FI3365334T3 - Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä - Google Patents
Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä Download PDFInfo
- Publication number
- FI3365334T3 FI3365334T3 FIEP16788794.2T FI16788794T FI3365334T3 FI 3365334 T3 FI3365334 T3 FI 3365334T3 FI 16788794 T FI16788794 T FI 16788794T FI 3365334 T3 FI3365334 T3 FI 3365334T3
- Authority
- FI
- Finland
- Prior art keywords
- yyl
- chloro
- dihydro
- oxo
- isoindol
- Prior art date
Links
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 239000003909 protein kinase inhibitor Substances 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 167
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 144
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 103
- PMDCZENCAXMSOU-UHFFFAOYSA-N N-ethylacetamide Chemical compound CCNC(C)=O PMDCZENCAXMSOU-UHFFFAOYSA-N 0.000 claims 55
- -1 4-chloro-2-methoxyphenyl Chemical group 0.000 claims 39
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 38
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 23
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 208000032839 leukemia Diseases 0.000 claims 7
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 5
- 125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 claims 5
- UNFGQCCHVMMMRF-UHFFFAOYSA-N 2-phenylbutanamide Chemical compound CCC(C(N)=O)C1=CC=CC=C1 UNFGQCCHVMMMRF-UHFFFAOYSA-N 0.000 claims 3
- CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 3
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000006311 cyclobutyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical group C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- DXASQZJWWGZNSF-UHFFFAOYSA-N n,n-dimethylmethanamine;sulfur trioxide Chemical group CN(C)C.O=S(=O)=O DXASQZJWWGZNSF-UHFFFAOYSA-N 0.000 claims 2
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 2
- SZAWXSXWNOZRNJ-MRVPVSSYSA-N (3R)-3-(3-methoxyphenyl)butanamide Chemical compound COC=1C=C(C=CC=1)[C@H](C)CC(=O)N SZAWXSXWNOZRNJ-MRVPVSSYSA-N 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- JJQXZWAHTLVGHM-UHFFFAOYSA-N 2-cyclobutylacetamide Chemical compound NC(=O)CC1CCC1 JJQXZWAHTLVGHM-UHFFFAOYSA-N 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- IWTFOFMTUOBLHG-UHFFFAOYSA-N 2-methoxypyridine Chemical compound COC1=CC=CC=N1 IWTFOFMTUOBLHG-UHFFFAOYSA-N 0.000 claims 1
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- KRNSYSYRLQDHDK-UHFFFAOYSA-N 6,7-dihydro-5h-cyclopenta[b]pyridine Chemical compound C1=CN=C2CCCC2=C1 KRNSYSYRLQDHDK-UHFFFAOYSA-N 0.000 claims 1
- ZDCVFJZMIWNGFL-SECBINFHSA-N COC1=CC=CC(=C1)[C@H](CC(=O)N)CO Chemical compound COC1=CC=CC(=C1)[C@H](CC(=O)N)CO ZDCVFJZMIWNGFL-SECBINFHSA-N 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 102000019149 MAP kinase activity proteins Human genes 0.000 claims 1
- 108040008097 MAP kinase activity proteins Proteins 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 206010060880 Monoclonal gammopathy Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- OHLUUHNLEMFGTQ-UHFFFAOYSA-N N-methylacetamide Chemical compound CNC(C)=O OHLUUHNLEMFGTQ-UHFFFAOYSA-N 0.000 claims 1
- UQFQONCQIQEYPJ-UHFFFAOYSA-N N-methylpyrazole Chemical compound CN1C=CC=N1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 1
- 208000000389 T-cell leukemia Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 235000010290 biphenyl Nutrition 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- CJJZCWJJAZMVCJ-UHFFFAOYSA-N n-benzyl-2,5-dimethylaniline Chemical compound CC1=CC=C(C)C(NCC=2C=CC=CC=2)=C1 CJJZCWJJAZMVCJ-UHFFFAOYSA-N 0.000 claims 1
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 claims 1
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 claims 1
- 208000037244 polycythemia vera Diseases 0.000 claims 1
- 235000019260 propionic acid Nutrition 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 1
- UWYZHKAOTLEWKK-UHFFFAOYSA-N tetrahydro-isoquinoline Natural products C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
Classifications
-
- 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
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/535—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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D497/08—Bridged systems
-
- 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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
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)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1518676.0A GB201518676D0 (en) | 2015-10-21 | 2015-10-21 | Benzolactam compounds |
| GBGB1611351.6A GB201611351D0 (en) | 2016-06-30 | 2016-06-30 | Benzolactam compounds |
| PCT/IB2016/001507 WO2017068412A1 (en) | 2015-10-21 | 2016-10-20 | Benzolactam compounds as protein kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI3365334T3 true FI3365334T3 (fi) | 2024-09-19 |
Family
ID=57218943
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP16788794.2T FI3365334T3 (fi) | 2015-10-21 | 2016-10-20 | Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US10457669B2 (enExample) |
| EP (1) | EP3365334B1 (enExample) |
| JP (2) | JP6931646B2 (enExample) |
| KR (1) | KR102769567B1 (enExample) |
| CN (2) | CN108617166B (enExample) |
| AU (2) | AU2016341520C1 (enExample) |
| CA (1) | CA3001799A1 (enExample) |
| DK (1) | DK3365334T3 (enExample) |
| ES (1) | ES2989326T3 (enExample) |
| FI (1) | FI3365334T3 (enExample) |
| HR (1) | HRP20241210T1 (enExample) |
| HU (1) | HUE068392T2 (enExample) |
| IL (2) | IL291017B2 (enExample) |
| LT (1) | LT3365334T (enExample) |
| MA (1) | MA47013A (enExample) |
| MX (1) | MX382927B (enExample) |
| MY (1) | MY204050A (enExample) |
| PH (1) | PH12018500792A1 (enExample) |
| PL (1) | PL3365334T3 (enExample) |
| PT (1) | PT3365334T (enExample) |
| SA (1) | SA518391342B1 (enExample) |
| SG (1) | SG10201912959QA (enExample) |
| SI (1) | SI3365334T1 (enExample) |
| TW (1) | TWI747846B (enExample) |
| WO (1) | WO2017068412A1 (enExample) |
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| US10246424B2 (en) | 2015-04-10 | 2019-04-02 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| MX2017013275A (es) | 2015-04-15 | 2018-01-26 | Araxes Pharma Llc | Inhibidores triciclicos fusionados de kras y metodos de uso de los mismos. |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | 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 |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10875842B2 (en) | 2015-09-28 | 2020-12-29 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| GB201517216D0 (en) | 2015-09-29 | 2015-11-11 | Cancer Res Technology Ltd And Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201517217D0 (en) | 2015-09-29 | 2015-11-11 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
| DK3365334T3 (da) | 2015-10-21 | 2024-09-23 | Otsuka Pharma Co Ltd | Benzolactamforbindelser som proteinkinaseinhibitorer |
| CN108779097A (zh) | 2015-11-16 | 2018-11-09 | 亚瑞克西斯制药公司 | 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| CN108602802B (zh) * | 2016-07-26 | 2020-01-21 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| CA3041033A1 (en) | 2016-09-12 | 2018-03-15 | Numerate, Inc. | Monocyclic compounds useful as gpr120 modulators |
| US10865201B2 (en) * | 2016-09-12 | 2020-12-15 | Valo Health, Inc. | Bicyclic compounds useful as GPR120 modulators |
| US10280172B2 (en) | 2016-09-29 | 2019-05-07 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| CN110312711A (zh) * | 2016-10-07 | 2019-10-08 | 亚瑞克西斯制药公司 | 作为ras抑制剂的杂环化合物及其使用方法 |
| CN106588884B (zh) * | 2016-11-10 | 2019-04-09 | 浙江大学 | 2-多取代芳环-嘧啶类衍生物及制备和医药用途 |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)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 |
| 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 |
| 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 |
| GB201704966D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201704965D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201706327D0 (en) * | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| CN110831933A (zh) | 2017-05-25 | 2020-02-21 | 亚瑞克西斯制药公司 | 喹唑啉衍生物作为突变kras、hras或nras的调节剂 |
| US10736897B2 (en) | 2017-05-25 | 2020-08-11 | Araxes Pharma Llc | Compounds and methods of use thereof for treatment of cancer |
| CA3063440A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Covalent inhibitors of kras |
| IL273428B2 (en) | 2017-09-22 | 2023-09-01 | Jubilant Epipad LLC | Heterocyclic compounds as pad inhibitors |
| EP3697785B1 (en) | 2017-10-18 | 2022-12-28 | Jubilant Epipad LLC | Imidazo-pyridine compounds as pad inhibitors |
| JP7279057B6 (ja) | 2017-11-06 | 2024-02-15 | ジュビラント プローデル エルエルシー | Pd1/pd-l1活性化の阻害剤としてのピリミジン誘導体 |
| SG11202004537UA (en) | 2017-11-24 | 2020-06-29 | Jubilant Episcribe Llc | Heterocyclic compounds as prmt5 inhibitors |
| US11384065B2 (en) | 2018-01-03 | 2022-07-12 | Medshine Discovery Inc. | Heterocyclic compound as CSF-1R inhibitor and use thereof |
| US11529341B2 (en) | 2018-03-13 | 2022-12-20 | Jubilant Prodel LLC | Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation |
| JP7487110B2 (ja) * | 2018-04-05 | 2024-05-20 | フュージョン ファーマシューティカルズ インコーポレイテッド | Hsp90標的化コンジュゲート及びその製剤 |
| WO2019223632A1 (en) * | 2018-05-22 | 2019-11-28 | Js Innomed Holdings Ltd. | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| TWI707683B (zh) | 2018-06-13 | 2020-10-21 | 美商輝瑞股份有限公司 | Glp-1受體促效劑及其用途 |
| MX2021000887A (es) | 2018-08-01 | 2021-03-31 | Araxes Pharma Llc | Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer. |
| CN109377846B (zh) * | 2018-10-11 | 2020-12-08 | 内蒙古科技大学包头医学院 | 人体解剖学内脏标本的制作方法 |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| IL283901B2 (en) | 2018-12-18 | 2025-03-01 | Astrazeneca Ab | Process and intermediates for the preparation of 4-{4-[(3R)-3-methylmorpholin-4-yl]-6-[1-((R)-S-methylsulfonimidoyl)cyclopropyl]pyrimidin-2-yl}-1H-pyrrolo[2,3-b]pyridine |
| CN111057048B (zh) * | 2019-01-30 | 2022-03-18 | 上海凌达生物医药有限公司 | 一类氨基吡嗪/吡啶类化合物、制备方法和用途 |
| JP7426398B2 (ja) * | 2019-02-26 | 2024-02-01 | 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 | Ras阻害剤としての新規イソインドリノン置換インドールおよび誘導体 |
| TWI870398B (zh) * | 2019-04-03 | 2025-01-21 | 美商Tva(Abc)公司 | Hsp90靶定性共軛體類及其調製劑 |
| US20220204512A1 (en) * | 2019-05-24 | 2022-06-30 | Jiangsu Hengrui Medicine Co., Ltd. | Substituted fused bicyclic derivative, preparation method therefor, and application thereof in medicines |
| MX2021012756A (es) * | 2019-05-31 | 2022-04-18 | Haisco Pharmaceuticals Pte Ltd | Derivado de un anillo inhibidor de btk, metodo de preparacion de este y aplicacion farmaceutica para este. |
| CN114206852A (zh) | 2019-08-09 | 2022-03-18 | 卡尔维斯塔制药有限公司 | 血浆激肽释放酶抑制剂 |
| EP4031542B1 (en) | 2019-09-18 | 2025-10-15 | Merck Sharp & Dohme LLC | Small molecule inhibitors of kras g12c mutant |
| CN112574207B (zh) * | 2019-09-30 | 2023-04-11 | 南京药石科技股份有限公司 | Erk1/2蛋白激酶抑制剂及其用途 |
| MX2022003933A (es) | 2019-10-02 | 2022-04-25 | Domain Therapeutics | Antagonistas del receptor ep4 de prostaglandina e2 (pge2). |
| GEAP202415960A (en) | 2019-10-28 | 2024-08-12 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12c mutant |
| JP2023515235A (ja) | 2019-10-31 | 2023-04-12 | 大鵬薬品工業株式会社 | 4-アミノブタ-2-エンアミド誘導体及びその塩 |
| WO2021106231A1 (en) | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| AU2020398022B2 (en) * | 2019-12-06 | 2023-04-27 | D3 Bio (Wuxi) Co., Ltd. | Thiazololactam compound as ERK inhibitor and use thereof |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| WO2021215545A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c |
| JP7296017B2 (ja) * | 2020-04-30 | 2023-06-21 | メッドシャイン ディスカバリー インコーポレイテッド | ベンゾスルタムを含む化合物 |
| WO2021224818A1 (en) * | 2020-05-08 | 2021-11-11 | Pfizer Inc. | Isoindolone compounds as hpk1 inhibitors |
| AU2021326929A1 (en) * | 2020-08-21 | 2023-04-27 | Shanghai Ringene Biopharma Co., Ltd. | Aromatic ring-lactam compound, preparation method therefor and use thereof |
| EP4249481A4 (en) * | 2020-11-20 | 2024-10-30 | Hefei Institutes of Physical Science, Chinese Academy of Sciences | DIHYDROISOQUINOLINONE AND ISOINDOLINONE DERIVATIVES AND USES THEREOF |
| US20240317759A1 (en) | 2021-05-28 | 2024-09-26 | Taiho Pharmaceutical Co., Ltd. | Small molecule inhibitors of kras mutated proteins |
| WO2022253186A1 (zh) * | 2021-06-02 | 2022-12-08 | 南京明德新药研发有限公司 | 一种二甲基取代的噻唑并吡咯酮类化合物的晶型及其制备方法 |
| KR20240021198A (ko) | 2021-06-11 | 2024-02-16 | 오츠카 세이야쿠 가부시키가이샤 | Erk 억제제의 제조 방법 |
| WO2023039548A1 (en) * | 2021-09-10 | 2023-03-16 | Fred Hutchinson Cancer Center | Kinase inhibitors for the treatment of prostate cancer |
| CA3235680A1 (en) | 2021-10-26 | 2023-05-04 | Aaron Goodwin | Compositions comprising an erk inhibitor |
| KR20250087545A (ko) | 2022-09-13 | 2025-06-16 | 암피스타 테라퓨틱스 엘티디 | 표적 단백질 분해를 위한 화합물 |
| JP2025534418A (ja) * | 2022-09-29 | 2025-10-15 | 蘇州愛科百発生物医薬技術有限公司 | 含窒素縮合複素環化合物、その調製方法、および医薬におけるその使用 |
| CN119790049A (zh) * | 2022-09-30 | 2025-04-08 | 楚浦创制(武汉)医药科技有限公司 | 2-氨基嘧啶类化合物及其应用、药用组合物 |
| WO2024220866A1 (en) * | 2023-04-19 | 2024-10-24 | Accutar Biotechnology Inc. | Novel aminopyrimidine derivatives as cyclin-dependent kinase inhibitors |
| US12466840B2 (en) | 2023-10-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS proteins |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5629327A (en) | 1993-03-01 | 1997-05-13 | Childrens Hospital Medical Center Corp. | Methods and compositions for inhibition of angiogenesis |
| US5463063A (en) | 1993-07-02 | 1995-10-31 | Celgene Corporation | Ring closure of N-phthaloylglutamines |
| US5958934A (en) | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
| CA2333927A1 (en) | 1998-04-01 | 1999-10-07 | Dupont Pharmaceuticals Company | Pyrimidines and triazines as integrin antagonists |
| EP1397142A4 (en) | 2001-06-19 | 2004-11-03 | Bristol Myers Squibb Co | PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7 |
| ES2290743T3 (es) | 2003-04-30 | 2008-02-16 | The Institutes For Pharmaceutical Discovery, Llc | Heteroarilos sustituidos como inhibidores de las proteina-tirosina fosfatasas. |
| US7504401B2 (en) | 2003-08-29 | 2009-03-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| AU2004268621C1 (en) | 2003-08-29 | 2011-08-18 | Exelixis, Inc. | c-Kit modulators and methods of use |
| TW200607803A (en) | 2004-05-14 | 2006-03-01 | Vertex Pharma | Pyrrole inhibitors of erk protein kinase, synthesis thereof and intermediates thereto |
| WO2006113769A1 (en) | 2005-04-15 | 2006-10-26 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| RS51981B (sr) | 2005-12-13 | 2012-02-29 | Schering Corporation | Policiklični derivati indazola koji su inhibitori erk |
| US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| JP2009542604A (ja) | 2006-07-06 | 2009-12-03 | 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 | 4−ヘテロシクロアルキルピリミジン、それらの調製方法及び医薬としての使用 |
| WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
| WO2008124085A2 (en) | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
| WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| US20090082368A1 (en) | 2007-09-24 | 2009-03-26 | Painceptor Pharma Corporation | Methods of modulating neurotrophin-mediated activity |
| EP2573080A1 (en) * | 2007-09-27 | 2013-03-27 | The United States of America, as Represented by the Secretary, Department of Health and Human Services | Isoindoline compounds for the treatment of spinal muscular atrophy and other uses |
| ES2388475T3 (es) | 2008-01-24 | 2012-10-15 | Merck Patent Gmbh | Derivados de beta-aminoácidos para el tratamiento de la diabetes |
| KR20110025224A (ko) | 2008-06-27 | 2011-03-09 | 아빌라 테라퓨틱스, 인크. | 헤테로아릴 화합물 및 이의 용도 |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| GB0815369D0 (en) | 2008-08-22 | 2008-10-01 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶,其組合物及使用其之治療方法 |
| GB0821307D0 (en) | 2008-11-21 | 2008-12-31 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| AU2009335821A1 (en) | 2008-12-19 | 2010-07-15 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| JP5713999B2 (ja) | 2009-05-15 | 2015-05-07 | コリア リサーチ インスティテュート オブ ケミカル テクノロジー | アミド化合物、その製造方法及びそれを含む薬学組成物 |
| WO2010151747A1 (en) | 2009-06-26 | 2010-12-29 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimine compounds and methods of making and using same |
| WO2011008931A2 (en) | 2009-07-15 | 2011-01-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders |
| NZ600954A (en) | 2009-12-22 | 2013-11-29 | Isoindolinone inhibitors of phosphatidylinositol 3-kinase | |
| AU2010336027A1 (en) * | 2009-12-23 | 2012-07-19 | Auckland Uniservices Limited | Compounds, preparations and uses thereof |
| RU2012132682A (ru) * | 2009-12-31 | 2014-02-10 | Пирамал Энтерпрайзис Лимитед | Ингибиторы диацилглицерин ацилтрансферазы |
| US9200008B2 (en) | 2010-07-02 | 2015-12-01 | Aska Pharmaceutical Co., Ltd. | Heterocyclic compound and p27Kip1 degradation inhibitor |
| MX338707B (es) | 2010-07-29 | 2016-04-28 | Rigel Pharmaceuticals Inc | Compuestos heterociclicos activadores de proteina cinasa activada por 5'-amp (ampk) y metodos para emplearlos. |
| US9938269B2 (en) | 2011-06-30 | 2018-04-10 | Abbvie Inc. | Inhibitor compounds of phosphodiesterase type 10A |
| PT3321262T (pt) | 2012-03-01 | 2021-03-04 | Array Biopharma Inc | Inibidores de serina/treonina quinases |
| SG10201704095UA (en) * | 2012-04-24 | 2017-06-29 | Vertex Pharma | Dna-pk inhibitors |
| WO2014040555A1 (zh) | 2012-09-12 | 2014-03-20 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物 |
| US20150272939A1 (en) | 2012-10-02 | 2015-10-01 | Yale University | Identification of Small Molecule Inhibitors of Jumonji AT-Rich Interactive Domain 1A (JARID1A) and 1B (JARID1B) Histone Demethylase |
| PT2914296T (pt) | 2012-11-01 | 2018-10-30 | Infinity Pharmaceuticals Inc | Tratamento de cancros utilizando moduladores de isoformas de pi3-quinase |
| SG11201505850WA (en) | 2013-02-08 | 2015-08-28 | Celgene Avilomics Res Inc | Erk inhibitors and uses thereof |
| WO2014130856A2 (en) | 2013-02-21 | 2014-08-28 | Wayne Rothbaum | Treatment of skeletal-related disorders |
| WO2015030847A1 (en) | 2013-08-30 | 2015-03-05 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| US20150087673A1 (en) | 2013-09-26 | 2015-03-26 | Rigel Pharmaceuticals, Inc. | Methods for using and biomarkers for ampk-activating compounds |
| MY182908A (en) * | 2014-01-14 | 2021-02-05 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| SI3126352T1 (sl) | 2014-04-04 | 2019-03-29 | Syros Pharmaceuticals, Inc. | Zaviralci ciklinsko odvisne kinaze 7 (CDK7) |
| WO2015157556A1 (en) | 2014-04-09 | 2015-10-15 | Kadmon Corporation, Llc | Treatment of gvhd |
| WO2016025649A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a dot1l inhibitor and related methods |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Erk抑制劑 |
| WO2016162325A1 (en) | 2015-04-07 | 2016-10-13 | Astrazeneca Ab | Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors |
| CN113200961B (zh) | 2015-06-15 | 2023-12-22 | 阿沙纳生物科学公司 | Erk1与erk2的杂环抑制剂及其在癌症治疗中的应用 |
| WO2017004383A1 (en) * | 2015-06-30 | 2017-01-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| DK3365334T3 (da) | 2015-10-21 | 2024-09-23 | Otsuka Pharma Co Ltd | Benzolactamforbindelser som proteinkinaseinhibitorer |
| EA038028B1 (ru) | 2015-11-09 | 2021-06-24 | Астразенека Аб | Производные дигидроимидазопиразинона, применимые в лечении рака |
| CN108602802B (zh) | 2016-07-26 | 2020-01-21 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| GB201706327D0 (en) * | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| KR20240021198A (ko) * | 2021-06-11 | 2024-02-16 | 오츠카 세이야쿠 가부시키가이샤 | Erk 억제제의 제조 방법 |
| CA3235680A1 (en) * | 2021-10-26 | 2023-05-04 | Aaron Goodwin | Compositions comprising an erk inhibitor |
-
2016
- 2016-10-20 DK DK16788794.2T patent/DK3365334T3/da active
- 2016-10-20 MA MA047013A patent/MA47013A/fr unknown
- 2016-10-20 AU AU2016341520A patent/AU2016341520C1/en active Active
- 2016-10-20 CN CN201680061146.4A patent/CN108617166B/zh active Active
- 2016-10-20 CN CN202210512050.2A patent/CN114948963B/zh active Active
- 2016-10-20 SI SI201631846T patent/SI3365334T1/sl unknown
- 2016-10-20 KR KR1020187013571A patent/KR102769567B1/ko active Active
- 2016-10-20 HR HRP20241210TT patent/HRP20241210T1/hr unknown
- 2016-10-20 CA CA3001799A patent/CA3001799A1/en active Pending
- 2016-10-20 IL IL291017A patent/IL291017B2/en unknown
- 2016-10-20 US US15/767,775 patent/US10457669B2/en active Active
- 2016-10-20 WO PCT/IB2016/001507 patent/WO2017068412A1/en not_active Ceased
- 2016-10-20 PT PT167887942T patent/PT3365334T/pt unknown
- 2016-10-20 JP JP2018519702A patent/JP6931646B2/ja active Active
- 2016-10-20 MY MYPI2018701450A patent/MY204050A/en unknown
- 2016-10-20 FI FIEP16788794.2T patent/FI3365334T3/fi active
- 2016-10-20 SG SG10201912959QA patent/SG10201912959QA/en unknown
- 2016-10-20 EP EP16788794.2A patent/EP3365334B1/en active Active
- 2016-10-20 ES ES16788794T patent/ES2989326T3/es active Active
- 2016-10-20 PL PL16788794.2T patent/PL3365334T3/pl unknown
- 2016-10-20 HU HUE16788794A patent/HUE068392T2/hu unknown
- 2016-10-20 MX MX2018004643A patent/MX382927B/es unknown
- 2016-10-20 TW TW105133824A patent/TWI747846B/zh active
- 2016-10-20 LT LTEPPCT/IB2016/001507T patent/LT3365334T/lt unknown
-
2018
- 2018-04-12 IL IL258662A patent/IL258662B/en unknown
- 2018-04-12 PH PH12018500792A patent/PH12018500792A1/en unknown
- 2018-04-12 SA SA518391342A patent/SA518391342B1/ar unknown
-
2019
- 2019-08-15 US US16/541,863 patent/US11001575B1/en active Active
-
2021
- 2021-02-12 AU AU2021200951A patent/AU2021200951B2/en active Active
- 2021-04-07 US US17/224,733 patent/US11939321B2/en active Active
- 2021-08-13 JP JP2021132047A patent/JP7254127B2/ja active Active
-
2023
- 2023-10-19 US US18/490,403 patent/US20240368136A1/en active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| FI3365334T3 (fi) | Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä | |
| US12115163B2 (en) | Combination therapy comprising a MAT2A inhibitor and a type II PRMT inhibitor | |
| IL273924B1 (en) | Muscarinic acetylcholine M4 receptor antagonists | |
| JP2013508404A5 (enExample) | ||
| RU2012137489A (ru) | Производные 2,3-дигидро-1н-инден-1-ил-2,7-диазаспиро[3.5]нонана и их применение в качестве антагонистов или обратных агонистов грелинового рецептора | |
| RU2017134901A (ru) | Соединения 1-циано-пирролидинов в качестве ингибиторов USP30 | |
| JP2016500671A5 (enExample) | ||
| RU2019120986A (ru) | Фармацевтическая комбинация, содержащая ингибитор alk и ингибитор shp2 | |
| RU2015152576A (ru) | Производные индолин-2-она или пирролопиридин/пиримидин-2-она | |
| JP2018118992A5 (enExample) | ||
| HRP20120105T1 (hr) | Aminoheterociklički spojevi | |
| AU2011338389A1 (en) | Bicyclic compounds as Pim inhibitors | |
| RU2011136825A (ru) | Производные аминопиразина и лекарственные средства | |
| RU2014102962A (ru) | Новые соединения-ингибиторы фосфодиэстеразы типа 10а | |
| HRP20160635T1 (hr) | Inhibitori pirimidina pde10 | |
| RU2014131707A (ru) | Соединения пиридазинамида и их применение в качестве ингибиторов тирозинкиназы селезенки (syk) | |
| JP2013520407A5 (enExample) | ||
| HRP20180384T1 (hr) | Derivati 2,3-dihidro-benzo[1,4]oksazina i odgovarajući spojevi kao inhibitori kinaze fosfoinozitida-3 (pi3k) za liječenje primjerice reumatoidnog artritisa | |
| CA2816594A1 (en) | Nampt and rock inhibitors | |
| CA2873060A1 (en) | Nampt inhibitors | |
| RU2017121278A (ru) | Триазоло-пиразинильные производные, применимые в качестве растворимых активаторов гуанилатциклазы | |
| HRP20201469T1 (hr) | Derivati tetrahidroizokinolina | |
| JP2021504380A5 (enExample) | ||
| IL306126A (en) | Heterocyclic compounds | |
| ES2488219T3 (es) | Pirrolopiridinas como inhibidores de quinasas |