-08-23 | 1998-02-26 | Sugen, Inc. | Indolinone combinatorial libraries and related products and methods for the treatment of disease |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6133305A (en) * | 1997-09-26 | 2000-10-17 | Sugen, Inc. | 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity |
| CA2383623A1 (en) | 1998-08-04 | 2000-02-17 | Sugen, Inc. | 3-methylidenyl-2-indolinone modulators of protein kinase |
| JP2002540096A (ja) | 1999-03-24 | 2002-11-26 | スージェン・インコーポレーテッド | キナーゼ阻害剤としてのインドリノン化合物 |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| CA2410509A1 (en) | 2000-06-02 | 2001-12-13 | Sugen, Inc. | Indolinone derivatives as protein kinase/phosphatase inhibitors |
| US6897231B2 (en) | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| IL164209A0 (en) | 2002-05-31 | 2005-12-18 | Eisai Co Ltd | Pyrazole derivatives and pharmaceutical compositions containing the same |
| US7148249B2 (en) | 2002-09-12 | 2006-12-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments |
| AU2003286604A1 (en) * | 2002-10-21 | 2004-05-13 | Irm Llc | Oxindoles with anti-hiv activity |
| EP1696906A1 (en) | 2003-12-16 | 2006-09-06 | Leo Pharma A/S | Novel therapeutic use of indolinone derivatives |
| US20050211590A1 (en) | 2004-03-26 | 2005-09-29 | Mcclure George K | Protective cover for medical devices |
| DE102005005395A1 (de) | 2005-02-03 | 2006-08-10 | Schering Aktiengesellschaft | Thiazolidinone, deren Herstellung und Verwendung als Arzneimittel |
| US7309787B2 (en) | 2005-07-13 | 2007-12-18 | Allergan, Inc. | Kinase inhibitors |
| WO2007058626A1 (en) * | 2005-11-16 | 2007-05-24 | S*Bio Pte Ltd | Indazole compounds |
| US20070135509A1 (en) | 2005-12-09 | 2007-06-14 | Blackburn Thomas P | Indolone compounds useful to treat cognitive impairment |
| FR2896503B1 (fr) | 2006-01-23 | 2012-07-13 | Aventis Pharma Sa | Nouveaux derives soufres d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| WO2007109026A2 (en) | 2006-03-15 | 2007-09-27 | The Trustees Of Columbia University In The City Of New York | Pten compositions and methods for detecting breast cancer |
| GB0606234D0 (en) | 2006-03-29 | 2006-05-10 | Pliva Istrazivanje I Razvoj D | Pharmaceutically acceptable salts and polymorphic forms |
| US8207179B2 (en) * | 2007-06-12 | 2012-06-26 | Boehringer Ingelheim International Gmbh | Substituted indolines as tyrosine kinase inhibitors |
| MX2010003249A (es) | 2007-09-25 | 2010-11-09 | Takeda Pharmaceutical | Inhibidores de quinasas símil polo. |
| CA2706075A1 (en) | 2007-11-20 | 2009-05-28 | University Health Network | Cancer diagnostic and therapeutic methods that target plk4/sak |
| JP2009173629A (ja) * | 2007-12-21 | 2009-08-06 | Banyu Pharmaceut Co Ltd | Ｒｓｋ１阻害作用を有する新規スピロインダン誘導体 |
| EP2235004A4 (en) | 2007-12-21 | 2011-05-04 | Univ Health Network | INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL-SUBSTITUTED INDOLUND DERIVATIVES AS A KINASE-HEMMER FOR CANCER TREATMENT |
| US8765791B2 (en) * | 2008-03-11 | 2014-07-01 | University Health Network | Method of treating cancer using a neuropeptide Y 5R (NP Y5R) antagonist |
| EP2108641A1 (en) * | 2008-04-11 | 2009-10-14 | Laboratorios Almirall, S.A. | New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors |
| EP2113503A1 (en) * | 2008-04-28 | 2009-11-04 | Laboratorios Almirall, S.A. | New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors |
| JP2011524374A (ja) | 2008-06-16 | 2011-09-01 | ティグリス ファーマスーティカルズ，インク． | アミノフラボンに対する感応性を判定する方法 |
| DE102008040187A1 (de) | 2008-07-04 | 2010-01-07 | Robert Bosch Gmbh | Sensorelement, Verfahren zu seiner Herstellung sowie Verwendung |
| JP2011530511A (ja) | 2008-08-05 | 2011-12-22 | メルク・シャープ・エンド・ドーム・コーポレイション | 治療用化合物 |
| WO2010115279A1 (en) | 2009-04-06 | 2010-10-14 | University Health Network | Kinase inhibitors and method of treating cancer with same |
| WO2011069298A1 (en) * | 2009-12-11 | 2011-06-16 | F. Hoffmann-La Roche Ag | Novel cyclopropane indolinone derivatives |
| JP5056876B2 (ja) | 2010-03-19 | 2012-10-24 | Ｊｆｅスチール株式会社 | 冷間加工性と焼入れ性に優れた熱延鋼板およびその製造方法 |
| US8921545B2 (en) * | 2010-04-06 | 2014-12-30 | University Health Network | Synthesis of chiral 2-(1H-indazol-6-yl)-spiro[cyclopropane-1,3′-indolin]-2′-ones |
| US8933070B2 (en) | 2010-07-02 | 2015-01-13 | University Health Network | Methods of targeting PTEN mutant diseases and compositions therefor |
| WO2012048411A1 (en) | 2010-10-13 | 2012-04-19 | University Health Network | Plk-4 inhibitors and method of treating cancer with same |
| CN103476770B (zh) | 2010-11-25 | 2017-02-15 | 拉蒂欧制药有限责任公司 | 阿法替尼盐和多晶型物 |
| WO2012118812A2 (en) * | 2011-02-28 | 2012-09-07 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| GB201109966D0 (en) | 2011-06-10 | 2011-07-27 | Cancer Res Inst Royal | Materials and methods for treating pten mutated or deficient cancer |
| CA2850394C (en) | 2011-10-12 | 2019-05-21 | University Health Network | Indazole compounds as kinase inhibitors and method of treating cancer with same |
| KR102195494B1 (ko) | 2013-10-18 | 2020-12-28 | 유니버시티 헬스 네트워크 | 췌장암 치료 |
| HUE043194T2 (hu) | 2013-10-18 | 2019-08-28 | Univ Health Network | PLK-4 inhibitor sója és kristályformái |
-
2011
- 2011-04-06 US US13/639,648 patent/US8921545B2/en active Active
- 2011-04-06 WO PCT/CA2011/000387 patent/WO2011123947A1/en active Application Filing
- 2011-04-06 EP EP11764989.7A patent/EP2556070B1/en active Active
- 2011-04-06 BR BR112012025496-0A patent/BR112012025496B1/pt active IP Right Grant
- 2011-04-06 JP JP2013502966A patent/JP5442906B2/ja active Active
- 2011-04-06 EP EP11764988.9A patent/EP2556071B1/en active Active
- 2011-04-06 PL PL11764988T patent/PL2556071T3/pl unknown
- 2011-04-06 AU AU2011238384A patent/AU2011238384B2/en active Active
- 2011-04-06 DK DK11764988.9T patent/DK2556071T3/en active
- 2011-04-06 LT LTEP11764988.9T patent/LT2556071T/lt unknown
- 2011-04-06 EA EA201270752A patent/EA023173B1/ru unknown
- 2011-04-06 HU HUE11764988A patent/HUE030651T2/en unknown
- 2011-04-06 NZ NZ602350A patent/NZ602350A/en unknown
- 2011-04-06 ES ES11764989T patent/ES2639757T3/es active Active
- 2011-04-06 KR KR1020127029064A patent/KR101782668B1/ko active IP Right Grant
- 2011-04-06 TW TW100111767A patent/TWI516262B/zh active
- 2011-04-06 PT PT117649889T patent/PT2556071T/pt unknown
- 2011-04-06 SG SG2012065090A patent/SG183875A1/en unknown
- 2011-04-06 SI SI201131015A patent/SI2556071T1/sl unknown
- 2011-04-06 ME MEP-2016-265A patent/ME02545B/me unknown
- 2011-04-06 US US13/081,254 patent/US8263596B2/en active Active
- 2011-04-06 WO PCT/CA2011/000386 patent/WO2011123946A1/en active Application Filing
- 2011-04-06 MX MX2012011516A patent/MX2012011516A/es active IP Right Grant
- 2011-04-06 CN CN201180018148.2A patent/CN102892766B/zh active Active
- 2011-04-06 ES ES11764988.9T patent/ES2603613T3/es active Active
-
2012
- 2012-06-21 US US13/529,542 patent/US8481533B2/en active Active
- 2012-08-21 IL IL221556A patent/IL221556A/en active IP Right Grant
-
2013
- 2013-07-03 US US13/935,021 patent/US9139563B2/en active Active
-
2014
- 2014-12-23 US US14/580,658 patent/US9579327B2/en active Active
-
2015
- 2015-08-11 US US14/823,057 patent/US9907800B2/en active Active
-
2016
- 2016-11-14 HR HRP20161498TT patent/HRP20161498T1/hr unknown
- 2016-11-17 CY CY20161101184T patent/CY1118610T1/el unknown
- 2016-11-24 SM SM201600430T patent/SMT201600430B/it unknown
-
2017
- 2017-02-23 US US15/440,548 patent/US9796703B2/en active Active
- 2017-10-23 US US15/790,847 patent/US10077255B2/en active Active
-
2018
- 2018-02-22 US US15/902,143 patent/US10358436B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20161498T1 (hr) | Inhibitori kinaza i njihova upotreba u liječenju raka | |
| HRP20171957T1 (hr) | Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka | |
| CY1124117T1 (el) | Ετεροκυκλικες αλκυνυλοβενζολικες ενωσεις και ιατρικες συνθεσεις και χρησεις αυτων | |
| HRP20180202T1 (hr) | Purinski derivati, namijenjeni upotrebi u liječenju alergijskih, upalnih i zaraznih bolesti | |
| HRP20181048T1 (hr) | Neuroaktivni 19-alkoksi-17-supstituirani steroidi, korisni u postupcima liječenja | |
| CY1119381T1 (el) | Παραγωγα 2-μεθυλομορφολινο πυριδο-, πυραζο- και πυριμιδο-πυριμιδινης ως αναστολεις mtor | |
| RS53096B (en) | OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES | |
| GEP201706735B (en) | Kinase inhibitors | |
| RU2017145026A (ru) | Соединение, ингибирующее brk | |
| GEP20156389B (en) | Oxazolidin-2-one compounds and their usage as pi3ks inhibitors | |
| JP2013523784A5 (hr) | ||
| EA201391029A1 (ru) | Производные оксазина и их применение при лечении неврологических нарушений | |
| HK1149258A1 (en) | Compounds | |
| MX2013003036A (es) | Derivados de pirazina como bloqueadores de enac. | |
| PH12014501542B1 (en) | Substituted pyrrolidine -2- carboxamides | |
| TR201802944T4 (tr) | İlaç olarak azai̇ndazol veya di̇azai̇ndazol türünün türevleri̇ | |
| EA200802214A1 (ru) | 2,4-диаминопиримидины в качестве ингибиторов киназ, участвующих в регуляции клеточного цикла | |
| MX2010006799A (es) | Benzofuropirimidinonas como inhibidores de la proteina cinasa. | |
| MX2013003019A (es) | Compuestos de azabenzotiazol, composiciones y metodos de uso. | |
| HRP20100195T1 (hr) | 1,4-dihidropiridinski kondenzirani heterocikli, postupak njihovog dobivanja, upotreba i pripravci koji ih sadrže | |
| CR20200286A (es) | DERIVADOS DE DIHIDRO-BENZO-OXAZINA Y DIHIDRO-PIRIDO-OXAZINA (Divisional 2014-0294) | |
| PH12015500063B1 (en) | Azaindole derivatives which act as pi3k inhibitors | |
| GEP20186878B (en) | 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders | |
| MX338551B (es) | Nuevos compuestos de piridina fusionada como inhibidores de caseina quinasa. | |
| RU2016122731A (ru) | Функционализированные и замещенные индолы в качестве противораковых агентов |