AR086367A1 - Compuestos de pirrolidinil urea y pirrolidinil tiourea como inhibidores de cinasa trka - Google Patents
Compuestos de pirrolidinil urea y pirrolidinil tiourea como inhibidores de cinasa trkaInfo
- Publication number
- AR086367A1 AR086367A1 ARP120101675A ARP120101675A AR086367A1 AR 086367 A1 AR086367 A1 AR 086367A1 AR P120101675 A ARP120101675 A AR P120101675A AR P120101675 A ARP120101675 A AR P120101675A AR 086367 A1 AR086367 A1 AR 086367A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- independently selected
- optionally substituted
- halogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 50
- 229910052736 halogen Inorganic materials 0.000 abstract 20
- 150000002367 halogens Chemical group 0.000 abstract 20
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 15
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 14
- 125000004950 trifluoroalkyl group Chemical group 0.000 abstract 13
- 125000005842 heteroatom Chemical group 0.000 abstract 12
- 229910052760 oxygen Inorganic materials 0.000 abstract 11
- 229910052717 sulfur Inorganic materials 0.000 abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 6
- -1 OH Chemical group 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 6
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 3
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000006339 pentafluoro alkyl group Chemical group 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 2
- 101150111783 NTRK1 gene Proteins 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 abstract 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000006336 tetrafluoro alkyl group Chemical group 0.000 abstract 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 2
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 abstract 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 1
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000005157 alkyl carboxy group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- 125000005121 aminocarbonylalkoxy group Chemical group 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000005159 cyanoalkoxy group Chemical group 0.000 abstract 1
- 125000004990 dihydroxyalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000006413 ring segment Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
-
- 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
- A61K31/4155—1,2-Diazoles non 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
- A61K31/41—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
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles 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
- A61K31/41—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
- A61K31/4245—Oxadiazoles
-
- 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
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles 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
- A61K31/41—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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K31/495—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
-
- A—HUMAN NECESSITIES
- 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]
-
- A—HUMAN NECESSITIES
- 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]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrrole Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161485858P | 2011-05-13 | 2011-05-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086367A1 true AR086367A1 (es) | 2013-12-11 |
Family
ID=46614580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101675A AR086367A1 (es) | 2011-05-13 | 2012-05-11 | Compuestos de pirrolidinil urea y pirrolidinil tiourea como inhibidores de cinasa trka |
Country Status (35)
| Country | Link |
|---|---|
| US (4) | US9562055B2 (OSRAM) |
| EP (1) | EP2712358B1 (OSRAM) |
| JP (4) | JP5933902B2 (OSRAM) |
| KR (2) | KR101960555B1 (OSRAM) |
| CN (3) | CN105130967B (OSRAM) |
| AR (1) | AR086367A1 (OSRAM) |
| AU (2) | AU2012256237B2 (OSRAM) |
| BR (1) | BR112013029201B1 (OSRAM) |
| CA (1) | CA2835835C (OSRAM) |
| CL (1) | CL2013003257A1 (OSRAM) |
| CO (1) | CO6821961A2 (OSRAM) |
| CR (1) | CR20130646A (OSRAM) |
| CY (1) | CY1119014T1 (OSRAM) |
| DK (1) | DK2712358T3 (OSRAM) |
| ES (1) | ES2615738T3 (OSRAM) |
| HR (1) | HRP20161786T1 (OSRAM) |
| HU (1) | HUE030791T2 (OSRAM) |
| IL (2) | IL229377A (OSRAM) |
| LT (1) | LT2712358T (OSRAM) |
| ME (1) | ME02583B (OSRAM) |
| MX (2) | MX369142B (OSRAM) |
| MY (1) | MY173181A (OSRAM) |
| NZ (1) | NZ618795A (OSRAM) |
| PH (1) | PH12013502319A1 (OSRAM) |
| PL (1) | PL2712358T3 (OSRAM) |
| PT (1) | PT2712358T (OSRAM) |
| RS (1) | RS55582B1 (OSRAM) |
| RU (1) | RU2606131C2 (OSRAM) |
| SG (2) | SG194902A1 (OSRAM) |
| SI (1) | SI2712358T1 (OSRAM) |
| SM (2) | SMT201700035T1 (OSRAM) |
| TW (2) | TWI649315B (OSRAM) |
| UA (1) | UA114711C2 (OSRAM) |
| UY (1) | UY34067A (OSRAM) |
| WO (1) | WO2012158413A2 (OSRAM) |
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2116539A1 (en) | 2008-04-25 | 2009-11-11 | Laboratorios Del. Dr. Esteve, S.A. | 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof |
| EP2350075B1 (en) | 2008-09-22 | 2014-03-05 | Array Biopharma, Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| KR101853026B1 (ko) | 2008-10-22 | 2018-04-27 | 어레이 바이오파마 인크. | TRK 키나아제 억제제로서 치환된 피라졸로[1,5a] 피리미딘 화합물 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| EP2353591A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof |
| EP2353598A1 (en) | 2010-02-04 | 2011-08-10 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for use in the prevention and/or treatment of postoperative pain |
| CN105693720B (zh) | 2010-05-20 | 2019-01-18 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| EP2388005A1 (en) | 2010-05-21 | 2011-11-23 | Laboratorios Del. Dr. Esteve, S.A. | Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy |
| EP2415471A1 (en) | 2010-08-03 | 2012-02-08 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in opioid-induced hyperalgesia |
| CN105130967B (zh) | 2011-05-13 | 2018-04-17 | 阵列生物制药公司 | 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物 |
| EP2524694A1 (en) | 2011-05-19 | 2012-11-21 | Laboratorios Del. Dr. Esteve, S.A. | Use of sigma ligands in diabetes type-2 associated pain |
| WO2014078372A1 (en) * | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| MX365733B (es) * | 2012-11-13 | 2019-06-12 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| WO2014078378A1 (en) * | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078328A1 (en) * | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| US9969694B2 (en) | 2012-11-13 | 2018-05-15 | Array Biopharma Inc. | N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| US9790210B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| TWI498325B (zh) * | 2013-01-18 | 2015-09-01 | Hoffmann La Roche | 3-取代吡唑及其用途 |
| EP2818166A1 (en) * | 2013-06-26 | 2014-12-31 | Laboratorios del Dr. Esteve S.A. | Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS) |
| WO2015039334A1 (en) * | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| WO2015039333A1 (en) * | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| BR112016011755B1 (pt) | 2013-11-28 | 2023-05-02 | Kyorin Pharmaceutical Co., Ltd | Derivado de ureia ou sal farmacologicamente aceitável do mesmo, seu uso e composição farmacêutica que os compreende |
| CA2933511A1 (en) | 2013-12-17 | 2015-06-25 | Laboratorios Del Dr. Esteve, S.A. | Serotonin-norepinephrine reuptake inhibitors (snris) and sigma receptor ligands combinations |
| US20160318897A1 (en) | 2013-12-18 | 2016-11-03 | Basf Se | Azole compounds carrying an imine-derived substituent |
| WO2015092610A1 (en) | 2013-12-20 | 2015-06-25 | Pfizer Limited | N-acylpiperidine ether tropomyosin-related kinase inhibitors |
| WO2015143652A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143654A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| WO2015143653A1 (en) | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| EP3131891A1 (en) | 2014-04-15 | 2017-02-22 | Pfizer Inc. | Tropomyosin-related kinase inhibitors containing both a 1h-pyrazole and a pyrimidine moiety |
| EP3140298A1 (en) | 2014-05-07 | 2017-03-15 | Pfizer Inc. | Tropomyosin-related kinase inhibitors |
| HUE045340T2 (hu) * | 2014-05-15 | 2019-12-30 | Array Biopharma Inc | 1-((3S,4R)-4-(3-fluorfenil)-1-(2-metoxietil)pirrolidin-3-il)-3-(4-metil-3-(2- metilpirimidin-5-il)-1-fenil-1H-pirazol-5-il)karbamid mint TrkA kináz inhibitor |
| WO2016009296A1 (en) | 2014-07-16 | 2016-01-21 | Pfizer Inc. | N-acylpiperidine ether tropomyosin-related kinase inhibitors |
| WO2016020784A1 (en) | 2014-08-05 | 2016-02-11 | Pfizer Inc. | N-acylpyrrolidine ether tropomyosin-related kinase inhibitors |
| WO2016021629A1 (ja) | 2014-08-06 | 2016-02-11 | 塩野義製薬株式会社 | TrkA阻害活性を有する複素環および炭素環誘導体 |
| TWI746426B (zh) | 2014-11-16 | 2021-11-21 | 美商亞雷生物製藥股份有限公司 | (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型 |
| SG11201702924WA (en) | 2014-12-08 | 2017-05-30 | Du Pont | 3-oxo-3-(arylamino)propanoates, a process for their preparation, and their use in preparing pyrrolidinones |
| WO2016161572A1 (en) | 2015-04-08 | 2016-10-13 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
| BR112017024966A2 (pt) * | 2015-05-27 | 2018-08-07 | Kyorin Seiyaku Kk | derivado de ureia ou sal farmacologicamente aceitável do mesmo |
| KR20180021745A (ko) | 2015-06-01 | 2018-03-05 | 록쏘 온콜로지, 인코포레이티드 | 암을 진단하고 치료하는 방법 |
| EP3330256B1 (en) | 2015-07-07 | 2021-06-16 | Shionogi & Co., Ltd. | HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY |
| EP3322706B1 (en) | 2015-07-16 | 2020-11-11 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| TN2018000138A1 (en) | 2015-10-26 | 2019-10-04 | Array Biopharma Inc | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| EP3393245A1 (en) | 2015-12-22 | 2018-10-31 | Syngenta Participations AG | Pesticidally active pyrazole derivatives |
| JP6898043B2 (ja) * | 2016-02-04 | 2021-07-07 | 塩野義製薬株式会社 | TrkA阻害活性を有する含窒素複素環および炭素環誘導体 |
| RS65988B1 (sr) | 2016-04-04 | 2024-10-31 | Loxo Oncology Inc | Postupak lečenja pedijatrijskih karcinoma |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| HUE068971T2 (hu) | 2016-04-04 | 2025-02-28 | Loxo Oncology Inc | (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid folyékony készítményei |
| SI3458456T1 (sl) | 2016-05-18 | 2021-04-30 | Loxo Oncology, Inc. | Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US11472797B2 (en) | 2017-04-05 | 2022-10-18 | Syngenta Participations Ag | Pesticidally active pyrazole derivatives |
| CN110770223B (zh) | 2017-06-19 | 2023-08-22 | 先正达参股股份有限公司 | 杀有害生物活性吡唑衍生物 |
| JP2019026646A (ja) * | 2017-08-03 | 2019-02-21 | 塩野義製薬株式会社 | 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および/または予防用医薬組成物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| EP3700576A1 (en) | 2017-10-26 | 2020-09-02 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| CN111433198A (zh) * | 2017-11-17 | 2020-07-17 | 合帕吉恩治疗公司 | 作为ask1的抑制剂的脲衍生物 |
| CN111971286B (zh) | 2018-01-18 | 2023-04-14 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物 |
| TW201938169A (zh) | 2018-01-18 | 2019-10-01 | 美商亞雷生物製藥股份有限公司 | 作為RET激酶抑制劑之經取代吡唑并[3,4-d]嘧啶化合物 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| KR102803660B1 (ko) | 2018-03-05 | 2025-05-02 | 브리스톨-마이어스 스큅 컴퍼니 | 페닐피롤리디논 포르밀 펩티드 2 수용체 효능제 |
| CA3095366A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN112823036B (zh) | 2018-07-03 | 2024-11-08 | 艾福姆德尤股份有限公司 | 用于治疗与sting活性有关的疾病的化合物和组合物 |
| CN112424189B (zh) * | 2018-07-12 | 2023-07-07 | 漳州片仔癀药业股份有限公司 | 吡咯烷基脲衍生物及其在TrkA相关疾病的应用 |
| GB201811825D0 (en) | 2018-07-19 | 2018-09-05 | Benevolentai Bio Ltd | Organic compounds |
| KR102653681B1 (ko) | 2018-07-31 | 2024-04-03 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제 |
| GB201813791D0 (en) | 2018-08-23 | 2018-10-10 | Benevolental Bio Ltd | Organic compounds |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| WO2020131674A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| EP3898626A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| WO2020127345A1 (en) | 2018-12-21 | 2020-06-25 | Syngenta Participations Ag | Pesticidally active pyrazole derivatives |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021095577A1 (ja) * | 2019-11-14 | 2021-05-20 | ユニマテック株式会社 | 含フッ素ピラゾール化合物およびその製造方法 |
| US11708357B2 (en) | 2020-01-10 | 2023-07-25 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Crystal form of pyrrolidinyl urea derivative and application thereof |
| WO2021139795A1 (zh) * | 2020-01-10 | 2021-07-15 | 漳州片仔癀药业股份有限公司 | 吡咯烷基脲衍生物的制备方法 |
| EP4093404A1 (en) | 2020-01-22 | 2022-11-30 | BenevolentAI Bio Limited | Topical pharmaceutical compositions comprising imidazo[1,2-b]pyridazine compounds |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4093376A1 (en) | 2020-01-22 | 2022-11-30 | BenevolentAI Bio Limited | Pharmaceutical compositions and their uses |
| WO2022003377A1 (en) | 2020-07-02 | 2022-01-06 | Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A. | Thieno[3,4-c]pyrazol-3-yl acetamides as autotaxin inhibitors |
| WO2022150585A1 (en) | 2021-01-08 | 2022-07-14 | Ifm Due, Inc. | Heterobicyclic compounds having an urea or analogue and their compositions for treating conditions associated with sting activity |
| CN117480169A (zh) * | 2021-01-08 | 2024-01-30 | 艾福姆德尤股份有限公司 | 用于治疗与sting活性有关的疾病的化合物和组合物 |
| WO2022218289A1 (en) * | 2021-04-12 | 2022-10-20 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| WO2022234287A1 (en) | 2021-05-06 | 2022-11-10 | Benevolentai Bio Limited | Imidazopyridazine derivatives useful as trk inhibitors |
| CN114031556B (zh) * | 2021-11-08 | 2023-03-31 | 温州大学 | 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法 |
| US12404348B2 (en) | 2021-11-19 | 2025-09-02 | The Brigham And Women's Hospital, Inc. | Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof |
| CN121152788A (zh) * | 2023-05-23 | 2025-12-16 | 上海海雁医药科技有限公司 | 稠合三环取代的异噁唑烷基脲衍生物、其药物组合物及应用 |
| US11970499B1 (en) * | 2023-12-22 | 2024-04-30 | King Faisal University | Pyrazolo[1,5-c]pyrimidine compounds as CK2 inhibitors |
Family Cites Families (108)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63198664A (ja) * | 1986-03-31 | 1988-08-17 | Sankyo Co Ltd | キノロンカルボン酸誘導体 |
| DE3906365A1 (de) * | 1988-07-15 | 1990-01-18 | Bayer Ag | 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe |
| ATE194612T1 (de) * | 1990-12-05 | 2000-07-15 | Naeja Pharmaceutical Inc | 7-substituierte-6-fluor-1,4-dihydro-4-oxo- chinolin-3-carbonsäurederivate als antibakterielle wirkstoffe |
| JP3086837B2 (ja) * | 1991-06-06 | 2000-09-11 | 三協化学株式会社 | 3−アミノピロリジン類の製造方法 |
| PL181867B1 (pl) * | 1994-06-14 | 2001-09-28 | Dainippon Pharmaceutical Co | Nowe zwiazki, sposoby ich wytwarzania i srodki przeciw nowotworowe PL |
| AU679887B2 (en) | 1995-09-11 | 1997-07-10 | Nihon Nohyaku Co., Ltd. | Azole derivatives, their use, production and usage |
| CA2206201A1 (en) | 1996-05-29 | 1997-11-29 | Yoshiaki Isobe | Pyrazole derivatives and their pharmaceutical use |
| US6083986A (en) | 1996-07-26 | 2000-07-04 | Icagen, Inc. | Potassium channel inhibitors |
| US5998424A (en) | 1997-06-19 | 1999-12-07 | Dupont Pharmaceuticals Company | Inhibitors of factor Xa with a neutral P1 specificity group |
| US6080763A (en) | 1997-11-03 | 2000-06-27 | Boehringer Ingelheim Pharmaceuticals, Inc. | Aromatic heterocyclic compounds and their use as anti-inflammatory agents |
| US7329670B1 (en) | 1997-12-22 | 2008-02-12 | Bayer Pharmaceuticals Corporation | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas |
| DE69836563T2 (de) | 1997-12-22 | 2007-05-16 | Bayer Pharmaceuticals Corp., West Haven | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN |
| US6197798B1 (en) | 1998-07-21 | 2001-03-06 | Novartis Ag | Amino-benzocycloalkane derivatives |
| DE69926542T2 (de) | 1998-12-25 | 2006-04-27 | Teikoku Hormone Mfg. Co., Ltd. | Aminopyrazolderivate |
| UA73492C2 (en) | 1999-01-19 | 2005-08-15 | Aromatic heterocyclic compounds as antiinflammatory agents | |
| US6387900B1 (en) | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| US6608227B1 (en) * | 1999-10-15 | 2003-08-19 | Bristol-Myers Squibb Pharma | Benzylcycloalkyl amines as modulators of chemokine receptor activity |
| US6410533B1 (en) | 2000-02-10 | 2002-06-25 | Genzyme Corporation | Antibacterial compounds |
| CA2413245A1 (en) * | 2000-06-30 | 2002-01-10 | Bristol-Myers Squibb Pharma Company | N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity |
| AU2002256418A1 (en) | 2001-04-27 | 2002-11-11 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| GB0110901D0 (en) | 2001-05-02 | 2001-06-27 | Smithkline Beecham Plc | Novel Compounds |
| EP1451160B1 (en) | 2001-11-01 | 2010-01-13 | Icagen, Inc. | Pyrazole-amides for use in the treatment of pain |
| WO2003045920A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 4-aminoquinoline compounds |
| SE0104248D0 (sv) | 2001-12-14 | 2001-12-14 | Astrazeneca Ab | Method of treatment |
| ES2361011T3 (es) | 2002-05-20 | 2011-06-13 | Bristol-Myers Squibb Company | Inhibidores del virus de la hepatitis c. |
| CN1678608A (zh) | 2002-07-02 | 2005-10-05 | 先灵公司 | 新的神经肽yy5受体拮抗剂 |
| PT1556083E (pt) | 2002-10-08 | 2011-03-17 | Rinat Neuroscience Corp | Métodos para tratar a dor pós-cirúrgica pela administração de um anticorpo contra o factor de crescimento nervoso e composições que contêm o mesmo |
| BRPI0315188B8 (pt) * | 2002-10-30 | 2021-05-25 | Astellas Pharma Inc | composto e composição farmacêutica |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| WO2005024755A2 (en) | 2002-12-31 | 2005-03-17 | Deciphera Pharmaceuticals, Llc. | Medicaments for the treatment of neurodegenerative disorders or diabetes |
| US20040171075A1 (en) | 2002-12-31 | 2004-09-02 | Flynn Daniel L | Modulation of protein functionalities |
| US7202257B2 (en) | 2003-12-24 | 2007-04-10 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
| PL1658269T3 (pl) | 2003-06-12 | 2009-08-31 | Abbvie Inc | Związki skondensowane, które hamują receptor waniloidowy podtypu 1 (VR1) |
| US20050171172A1 (en) | 2003-11-13 | 2005-08-04 | Ambit Biosciences Corporation | Amide derivatives as PDGFR modulators |
| MY141220A (en) * | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| US20080220497A1 (en) | 2003-12-24 | 2008-09-11 | Flynn Daniel L | Modulation of protein functionalities |
| JP4573223B2 (ja) | 2004-01-23 | 2010-11-04 | 東レ・ファインケミカル株式会社 | 光学活性trans−4−アミノ−1−ベンジル−3−ピロリジノールの製造方法 |
| CA2564325A1 (en) * | 2004-04-30 | 2005-11-24 | Bayer Pharmaceuticals Corporation | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| US20070270471A1 (en) * | 2004-08-09 | 2007-11-22 | Glaxo Group Limited | Compounds Which Potentiate Glutamate Receptor and Uses Thereof in Medicine |
| WO2006068591A1 (en) | 2004-12-20 | 2006-06-29 | Astrazeneca Ab | Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors |
| JP2008525502A (ja) | 2004-12-23 | 2008-07-17 | デシファラ ファーマスーティカルズ, エルエルシー | 抗炎症薬 |
| WO2006071940A2 (en) | 2004-12-23 | 2006-07-06 | Deciphera Pharmaceuticals, Llc | Enzyme modulators and treatments |
| NZ555770A (en) | 2004-12-24 | 2010-12-24 | Astrazeneca Ab | Heterocyclic piperazine-carboxamide compounds as CCR2B antagonists |
| EP1836188A1 (en) | 2004-12-30 | 2007-09-26 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| GB0510141D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| US20060281768A1 (en) | 2005-06-10 | 2006-12-14 | Gaul Michael D | Thienopyrimidine and thienopyridine kinase modulators |
| WO2007059202A2 (en) | 2005-11-15 | 2007-05-24 | Bayer Healthcare Ag | Pyrazolyl urea derivatives useful in the treatment of cancer |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP2044053A2 (en) | 2005-12-01 | 2009-04-08 | Bayer Healthcare, LLC | Urea compounds useful in the treatment of cancer |
| RU2442777C2 (ru) | 2006-01-31 | 2012-02-20 | Эррэй Биофарма Инк. | Ингибиторы киназ и способы их применения |
| GB0607953D0 (en) | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| WO2008016811A2 (en) | 2006-07-31 | 2008-02-07 | Neurogen Corporation | Aminopiperidines and realted compounds |
| ES2393410T3 (es) | 2006-08-09 | 2012-12-21 | Bristol-Myers Squibb Company | Pirrolotriazinas inhibidoras de quinasas |
| US8188113B2 (en) | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| US7897762B2 (en) | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| US7790756B2 (en) | 2006-10-11 | 2010-09-07 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| JP2010513232A (ja) | 2006-12-15 | 2010-04-30 | バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト | 3−h−ピラゾロピリジン類及びそれらの塩類、それらを含んで成る医薬組成物類、それらの調製方法及びそれらの使用 |
| CA2684950A1 (en) | 2007-04-20 | 2008-10-30 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases |
| CN101657418B (zh) * | 2007-04-20 | 2012-05-30 | 弗·哈夫曼-拉罗切有限公司 | 作为nk1/nk3受体双重拮抗剂的吡咯烷衍生物 |
| WO2008150899A1 (en) | 2007-05-29 | 2008-12-11 | Emory University | Combination therapies for treatment of cancer and inflammatory diseases |
| RU2493826C2 (ru) | 2007-07-12 | 2013-09-27 | Новартис Аг | Пероральные фармацевтические растворы, содержащие телбивудин |
| ITMI20071731A1 (it) | 2007-09-06 | 2009-03-07 | Univ Degli Studi Genova | Nuovi derivati ureici dell'acido 1h-pirazol-4-carbossilico con attivita inibente nei confronti della chemiotassi di neutrofili |
| WO2009053694A1 (en) * | 2007-10-24 | 2009-04-30 | Cancer Research Technology Limited | Therapeutic oxy-phenyl-aryl compounds and their use |
| EP2070929A1 (en) * | 2007-12-11 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| PT2268623E (pt) | 2008-03-17 | 2015-09-17 | Ambit Biosciences Corp | Derivados de quinazolina como moduladores de cinase raf e métodos para utilização dos mesmos |
| BRPI0912668A2 (pt) | 2008-05-13 | 2016-01-26 | Irm Llc | composto e composições como inibidores de quinase |
| BRPI0914779A2 (pt) * | 2008-06-16 | 2015-10-20 | Hoffmann La Roche | derivados de pirrolidina como antagonistas de receptor de nk2 |
| EP2334683B1 (en) | 2008-08-29 | 2017-03-22 | MSD Italia S.r.l. | Saturated bicyclic heterocyclic derivatives as smo antagonists |
| USRE49686E1 (en) | 2008-09-19 | 2023-10-10 | Takeda Pharmaceutical Company Limited | Nitrogen-containing heterocyclic compound and use of same |
| EP2350075B1 (en) | 2008-09-22 | 2014-03-05 | Array Biopharma, Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| CA2738870A1 (en) * | 2008-10-09 | 2010-04-15 | F. Hoffmann-La Roche Ag | Pyrrolidine n-benzyl derivatives |
| KR101853026B1 (ko) * | 2008-10-22 | 2018-04-27 | 어레이 바이오파마 인크. | TRK 키나아제 억제제로서 치환된 피라졸로[1,5a] 피리미딘 화합물 |
| US8022099B2 (en) * | 2008-11-03 | 2011-09-20 | Hoffmann-La Roche Inc. | N-benzyl pyrrolidine derivatives |
| EP2364300B1 (en) | 2008-11-19 | 2016-10-19 | Merial, Inc. | Dimeric 1-arylpyrazole derivatives |
| WO2010077680A2 (en) | 2008-12-08 | 2010-07-08 | Vm Discovery Inc. | Compositions of protein receptor tyrosine kinase inhibitors |
| MX2011006332A (es) | 2008-12-23 | 2011-06-27 | Abbott Lab | Compuestos antivirales. |
| EP2398323A4 (en) | 2009-02-19 | 2012-08-08 | Univ Connecticut | NEW HETEROPYRROLANALOGES THAT ACTIVATE ON CANNABINOID RECEPTORS |
| GB0904285D0 (en) * | 2009-03-12 | 2009-04-22 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| US8680139B2 (en) * | 2009-04-01 | 2014-03-25 | Progenra | Anti-neoplastic compounds, compositions and methods |
| US20120071475A1 (en) | 2009-04-27 | 2012-03-22 | Shionogi & Co., Ltd. | Urea derivatives having pi3k-inhibiting activity |
| US20120083476A1 (en) | 2009-06-05 | 2012-04-05 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| KR20120059558A (ko) | 2009-08-19 | 2012-06-08 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 화합물 및 이의 사용 방법 |
| WO2011032291A1 (en) | 2009-09-18 | 2011-03-24 | Zalicus Pharmaceuticals Ltd . | Selective calcium channel modulators |
| US20110144081A1 (en) * | 2009-12-15 | 2011-06-16 | Henner Knust | Pyrrolidine derivatives |
| US20110152233A1 (en) * | 2009-12-18 | 2011-06-23 | Henner Knust | Pyrrolidine compounds |
| CN105693720B (zh) | 2010-05-20 | 2019-01-18 | 阵列生物制药公司 | 作为trk激酶抑制剂的大环化合物 |
| US9296722B2 (en) | 2010-05-27 | 2016-03-29 | Ambit Biosciences Corporation | Azolyl urea compounds and methods of use thereof |
| EP2598497B1 (en) * | 2010-07-29 | 2019-03-06 | Merck Patent GmbH | Cyclic amine azaheterocyclic carboxamides |
| EP2615916B1 (en) * | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel erk inhibitors |
| WO2012066077A1 (en) * | 2010-11-18 | 2012-05-24 | Prosidion Limited | 1,4 di substituted pyrrolidine - 3 - yl -amine derivatives and their use for the treatment of metabolic disorders |
| CN105130967B (zh) | 2011-05-13 | 2018-04-17 | 阵列生物制药公司 | 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物 |
| US9023865B2 (en) | 2011-10-27 | 2015-05-05 | Merck Sharp & Dohme Corp. | Compounds that are ERK inhibitors |
| US8969325B2 (en) | 2011-12-19 | 2015-03-03 | Abbvie Inc. | TRPV1 antagonists |
| EP2858501A4 (en) | 2012-05-22 | 2015-12-09 | Merck Sharp & Dohme | TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR |
| EP2900241B1 (en) | 2012-09-28 | 2018-08-08 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP2900223B1 (en) | 2012-09-28 | 2017-10-25 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9822118B2 (en) | 2012-11-13 | 2017-11-21 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| RU2664541C2 (ru) | 2012-11-13 | 2018-08-20 | Эррэй Биофарма Инк. | Бициклические соединения мочевины, тиомочевины, гуанидина и цианогуанидина, пригодные для лечения боли |
| US9809578B2 (en) | 2012-11-13 | 2017-11-07 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors |
| US9969694B2 (en) | 2012-11-13 | 2018-05-15 | Array Biopharma Inc. | N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| MX365733B (es) * | 2012-11-13 | 2019-06-12 | Array Biopharma Inc | Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa. |
| WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
| US9790210B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
| WO2015039333A1 (en) | 2013-09-22 | 2015-03-26 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
-
2012
- 2012-05-09 CN CN201510473903.6A patent/CN105130967B/zh active Active
- 2012-05-09 CN CN201810204068.XA patent/CN108329246B/zh active Active
- 2012-05-09 CN CN201280034583.9A patent/CN103649076B/zh active Active
- 2012-05-09 SI SI201230829A patent/SI2712358T1/sl unknown
- 2012-05-09 BR BR112013029201-6A patent/BR112013029201B1/pt active IP Right Grant
- 2012-05-09 MY MYPI2013702146A patent/MY173181A/en unknown
- 2012-05-09 HR HRP20161786TT patent/HRP20161786T1/hr unknown
- 2012-05-09 MX MX2017006568A patent/MX369142B/es unknown
- 2012-05-09 AU AU2012256237A patent/AU2012256237B2/en active Active
- 2012-05-09 LT LTEP12743553.5T patent/LT2712358T/lt unknown
- 2012-05-09 SG SG2013083498A patent/SG194902A1/en unknown
- 2012-05-09 KR KR1020137033192A patent/KR101960555B1/ko active Active
- 2012-05-09 SM SM20170035T patent/SMT201700035T1/it unknown
- 2012-05-09 RU RU2013155456A patent/RU2606131C2/ru active
- 2012-05-09 KR KR1020197007332A patent/KR102001364B1/ko active Active
- 2012-05-09 PH PH1/2013/502319A patent/PH12013502319A1/en unknown
- 2012-05-09 CA CA2835835A patent/CA2835835C/en active Active
- 2012-05-09 ES ES12743553.5T patent/ES2615738T3/es active Active
- 2012-05-09 DK DK12743553.5T patent/DK2712358T3/en active
- 2012-05-09 US US14/117,615 patent/US9562055B2/en active Active
- 2012-05-09 PT PT127435535T patent/PT2712358T/pt unknown
- 2012-05-09 PL PL12743553T patent/PL2712358T3/pl unknown
- 2012-05-09 ME MEP-2017-7A patent/ME02583B/me unknown
- 2012-05-09 HU HUE12743553A patent/HUE030791T2/en unknown
- 2012-05-09 NZ NZ618795A patent/NZ618795A/en unknown
- 2012-05-09 SG SG10201913053QA patent/SG10201913053QA/en unknown
- 2012-05-09 JP JP2014510416A patent/JP5933902B2/ja active Active
- 2012-05-09 WO PCT/US2012/037003 patent/WO2012158413A2/en not_active Ceased
- 2012-05-09 MX MX2013013342A patent/MX347952B/es active IP Right Grant
- 2012-05-09 EP EP12743553.5A patent/EP2712358B1/en active Active
- 2012-05-09 UA UAA201314472A patent/UA114711C2/uk unknown
- 2012-05-09 RS RS20170020A patent/RS55582B1/sr unknown
- 2012-05-11 TW TW106112291A patent/TWI649315B/zh active
- 2012-05-11 AR ARP120101675A patent/AR086367A1/es active IP Right Grant
- 2012-05-11 UY UY0001034067A patent/UY34067A/es unknown
- 2012-05-11 TW TW101116963A patent/TWI589573B/zh active
-
2013
- 2013-11-11 IL IL229377A patent/IL229377A/en active IP Right Grant
- 2013-11-13 CL CL2013003257A patent/CL2013003257A1/es unknown
- 2013-12-11 CR CR20130646A patent/CR20130646A/es unknown
- 2013-12-13 CO CO13291998A patent/CO6821961A2/es active IP Right Grant
-
2016
- 2016-02-15 JP JP2016026184A patent/JP6382867B2/ja active Active
- 2016-12-16 US US15/382,028 patent/US9878997B2/en active Active
-
2017
- 2017-01-19 SM SM201700035T patent/SMT201700035B/it unknown
- 2017-01-24 CY CY20171100107T patent/CY1119014T1/el unknown
- 2017-03-01 AU AU2017201418A patent/AU2017201418B2/en active Active
- 2017-04-28 JP JP2017090432A patent/JP2017171672A/ja not_active Withdrawn
- 2017-06-12 IL IL252841A patent/IL252841B/en active IP Right Grant
- 2017-12-12 US US15/839,706 patent/US10323022B2/en active Active
-
2018
- 2018-09-14 JP JP2018172485A patent/JP2019001819A/ja active Pending
-
2019
- 2019-05-02 US US16/402,080 patent/US20190359597A1/en not_active Abandoned
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR086367A1 (es) | Compuestos de pirrolidinil urea y pirrolidinil tiourea como inhibidores de cinasa trka | |
| AR079541A1 (es) | Compuestos sustituidos de n-(1h-indazol-4-il) imidazo (1,2-a) piridin-3-carboxamida como inhibidores de cfms | |
| AR076900A1 (es) | Derivados heterociclicos nitrogenados utiles como agentes antivirales, composiciones farmaceuticas que los contienen y uso de los mismos como inhibidores del vhc | |
| CY1124284T1 (el) | Ενωσεις σπειρο[3η-ινδολο-3,2'-πυρρολιδιν]-2(1η)-ονης και παραγωγα ως αναστολεις mdm2-p53 | |
| AR057131A1 (es) | Derivados de purina como inmunomodulador | |
| AR083339A1 (es) | Compuestos de quinazolina como bloqueadores de los canales de sodio | |
| AR087591A1 (es) | Derivados de ciclohexil azetidina como inhibidores de jak | |
| ES2625256T3 (es) | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIA | |
| AR077468A1 (es) | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa | |
| AR081075A1 (es) | Derivados de imidazo[1,2-c]pirimidina, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias. | |
| ES2606197T3 (es) | Moduladores pirrolidina de GPR40 | |
| AR087288A1 (es) | Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a | |
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| AR070136A1 (es) | Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa | |
| AR076435A1 (es) | Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos | |
| AR076922A1 (es) | Benzodiazepinas como inhibidores de pi3k/mtor, una composicion farmaceutica que las comprende, metodos para su fabricacion y su uso en el tratamiento del cancer. | |
| MX359882B (es) | Amidas como moduladores de canales de sodio. | |
| MX2015009602A (es) | Piridona amidas como moduladores de canales de sodio. | |
| AR064471A1 (es) | Macrociclos inhibidores selectivos del factor de coagulacion viia, composiciones farmaceuticas que los comprenden y uso de los mismos como agentes anticoagulantes. | |
| AR082201A1 (es) | Bencenosulfonamidas utiles como inhibidores del canal de sodio | |
| AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| AR082153A1 (es) | N-sulfonilbenzamidas utiles como inhibidor del canal de sodio | |
| AR085489A1 (es) | Derivados de triazolopiridinas, composiciones farmaceuticas que los contienen, proceso para prepararlos, intermediarios de dicho proceso y uso de los mismos para el tratamiento de enfermedades autoinmunes e inflamatorias | |
| AR079648A1 (es) | Inhibidores de la replicacion del virus de la hepatitis c | |
| CR20140294A (es) | Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal | ||
| FG | Grant, registration |