ZA200401846B - Ihibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma. - Google Patents
Ihibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma. Download PDFInfo
- Publication number
- ZA200401846B ZA200401846B ZA200401846A ZA200401846A ZA200401846B ZA 200401846 B ZA200401846 B ZA 200401846B ZA 200401846 A ZA200401846 A ZA 200401846A ZA 200401846 A ZA200401846 A ZA 200401846A ZA 200401846 B ZA200401846 B ZA 200401846B
- Authority
- ZA
- South Africa
- Prior art keywords
- amino
- triazole
- anilino
- phenylaminothiazol
- methanone
- Prior art date
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- 102000001267 GSK3 Human genes 0.000 title claims description 50
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 title claims description 50
- 208000010412 Glaucoma Diseases 0.000 title description 19
- 239000000203 mixture Substances 0.000 claims description 44
- 239000003112 inhibitor Substances 0.000 claims description 33
- 150000001875 compounds Chemical class 0.000 claims description 31
- 230000004410 intraocular pressure Effects 0.000 claims description 20
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- -1 (4-amino-2-phenylaminothiazol-5-yl)-3-fluorophenyl Chemical group 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- LJVQHXICFCZRJN-UHFFFAOYSA-N 1h-1,2,4-triazole-5-carboxylic acid Chemical class OC(=O)C1=NC=NN1 LJVQHXICFCZRJN-UHFFFAOYSA-N 0.000 claims description 8
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 claims description 8
- WKXCZMFWXZRMEZ-UHFFFAOYSA-N 1,3-thiazole-2,4-diamine Chemical class NC1=CSC(N)=N1 WKXCZMFWXZRMEZ-UHFFFAOYSA-N 0.000 claims description 7
- AQNWXPHYWRBUPD-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-(3-bromophenyl)methanone Chemical compound N=1N(C(=O)C=2C=C(Br)C=CC=2)C(N)=NC=1NC1=CC=CC=C1 AQNWXPHYWRBUPD-UHFFFAOYSA-N 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- QPCBNXNDVYOBIP-WHFBIAKZSA-N hymenialdisine Chemical group NC1=NC(=O)C([C@@H]2[C@@H]3C=C(Br)N=C3C(=O)NCC2)=N1 QPCBNXNDVYOBIP-WHFBIAKZSA-N 0.000 claims description 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 230000000699 topical effect Effects 0.000 claims description 6
- ATBAETXFFCOZOY-UHFFFAOYSA-N hymenialdisine Natural products N1C(N)=NC(=O)C1=C1C(C=C(Br)N2)=C2C(=O)NCC1 ATBAETXFFCOZOY-UHFFFAOYSA-N 0.000 claims description 5
- VGMDAWVZNAXVDG-UHFFFAOYSA-N paullone Chemical class C12=CC=CC=C2NC(=O)CC2=C1NC1=CC=CC=C21 VGMDAWVZNAXVDG-UHFFFAOYSA-N 0.000 claims description 5
- JYRJOQGKGMHTOO-UHFFFAOYSA-N Debromohymenialdisine hydrochloride Natural products N1C(N)=NC(=O)C1=C1C(C=CN2)=C2C(=O)NCC1 JYRJOQGKGMHTOO-UHFFFAOYSA-N 0.000 claims description 4
- KIUKVBCITYHMSN-UHFFFAOYSA-N (3-amino-5-anilinothiophen-2-yl)-(4-fluorophenyl)methanone Chemical compound S1C(C(=O)C=2C=CC(F)=CC=2)=C(N)C=C1NC1=CC=CC=C1 KIUKVBCITYHMSN-UHFFFAOYSA-N 0.000 claims description 3
- CBRJQALCGJQKIP-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-(2-methoxyphenyl)methanone Chemical compound COC1=CC=CC=C1C(=O)C1=C(N)N=C(NC=2C=CC=CC=2)S1 CBRJQALCGJQKIP-UHFFFAOYSA-N 0.000 claims description 3
- LXKAYWZVBXYTGU-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-(3-methoxyphenyl)methanone Chemical compound COC1=CC=CC(C(=O)C2=C(N=C(NC=3C=CC=CC=3)S2)N)=C1 LXKAYWZVBXYTGU-UHFFFAOYSA-N 0.000 claims description 3
- OUEOKGGLZBYZLG-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-(4-chloro-3-methylphenyl)methanone Chemical compound C1=C(Cl)C(C)=CC(C(=O)C2=C(N=C(NC=3C=CC=CC=3)S2)N)=C1 OUEOKGGLZBYZLG-UHFFFAOYSA-N 0.000 claims description 3
- MWRZPNGRLYXGKP-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-(4-methoxyphenyl)methanone Chemical compound C1=CC(OC)=CC=C1C(=O)C1=C(N)N=C(NC=2C=CC=CC=2)S1 MWRZPNGRLYXGKP-UHFFFAOYSA-N 0.000 claims description 3
- SJYNBJHBIDSODI-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-(4-phenylphenyl)methanone Chemical compound S1C(C(=O)C=2C=CC(=CC=2)C=2C=CC=CC=2)=C(N)N=C1NC1=CC=CC=C1 SJYNBJHBIDSODI-UHFFFAOYSA-N 0.000 claims description 3
- YLSSZUIMVBZWMK-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-cyclopropylmethanone Chemical compound S1C(C(=O)C2CC2)=C(N)N=C1NC1=CC=CC=C1 YLSSZUIMVBZWMK-UHFFFAOYSA-N 0.000 claims description 3
- YOZXSIIEHFGLLO-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-phenylmethanone Chemical compound S1C(C(=O)C=2C=CC=CC=2)=C(N)N=C1NC1=CC=CC=C1 YOZXSIIEHFGLLO-UHFFFAOYSA-N 0.000 claims description 3
- BWPYRRUOUILTPU-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-pyridin-2-ylmethanone Chemical compound S1C(C(=O)C=2N=CC=CC=2)=C(N)N=C1NC1=CC=CC=C1 BWPYRRUOUILTPU-UHFFFAOYSA-N 0.000 claims description 3
- LERGLIZTDGVNRO-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-pyridin-3-ylmethanone Chemical compound S1C(C(=O)C=2C=NC=CC=2)=C(N)N=C1NC1=CC=CC=C1 LERGLIZTDGVNRO-UHFFFAOYSA-N 0.000 claims description 3
- XPKVIZDAFGYGOY-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-thiophen-2-ylmethanone Chemical compound S1C(C(=O)C=2SC=CC=2)=C(N)N=C1NC1=CC=CC=C1 XPKVIZDAFGYGOY-UHFFFAOYSA-N 0.000 claims description 3
- IFTIYGIGGFHYGS-UHFFFAOYSA-N (4-amino-2-anilino-1,3-thiazol-5-yl)-thiophen-3-ylmethanone Chemical compound S1C(C(=O)C2=CSC=C2)=C(N)N=C1NC1=CC=CC=C1 IFTIYGIGGFHYGS-UHFFFAOYSA-N 0.000 claims description 3
- XSDKWAUOJXYJGA-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-(1,3-benzodioxol-5-yl)methanone Chemical compound N=1N(C(=O)C=2C=C3OCOC3=CC=2)C(N)=NC=1NC1=CC=CC=C1 XSDKWAUOJXYJGA-UHFFFAOYSA-N 0.000 claims description 3
- JWHANWDZXLKUDX-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-(2-phenoxyphenyl)methanone Chemical compound N=1N(C(=O)C=2C(=CC=CC=2)OC=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC=C1 JWHANWDZXLKUDX-UHFFFAOYSA-N 0.000 claims description 3
- UJNJSOKQSPNASJ-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-(3,5-dichlorophenyl)methanone Chemical compound N=1N(C(=O)C=2C=C(Cl)C=C(Cl)C=2)C(N)=NC=1NC1=CC=CC=C1 UJNJSOKQSPNASJ-UHFFFAOYSA-N 0.000 claims description 3
- BMVYDSFWVQQGFZ-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-(4-chlorophenyl)methanone Chemical compound N=1N(C(=O)C=2C=CC(Cl)=CC=2)C(N)=NC=1NC1=CC=CC=C1 BMVYDSFWVQQGFZ-UHFFFAOYSA-N 0.000 claims description 3
- WNAZAYNAVGRRAW-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-[4-(trifluoromethyl)phenyl]methanone Chemical compound N=1N(C(=O)C=2C=CC(=CC=2)C(F)(F)F)C(N)=NC=1NC1=CC=CC=C1 WNAZAYNAVGRRAW-UHFFFAOYSA-N 0.000 claims description 3
- RBHFKINQTKFFAH-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-cyclohexylmethanone Chemical compound N=1N(C(=O)C2CCCCC2)C(N)=NC=1NC1=CC=CC=C1 RBHFKINQTKFFAH-UHFFFAOYSA-N 0.000 claims description 3
- GPWONEKAEXFDIJ-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-naphthalen-2-ylmethanone Chemical compound N=1N(C(=O)C=2C=C3C=CC=CC3=CC=2)C(N)=NC=1NC1=CC=CC=C1 GPWONEKAEXFDIJ-UHFFFAOYSA-N 0.000 claims description 3
- MDYVPKCEHAOTPR-UHFFFAOYSA-N (5-amino-3-anilino-1,2,4-triazol-1-yl)-phenylmethanone Chemical compound N=1N(C(=O)C=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC=C1 MDYVPKCEHAOTPR-UHFFFAOYSA-N 0.000 claims description 3
- ZIPTVBLEXXRQIA-UHFFFAOYSA-N 1-(3-amino-5-anilino-1,2,4-triazol-1-yl)-2-cyclopent-2-en-1-ylethanone Chemical compound C1CC=CC1CC(=O)N1N=C(N)N=C1NC1=CC=CC=C1 ZIPTVBLEXXRQIA-UHFFFAOYSA-N 0.000 claims description 3
- COIULFCMHXNEAK-UHFFFAOYSA-N 1-(3-amino-5-anilino-1,2,4-triazol-1-yl)-2-phenylethanone Chemical compound C=1C=CC=CC=1CC(=O)N1N=C(N)N=C1NC1=CC=CC=C1 COIULFCMHXNEAK-UHFFFAOYSA-N 0.000 claims description 3
- ZYCCMMGEMIRHJZ-UHFFFAOYSA-N 1-(4-amino-2-anilino-1,3-thiazol-5-yl)ethanone Chemical compound NC1=C(C(=O)C)SC(NC=2C=CC=CC=2)=N1 ZYCCMMGEMIRHJZ-UHFFFAOYSA-N 0.000 claims description 3
- MIJJYKPHIIBMBN-UHFFFAOYSA-N 1-(5-amino-3-anilino-1,2,4-triazol-1-yl)-2-(1h-indol-3-yl)ethanone Chemical compound N=1N(C(=O)CC=2C3=CC=CC=C3NC=2)C(N)=NC=1NC1=CC=CC=C1 MIJJYKPHIIBMBN-UHFFFAOYSA-N 0.000 claims description 3
- JQADZCNSJILHIF-UHFFFAOYSA-N 1-(5-amino-3-anilino-1,2,4-triazol-1-yl)-2-(4-fluorophenyl)ethanone Chemical compound N=1N(C(=O)CC=2C=CC(F)=CC=2)C(N)=NC=1NC1=CC=CC=C1 JQADZCNSJILHIF-UHFFFAOYSA-N 0.000 claims description 3
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- CLIBZBQUNLIVTN-UHFFFAOYSA-N 1-[5-amino-3-(3-chloroanilino)-1,2,4-triazol-1-yl]-3,3-diphenylpropan-1-one Chemical compound N=1N(C(=O)CC(C=2C=CC=CC=2)C=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC(Cl)=C1 CLIBZBQUNLIVTN-UHFFFAOYSA-N 0.000 claims description 3
- NJAIVALYSJBHKD-UHFFFAOYSA-N 1-[5-amino-3-(3-chloroanilino)-1,2,4-triazol-1-yl]-4-phenylbutane-1,4-dione Chemical compound N=1N(C(=O)CCC(=O)C=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC(Cl)=C1 NJAIVALYSJBHKD-UHFFFAOYSA-N 0.000 claims description 3
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- BRUXPEXNSDOYTJ-UHFFFAOYSA-N 4-[5-amino-3-(3-chloroanilino)-1,2,4-triazol-1-yl]-2-methyl-1-phenylbutane-1,4-dione Chemical compound C=1C=CC=CC=1C(=O)C(C)CC(=O)N(C(=N1)N)N=C1NC1=CC=CC(Cl)=C1 BRUXPEXNSDOYTJ-UHFFFAOYSA-N 0.000 claims description 3
- IEPJSURKNFXCPB-UHFFFAOYSA-N 5-amino-3-anilino-1,2,4-triazole-1-carboxylic acid;4-phenylbenzamide Chemical compound C1=CC(C(=O)N)=CC=C1C1=CC=CC=C1.OC(=O)N1C(N)=NC(NC=2C=CC=CC=2)=N1 IEPJSURKNFXCPB-UHFFFAOYSA-N 0.000 claims description 3
- FOXRJMAZHSGDLO-UHFFFAOYSA-N 5-amino-3-anilino-n-(3-methoxyphenyl)-1,2,4-triazole-1-carboxamide Chemical compound COC1=CC=CC(NC(=O)N2C(=NC(NC=3C=CC=CC=3)=N2)N)=C1 FOXRJMAZHSGDLO-UHFFFAOYSA-N 0.000 claims description 3
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- LPPMDPRPEQCOPW-UHFFFAOYSA-N 5-amino-3-anilino-n-cyclohexyl-1,2,4-triazole-1-carboxamide Chemical compound N=1N(C(=O)NC2CCCCC2)C(N)=NC=1NC1=CC=CC=C1 LPPMDPRPEQCOPW-UHFFFAOYSA-N 0.000 claims description 3
- DOBHLKAMPAQXKC-UHFFFAOYSA-N 5-amino-3-anilino-n-naphthalen-1-yl-1,2,4-triazole-1-carboxamide Chemical compound N=1N(C(=O)NC=2C3=CC=CC=C3C=CC=2)C(N)=NC=1NC1=CC=CC=C1 DOBHLKAMPAQXKC-UHFFFAOYSA-N 0.000 claims description 3
- KNUBLBZSYZLDJB-UHFFFAOYSA-N 5-amino-3-anilino-n-phenyl-1,2,4-triazole-1-carboxamide Chemical compound N=1N(C(=O)NC=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC=C1 KNUBLBZSYZLDJB-UHFFFAOYSA-N 0.000 claims description 3
- CWVPBBILDVOUCB-UHFFFAOYSA-N 5-amino-n-(4-chlorophenyl)-3-(4-methoxyanilino)-1,2,4-triazole-1-carboxamide Chemical compound C1=CC(OC)=CC=C1NC1=NN(C(=O)NC=2C=CC(Cl)=CC=2)C(N)=N1 CWVPBBILDVOUCB-UHFFFAOYSA-N 0.000 claims description 3
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims description 3
- 206010061323 Optic neuropathy Diseases 0.000 claims description 3
- SCUSPKIJTTXPKV-UHFFFAOYSA-N [3-(5-amino-3-anilino-1,2,4-triazole-1-carbonyl)phenyl]-phenylmethanone Chemical compound N=1N(C(=O)C=2C=C(C=CC=2)C(=O)C=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC=C1 SCUSPKIJTTXPKV-UHFFFAOYSA-N 0.000 claims description 3
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- 208000020911 optic nerve disease Diseases 0.000 claims description 3
- LEVJVKGPFAQPOI-UHFFFAOYSA-N phenylmethanone Chemical compound O=[C]C1=CC=CC=C1 LEVJVKGPFAQPOI-UHFFFAOYSA-N 0.000 claims description 3
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- 229940124530 sulfonamide Drugs 0.000 claims description 3
- 150000003456 sulfonamides Chemical class 0.000 claims description 3
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- JNTYRUUIWJEEJL-UHFFFAOYSA-N 1-(5-amino-3-anilino-1,2,4-triazol-1-yl)-2-(4-phenylphenyl)ethanone Chemical compound N=1N(C(=O)CC=2C=CC(=CC=2)C=2C=CC=CC=2)C(N)=NC=1NC1=CC=CC=C1 JNTYRUUIWJEEJL-UHFFFAOYSA-N 0.000 claims 2
- SSSBHYRKQGGOQM-UHFFFAOYSA-N 1-[3-amino-5-(3-chloroanilino)-1,2,4-triazol-1-yl]-2-phenylethanethione Chemical compound C=1C=CC=CC=1CC(=S)N1N=C(N)N=C1NC1=CC=CC(Cl)=C1 SSSBHYRKQGGOQM-UHFFFAOYSA-N 0.000 claims 2
- GDSXGXCSFWNMDA-UHFFFAOYSA-N 1-[4-(5-amino-3-anilino-1,2,4-triazole-1-carbonyl)phenyl]ethanone Chemical compound C1=CC(C(=O)C)=CC=C1C(=O)N1C(N)=NC(NC=2C=CC=CC=2)=N1 GDSXGXCSFWNMDA-UHFFFAOYSA-N 0.000 claims 2
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- 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
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32539001P | 2001-09-27 | 2001-09-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200401846B true ZA200401846B (en) | 2005-03-07 |
Family
ID=23267686
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200401846A ZA200401846B (en) | 2001-09-27 | 2004-03-05 | Ihibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucoma. |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US7598288B2 (fr) |
| EP (2) | EP1430120A4 (fr) |
| JP (2) | JP2005504101A (fr) |
| KR (1) | KR20040047824A (fr) |
| CN (2) | CN101380319A (fr) |
| AR (1) | AR036684A1 (fr) |
| AU (1) | AU2002334635B2 (fr) |
| BR (1) | BR0212924A (fr) |
| CA (1) | CA2460000C (fr) |
| MX (1) | MXPA04002137A (fr) |
| PL (1) | PL207022B1 (fr) |
| RU (1) | RU2297243C2 (fr) |
| TW (2) | TW201041580A (fr) |
| WO (1) | WO2003027275A1 (fr) |
| ZA (1) | ZA200401846B (fr) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2400543C (fr) * | 2001-08-31 | 2011-11-01 | Centre For Addiction And Mental Health | Role du gene bdnf dans les troubles de l'humeur |
| KR20040104566A (ko) | 2002-04-30 | 2004-12-10 | 알콘, 인코퍼레이티드 | 안압 저하 및 녹내장성 망막병증/시신경병증 치료를 위한특유의 수단으로서의 결합 조직 성장 인자 (ｃｔｇｆ)의활성 및/또는 발현 조절, 저해, 또는 변조제 |
| EP1925306A3 (fr) * | 2002-04-30 | 2008-09-17 | Alcon, Inc. | Agents regulant, inhibant ou modulant l'activite et/ou l'expression du facteur de croissance du tissu conjonctif (ctgf) pour reduire la pression intraoculaire |
| WO2004103958A2 (fr) | 2003-05-19 | 2004-12-02 | Michigan State University | Preparation de derives d'hymenialdisine et leur utilisation |
| MXPA06006862A (es) * | 2003-12-22 | 2007-01-26 | Alcon Inc | Agentes para el tratamiento de la retinopatia diabetica y formacion de drusen en degeneracion macular. |
| TW200526224A (en) * | 2003-12-22 | 2005-08-16 | Alcon Inc | Short form c-Maf transcription factor antagonists for treatment of glaucoma |
| DE602004005617T2 (de) * | 2003-12-22 | 2007-12-13 | Alcon Inc. | Mittel zur behandlung von glaukomatöser retinopathie und optischer neuropathie |
| CA2550891A1 (fr) * | 2003-12-24 | 2005-07-14 | Bayer Cropscience Gmbh | Regulation de la croissance d'une plante |
| US20080096238A1 (en) * | 2004-03-30 | 2008-04-24 | Alcon, Inc. | High throughput assay for human rho kinase activity with enhanced signal-to-noise ratio |
| WO2005102345A1 (fr) * | 2004-03-30 | 2005-11-03 | Alcon, Inc. | Utilisation d'inhibiteurs de kinase rho dans le traitement de deficits auditifs, d'acouphenes et dans l'amelioration de l'equilibre corporel |
| WO2005107465A1 (fr) * | 2004-05-12 | 2005-11-17 | Bayer Cropscience Gmbh | Regulation de la croissance vegetale |
| WO2006089874A1 (fr) * | 2005-02-22 | 2006-08-31 | Gpc Biotech Ag | BENZO[2,3]AZÉPINO[4,5-b]INDOL-6-ONES |
| WO2006099353A1 (fr) * | 2005-03-11 | 2006-09-21 | Alcon, Inc. | Inhibition de la proteine-1 apparentee a frizzled induite par l'arni pour le traitement du glaucome |
| EP1885454A2 (fr) | 2005-05-04 | 2008-02-13 | DeveloGen Aktiengesellschaft | Utilisation des inhibiteurs gsk-3 dans la prevention et le traitement des maladies auto-immunes pancreatiques |
| EP1757607A1 (fr) | 2005-08-24 | 2007-02-28 | Molisa GmbH | Benzo¬2,3|azepino¬4,5-b|indol-6-ones N5-substitués pour le traitement des maladies tropiques |
| EP1922310A2 (fr) | 2005-09-07 | 2008-05-21 | Rigel Pharmaceuticals, Inc. | Derives de triazole utiles comme inhibiteurs d'axl |
| EP2032130A4 (fr) * | 2006-06-12 | 2011-03-02 | Merck Sharp & Dohme | Compositions ophtalmiques pour traiter une hypertension oculaire |
| EP2114954B1 (fr) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Triazoles à substitution aryle bicycliques et hétéroaryle bicycliques utiles en tant qu'inhibiteurs axl |
| JP5567837B2 (ja) | 2006-12-29 | 2014-08-06 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌインヒビターとして有用なＮ３−ヘテロアリール置換トリアゾールおよびＮ５−ヘテロアリール置換トリアゾール |
| EP2114955B1 (fr) | 2006-12-29 | 2013-02-13 | Rigel Pharmaceuticals, Inc. | Triazoles substitués par aryle bicyclique ponté et hétéroaryle bicyclique ponté utilisés comme inhibiteurs d'axl |
| CN110551105B (zh) | 2006-12-29 | 2022-10-18 | 里格尔制药公司 | 用作axl抑制剂的取代三唑 |
| ME01832B (me) | 2006-12-29 | 2014-12-20 | Rigel Pharmaceuticals Inc | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| WO2009054864A1 (fr) | 2007-10-26 | 2009-04-30 | Rigel Pharmaceuticals, Inc. | Triazoles substitués par aryle polycyclique et triazoles substitués par hétéroaryle polycyclique utiles comme inhibiteurs d'axl |
| WO2010005876A2 (fr) | 2008-07-09 | 2010-01-14 | Rigel Pharmaceuticals, Inc. | Triazoles à substitution hétéroaryle polycycliques utiles en tant qu’inhibiteurs d’axl |
| WO2010005879A1 (fr) | 2008-07-09 | 2010-01-14 | Rigel Pharmaceuticals, Inc. | Triazoles substitués par hétéroaryle bicycliques pontés utiles comme inhibiteurs de axl |
| ES2528032T3 (es) | 2009-01-16 | 2015-02-03 | Rigel Pharmaceuticals, Inc. | Inhibidores de Axl para su uso en terapia de combinación para prevenir, tratar o manejar cáncer metastásico |
| UA103918C2 (en) * | 2009-03-02 | 2013-12-10 | Айерем Элелси | N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators |
| RU2456266C1 (ru) * | 2011-04-06 | 2012-07-20 | Максим Эдуардович Запольский | Производные 4,4'-бифениламидов, обладающие фармакологической активностью, и лекарственные средства на их основе |
| JP2016518815A (ja) | 2013-03-15 | 2016-06-30 | フンダシオ、インスティトゥト、デ、レセルカ、ビオメディカ（イエレベ、バルセロナ）Ｆｕｎｄａｃｉｏ Ｉｎｓｔｉｔｕｔ Ｄｅ Ｒｅｃｅｒｃａ Ｂｉｏｍｅｄｉｃａ （Ｉｒｂ Ｂａｒｃｅｌｏｎａ） | 転移性がんの診断、予後、および処置の方法 |
| US10143703B2 (en) | 2014-01-02 | 2018-12-04 | Massachusetts Eye And Ear Infirmary | Treating ocular neovascularization |
| WO2015155738A2 (fr) | 2014-04-09 | 2015-10-15 | Christopher Rudd | Utilisation d'inhibiteurs ou d'activateurs de gsk -3 qui modulent l'expression de pd -1 ou de t-bet pour moduler l'immunité due aux lymphocytes t |
| US10925889B2 (en) | 2014-05-12 | 2021-02-23 | Gholam A. Peyman | Method of treating, reducing, or alleviating a medical condition in a patient |
| US11338059B2 (en) | 2014-05-12 | 2022-05-24 | Gholam A. Peyman | Method of corneal and scleral inlay crosslinking and preservation |
| US10583221B2 (en) | 2014-05-12 | 2020-03-10 | Gholam A. Peyman | Method of corneal transplantation or corneal inlay implantation with cross-linking |
| US11565023B2 (en) | 2014-05-12 | 2023-01-31 | Gholam A. Peyman | Method of corneal transplantation or corneal inlay implantation with cross-linking |
| US11045352B2 (en) | 2014-05-12 | 2021-06-29 | Gholam A. Peyman | Methods for treatment of dry eye and other acute or chronic inflammatory processes |
| US11666777B2 (en) | 2014-05-12 | 2023-06-06 | Gholam A. Peyman | Photodynamic therapy technique for preventing damage to the fovea of the eye or another body portion of a patient |
| US10881503B2 (en) | 2014-05-12 | 2021-01-05 | Gholam A. Peyman | Method of corneal transplantation or corneal inlay implantation with cross-linking |
| US11648261B2 (en) | 2014-05-12 | 2023-05-16 | Gholam A. Peyman | Method of treating, reducing, or alleviating a medical condition in a patient |
| TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| WO2019221959A1 (fr) * | 2018-05-16 | 2019-11-21 | Peyman Gholam A | Méthode de traitement, de réduction ou de soulagement d'une pathologie chez un patient |
| US11707518B2 (en) | 2019-04-28 | 2023-07-25 | Gholam A. Peyman | Method of treating, reducing, or alleviating a medical condition in a patient |
| US20220112166A1 (en) * | 2020-10-13 | 2022-04-14 | Yale University | Selective JAK2 Pseudokinase Ligands and Methods of Use |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ227850A (en) | 1988-02-10 | 1991-11-26 | Hoffmann La Roche | Indole substituted pyrrole derivatives; preparatory process and medicaments for use against inflammatory immunological, bronchopulmonary or vascular disorders |
| MC2096A1 (fr) | 1989-02-23 | 1991-02-15 | Hoffmann La Roche | Pyrroles substitues |
| DE3914764A1 (de) | 1989-05-05 | 1990-11-08 | Goedecke Ag | Maleinimid-derivate und deren verwendung als arzneimittel |
| CA2015996C (fr) | 1989-05-05 | 2001-08-28 | Hartmut Osswald | Derives de bis-(1h-indole-3-yl)-maleinimide et leur utilisation comme produits pharmaceutiques |
| DE4005970A1 (de) | 1990-02-26 | 1991-08-29 | Boehringer Mannheim Gmbh | Neue trisubstituierte maleinimide, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten |
| DE4005969A1 (de) | 1990-02-26 | 1991-08-29 | Boehringer Mannheim Gmbh | Neue trisubstituierte pyrrole, verfahren zu ihrer herstellung sowie arzneimittel, die diese verbindungen enthalten |
| CA2046801C (fr) | 1990-08-07 | 2002-02-26 | Peter D. Davis | Pyrroles substitues |
| WO1992018507A1 (fr) | 1991-04-11 | 1992-10-29 | Schering Corporation | Agents antitumoraux et antipsoriasiques |
| GB9123396D0 (en) | 1991-11-04 | 1991-12-18 | Hoffmann La Roche | A process for the manufacture of substituted maleimides |
| WO1993018765A1 (fr) | 1992-03-20 | 1993-09-30 | The Wellcome Foundation Limited | Derives d'indole presentant une action antivirale |
| CA2130836A1 (fr) | 1992-03-20 | 1993-09-30 | Martin J. Slater | Autres derives indoles a activite antivirale |
| DE4217964A1 (de) | 1992-05-30 | 1993-12-02 | Goedecke Ag | Indolocarbazol-Imide und deren Verwendung |
| DE4243321A1 (de) | 1992-12-21 | 1994-06-23 | Goedecke Ag | Aminosäurederivate von Heterocyclen als PKC-Inhibitoren |
| GB9319297D0 (en) | 1993-09-17 | 1993-11-03 | Wellcome Found | Indole derivatives |
| GB9416467D0 (en) | 1994-08-13 | 1994-10-05 | Wellcome Found | Compounds for use in medicine |
| US5681854A (en) * | 1995-11-22 | 1997-10-28 | Alcon Laboratories, Inc. | Use of aliphatic carboxylic acid derivatives in ophthalmic disorders |
| US6057117A (en) * | 1996-04-04 | 2000-05-02 | Chiron Corporation | Identification and use of selective inhibitors of glycogen synthase kinase 3 |
| EP1019043A4 (fr) * | 1996-05-07 | 2003-07-30 | Univ Pennsylvania | Inhibiteurs de glycogene synthetase kinase-3 et procedes d'identification et d'utilisation de ces inhibiteurs |
| PE91598A1 (es) | 1996-07-29 | 1998-12-24 | Hoffmann La Roche | Pirroles sustituidos |
| PE91498A1 (es) * | 1996-07-29 | 1998-12-22 | Hoffmann La Roche | Pirroles sustituidos |
| PE91698A1 (es) | 1996-07-29 | 1998-12-24 | Hoffmann La Roche | Pirroles sustituidos |
| SE9603283D0 (sv) | 1996-09-10 | 1996-09-10 | Astra Ab | New compounds |
| SE9603285D0 (sv) | 1996-09-10 | 1996-09-10 | Astra Ab | New compounds |
| EP1003746A1 (fr) * | 1997-08-07 | 2000-05-31 | The Regents Of The University Of California | Purines inhibant des proteine kinases, des proteines g et des polymerases |
| EP1057484A4 (fr) | 1998-02-23 | 2002-11-20 | Sagami Chem Res | Inhibiteurs de la mort cellulaire |
| JP2002516851A (ja) * | 1998-05-29 | 2002-06-11 | ゲルハルト アイゼンブランド | サイクリン依存性キナーゼを阻害する医薬製造のためのインジゴイドビスインドール誘導体の使用 |
| ES2234300T3 (es) | 1998-10-08 | 2005-06-16 | Smithkline Beecham Plc | 3-(3-cloro-4-hidroxifenilamino)-4-(2-nitrofenil)-1h-pirrol-2,5-diona como inhibidor de glucogeno cinasa-3 (gsk-3)sintetasa. |
| GB9828640D0 (en) | 1998-12-23 | 1999-02-17 | Smithkline Beecham Plc | Novel method and compounds |
| GB9918180D0 (en) | 1999-08-02 | 1999-10-06 | Smithkline Beecham Plc | Novel compositions |
| EP1224932A4 (fr) * | 1999-08-20 | 2002-10-16 | Sagami Chem Res | Medicaments inhibant la mort cellulaire |
| FR2801216A1 (fr) | 1999-11-23 | 2001-05-25 | Centre Nat Rech Scient | Utilisation de derives d'indirubine pour la fabrication de medicaments |
| DE69912808T2 (de) * | 1999-12-08 | 2004-09-30 | Centre National De La Recherche Scientifique (C.N.R.S.) | Verwendung von Hymenialdisin und dessen Derivaten zur Herstellung therapeutischer Mittel |
| EP1244461A2 (fr) | 1999-12-23 | 2002-10-02 | The Ontario Cancer Institute | INHIBITION DE L'ENZYME GLYCOGENE SYNTHETASE KINASE-3 (GSK-3$g(b) |
| WO2001049709A1 (fr) | 2000-01-03 | 2001-07-12 | Ramot University Authority For Applied Research & Industrial Development Ltd. | Inhibiteurs de glycogene synthase kinase-3 |
| WO2001056567A1 (fr) | 2000-02-04 | 2001-08-09 | Novo Nordisk A/S | Derives de 2,4-diaminothiazole |
| CA2401775A1 (fr) * | 2000-02-29 | 2001-09-07 | Abbot F. Clark | Diagnostic et traitement du glaucome |
| WO2001070727A1 (fr) * | 2000-03-23 | 2001-09-27 | Sanofi-Synthelabo | Derives de 2-(arylalkylamino)pyrimidone et derives de 2-(heteroarylalkylamino)pyrimidone |
| EP1136099A1 (fr) * | 2000-03-23 | 2001-09-26 | Sanofi-Synthelabo | Dérivés de 2-(indolylalkylamino)pyridone comme inhibiteurs de GSK3bêta |
| EP1136482A1 (fr) * | 2000-03-23 | 2001-09-26 | Sanofi-Synthelabo | Dérivés de 2-amino-3-(alkyl)-pyrimidone comme inhibiteurs de GSK3bêta |
| DK1430057T3 (da) | 2001-09-21 | 2006-01-16 | Sanofi Aventis | Substituerede 2-pyridinyl-6,7,8, 9-tetrahydropyrimido [1,2-a] pyrimidin-4-on- og 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)onderivater |
-
2002
- 2002-09-10 TW TW099127943A patent/TW201041580A/zh unknown
- 2002-09-10 TW TW091120600A patent/TWI335221B/zh not_active IP Right Cessation
- 2002-09-23 CA CA2460000A patent/CA2460000C/fr not_active Expired - Fee Related
- 2002-09-23 WO PCT/US2002/030059 patent/WO2003027275A1/fr active IP Right Grant
- 2002-09-23 CN CNA2008100990379A patent/CN101380319A/zh active Pending
- 2002-09-23 RU RU2004112766/14A patent/RU2297243C2/ru not_active IP Right Cessation
- 2002-09-23 PL PL369130A patent/PL207022B1/pl not_active IP Right Cessation
- 2002-09-23 MX MXPA04002137A patent/MXPA04002137A/es active IP Right Grant
- 2002-09-23 JP JP2003530847A patent/JP2005504101A/ja active Pending
- 2002-09-23 EP EP02799603A patent/EP1430120A4/fr not_active Withdrawn
- 2002-09-23 US US10/488,496 patent/US7598288B2/en not_active Expired - Fee Related
- 2002-09-23 AU AU2002334635A patent/AU2002334635B2/en not_active Ceased
- 2002-09-23 EP EP10181455A patent/EP2281560A1/fr not_active Withdrawn
- 2002-09-23 CN CNA028190106A patent/CN1561393A/zh active Pending
- 2002-09-23 BR BR0212924-8A patent/BR0212924A/pt not_active IP Right Cessation
- 2002-09-23 KR KR10-2004-7003638A patent/KR20040047824A/ko active Search and Examination
- 2002-09-26 AR ARP020103638A patent/AR036684A1/es unknown
-
2004
- 2004-03-05 ZA ZA200401846A patent/ZA200401846B/en unknown
-
2005
- 2005-07-21 JP JP2005211956A patent/JP2005320350A/ja active Pending
-
2009
- 2009-08-21 US US12/545,611 patent/US20090312390A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2005320350A (ja) | 2005-11-17 |
| MXPA04002137A (es) | 2004-06-29 |
| CN1561393A (zh) | 2005-01-05 |
| BR0212924A (pt) | 2005-01-04 |
| EP1430120A1 (fr) | 2004-06-23 |
| US20040186159A1 (en) | 2004-09-23 |
| CA2460000C (fr) | 2013-01-29 |
| PL369130A1 (en) | 2005-04-18 |
| EP1430120A4 (fr) | 2007-06-20 |
| CA2460000A1 (fr) | 2003-04-03 |
| TWI335221B (en) | 2011-01-01 |
| RU2004112766A (ru) | 2005-03-27 |
| CN101380319A (zh) | 2009-03-11 |
| KR20040047824A (ko) | 2004-06-05 |
| AR036684A1 (es) | 2004-09-29 |
| WO2003027275A1 (fr) | 2003-04-03 |
| JP2005504101A (ja) | 2005-02-10 |
| PL207022B1 (pl) | 2010-10-29 |
| AU2002334635B2 (en) | 2007-06-21 |
| EP2281560A1 (fr) | 2011-02-09 |
| US7598288B2 (en) | 2009-10-06 |
| TW201041580A (en) | 2010-12-01 |
| US20090312390A1 (en) | 2009-12-17 |
| RU2297243C2 (ru) | 2007-04-20 |
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