ES2553610T3 - Inhibidores de la caseína cinasa 1 delta (CK1delta) - Google Patents
Inhibidores de la caseína cinasa 1 delta (CK1delta) Download PDFInfo
- Publication number
- ES2553610T3 ES2553610T3 ES11804754.7T ES11804754T ES2553610T3 ES 2553610 T3 ES2553610 T3 ES 2553610T3 ES 11804754 T ES11804754 T ES 11804754T ES 2553610 T3 ES2553610 T3 ES 2553610T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- aryl
- tau
- heteroaryl
- groups
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 239000003112 inhibitor Substances 0.000 title description 5
- 108010047048 Casein Kinase Idelta Proteins 0.000 title description 3
- 102100037402 Casein kinase I isoform delta Human genes 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 abstract description 52
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 7
- 125000001041 indolyl group Chemical group 0.000 abstract description 5
- 125000003118 aryl group Chemical group 0.000 abstract description 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 102000013498 tau Proteins Human genes 0.000 description 34
- 108010026424 tau Proteins Proteins 0.000 description 34
- 210000004027 cell Anatomy 0.000 description 28
- 101150047910 CSNK1D gene Proteins 0.000 description 19
- 230000026731 phosphorylation Effects 0.000 description 14
- 238000006366 phosphorylation reaction Methods 0.000 description 14
- 210000004556 brain Anatomy 0.000 description 11
- 208000024827 Alzheimer disease Diseases 0.000 description 8
- 238000003556 assay Methods 0.000 description 7
- 102100034357 Casein kinase I isoform alpha Human genes 0.000 description 6
- 208000034799 Tauopathies Diseases 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 210000002569 neuron Anatomy 0.000 description 6
- 238000012360 testing method Methods 0.000 description 6
- 101710118321 Casein kinase I isoform alpha Proteins 0.000 description 5
- 108091000080 Phosphotransferase Proteins 0.000 description 5
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 5
- 102000020233 phosphotransferase Human genes 0.000 description 5
- 230000005764 inhibitory process Effects 0.000 description 4
- 239000006166 lysate Substances 0.000 description 4
- 235000018102 proteins Nutrition 0.000 description 4
- 102000004169 proteins and genes Human genes 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 3
- 208000037259 Amyloid Plaque Diseases 0.000 description 3
- 206010012289 Dementia Diseases 0.000 description 3
- 201000011240 Frontotemporal dementia Diseases 0.000 description 3
- 102000029749 Microtubule Human genes 0.000 description 3
- 108091022875 Microtubule Proteins 0.000 description 3
- 125000002619 bicyclic group Chemical group 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 125000005842 heteroatom Chemical group 0.000 description 3
- 239000002609 medium Substances 0.000 description 3
- 210000004688 microtubule Anatomy 0.000 description 3
- 208000015122 neurodegenerative disease Diseases 0.000 description 3
- 210000002682 neurofibrillary tangle Anatomy 0.000 description 3
- 238000001262 western blot Methods 0.000 description 3
- 102000008122 Casein Kinase I Human genes 0.000 description 2
- 108010049812 Casein Kinase I Proteins 0.000 description 2
- 101000891579 Homo sapiens Microtubule-associated protein tau Proteins 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 208000001089 Multiple system atrophy Diseases 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 102000001253 Protein Kinase Human genes 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 2
- 239000004473 Threonine Substances 0.000 description 2
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 2
- 125000004429 atom Chemical group 0.000 description 2
- 230000033228 biological regulation Effects 0.000 description 2
- 239000013592 cell lysate Substances 0.000 description 2
- 230000003833 cell viability Effects 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- BRZYSWJRSDMWLG-CAXSIQPQSA-N geneticin Chemical compound O1C[C@@](O)(C)[C@H](NC)[C@@H](O)[C@H]1O[C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](C(C)O)O2)N)[C@@H](N)C[C@H]1N BRZYSWJRSDMWLG-CAXSIQPQSA-N 0.000 description 2
- 102000057063 human MAPT Human genes 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 229940043355 kinase inhibitor Drugs 0.000 description 2
- 238000004949 mass spectrometry Methods 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- VMGAPWLDMVPYIA-HIDZBRGKSA-N n'-amino-n-iminomethanimidamide Chemical compound N\N=C\N=N VMGAPWLDMVPYIA-HIDZBRGKSA-N 0.000 description 2
- 230000004770 neurodegeneration Effects 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 2
- 229940076606 Casein kinase 1 inhibitor Drugs 0.000 description 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 description 1
- 108010025454 Cyclin-Dependent Kinase 5 Proteins 0.000 description 1
- 102100026805 Cyclin-dependent-like kinase 5 Human genes 0.000 description 1
- 101710088194 Dehydrogenase Proteins 0.000 description 1
- 239000006144 Dulbecco’s modified Eagle's medium Substances 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 229930182566 Gentamicin Natural products 0.000 description 1
- CEAZRRDELHUEMR-URQXQFDESA-N Gentamicin Chemical compound O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N CEAZRRDELHUEMR-URQXQFDESA-N 0.000 description 1
- 101000994700 Homo sapiens Casein kinase I isoform alpha Proteins 0.000 description 1
- 229940118135 JNK inhibitor Drugs 0.000 description 1
- 239000012825 JNK inhibitor Substances 0.000 description 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 1
- 238000000134 MTT assay Methods 0.000 description 1
- 231100000002 MTT assay Toxicity 0.000 description 1
- 102000009664 Microtubule-Associated Proteins Human genes 0.000 description 1
- 108010020004 Microtubule-Associated Proteins Proteins 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 229940122907 Phosphatase inhibitor Drugs 0.000 description 1
- 108010001441 Phosphopeptides Proteins 0.000 description 1
- 108010089430 Phosphoproteins Proteins 0.000 description 1
- 102000007982 Phosphoproteins Human genes 0.000 description 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 description 1
- 102000011732 Proline-Directed Protein Kinases Human genes 0.000 description 1
- 108010076669 Proline-Directed Protein Kinases Proteins 0.000 description 1
- 239000004365 Protease Substances 0.000 description 1
- 108010026552 Proteome Proteins 0.000 description 1
- 239000012083 RIPA buffer Substances 0.000 description 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 1
- 206010039966 Senile dementia Diseases 0.000 description 1
- 108700019146 Transgenes Proteins 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 description 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 description 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000006285 cell suspension Substances 0.000 description 1
- 238000013043 cell viability test Methods 0.000 description 1
- 230000007541 cellular toxicity Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- -1 cinolinyl Chemical group 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- 125000000392 cycloalkenyl group Chemical group 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 230000003412 degenerative effect Effects 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 125000003838 furazanyl group Chemical group 0.000 description 1
- 125000004612 furopyridinyl group Chemical group O1C(=CC2=C1C=CC=N2)* 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 229960002518 gentamicin Drugs 0.000 description 1
- 230000002518 glial effect Effects 0.000 description 1
- 210000001320 hippocampus Anatomy 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 238000010874 in vitro model Methods 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 125000001977 isobenzofuranyl group Chemical group C=1(OC=C2C=CC=CC12)* 0.000 description 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 108020004999 messenger RNA Proteins 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000002438 mitochondrial effect Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 238000003566 phosphorylation assay Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 238000000734 protein sequencing Methods 0.000 description 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 229930002330 retinoic acid Natural products 0.000 description 1
- 125000006413 ring segment Chemical group 0.000 description 1
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 238000011830 transgenic mouse model Methods 0.000 description 1
- 229960001727 tretinoin Drugs 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
- 230000035899 viability Effects 0.000 description 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
-
- 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
- A61K31/423—Oxazoles condensed with carbocyclic 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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic 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
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles 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
- A61K31/433—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
- A61K31/44—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
- A61K31/4427—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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines 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
- A61K31/4965—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-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
- A61K31/495—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
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-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
- A61K31/495—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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/535—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
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic 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
- A61K31/54—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
- A61K31/549—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 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- 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
- 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
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles 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 in position 2
-
- 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
- C07D401/02—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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- 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
- C07D495/12—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 three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Toxicology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyrrole Compounds (AREA)
- Quinoline Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Pyridine Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1021161.3A GB201021161D0 (en) | 2010-12-14 | 2010-12-14 | Casein kinase 1delta (CK1Delta) inhibitors |
| GB201021161 | 2010-12-14 | ||
| GBGB1109162.6A GB201109162D0 (en) | 2011-06-01 | 2011-06-01 | Casein kinase 1Delta (CK1Delta) inhibitors |
| GB201109162 | 2011-06-01 | ||
| PCT/GB2011/052473 WO2012080727A2 (en) | 2010-12-14 | 2011-12-14 | Casein kinase 1delta (ck1delta) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2553610T3 true ES2553610T3 (es) | 2015-12-10 |
Family
ID=45444638
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11804754.7T Active ES2553610T3 (es) | 2010-12-14 | 2011-12-14 | Inhibidores de la caseína cinasa 1 delta (CK1delta) |
| ES14190691.7T Active ES2650744T3 (es) | 2010-12-14 | 2011-12-14 | Inhibidores de la caseína quinasa 1 delta (CK1delta) |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES14190691.7T Active ES2650744T3 (es) | 2010-12-14 | 2011-12-14 | Inhibidores de la caseína quinasa 1 delta (CK1delta) |
Country Status (10)
| Country | Link |
|---|---|
| US (5) | US20140031547A1 (enExample) |
| EP (3) | EP2651404B1 (enExample) |
| JP (4) | JP5937102B2 (enExample) |
| CN (3) | CN103298460B (enExample) |
| AU (2) | AU2011343039B2 (enExample) |
| CA (1) | CA2818903C (enExample) |
| DK (1) | DK2835131T3 (enExample) |
| ES (2) | ES2553610T3 (enExample) |
| HK (1) | HK1214527A1 (enExample) |
| WO (2) | WO2012080729A2 (enExample) |
Families Citing this family (235)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1993360T3 (en) | 2005-12-28 | 2017-05-22 | Vertex Pharma | SOLID FORMS OF N- [2,4-BIS (1,1-DIMETHYLETHYL) -5-HYDROXYPHENYL] -1,4-DIHYDRO-4-OXOQUINOLIN-3-CARBOXAMIDE |
| CN101965335B (zh) | 2008-01-04 | 2015-01-14 | 英特利凯恩有限责任公司 | 某些化学实体、组合物和方法 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| AR077280A1 (es) | 2009-06-29 | 2011-08-17 | Incyte Corp | Pirimidinonas como inhibidores de pi3k, y composiciones farmaceuticas que los comprenden |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| EP2552208A4 (en) * | 2010-03-31 | 2014-07-09 | Glaxo Group Ltd | IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS |
| US9193721B2 (en) | 2010-04-14 | 2015-11-24 | Incyte Holdings Corporation | Fused derivatives as PI3Kδ inhibitors |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| CN103298460B (zh) * | 2010-12-14 | 2016-06-01 | 电泳有限公司 | 酪蛋白激酶1δ(CK1δ)抑制剂 |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| EP2663309B1 (en) | 2011-01-10 | 2017-03-15 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| AR087701A1 (es) | 2011-08-31 | 2014-04-09 | Japan Tobacco Inc | Derivados de pirazol con actividad inhibidora de sglt1 |
| IL299533B2 (en) | 2011-09-02 | 2025-01-01 | Incyte Holdings Corp | Heterocycloamines as PI3K inhibitors |
| AU2012321815B2 (en) | 2011-10-07 | 2017-03-09 | Takeda Pharmaceutical Company Limited | 1 - arylcarbonyl - 4 - oxy - piperidine compounds useful for the treatment of neurodegenerative diseases |
| LT2772484T (lt) | 2011-10-18 | 2017-12-27 | Astellas Pharma Inc. | Biciklinis heterociklinis junginys |
| AR090037A1 (es) | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| JP6141864B2 (ja) | 2011-12-01 | 2017-06-07 | ケモセントリックス,インコーポレイティド | Ccr(4)アンタゴニストとしての置換アニリン |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| SMT201700146T1 (it) | 2012-06-13 | 2017-05-08 | Incyte Holdings Corp | Composti triciclici sostituiti come inibitori di fgfr |
| CN104364239B (zh) | 2012-06-13 | 2017-08-25 | 霍夫曼-拉罗奇有限公司 | 二氮杂螺环烷烃和氮杂螺环烷烃 |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| US9630976B2 (en) | 2012-07-03 | 2017-04-25 | Ono Pharmaceutical Co., Ltd. | Compound having agonistic activity on somatostatin receptor, and use thereof for medical purposes |
| WO2014009891A1 (en) * | 2012-07-11 | 2014-01-16 | Piramal Enterprises Limited | Heterocyclic compounds for use in the treatment of cancers |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| CA3139033A1 (en) | 2012-08-22 | 2014-02-27 | Cornell University | Methods for inhibiting fascin |
| NZ705167A (en) * | 2012-08-24 | 2017-12-22 | Treventis Corp | Benzofurazan anti-amyloid compounds and methods |
| CN102850341B (zh) * | 2012-09-05 | 2015-02-18 | 浙江工业大学 | 一种噻二唑类化合物及其制备与应用 |
| GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
| PT2900669T (pt) | 2012-09-25 | 2019-10-29 | Hoffmann La Roche | Derivados de hexahidropirrolo[3,4−c]pirrol e compostos relacionados enquanto inibidores da autotaxina (atx) e enquanto inibidores da produção de ácido lisofosfatídico (lpa) para o tratamento de, por exemplo, doenças renais |
| CN103739594A (zh) * | 2012-10-17 | 2014-04-23 | 南京大学 | 一类含吡嗪环和三氮唑结构的席夫碱类衍生物及其制法 |
| LT2914296T (lt) | 2012-11-01 | 2018-09-25 | Infinity Pharmaceuticals, Inc. | Vėžio gydymas, panaudojant p13 kinazės izoformos moduliatorius |
| PL2925744T3 (pl) | 2012-11-27 | 2021-06-14 | Thomas Helledays Stiftelse För Medicinsk Forskning | Pochodne pirymidyno-2,4-diaminy do leczenia nowotworu |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| JP6284490B2 (ja) | 2012-12-28 | 2018-02-28 | 株式会社新日本科学 | イミダゾピリジン誘導体を有効成分として含むoct3活性阻害剤又はoct3検出剤 |
| WO2014124458A1 (en) * | 2013-02-11 | 2014-08-14 | The Regents Of The University Of California | Compositions and methods for treating neurodegenerative diseases |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| EP2967046A4 (en) | 2013-03-15 | 2016-12-21 | Whitehead Inst Biomedical Res | BENZIMIDAZOLE DERIVATIVES AND USES THEREOF |
| WO2014144747A1 (en) * | 2013-03-15 | 2014-09-18 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US9045477B2 (en) | 2013-03-15 | 2015-06-02 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| CA2909207C (en) | 2013-04-19 | 2021-11-02 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US9238034B2 (en) * | 2013-07-09 | 2016-01-19 | The Translational Genomics Research Institute | FN14 antagonists and therapeutic uses thereof |
| US9797882B2 (en) | 2013-07-09 | 2017-10-24 | The Translational Genomics Research Institute | Method of screening for a compound for inhibitory activity of FN14-tweak interaction |
| TWI649308B (zh) | 2013-07-24 | 2019-02-01 | 小野藥品工業股份有限公司 | 喹啉衍生物 |
| GB201314452D0 (en) | 2013-08-13 | 2013-09-25 | Ostara Biomedical Ltd | Embryo implantation |
| RU2570907C2 (ru) * | 2013-10-21 | 2015-12-20 | Автономная Некоммерческая Организация "Научно-Исследовательский Центр Биотехнологии Антибиотиков И Других Биологически Активных Веществ "Биоан" | Производные 3-ациламинопиридин-2(1h)-она, применимые как ингибиторы серин-треониновой протеинкиназы gsk3b в качестве лекарственных препаратов для лечения диабета ii типа. |
| DK3071206T3 (da) | 2013-11-22 | 2021-05-25 | CL BioSciences LLC | Gastrinantagonister (eg yf476, netazepid) til behandling og forebyggelse af osteoporose |
| PL3074400T3 (pl) | 2013-11-26 | 2018-03-30 | F.Hoffmann-La Roche Ag | Pochodne oktahydrocyklobuta[1,2-c;3,4-c']dipirolu jako inhibitory autotaksyny |
| GB201321738D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| US10087151B2 (en) | 2014-01-09 | 2018-10-02 | The J. David Gladstone Institutes, A Testimentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
| EP3099695B1 (en) | 2014-01-29 | 2020-04-08 | GlaxoSmithKline Intellectual Property Development Limited | Compounds |
| CN105980388B (zh) | 2014-01-29 | 2018-01-16 | 葛兰素史密斯克莱知识产权发展有限公司 | 化合物 |
| ES2919024T3 (es) | 2014-02-11 | 2022-07-21 | Mitokinin Inc | Composiciones y procedimientos que utilizan las mismas para el tratamiento de enfermedades neurodegenerativas y mitocondriales |
| JP6602778B2 (ja) | 2014-02-13 | 2019-11-06 | インサイト・コーポレイション | Lsd1阻害剤としてのシクロプロピルアミン類 |
| ES2750956T3 (es) | 2014-02-13 | 2020-03-30 | Incyte Corp | Ciclopropilaminas como inhibidores de LSD1 |
| TW201613860A (en) | 2014-02-13 | 2016-04-16 | Incyte Corp | Cyclopropylamines as LSD1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2015127125A1 (en) | 2014-02-20 | 2015-08-27 | Cornell University | Compounds and methods for inhibiting fascin |
| JP6663361B2 (ja) | 2014-02-27 | 2020-03-11 | トレヴェンティス コーポレーション | ベンゾフラザンを含有する抗アミロイド化合物 |
| CN106029667B (zh) | 2014-03-26 | 2019-08-23 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的稠合[1,4]二氮杂*化合物 |
| MA39792B1 (fr) | 2014-03-26 | 2019-12-31 | Hoffmann La Roche | Composés bicycliques en tant qu'inhibiteurs de production d'autotaxine (atx) et d'acide lysophosphatidique (lpa) |
| CN106164059A (zh) * | 2014-04-11 | 2016-11-23 | 爱默蕾大学 | 用天冬酰胺内肽酶(aep)抑制剂以及相关组合物对神经退行性疾病的治疗 |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| US9840482B2 (en) * | 2014-04-19 | 2017-12-12 | Sunshine Lake Pharma Co., Ltd. | Sulfonamide derivatives and pharmaceutical applications thereof |
| PL3597649T3 (pl) * | 2014-04-23 | 2022-04-04 | Dart Neuroscience Llc | Kompozycje zawierające podstawione związki [1,2,4]triazolo[1,5-a]pirymidyn-7-ylowe jako inhibitory pde2 |
| WO2015170218A1 (en) | 2014-05-07 | 2015-11-12 | Pfizer Inc. | Tropomyosin-related kinase inhibitors |
| CN104059060B (zh) * | 2014-05-30 | 2017-08-01 | 西安交通大学 | 一种5‑(1h‑吲哚‑3‑亚甲基)‑1,3‑噻唑烷‑4‑酮类衍生物及其合成方法和应用 |
| WO2015187088A1 (en) | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Mth1 inhibitors for treatment of cancer |
| WO2015187089A1 (en) | 2014-06-04 | 2015-12-10 | Thomas Helledays Stiftelse För Medicinsk Forskning | Mth1 inhibitors for treatment of inflammatory and autoimmune conditions |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| CN107001356B (zh) * | 2014-07-31 | 2019-09-03 | 默克专利有限公司 | 用于神经退化性疾病的中氮茚衍生物 |
| US20170204089A1 (en) | 2014-08-04 | 2017-07-20 | Drexel University | Novel compounds and methods of treating or ameliorating an il-1r-mediated disease or disorder using same |
| JO3589B1 (ar) | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
| US9701639B2 (en) | 2014-10-07 | 2017-07-11 | Vertex Pharmaceuticals Incorporated | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| GB201419579D0 (en) * | 2014-11-03 | 2014-12-17 | Iomet Pharma Ltd | Pharmaceutical compound |
| WO2016073424A1 (en) | 2014-11-05 | 2016-05-12 | Dart Neuroscience, Llc | Substituted 5-methyl-[1, 2, 4] triazolo [1,5-a) pyrimidin-2-amine compounds as pde2 inhibitors |
| WO2016104617A1 (ja) | 2014-12-25 | 2016-06-30 | 小野薬品工業株式会社 | キノリン誘導体 |
| GB201501302D0 (en) | 2015-01-27 | 2015-03-11 | Ostara Biomedical Ltd | Embryo implantation |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| SG11201706917WA (en) | 2015-02-27 | 2017-09-28 | Incyte Corp | Salts of pi3k inhibitor and processes for their preparation |
| US10722513B2 (en) | 2015-03-23 | 2020-07-28 | The University Of Melbourne | Treatment of respiratory diseases |
| EA201792205A1 (ru) | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| WO2016176420A1 (en) * | 2015-04-30 | 2016-11-03 | Musc Foundation For Research Development | Oxindole compounds and pharmaceutical compositions thereof |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| GB201508276D0 (en) | 2015-05-14 | 2015-06-24 | Electrophoretics Ltd | A casein kinase 1 delta inhibitor |
| GB201509134D0 (en) | 2015-05-28 | 2015-07-15 | Electrophoretics Ltd | Biomolecules involved in Alzheimer's disease |
| MX2017015456A (es) * | 2015-06-01 | 2018-11-29 | Bantam Pharmaceutical Llc | Compuestos de pirazol y pirrol sustituidos y metodos para su uso por inhibición de iniciación de traducción y tratamiento de enfermedades y trastornos relacionados con ellos. |
| WO2016202758A1 (en) | 2015-06-18 | 2016-12-22 | Bayer Pharma Aktiengesellschaft | Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds |
| WO2016202756A1 (en) | 2015-06-18 | 2016-12-22 | Bayer Pharma Aktiengesellschaft | Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds |
| WO2017004405A1 (en) * | 2015-07-01 | 2017-01-05 | Northwestern University | Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity |
| WO2017000277A1 (en) * | 2015-07-01 | 2017-01-05 | Merck Sharp & Dohme Corp. | Substituted triazolo bicycliccompounds as pde2 inhibitors |
| BR112018002553A8 (pt) | 2015-08-12 | 2023-01-24 | Incyte Corp | Sais de um inibidor de lsd1 |
| CN105061462B (zh) * | 2015-08-18 | 2017-05-24 | 沈阳药科大学 | 含有酰胺的四氢苯并[4,5]噻吩并[2,3‑d]嘧啶类化合物及其应用 |
| WO2017037146A1 (en) * | 2015-09-04 | 2017-03-09 | F. Hoffmann-La Roche Ag | Phenoxymethyl derivatives |
| KR20180052635A (ko) | 2015-09-18 | 2018-05-18 | 가켄 세이야쿠 가부시키가이샤 | 바이아릴 유도체 및 이를 포함하는 약제 |
| EP3353180B1 (en) | 2015-09-24 | 2022-03-16 | F. Hoffmann-La Roche AG | Bicyclic compounds as atx inhibitors |
| EP3353176B1 (en) | 2015-09-24 | 2022-01-19 | F. Hoffmann-La Roche AG | Bicyclic compounds as atx inhibitors |
| WO2017050747A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| MX372962B (es) | 2015-09-24 | 2020-03-27 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca). |
| GB201517523D0 (en) | 2015-10-05 | 2015-11-18 | Ostara Biomedical Ltd | Methods and compositions for managing reproduction |
| MX2018004109A (es) | 2015-10-05 | 2018-09-27 | Univ Columbia | Activadores de flujo autofágico y fosfolipasa d y depuración de acumulaciones de proteína que incluyen tau y tratamiento de proteinopatías. |
| WO2017063966A1 (en) | 2015-10-13 | 2017-04-20 | Bayer Pharma Aktiengesellschaft | Substituted 2-(1h-pyrazol-1-yl)-benzothiazole compounds |
| US10947239B2 (en) * | 2015-11-02 | 2021-03-16 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidin-7-yl compound |
| US10450274B2 (en) * | 2015-12-07 | 2019-10-22 | Hinova Pharmaceuticals Inc. | Quinoline compounds, preparation methods thereof, and uses thereof as urate transporter inhibitor drug |
| WO2017106367A1 (en) * | 2015-12-15 | 2017-06-22 | D.E. Shaw Research, Llc | Method of treating neurodegenerative disorders by rescuing alpha-synuclein toxicity |
| WO2017133258A1 (zh) * | 2016-02-04 | 2017-08-10 | 西华大学 | 1h-吲唑类衍生物及其作为ido抑制剂的用途 |
| CN107840826B (zh) * | 2016-09-19 | 2021-07-09 | 西华大学 | 1h-吲唑类衍生物及其作为ido抑制剂的用途 |
| CN107033087B (zh) * | 2016-02-04 | 2020-09-04 | 西华大学 | 1h-吲唑-4-胺类化合物及其作为ido抑制剂的用途 |
| PE20190377A1 (es) | 2016-04-22 | 2019-03-08 | Incyte Corp | Formulaciones de un inhibidor de lsd 1 |
| WO2017210545A1 (en) | 2016-06-02 | 2017-12-07 | Cadent Therapeutics, Inc. | Potassium channel modulators |
| CA3026784A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Heterocyclic pyrazine derivatives useful as shp2 inhibitors |
| BR112018077021A2 (pt) | 2016-06-24 | 2019-04-02 | Infinity Pharmaceuticals, Inc. | terapias de combinação |
| MX2019000536A (es) | 2016-07-14 | 2019-04-01 | Pfizer | Nuevas pirimidinas carboxamidas como inhibidores de enzima vanina-1. |
| ES2901059T3 (es) * | 2016-08-09 | 2022-03-21 | Zincure Corp | Composición farmacéutica para el tratamiento de apoplejía basado en la inhibición de AMPK |
| JP7471818B2 (ja) | 2016-08-18 | 2024-04-22 | ヴィダック ファーマ リミテッド | ピペラジン誘導体、医薬組成物、及びその使用方法 |
| KR102568384B1 (ko) | 2016-09-02 | 2023-08-22 | 사이클리온 테라퓨틱스, 인크. | 융합된 비시클릭 sGC 자극제 |
| CN106432235B (zh) * | 2016-10-19 | 2018-02-02 | 南通大学 | 靶向CDK和DNA的β‑咔啉衍生物及其制备方法和医药用途 |
| CN110099898B (zh) | 2016-10-24 | 2023-07-25 | 优曼尼蒂治疗公司 | 化合物及其用途 |
| WO2018083098A1 (en) | 2016-11-02 | 2018-05-11 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as pde2 inhibitors |
| AU2017353315B2 (en) | 2016-11-02 | 2021-09-16 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
| US11319321B2 (en) | 2016-11-02 | 2022-05-03 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[1,5-a]pyrimidine compounds as PDE2 inhibitors |
| EP3538101B1 (en) | 2016-11-14 | 2024-06-19 | Virginia Commonwealth University | Inhibitors of cancer and/or metastasis |
| WO2018094106A2 (en) | 2016-11-16 | 2018-05-24 | University Of South Florida | ALLOSTERIC ANTAGONISTS OF GPRC6a AND THEIR USE IN MITIGATING PROTEINOPATHIES |
| CN110392833A (zh) | 2017-01-06 | 2019-10-29 | 优曼尼蒂治疗公司 | 治疗神经病症的方法 |
| CN110494136A (zh) * | 2017-01-10 | 2019-11-22 | 瑞士苏黎世联邦理工学院 | 细胞保护性化合物及其用途 |
| SI3571193T1 (sl) | 2017-01-23 | 2022-04-29 | Cadent Therapeutics, Inc. | Modulatorji kalijevega kanalčka |
| CN106748969B (zh) * | 2017-01-23 | 2019-06-18 | 南阳师范学院 | 一种n-(4-苄基哌啶基)-阿魏酰胺化合物、制备方法及其用途 |
| CN106831573B (zh) * | 2017-01-23 | 2019-05-24 | 南阳师范学院 | (n-1,2,3,4-四氢异喹啉基)-阿魏酰胺化合物、制备方法及其应用 |
| WO2018139527A1 (ja) | 2017-01-26 | 2018-08-02 | 小野薬品工業株式会社 | キノリン誘導体のエタンスルホン酸塩 |
| WO2018142393A1 (en) * | 2017-02-01 | 2018-08-09 | Yissum Research Development Company Of The Hebrew | N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer |
| CN109846879B (zh) * | 2017-03-01 | 2021-06-29 | 浙江大学 | 亚胺结构类型雄激素受体拮抗剂及其应用 |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| KR20190129924A (ko) | 2017-03-16 | 2019-11-20 | 에프. 호프만-라 로슈 아게 | 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서 유용한 헤테로환형 화합물 |
| SMT201900517T1 (it) | 2017-03-20 | 2019-11-13 | Forma Therapeutics Inc | Composizioni di pirrolopirrolo come attivatori di piruvato chinasi (pkr) |
| MY200227A (en) | 2017-03-23 | 2023-12-15 | Jacobio Pharmaceuticals Co Ltd | Novel heterocyclic derivatives useful as shp2 inhibitors |
| WO2018197475A1 (en) | 2017-04-26 | 2018-11-01 | Basilea Pharmaceutica International AG | Processes for the preparation of furazanobenzimidazoles and crystalline forms thereof |
| WO2018209267A2 (en) * | 2017-05-12 | 2018-11-15 | Board Of Trustees Of The Southern Illinois University On Behalf Of Southern Illinois University Edwardsville | 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| JOP20190282A1 (ar) | 2017-06-09 | 2019-12-05 | Novartis Ag | مركبات وتركيبات لحث تكوّن الغضاريف |
| JP2020523379A (ja) * | 2017-06-14 | 2020-08-06 | ヨーロピアン モレキュラー バイオロジー ラボラトリーEuropean Molecular Biology Laboratory | 治療への使用のためのベンゾフランアミドおよびそれらの複素芳香族アナログ |
| EP3641545A4 (en) | 2017-06-21 | 2021-02-24 | Mitokinin, Inc. | COMPOSITIONS AND METHODS USING THEM FOR THE TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE |
| GB201710851D0 (en) * | 2017-07-06 | 2017-08-23 | Galápagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis |
| PL3651766T3 (pl) | 2017-07-10 | 2025-03-03 | Celgene Corporation | 4-(4-(4-(((2-(2,6-dioksopiperydyn-3-ylo)-1-oksoizoindolin-4-ylo)oksy)metylo)benzylo)piperazyn-1-ylo)-3-fluorobenzonitryl jako związek przeciwproliferacyjny |
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| KR102603365B1 (ko) * | 2017-09-11 | 2023-11-16 | 호도가야 가가쿠 고교 가부시키가이샤 | 피리미딘 고리 구조를 갖는 화합물 및 유기 일렉트로 루미네선스 소자 |
| TWI795440B (zh) | 2017-09-15 | 2023-03-11 | 美商佛瑪治療公司 | 作為CBP/p300抑制劑之四氫─咪唑並喹啉化合物 |
| WO2019074116A1 (ja) | 2017-10-13 | 2019-04-18 | 小野薬品工業株式会社 | Axl阻害剤を有効成分として含む固形がん治療剤 |
| MA50413A (fr) | 2017-10-19 | 2020-08-26 | Amgen Inc | Dérivés de benzimidazole et leurs utilisations |
| WO2019084157A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | COMPOUNDS AND USES THEREOF |
| CN111655669A (zh) * | 2017-12-21 | 2020-09-11 | 格利亚制药股份公司 | 治疗包括运动神经元疾病的神经紊乱的组合物和方法 |
| EP3728201A1 (en) * | 2017-12-21 | 2020-10-28 | Gliapharm SA | Compositions and methods of treatment for neurological disorders comprising a dementia |
| KR20200139153A (ko) | 2018-02-27 | 2020-12-11 | 인사이트 코포레이션 | A2a / a2b 억제제로서의 이미다조피리미딘 및 트리아졸로피리미딘 |
| EP3762383B1 (en) * | 2018-03-06 | 2023-12-06 | The United States of America, as represented by the Secretary, Department of Health and Human Services | Positive allosteric modulators of dopamine 1 receptor and method of use thereof |
| EP3543231A1 (en) * | 2018-03-19 | 2019-09-25 | ETH Zurich | Compounds for treating cns- and neurodegenerative diseases |
| CN112312913B (zh) | 2018-03-23 | 2024-03-08 | 詹森药业有限公司 | 化合物和其用途 |
| SMT202400507T1 (it) | 2018-05-04 | 2025-01-14 | Incyte Corp | Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| TWI815887B (zh) * | 2018-05-15 | 2023-09-21 | 美商愛彼特生物製藥股份有限公司 | 經取代的2,2'-雙嘧啶基化合物、其類似物及其使用方法 |
| CA3100731A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| SG11202011680YA (en) | 2018-06-01 | 2020-12-30 | Incyte Corp | Dosing regimen for the treatment of pi3k related disorders |
| GB201810092D0 (en) | 2018-06-20 | 2018-08-08 | Ctxt Pty Ltd | Compounds |
| GB201810581D0 (en) | 2018-06-28 | 2018-08-15 | Ctxt Pty Ltd | Compounds |
| CN116178369A (zh) | 2018-06-29 | 2023-05-30 | 福马疗法公司 | 抑制creb结合蛋白(cbp) |
| CA3105721A1 (en) | 2018-07-05 | 2020-01-09 | Incyte Corporation | Fused pyrazine derivatives as a2a / a2b inhibitors |
| US12195432B2 (en) * | 2018-08-06 | 2025-01-14 | The Board Of Trustees Of The Leland Stanford Junior University | 2-arylbenzimidazoles as Ppargc1a activators for treating neurodegenerative diseases |
| CA3109498A1 (en) | 2018-08-29 | 2020-03-05 | Chemocentryx, Inc. | Combination therapy using c-c chemokine receptor 4 (ccr4) antagonists and one or more immune checkpoint inhibitors |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| US11278527B2 (en) | 2018-09-04 | 2022-03-22 | Brown University | Compositions and methods for the modulation of the corticotropin releasing factor binding protein and the treatment of alcohol use disorder |
| BR112021005082A2 (pt) | 2018-09-18 | 2021-06-08 | Nikang Therapeutics, Inc. | derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase |
| US11001588B2 (en) | 2018-09-19 | 2021-05-11 | Forma Therapeutics, Inc. | Activating pyruvate kinase R and mutants thereof |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| WO2020086456A1 (en) | 2018-10-22 | 2020-04-30 | Cadent Therapeutics, Inc. | Crystalline forms of potassium channel modulators |
| TWI828783B (zh) * | 2018-10-23 | 2024-01-11 | 日商第一三共股份有限公司 | 聯芳基衍生物及其用途 |
| AU2019374731B2 (en) | 2018-11-07 | 2025-08-21 | Tianli Biotech Pty Ltd | Compounds and compositions for the treatment of respiratory diseases |
| CN109503563B (zh) * | 2018-12-10 | 2020-05-12 | 济南大学 | 多功能乙酰胆碱酯酶抑制剂及其应用 |
| KR102128509B1 (ko) * | 2018-12-19 | 2020-07-01 | 한국과학기술연구원 | 말단 아민기에 아릴 또는 헤테로아릴기가 치환된 신규한 히드라존 유도체 및 이의 용도 |
| JP7507162B2 (ja) * | 2019-01-04 | 2024-06-27 | ベルブルック ラボズ,エルエルシー | 治療薬としてのcGAS活性の阻害剤 |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| CN113906019A (zh) | 2019-01-24 | 2022-01-07 | 优曼尼蒂治疗公司 | 化合物及其用途 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| AR118362A1 (es) | 2019-03-15 | 2021-09-29 | Forma Therapeutics Inc | Inhibición de la proteína de unión al elemento de respuesta a amp cíclico (creb) |
| CN114072395A (zh) | 2019-04-26 | 2022-02-18 | 新基公司 | 杂环化合物及其治疗蠕虫感染和疾病的用途 |
| AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
| JP7352662B2 (ja) | 2019-06-18 | 2023-09-28 | ファイザー・インク | ベンゾイソオキサゾールスルホンアミド誘導体 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7721501B2 (ja) | 2019-07-31 | 2025-08-12 | 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 | Cd38の阻害剤としてのヘテロ二環式アミド |
| RU2746423C2 (ru) * | 2019-09-02 | 2021-04-13 | Общество с ограниченной ответственностью "Научно-исследовательский институт ХимРар" (ООО "НИИ ХимРар") | Ингибитор вируса гепатита В (ВГВ) |
| MX2022003254A (es) | 2019-09-19 | 2022-04-18 | Forma Therapeutics Inc | Composiciones activadoras de piruvato cinasa r (pkr). |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| US12343335B2 (en) | 2019-11-14 | 2025-07-01 | Zincure Corp. | Pharmaceutical composition for treating multiple sclerosis on basis of AMPK inhibitory function and zinc homeostasis control function |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| US11897891B2 (en) | 2019-12-04 | 2024-02-13 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| HRP20241695T1 (hr) | 2019-12-06 | 2025-02-14 | Vertex Pharmaceuticals Incorporated | Supstituirani tetrahidrofurani kao modulatori natrijevih kanala |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| AR122711A1 (es) | 2020-06-25 | 2022-09-28 | Alchemedicine Inc | COMPUESTO HETEROCÍCLICO COMO INHIBIDOR DE CASEÍNA QUINASA 1d Y/O QUINASA 5 TIPO RECEPTOR DE ACTIVINA |
| AU2021325872A1 (en) * | 2020-08-10 | 2023-03-16 | Dana-Farber Cancer Institute, Inc. | Substituted 1,2,4-oxadiazoles as small molecule inhibitors of ubiquitin-specific protease 28 |
| US20230339900A1 (en) * | 2020-09-17 | 2023-10-26 | Janssen Pharmaceutica Nv | Casein kinase 1 delta modulators |
| US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
| US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
| WO2022175752A1 (en) | 2021-02-19 | 2022-08-25 | Sudo Biosciences Limited | Tyk2 inhibitors and uses thereof |
| WO2022175747A1 (en) | 2021-02-19 | 2022-08-25 | Sudo Biosciences Limited | Tyk2 inhibitors and uses thereof |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CN117177974A (zh) * | 2021-04-21 | 2023-12-05 | 长春金赛药业有限责任公司 | 含咪唑稠环类衍生物、其制备方法及其在医药上的应用 |
| KR20240031300A (ko) | 2021-06-04 | 2024-03-07 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널 조절제로서의 n-(하이드록시알킬 (헤테로)아릴) 테트라하이드로푸란 카르복스아미드 |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN118076605A (zh) * | 2021-10-15 | 2024-05-24 | 洛蒙治疗公司 | 经取代的1H-吡唑并[4,3-c]喹啉、制备方法及其用途 |
| CN115466211B (zh) * | 2022-06-09 | 2024-02-23 | 中国人民解放军空军军医大学 | 一种n-苯基喹啉-4-胺类化合物及其应用 |
| WO2024012554A1 (zh) * | 2022-07-14 | 2024-01-18 | 上海日馨医药科技股份有限公司 | Tpk激动剂及使用其治疗神经退行性疾病的方法 |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
| JP2025528595A (ja) * | 2022-10-19 | 2025-08-28 | 長春金賽薬業有限責任公司 | Nk3rアンタゴニストの結晶形及びその調製方法と用途 |
| CN120917015A (zh) * | 2023-01-20 | 2025-11-07 | 元启(苏州)生物制药有限公司 | Srpk1抑制剂和使用方法 |
| AR131690A1 (es) * | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y LOS KITS |
| EP4660182A1 (en) * | 2023-01-30 | 2025-12-10 | Eurofarma Laboratórios S.A. | Nav1.7- and/or nav1.8-inhibiting aryl pyridine compounds, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits |
| CN118666857B (zh) * | 2024-06-26 | 2025-02-25 | 江西农业大学 | 一种喹啉类化合物及其在农用杀菌剂中的应用 |
| CN119060061B (zh) * | 2024-08-26 | 2025-09-16 | 浙江师范大学 | 一类苯并嘧啶硫醚类化合物作为sting蛋白小分子抑制剂的应用 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9506197D0 (en) | 1995-03-27 | 1995-05-17 | Hoffmann La Roche | Inhibition of tau-tau association. |
| US5545656A (en) * | 1995-04-05 | 1996-08-13 | Pfizer Inc. | 2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease |
| US20030219427A1 (en) * | 1998-08-18 | 2003-11-27 | Allen Hamish J. | TPL-2/COT kinase and methods of use |
| US6184226B1 (en) * | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| US6087363A (en) * | 1999-07-16 | 2000-07-11 | Harbor Branch Oceanographic Institution, Inc. | Use of imidazole and indole compounds as inhibitors of nitric oxide synthase |
| AR030587A1 (es) * | 2000-09-01 | 2003-08-27 | Sanofi Aventis | Derivados de 2-piridinil-6,7,8,9-tetrahidropirimido[1,2-a]pirimidin-4-ona y 7-piridinil-2,3-dihidroimidazo[1,2-a]pirimidin-5(1h)-ona |
| EP1318814B1 (en) * | 2000-09-15 | 2007-05-30 | Vertex Pharmaceuticals Incorporated | Triazole compounds useful as protein kinase inhibitors |
| EP1345914A1 (en) * | 2000-12-22 | 2003-09-24 | AstraZeneca AB | Therapeutic compounds |
| EP1458383B1 (en) * | 2001-12-18 | 2007-11-21 | Merck & Co., Inc. | Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
| JP2003212859A (ja) * | 2002-01-24 | 2003-07-30 | Nippon Nohyaku Co Ltd | 置換フェニルヘテロ環類及びこれを有効成分とする除草剤 |
| KR20040091113A (ko) * | 2002-03-08 | 2004-10-27 | 일라이 릴리 앤드 캄파니 | 피롤-2,5-디온 유도체 및 gsk-3 억제제로서 그의 용도 |
| FR2836915B1 (fr) * | 2002-03-11 | 2008-01-11 | Aventis Pharma Sa | Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant |
| AU2003229305A1 (en) * | 2002-05-17 | 2003-12-02 | Scios, Inc. | TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS |
| WO2003106439A1 (ja) * | 2002-06-12 | 2003-12-24 | 株式会社ビーエフ研究所 | アミロイド蓄積性疾患の画像診断プローブ化合物、老人斑/びまん性老人斑染色用化合物、ならびにアミロイド蓄積性疾患の治療薬 |
| CL2004000409A1 (es) * | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
| US7060698B2 (en) * | 2003-05-19 | 2006-06-13 | Hoffmann-La Roche Inc. | Benzoxazepinone derivatives |
| CA2535980A1 (en) * | 2003-06-06 | 2005-01-06 | The Trustees Of The University Of Pennsylvania | P38 kinase inhibitor compositions and methods of use |
| GB0314943D0 (en) | 2003-06-25 | 2003-07-30 | Proteome Sciences Plc | Screening methods |
| ATE485824T1 (de) * | 2004-04-13 | 2010-11-15 | Icagen Inc | Polycyclische pyrimidine als kaliumionenkanal- modulatoren |
| MX2007001077A (es) * | 2004-08-19 | 2007-04-17 | Aventis Pharma Inc | Derivados de 3-ariltioindol-2-carboxamida y analogos de los mismos como inhibidores de caseina quinasa ie. |
| WO2007015866A2 (en) * | 2005-07-20 | 2007-02-08 | Kalypsys, Inc. | Inhibitors of p38 kinase and methods of treating inflammatory disorders |
| EP1842541A1 (en) * | 2006-03-29 | 2007-10-10 | G.I.M.-Gesellschaft Für Innovative Medizin Gmbh Nfg Ohg | Plant components and extracts and uses thereof |
| TW200813035A (en) * | 2006-06-19 | 2008-03-16 | Astrazeneca Ab | Novel heteroaryl substituted benzoxazoles |
| KR20090031913A (ko) * | 2006-06-21 | 2009-03-30 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 세포 증식 억제제로서의 피라지논 |
| US7622495B2 (en) * | 2006-10-03 | 2009-11-24 | Neurim Pharmaceuticals (1991) Ltd. | Substituted aryl-indole compounds and their kynurenine/kynuramine-like metabolites as therapeutic agents |
| CN101535292A (zh) * | 2006-11-02 | 2009-09-16 | 弗·哈夫曼-拉罗切有限公司 | 作为痕量胺相关受体的调节剂的取代的2-咪唑类化合物 |
| US8362066B2 (en) * | 2006-11-17 | 2013-01-29 | Treventis Corporation | Compounds and methods for treating protein folding disorders |
| WO2008077138A1 (en) * | 2006-12-19 | 2008-06-26 | The Board Of Trustees Of The University Of Illinois | 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders |
| WO2008156715A1 (en) * | 2007-06-20 | 2008-12-24 | Merck & Co., Inc. | Cetp inhibitors derived from benzoxazole arylamides |
| FR2918061B1 (fr) * | 2007-06-28 | 2010-10-22 | Sanofi Aventis | Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique. |
| FR2918986B1 (fr) * | 2007-07-19 | 2009-09-04 | Sanofi Aventis Sa | Derives de 6-cycloamino-3-(pyridazin-4-yl)imidazo[1,2-b]- pyridazine, leur preparation et leur application en therapeutique |
| GB0715939D0 (en) * | 2007-08-15 | 2007-09-26 | Vastox Plc | Method of treatment of duchenne muscular dystrophy |
| US20110065715A1 (en) * | 2007-11-28 | 2011-03-17 | Yale University | Nogo Receptor Binding Small Molecules to Promote Axonal Growth |
| EP2219646A4 (en) * | 2007-12-21 | 2010-12-22 | Univ Rochester | PROCESS FOR EXTENDING THE LIFE OF EUKARYOTIC ORGANISMS |
| EP2149551A1 (de) | 2008-07-30 | 2010-02-03 | Bayer Schering Pharma AG | N-(Indol-3-ylalkyl)-(hetero)arylamidderivate als Modulatoren des EP2-Rezeptors |
| FR2934994B1 (fr) * | 2008-08-12 | 2010-09-17 | Sanofi Aventis | Derives de 2-alkyl-6cycloamino-3-(pyridin-4-yl)imidaz°1,2-b! pyridazine, leur preparation et leur application en therapeutique |
| KR101257695B1 (ko) * | 2008-12-24 | 2013-04-24 | 제일모직주식회사 | 신규한 유기광전소자용 화합물 및 이를 포함하는 유기광전소자 |
| FR2945289A1 (fr) * | 2009-05-11 | 2010-11-12 | Sanofi Aventis | Derives de 2-cycloamino-5-(pyridin-4-yl)imidazo°2,1-b! °1,3,4!thiadiazole, leur preparation et leur application en therapeutique |
| JP2013518046A (ja) * | 2010-01-25 | 2013-05-20 | シーエイチディーアイ ファウンデーション,インコーポレーテッド | 特定のキヌレニン−3−モノオキシゲナーゼインヒビターおよびその医薬組成物ならびにこれらの使用方法 |
| CN103298460B (zh) * | 2010-12-14 | 2016-06-01 | 电泳有限公司 | 酪蛋白激酶1δ(CK1δ)抑制剂 |
| JP5851022B2 (ja) | 2011-05-09 | 2016-02-03 | イーアイピー ファーマ, エルエルシー | アルツハイマー病を処置するための組成物および方法 |
-
2011
- 2011-12-14 CN CN201180060132.8A patent/CN103298460B/zh not_active Expired - Fee Related
- 2011-12-14 US US13/993,288 patent/US20140031547A1/en not_active Abandoned
- 2011-12-14 EP EP11804754.7A patent/EP2651404B1/en not_active Not-in-force
- 2011-12-14 ES ES11804754.7T patent/ES2553610T3/es active Active
- 2011-12-14 WO PCT/GB2011/052475 patent/WO2012080729A2/en not_active Ceased
- 2011-12-14 EP EP11804755.4A patent/EP2651405A2/en not_active Withdrawn
- 2011-12-14 ES ES14190691.7T patent/ES2650744T3/es active Active
- 2011-12-14 WO PCT/GB2011/052473 patent/WO2012080727A2/en not_active Ceased
- 2011-12-14 JP JP2013543879A patent/JP5937102B2/ja not_active Expired - Fee Related
- 2011-12-14 JP JP2013543881A patent/JP2014503528A/ja active Pending
- 2011-12-14 US US13/993,303 patent/US20140018540A1/en not_active Abandoned
- 2011-12-14 CN CN201610264700.0A patent/CN105920010A/zh active Pending
- 2011-12-14 EP EP14190691.7A patent/EP2835131B1/en not_active Not-in-force
- 2011-12-14 CA CA2818903A patent/CA2818903C/en active Active
- 2011-12-14 AU AU2011343039A patent/AU2011343039B2/en not_active Ceased
- 2011-12-14 CN CN201510246272.4A patent/CN104906103B/zh not_active Expired - Fee Related
- 2011-12-14 DK DK14190691.7T patent/DK2835131T3/en active
-
2015
- 2015-04-02 US US14/677,273 patent/US9789111B2/en active Active
- 2015-09-01 US US14/842,155 patent/US9763947B2/en active Active
-
2016
- 2016-03-07 HK HK16102571.5A patent/HK1214527A1/zh unknown
- 2016-05-11 JP JP2016095027A patent/JP6243472B2/ja active Active
- 2016-06-02 US US15/171,582 patent/US20160354375A1/en not_active Abandoned
- 2016-09-08 JP JP2016175298A patent/JP2017025080A/ja not_active Withdrawn
-
2017
- 2017-02-06 AU AU2017200812A patent/AU2017200812B2/en not_active Ceased
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2553610T3 (es) | Inhibidores de la caseína cinasa 1 delta (CK1delta) | |
| ES2575914T3 (es) | Derivados condensados de aminodihidrotiazina como inhibidores de BACE | |
| US11548893B2 (en) | Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection | |
| ES2750956T3 (es) | Ciclopropilaminas como inhibidores de LSD1 | |
| ES2578735T3 (es) | Isotiazolopiridinonas útiles para el tratamiento de (entre otros) fibrosis quística | |
| ES2645095T3 (es) | Tratamiento de enfermedades neurodegenerativas a través de la inhibición de Hsp90 | |
| ES2886910T3 (es) | Cristal de pirrolopirimidina para preparar inhibidor de JAK | |
| US20090221647A1 (en) | N-(2-thiazolyl)-amide derivatives as gsk-3 inhibitors | |
| BRPI0712882A2 (pt) | pirrolopirimidinas para composições farmacêuticas | |
| BRPI0712132A2 (pt) | pirido[3,2-e] pirazinas, uso das mesmas como inibidores de fosfodiesterase 10 e processos para a preparação das mesmas | |
| KR20150128768A (ko) | 시르투인 조절제로서의 티에노[3,2-d]피리미딘-6-카르복스아미드 및 유사체 | |
| ES2676698T3 (es) | Compuestos de carbolina útiles en el tratamiento de enfermedades neurodegenerativas | |
| EA038796B1 (ru) | Индолиноновые соединения и их применение в лечении фиброзных заболеваний | |
| BR112017021507B1 (pt) | Uso de um inibidor seletivo ppp1r115b e de uma composição farmacêutica compreendendo o mesmo para tratar uma doença associada ao acúmulo de proteínas mal enoveladas | |
| ES2956036T3 (es) | Forma sólida de (S)-[2-cloro-4-fluoro-5-(7-morfolin-4-il-quinazolin-4-il)fenil]-(6-metoxi-piridazin-3-il)-metanol | |
| ES2808669T3 (es) | Compuestos inhibidores de la acetilcolinesterasa y agonistas de los receptores serotoninérgicos 5HT4, con efecto paramnesiante, sus procedimientos de preparación y composiciones farmacéuticas que los contienen | |
| ES2749743B2 (es) | Derivados de purina inhibidores de cdc7 y su uso para el tratamiento de patologias neurologicas | |
| ES2715960T3 (es) | Nuevo derivado de 1,4-bis(3-aminopropil)piperazina y su uso | |
| CN120463687A (zh) | 具有jnk抑制活性的嘧啶类衍生物及其应用 | |
| Zhang et al. | Part 3: Notch-sparing γ-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones | |
| ES2681285T3 (es) | Compuestos de aminotiazina | |
| ES2610206B1 (es) | Aminofenotiazinas para la modulación del número de sinapsis | |
| ES2526580B1 (es) | Uso de un compuesto de fórmula (I) como bactericida frente a Streptococcus | |
| US20250186373A1 (en) | Targeting an eukaryotic initiation factor 2 alpha kinase to regulate translation under stress | |
| ES2781377B2 (es) | Compuestos derivados de 2-iodo-7-(((2-(5-metoxi-1h-indol-3-il)etil)amino)metil)-1-alquil/aril-6,7,7a,8-tetrahidro-3h-pirrolo[2,1-j]quinolina-3,9(5h)-diona como agentes antioxidantes, inductores de nrf2 y moduladores nicotinicos para el tratamiento de enfermedades neurodegenerativas |