HRP20221518T1 - Diaril makrociklični spojevi kao modulatori protein kinaza - Google Patents
Diaril makrociklični spojevi kao modulatori protein kinaza Download PDFInfo
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- HRP20221518T1 HRP20221518T1 HRP20221518TT HRP20221518T HRP20221518T1 HR P20221518 T1 HRP20221518 T1 HR P20221518T1 HR P20221518T T HRP20221518T T HR P20221518TT HR P20221518 T HRP20221518 T HR P20221518T HR P20221518 T1 HRP20221518 T1 HR P20221518T1
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- Prior art keywords
- 4alkyl
- compound according
- pharmaceutically acceptable
- acceptable salt
- independently
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- -1 Diaryl macrocycles Chemical class 0.000 title claims 6
- 102000001253 Protein Kinase Human genes 0.000 title 1
- 108060006633 protein kinase Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 6
- 229910052805 deuterium Inorganic materials 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- 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
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/16—Anti-Parkinson drugs
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
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Claims (14)
1. Spoj odabran iz grupe koju čine
[image]
gdje
M je CH ili N;
X1 i X1' su neovisno -C(R1a)(R2a)-, -S-, -S(O)-, -S(O)2-, -O- ili -N(Rk')-;
svaki R1a i R2a je neovisno H, deuteriju, C1-6alkil, C3‑6cikloalkil, C6-10 aril, -C(O)ORa', ‑C(O)NRa'Rb', -NRa'Rb', -SRa', -S(O)Ra', -S(O)NRa', -S(O)2Ra', -S(O)2NRa' ili -ORa', pri čemu je svaki atom vodika u C1-6alkil grupi neovisno opcionalno supstituiran deuterijem , halogenom, ‑OH, -OC1-4alkil, -NH2, -NH(C1-4alkil), -N(C1-4alkil)2, -NHC(O)C1-4alkil, -N(C1-4alkil)C(O)C1-4alkil, ‑NHC(O)NHC1-4alkil, -N(C1-4alkil)C(O)NHC1-4alkil, -NHC(O)N(C1-4alkil)2, ‑N(C1‑4alkil)C(O)N(C1‑4alkil)2, -NHC(O)OC1-4alkil, -N(C1-4alkil)C(O)OC1-4alkil, -CO2H, -CO2C1-4alkil, ‑CONH2, -CONH(C1-4alkil), -CON(C1-4alkil)2, -SC1-4alkil, -S(O)C1-4alkil, -S(O)2C1-4alkil, ‑S(O)NH(C1‑4alkil), -S(O)2NH(C1-4alkil), -S(O)N(C1-4alkil)2, -S(O)2N(C1-4alkil)2, C3‑6cikloalkil ili 3- do 7-članom heterocikloalkil grupom;
svaki R3a i R3b je neovisno H, fluoro, kloro, bromo, metil, etil, propil, izopropil, metoksi, etoksi, izopropoksi, -CN ili -CF3;
R7a je H, C1-6alkil ili 3- do 7-člani heterocikloalkil, pri čemu je svaki atom vodika u C1-6alkil ili 3- do 7-članoj heterocikloalkilna grupa neovisno supstituirana halogenom, -OH, ‑OC1‑4alkil, -NH2, -NH(C1-4alkil), -N(C1-4alkil)2, -CO2H,-CO2C1-4alkil, -CONH2, -CONH(C1-4alkil), ‑CON(C1-4alkil)2, cikloalkil ili monocikličnom heterocikloalkilnom l grupom;
svaki Rk' je neovisno H, deuterij, C1-6alkil, C2‑6alkenil, C2‑6alkinil, C3‑6cikloalkil, 3- do 7-člani heterocikloalkil, C6-10aril ili mono- ili bicikličan heteroaril; pri čemu je svaki atom vodika u C1‑6alkil, C2‑6alkenil, C2‑6alkinil, C3‑6cikloalkil, 3- do 7-članoj heterocikloalkil, C6-10aril, ili mono- ili bicikličnoj heteroaril grupi u Rk' neovisno opcionalno zamijenjen deuterijem, halogenom, C1‑6alkil, C1-6haloalkil ili -ORa';
pri čemu je svaki Ra' i Rb' neovisnoH, deuterij , C1-6alkil, C2‑6alkenil, C2‑6alkinil, C3‑6cikloalkil, 3- do 7-člani heterocikloalkil, C6-10aril ili heteroaril; i
svaki Z1, Z2, Z3, Z4, Z5, Z6 ili Z7 je neovisno N, NH ili C(RX), gdje svaki RX, kada je prisutan, neovisno je H, deuterij , halogen, C1-4alkil, -O-C1-4alkil, -OH, -NH2, -NH(C1-4alkil), -NH(fenil), ‑NH(heteroaril), CN ili -CF3, pod uvjetom da je najmanje jedan od Z1, Z2, Z3, Z4, Z5, Z6 ili Z7 N ili NH; i
m' je 2 ili 3;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje Z1, Z4 i Z7 su N, a Z2, Z3, Z5 i Z6 su C(RX), pri čemu svaki RX, kada je prisutan, je H.
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje je M CH, Z1, Z4 i Z7 su N, a Z2, Z3, Z5 i Z6 su C(RX), pri čemu svaki RX, kada je prisutan, je H.
4. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje je M CH, Z1, Z4 i Z7 su N, a Z2, Z3, Z5 i Z6 su C(RX), pri čemu svaki RX, kada je prisutan, je H, a X1 je -N(Rk')-.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje je M CH, Z1, Z4 i Z7 su N i Z2, Z3, Z5 i Z6 su C(RX), pri čemu svaki RX, kada je prisutan, je H, X1 je -N(Rk')- i X1' je -O-.
6. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje je M CH, Z1, Z4 i Z7 su N, a Z2, Z3, Z5 i Z6 su C(RX), pri čemu svaki RX, kada je prisutan, je H, X1 je -C(R1a)(R2a)- i X1' je -O-.
7. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, gdje je Rk' izabran iz grupe koju čine H, metil, etil, propil, izo-propil, ciklopropil, 2-hidroksietil, 2-hidroksi-2-metil-propil i N-metil-pirol-3-il.
8. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, gdje je Rk' H ili metil.
9. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, gdje je R3b H.
10. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, gdje je R3a fluoro.
11. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, ili njegova farmaceutski prihvatljiva sol, formule
[image]
12. Spoj prema bilo kojem od prethodnih patentnih zahtjeva formule
[image]
13. Farmaceutski sastav koji sadrži (a) spoj prema bilo kojem od patentnih zahtjeva 1-12, i (b) najmanje jednu farmaceutski prihvatljivu pomoćnu tvar
14. Spoj prema bilo kojem od patentnih zahtjeva 1-12, za uporabu u liječenju raka , boli, neuroloških bolesti, autoimunih bolesti ili upala kod subjekta kojem je potrebno takvo liječenje.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461931506P | 2014-01-24 | 2014-01-24 | |
| US201462049326P | 2014-09-11 | 2014-09-11 | |
| US201562106301P | 2015-01-22 | 2015-01-22 | |
| EP19169041.1A EP3572416B1 (en) | 2014-01-24 | 2015-01-23 | Diaryl macrocycles as modulators of protein kinases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20221518T1 true HRP20221518T1 (hr) | 2023-02-17 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20221518TT HRP20221518T1 (hr) | 2014-01-24 | 2015-01-23 | Diaril makrociklični spojevi kao modulatori protein kinaza |
| HRP20240503TT HRP20240503T1 (hr) | 2014-01-24 | 2015-01-23 | Diaril makrocikli kao modulatori protein kinaza |
| HRP20191283TT HRP20191283T1 (hr) | 2014-01-24 | 2019-07-16 | Diaril makrocikli kao modulatori protein kinaze |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20240503TT HRP20240503T1 (hr) | 2014-01-24 | 2015-01-23 | Diaril makrocikli kao modulatori protein kinaza |
| HRP20191283TT HRP20191283T1 (hr) | 2014-01-24 | 2019-07-16 | Diaril makrocikli kao modulatori protein kinaze |
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| Country | Link |
|---|---|
| US (6) | US9714258B2 (hr) |
| EP (6) | EP3097107B1 (hr) |
| JP (5) | JP6490713B2 (hr) |
| KR (1) | KR102402179B1 (hr) |
| CN (3) | CN106170289B (hr) |
| AP (1) | AP2016009383A0 (hr) |
| AU (2) | AU2015209239B2 (hr) |
| CA (1) | CA2936079C (hr) |
| CL (1) | CL2016001876A1 (hr) |
| CY (1) | CY1121850T1 (hr) |
| DK (3) | DK3572416T3 (hr) |
| EA (2) | EA201892241A1 (hr) |
| ES (3) | ES2933350T3 (hr) |
| FI (1) | FI3636649T3 (hr) |
| HK (1) | HK1231407A1 (hr) |
| HR (3) | HRP20221518T1 (hr) |
| HU (3) | HUE066590T2 (hr) |
| IL (2) | IL246860B (hr) |
| LT (3) | LT3097107T (hr) |
| MX (2) | MX2016009588A (hr) |
| MY (1) | MY193524A (hr) |
| NZ (2) | NZ761094A (hr) |
| PE (1) | PE20160931A1 (hr) |
| PH (1) | PH12016501463A1 (hr) |
| PL (3) | PL3097107T3 (hr) |
| PT (3) | PT3636649T (hr) |
| RS (3) | RS65417B1 (hr) |
| SG (2) | SG11201605929RA (hr) |
| SI (3) | SI3097107T1 (hr) |
| UA (1) | UA121206C2 (hr) |
| WO (1) | WO2015112806A2 (hr) |
| ZA (2) | ZA201604654B (hr) |
Families Citing this family (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2350075T3 (pl) | 2008-09-22 | 2014-07-31 | Array Biopharma Inc | Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk |
| BRPI0919873B8 (pt) | 2008-10-22 | 2021-05-25 | Array Biopharma Inc | compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| LT3205654T (lt) | 2010-05-20 | 2019-05-27 | Array Biopharma, Inc. | Makrocikliniai junginiai kaip trk kinazės slopikliai |
| HRP20221518T1 (hr) | 2014-01-24 | 2023-02-17 | Turning Point Therapeutics, Inc. | Diaril makrociklični spojevi kao modulatori protein kinaza |
| PL3699181T3 (pl) | 2014-11-16 | 2023-05-22 | Array Biopharma, Inc. | Postać krystaliczna wodorosiarczanu (s)-n-(5-((r)-2-(2,5-difluorofenylo) - pirolidyn-1-ylo)-pirazolo[1,5-a]pirimidyn-3-ylo)-3-hydroksypirolidyno-1-karboksyamidu |
| US10758525B2 (en) | 2015-01-22 | 2020-09-01 | MyoKardia, Inc. | 4-methylsulfonyl-substituted piperidine urea compounds |
| EP3303631A1 (en) | 2015-06-01 | 2018-04-11 | Loxo Oncology Inc. | Methods of diagnosing and treating cancer |
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| EP3555137A1 (en) | 2016-12-14 | 2019-10-23 | Development Center for Biotechnology | Antibody-drug conjugates and uses thereof |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| PT3658148T (pt) | 2017-07-28 | 2024-08-26 | Turning Point Therapeutics Inc | Compostos macrocíclicos e utilizações dos mesmos |
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