JP2004520299A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2004520299A5 JP2004520299A5 JP2002549683A JP2002549683A JP2004520299A5 JP 2004520299 A5 JP2004520299 A5 JP 2004520299A5 JP 2002549683 A JP2002549683 A JP 2002549683A JP 2002549683 A JP2002549683 A JP 2002549683A JP 2004520299 A5 JP2004520299 A5 JP 2004520299A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- alkoxy
- cycloalkyl
- halogen
- 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.)
- Pending
Links
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 89
- 229910052736 halogen Inorganic materials 0.000 claims 55
- 150000002367 halogens Chemical class 0.000 claims 54
- 150000001875 compounds Chemical class 0.000 claims 49
- 229910052739 hydrogen Inorganic materials 0.000 claims 48
- 239000001257 hydrogen Substances 0.000 claims 48
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 41
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 38
- 125000004093 cyano group Chemical group *C#N 0.000 claims 35
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 30
- 150000002431 hydrogen Chemical class 0.000 claims 25
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 25
- 125000001424 substituent group Chemical group 0.000 claims 24
- 108010046593 Neuropeptide Y5 receptor Proteins 0.000 claims 23
- 102000028582 Neuropeptide Y5 receptor Human genes 0.000 claims 23
- 125000003545 alkoxy group Chemical group 0.000 claims 23
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 22
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 125000002837 carbocyclic group Chemical group 0.000 claims 20
- -1 hydroxy, amino Chemical group 0.000 claims 18
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 17
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims 5
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 5
- 125000002971 oxazolyl group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 4
- 125000005862 (C1-C6)alkanoyl group Chemical group 0.000 claims 4
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 4
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 3
- 125000006655 (C3-C8) heteroaryl group Chemical group 0.000 claims 3
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 239000003446 ligand Substances 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 238000000159 protein binding assay Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- IRDOMFKPNLFWGW-UHFFFAOYSA-N 1'-(6-methyl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(C)=CC=C2N1 IRDOMFKPNLFWGW-UHFFFAOYSA-N 0.000 claims 2
- XVMIZJDINZCQRH-UHFFFAOYSA-N C1=CN=C2NC=NC2=C1.C12=CC=CC=C2C(=O)OC21CCNCC2 Chemical compound C1=CN=C2NC=NC2=C1.C12=CC=CC=C2C(=O)OC21CCNCC2 XVMIZJDINZCQRH-UHFFFAOYSA-N 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 235000014632 disordered eating Nutrition 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- QCYXSEHOIKPNEU-UHFFFAOYSA-N 1'-(1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C12=CC=CC=C2C(=O)OC11CCN(C=2NC3=CC=CC=C3N=2)CC1 QCYXSEHOIKPNEU-UHFFFAOYSA-N 0.000 claims 1
- FSMWTPVKAMLPSN-UHFFFAOYSA-N 1'-(4,6-dichloro-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(Cl)=CC(Cl)=C2N1 FSMWTPVKAMLPSN-UHFFFAOYSA-N 0.000 claims 1
- PMRYRRQZWAWPNO-UHFFFAOYSA-N 1'-(4-chloro-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC(C=CC=C2Cl)=C2N1 PMRYRRQZWAWPNO-UHFFFAOYSA-N 0.000 claims 1
- QGOAHRMVFCYWPZ-UHFFFAOYSA-N 1'-(5,6-difluoro-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC(C=C(C(=C2)F)F)=C2N1 QGOAHRMVFCYWPZ-UHFFFAOYSA-N 0.000 claims 1
- PYRWXXAHWYRCJZ-UHFFFAOYSA-N 1'-(5,6-dimethoxy-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC(C=C(C(=C2)OC)OC)=C2N1 PYRWXXAHWYRCJZ-UHFFFAOYSA-N 0.000 claims 1
- ZETIZXFYVDSTGO-UHFFFAOYSA-N 1'-(5-phenyl-3h-imidazo[4,5-b]pyrazin-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C12=CC=CC=C2C(=O)OC1(CC1)CCN1C(NC1=NC=2)=NC1=NC=2C1=CC=CC=C1 ZETIZXFYVDSTGO-UHFFFAOYSA-N 0.000 claims 1
- CLDMDFGJPGYXPI-UHFFFAOYSA-N 1'-(6-acetyl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(C(=O)C)=CC=C2N1 CLDMDFGJPGYXPI-UHFFFAOYSA-N 0.000 claims 1
- MYGKOPZLGWXONJ-UHFFFAOYSA-N 1'-(6-benzoyl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C=1C=C2NC(N3CCC4(CC3)C3=CC=CC=C3C(=O)O4)=NC2=CC=1C(=O)C1=CC=CC=C1 MYGKOPZLGWXONJ-UHFFFAOYSA-N 0.000 claims 1
- ZMIPLTFCRFYPCJ-UHFFFAOYSA-N 1'-(6-chloro-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(Cl)=CC=C2N1 ZMIPLTFCRFYPCJ-UHFFFAOYSA-N 0.000 claims 1
- UJHHJWQXFSURDR-UHFFFAOYSA-N 1'-(6-ethoxy-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(OCC)=CC=C2N1 UJHHJWQXFSURDR-UHFFFAOYSA-N 0.000 claims 1
- QNXVMYVJXUTGAH-UHFFFAOYSA-N 1'-(6-fluoro-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(F)=CC=C2N1 QNXVMYVJXUTGAH-UHFFFAOYSA-N 0.000 claims 1
- APXYPHDCNPEEPO-UHFFFAOYSA-N 1'-(6-iodo-4-oxo-1h-quinazolin-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC(=O)C2=CC(I)=CC=C2N1 APXYPHDCNPEEPO-UHFFFAOYSA-N 0.000 claims 1
- BFRHFFHUPOVDTN-UHFFFAOYSA-N 1'-(6-methoxy-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(OC)=CC=C2N1 BFRHFFHUPOVDTN-UHFFFAOYSA-N 0.000 claims 1
- OOFZXDNGMLQFMR-UHFFFAOYSA-N 1'-(6-methylsulfonyl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(S(=O)(=O)C)=CC=C2N1 OOFZXDNGMLQFMR-UHFFFAOYSA-N 0.000 claims 1
- LPOLBQTZZHSRGO-UHFFFAOYSA-N 1'-(6-propylsulfonyl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(S(=O)(=O)CCC)=CC=C2N1 LPOLBQTZZHSRGO-UHFFFAOYSA-N 0.000 claims 1
- JNDLYOIUCCIUON-UHFFFAOYSA-N 1'-(6-pyrazin-2-yl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C12=CC=CC=C2C(=O)OC1(CC1)CCN1C(NC1=CC=2)=NC1=CC=2C1=CN=CC=N1 JNDLYOIUCCIUON-UHFFFAOYSA-N 0.000 claims 1
- JIVDRBRZFUEQBM-UHFFFAOYSA-N 1'-(6-pyridin-3-yl-1h-benzimidazol-2-yl)spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C12=CC=CC=C2C(=O)OC1(CC1)CCN1C(NC1=CC=2)=NC1=CC=2C1=CC=CN=C1 JIVDRBRZFUEQBM-UHFFFAOYSA-N 0.000 claims 1
- RQMKJTJDJCTLMI-UHFFFAOYSA-N 1'-[6-(1,3-oxazol-2-yl)-1h-benzimidazol-2-yl]spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound C12=CC=CC=C2C(=O)OC1(CC1)CCN1C(NC1=CC=2)=NC1=CC=2C1=NC=CO1 RQMKJTJDJCTLMI-UHFFFAOYSA-N 0.000 claims 1
- PUGBOUNLKDOYBK-UHFFFAOYSA-N 1'-[6-(3,5-dimethyl-1,2-oxazol-4-yl)-1h-benzimidazol-2-yl]spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound CC1=NOC(C)=C1C1=CC=C(NC(=N2)N3CCC4(CC3)C3=CC=CC=C3C(=O)O4)C2=C1 PUGBOUNLKDOYBK-UHFFFAOYSA-N 0.000 claims 1
- VDEGUCQDJLBHGP-UHFFFAOYSA-N 1'-[6-(trifluoromethoxy)-1h-benzimidazol-2-yl]spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(OC(F)(F)F)=CC=C2N1 VDEGUCQDJLBHGP-UHFFFAOYSA-N 0.000 claims 1
- GOSQWFMKXKORBV-UHFFFAOYSA-N 1'-[6-(trifluoromethyl)-1h-benzimidazol-2-yl]spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(C(F)(F)F)=CC=C2N1 GOSQWFMKXKORBV-UHFFFAOYSA-N 0.000 claims 1
- FGCDLQZYHPYSSV-UHFFFAOYSA-N 1'-[6-(trifluoromethylsulfonyl)-1h-benzimidazol-2-yl]spiro[2-benzofuran-3,4'-piperidine]-1-one Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(S(=O)(=O)C(F)(F)F)=CC=C2N1 FGCDLQZYHPYSSV-UHFFFAOYSA-N 0.000 claims 1
- XWCWKHBTXAFSRD-UHFFFAOYSA-N 2-(3-oxospiro[2-benzofuran-1,4'-piperidine]-1'-yl)-3h-benzimidazole-5-carbonitrile Chemical compound C12=CC=CC=C2C(=O)OC11CCN(C=2NC3=CC=C(C=C3N=2)C#N)CC1 XWCWKHBTXAFSRD-UHFFFAOYSA-N 0.000 claims 1
- UFUKIJYVRWRXGP-UHFFFAOYSA-N 2-(3-oxospiro[2-benzofuran-1,4'-piperidine]-1'-yl)-3h-benzimidazole-5-carboxylic acid Chemical compound O1C(=O)C2=CC=CC=C2C1(CC1)CCN1C1=NC2=CC(C(=O)O)=CC=C2N1 UFUKIJYVRWRXGP-UHFFFAOYSA-N 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- FAGMFPJUDWIQNI-UHFFFAOYSA-N 4-[[(3-oxospiro[2-benzofuran-1,4'-piperidine]-1'-carbonyl)amino]methyl]cyclohexane-1-carboxylic acid Chemical compound C1CC(C(=O)O)CCC1CNC(=O)N1CCC2(C3=CC=CC=C3C(=O)O2)CC1 FAGMFPJUDWIQNI-UHFFFAOYSA-N 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000000443 aerosol Substances 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 150000001924 cycloalkanes Chemical class 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 238000001514 detection method Methods 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 150000004702 methyl esters Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- LOFHXKUHUMVONQ-UHFFFAOYSA-N n-cyclohexyl-3-oxospiro[2-benzofuran-1,4'-piperidine]-1'-carboxamide Chemical compound C1CC2(C3=CC=CC=C3C(=O)O2)CCN1C(=O)NC1CCCCC1 LOFHXKUHUMVONQ-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 238000002601 radiography Methods 0.000 claims 1
- 229940075993 receptor modulator Drugs 0.000 claims 1
- 239000006188 syrup Substances 0.000 claims 1
- 235000020357 syrup Nutrition 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25499000P | 2000-12-12 | 2000-12-12 | |
| PCT/US2001/047863 WO2002048152A2 (en) | 2000-12-12 | 2001-12-11 | Spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004520299A JP2004520299A (ja) | 2004-07-08 |
| JP2004520299A5 true JP2004520299A5 (enExample) | 2005-12-22 |
Family
ID=22966369
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002549683A Pending JP2004520299A (ja) | 2000-12-12 | 2001-12-11 | スピロ［イソベンゾフラン−１，４’−ピペリジン］−３−オン類及び３ｈ−スピロイソベンゾフラン−１，４’−ピペリジン類 |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US20050033048A1 (enExample) |
| EP (1) | EP1347982B1 (enExample) |
| JP (1) | JP2004520299A (enExample) |
| AT (1) | ATE310004T1 (enExample) |
| AU (1) | AU2002220276A1 (enExample) |
| BR (1) | BR0116113A (enExample) |
| DE (1) | DE60115092T2 (enExample) |
| ES (1) | ES2249384T3 (enExample) |
| MX (1) | MXPA03004245A (enExample) |
| WO (1) | WO2002048152A2 (enExample) |
Families Citing this family (146)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6374762B1 (en) * | 1997-10-27 | 2002-04-23 | Correct Craft, Inc. | Water sport towing apparatus |
| DE69929235T2 (de) | 1998-11-10 | 2006-08-24 | Merck & Co., Inc. | Spiro-indole als y5-rezeptor antagonisten |
| AU7738100A (en) * | 1999-09-30 | 2001-04-30 | Neurogen Corporation | Certain alkylene diamine-substituted pyrazolo(1,5,-a)-1,5-pyrimidines and pyrazolo(1,5-a)-1,3,5-triazines |
| CZ20021086A3 (cs) * | 1999-09-30 | 2002-10-16 | Neurogen Corporation | Alkylendiaminem substituované heterocykly |
| EP1263768A4 (en) * | 2000-01-28 | 2004-05-12 | Neurogen Corp | CHIMEAN NEUROPEPTID Y RECEPTORS |
| MXPA03004245A (es) | 2000-12-12 | 2003-09-22 | Neurogen Corp | Espiro[isobenzofuran-1,4'piperidin]-3-onas y 3h-espiroisobenzofuran-1,4'-piperidinas. |
| US6900220B2 (en) * | 2001-01-02 | 2005-05-31 | Syntex (U.S.A.) Llc | Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists |
| WO2002094825A1 (en) * | 2001-05-22 | 2002-11-28 | Banyu Pharmaceutical Co., Ltd. | Novel spiropiperidine derivative |
| PL367983A1 (en) | 2001-08-07 | 2005-03-21 | Banyu Pharmaceutical Co, Ltd. | Spiro compounds |
| CA2403307A1 (en) | 2001-10-23 | 2003-04-23 | Neurogen Corporation | Substituted 2-cyclohexyl-4-phenyl-1h-imidazole derivatives |
| AUPR975601A0 (en) * | 2001-12-24 | 2002-01-31 | Fujisawa Pharmaceutical Co., Ltd. | Quinazolinone derivatives |
| JP4901102B2 (ja) * | 2002-05-03 | 2012-03-21 | エクセリクシス， インク． | プロテインキナーゼモジュレーターおよびその使用方法 |
| US7704995B2 (en) * | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7405234B2 (en) * | 2002-05-17 | 2008-07-29 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| JP4496722B2 (ja) * | 2002-06-28 | 2010-07-07 | 萬有製薬株式会社 | 新規ベンズイミダゾール誘導体 |
| SE0202462D0 (sv) * | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | Novel use |
| EP1407774A1 (en) * | 2002-09-10 | 2004-04-14 | LION Bioscience AG | 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds |
| EP1398032A1 (en) * | 2002-09-10 | 2004-03-17 | PheneX Pharmaceuticals AG | 4-Oxo-quinazolines as LXR nuclear receptor binding compounds |
| AU2003302084A1 (en) * | 2002-11-15 | 2004-06-15 | Bristol-Myers Squibb Company | Open chain prolyl urea-related modulators of androgen receptor function |
| US7365079B2 (en) | 2002-11-29 | 2008-04-29 | Banyu Pharmaceutical Co., Ltd. | Azole derivatives |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| MXPA05009245A (es) | 2003-03-11 | 2005-10-19 | Pfizer Prod Inc | Nuevos compuestos de pirazina como inhibidores del factor de crecimiento transformante (tgf). |
| BRPI0412285A (pt) | 2003-07-02 | 2006-09-19 | Hoffmann La Roche | os compostos de quinazolinona substituìda por arilamina |
| US7547693B2 (en) | 2003-09-22 | 2009-06-16 | Banyu Pharmaceutical Co. Ltd. | Piperidine derivative |
| MXPA06003380A (es) * | 2003-09-26 | 2006-06-08 | Pfizer Prod Inc | Uso de antagonista del receptor npy y5 para el tratamiento de trastornos del ritmo circadiano. |
| MXPA06003393A (es) * | 2003-09-26 | 2006-06-08 | Pfizer Prod Inc | Tratamiento de trastornos neurologicos relacionados con alteraciones del sueno de movimientos oculares rapidos (rem) con antagonistas de receptor npy y5. |
| US7256208B2 (en) * | 2003-11-13 | 2007-08-14 | Bristol-Myers Squibb Company | Monocyclic N-Aryl hydantoin modulators of androgen receptor function |
| WO2005056036A2 (en) * | 2003-12-09 | 2005-06-23 | Novo Nordisk A/S | Regulation of food preference using glp-1 agonists |
| US20050182105A1 (en) * | 2004-02-04 | 2005-08-18 | Nirschl Alexandra A. | Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function |
| US7820702B2 (en) * | 2004-02-04 | 2010-10-26 | Bristol-Myers Squibb Company | Sulfonylpyrrolidine modulators of androgen receptor function and method |
| US7388027B2 (en) * | 2004-03-04 | 2008-06-17 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
| US7625923B2 (en) | 2004-03-04 | 2009-12-01 | Bristol-Myers Squibb Company | Bicyclic modulators of androgen receptor function |
| US7696241B2 (en) * | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
| EP1734963A4 (en) | 2004-04-02 | 2008-06-18 | Merck & Co Inc | METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER |
| CA2568056A1 (en) | 2004-05-25 | 2005-12-08 | Pfizer Products Inc. | Tetraazabenzo[e]azulene derivatives and analogs thereof |
| US7786141B2 (en) * | 2004-08-19 | 2010-08-31 | Vertex Pharmaceuticals Incorporated | Dihydrospiroindene modulators of muscarinic receptors |
| JP2008510728A (ja) | 2004-08-19 | 2008-04-10 | バーテックス ファーマシューティカルズ インコーポレイテッド | ムスカリン受容体のモジュレーター |
| ES2325773T5 (es) | 2004-11-01 | 2014-02-24 | Amylin Pharmaceuticals, Llc. | Tratamiento de la obesidad y de los trastornos relacionados |
| US7863449B2 (en) * | 2004-11-29 | 2011-01-04 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| US7534796B2 (en) | 2005-02-18 | 2009-05-19 | Wyeth | Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7582634B2 (en) | 2005-02-18 | 2009-09-01 | Wyeth | 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7538113B2 (en) | 2005-02-18 | 2009-05-26 | Wyeth | 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| DE102005012874A1 (de) | 2005-03-19 | 2006-09-21 | Sanofi-Aventis Deutschland Gmbh | Amid substituierte 8-N-Benzimidazole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
| US7531542B2 (en) | 2005-05-18 | 2009-05-12 | Wyeth | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor |
| US7582636B2 (en) | 2005-05-26 | 2009-09-01 | Wyeth | Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor |
| EP1892241B1 (en) | 2005-05-30 | 2016-03-30 | Msd K.K. | Novel piperidine derivative |
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| US7825244B2 (en) | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
| EP1916239A4 (en) | 2005-08-10 | 2009-10-21 | Banyu Pharma Co Ltd | PYRIDOLVERBINDUNG |
| EP2330124B1 (en) | 2005-08-11 | 2015-02-25 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
| EP2330125A3 (en) | 2005-08-11 | 2012-12-12 | Amylin Pharmaceuticals, Inc. | Hybrid polypeptides with selectable properties |
| JPWO2007024004A1 (ja) | 2005-08-24 | 2009-03-05 | 萬有製薬株式会社 | フェニルピリドン誘導体 |
| US8211919B2 (en) * | 2005-09-02 | 2012-07-03 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| EP1939194A4 (en) | 2005-09-07 | 2010-12-08 | Banyu Pharma Co Ltd | BICYCLIC AROMATIC SUBSTITUTED PYRIDONE DERIVATIVE |
| KR20080048502A (ko) | 2005-09-29 | 2008-06-02 | 머크 앤드 캄파니 인코포레이티드 | 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체 |
| AU2006304836A1 (en) | 2005-10-21 | 2007-04-26 | Novartis Ag | Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent |
| JPWO2007049798A1 (ja) | 2005-10-27 | 2009-04-30 | 萬有製薬株式会社 | 新規ベンゾオキサチイン誘導体 |
| NZ568292A (en) | 2005-11-10 | 2011-08-26 | Msd Kk | Spiro[cyclohexane-1,1'-(3'H)-4'-azaisobenzofuran]-4-carboxamide derivatives |
| RU2008130094A (ru) * | 2005-12-22 | 2010-01-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Модуляторы мускариновых рецепторов |
| EP1988892A2 (en) | 2006-02-22 | 2008-11-12 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| ATE517106T1 (de) * | 2006-02-22 | 2011-08-15 | Vertex Pharma | Kondensierte spiropiperidine als modulatoren muskarinartiger rezeptoren |
| EP1847542A1 (en) * | 2006-04-21 | 2007-10-24 | Laboratorios del Dr. Esteve S.A. | Spiro[benzopyran] or spiro[benzofuran] derivatives which inhibit the sigma receptor |
| CN101500565A (zh) * | 2006-06-29 | 2009-08-05 | 弗特克斯药品有限公司 | 毒蕈碱性受体的调节剂 |
| FR2903985B1 (fr) | 2006-07-24 | 2008-09-05 | Sanofi Aventis Sa | Derives de n-(amino-heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique |
| FR2904316B1 (fr) | 2006-07-31 | 2008-09-05 | Sanofi Aventis Sa | Derives de n-(amino-heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique. |
| EP2051712A2 (en) * | 2006-08-15 | 2009-04-29 | Vertex Pharmceuticals Incorporated | Modulators of muscarinic receptors |
| JP2010501561A (ja) | 2006-08-18 | 2010-01-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | ムスカリン受容体の調節剤 |
| WO2008024497A2 (en) * | 2006-08-25 | 2008-02-28 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
| AU2007300627B2 (en) | 2006-09-22 | 2012-02-16 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
| EP2072519A4 (en) | 2006-09-28 | 2009-10-21 | Banyu Pharma Co Ltd | DIARYLKETIMINDERIVAT |
| EP2457913B1 (en) | 2006-10-19 | 2017-04-19 | Signal Pharmaceuticals, LLC | Heteroaryl compounds, compositions thereof, and methods of treatment therewith |
| JP2010513385A (ja) * | 2006-12-22 | 2010-04-30 | エフ．ホフマン−ラ ロシュ アーゲー | スピロ−ピペリジン誘導体 |
| FR2910473B1 (fr) * | 2006-12-26 | 2009-02-13 | Sanofi Aventis Sa | Derives de n-(amino-heteroaryl)-1h-pyrrolopyridine-2- carboxamides, leur preparation et leur application en therapeutique. |
| JP5319518B2 (ja) | 2007-04-02 | 2013-10-16 | Ｍｓｄ株式会社 | インドールジオン誘導体 |
| JP5546451B2 (ja) | 2007-06-04 | 2014-07-09 | シナジー ファーマシューティカルズ インコーポレイテッド | 胃腸の障害、炎症、癌および他の障害の処置に有用なグアニル酸シクラーゼのアゴニスト |
| US20100120694A1 (en) | 2008-06-04 | 2010-05-13 | Synergy Pharmaceuticals, Inc. | Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
| WO2009045519A1 (en) * | 2007-10-03 | 2009-04-09 | Vertex Pharmaceuticals Incorporated | Modulators of muscarinic receptors |
| WO2009070583A1 (en) * | 2007-11-30 | 2009-06-04 | Wyeth | Pyrido[3,2-e]pyrazines, process for preparing the same, and their use as inhibitors of phosphodiesterase 10 |
| CA2706866A1 (en) * | 2007-11-30 | 2009-06-04 | Biotie Therapies Gmbh | Aryl and heteroaryl fused imidazo[1,5-a]pyrazines as inhibitors of phosphodiesterase 10 |
| CA2716128A1 (en) * | 2008-02-27 | 2009-09-03 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11.beta.-hydroxysteroid dehydrogenase type 1 |
| AU2009220605A1 (en) | 2008-03-06 | 2009-09-11 | Msd K.K. | Alkylaminopyridine derivative |
| CN101981025A (zh) | 2008-03-28 | 2011-02-23 | 万有制药株式会社 | 具有黑色素浓缩激素受体拮抗作用的二芳基甲基酰胺衍生物 |
| AU2009261248A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diarylketoxime derivative |
| EP3241839B1 (en) | 2008-07-16 | 2019-09-04 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| US20110124674A1 (en) | 2008-07-30 | 2011-05-26 | Hiroyuki Kishino | 5/5-or 5/6-membered condensed ring cycloalkylamine derivative |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| EP2350010B1 (en) | 2008-10-30 | 2014-03-26 | Merck Sharp & Dohme Corp. | Isonicotinamide orexin receptor antagonists |
| AU2009309037A1 (en) | 2008-10-31 | 2010-05-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US20110243940A1 (en) | 2008-12-16 | 2011-10-06 | Schering Corporation | Bicyclic pyranone derivatives and methods of use thereof |
| US20110245209A1 (en) | 2008-12-16 | 2011-10-06 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
| TW201111383A (en) | 2009-05-29 | 2011-04-01 | Wyeth Llc | Substituted imidazo[1,5-a]quinoxalines as inhibitors of phosphodiesterase 10 |
| JP2013508456A (ja) | 2009-10-26 | 2013-03-07 | シグナル ファーマシューティカルズ， エルエルシー | ヘテロアリール化合物の合成方法および精製方法 |
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US8680098B2 (en) | 2010-03-05 | 2014-03-25 | Janssen Pharmaceutica, Nv | Substituted aza-bicyclic imidazole derivatives useful as TRPM8 receptor modulators |
| CA2799708A1 (en) | 2010-05-21 | 2011-11-24 | Pfizer Inc. | 2-phenyl benzoylamides |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| MY159058A (en) | 2011-02-25 | 2016-12-15 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agent |
| JP2014513923A (ja) | 2011-03-04 | 2014-06-19 | ファイザー・インク | Ｅｄｎ３様ペプチドおよびその使用 |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| SG10201912850WA (en) | 2011-10-19 | 2020-02-27 | Signal Pharm Llc | Treatment Of Cancer With TOR Kinase Inhibitors |
| ES2694413T3 (es) | 2011-12-02 | 2018-12-20 | Signal Pharmaceuticals, Llc | Composiciones farmacéuticas de 7-(6-(2-hidroxipropan-2-il)piridin-3-il)-1-((trans)-4-metoxiciclohexil)-3,4-dihidropirazino [2,3-b]pirazin-2(1H)-ona, una forma sólida de la misma y métodos para su uso |
| CA2864905A1 (en) | 2012-02-24 | 2013-08-29 | Signal Pharmaceuticals, Llc | Methods for treating non- small cell lung cancer using tor kinase inhibitor combination therapy |
| EP2880028B1 (en) | 2012-08-02 | 2020-09-30 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| EP2945636B1 (en) | 2013-01-16 | 2017-06-28 | Signal Pharmaceuticals, LLC | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| JP2016516004A (ja) | 2013-02-22 | 2016-06-02 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | 抗糖尿病二環式化合物 |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| HK1220696A1 (zh) | 2013-03-15 | 2017-05-12 | Bausch Health Ireland Limited | 鸟苷酸环化酶激动剂及其用途 |
| AU2014235209B2 (en) | 2013-03-15 | 2018-06-14 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists combined with other drugs |
| AU2014254057A1 (en) | 2013-04-17 | 2015-11-05 | Signal Pharmaceuticals, Llc | Combination therapy comprising a TOR kinase inhibitor and N-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| SG11201508527VA (en) | 2013-04-17 | 2015-11-27 | Signal Pharm Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
| KR102242505B1 (ko) | 2013-04-17 | 2021-04-20 | 시그날 파마소티칼 엘엘씨 | 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법 |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| ES2944478T3 (es) | 2013-04-17 | 2023-06-21 | Signal Pharm Llc | 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino[2,3-b]pirazin-2(1H)-ona para tratar el glioblastoma multiforme |
| NZ629411A (en) | 2013-04-17 | 2017-06-30 | Signal Pharm Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| JP6401250B2 (ja) | 2013-05-29 | 2018-10-10 | シグナル ファーマシューティカルズ，エルエルシー | ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法 |
| EP4424697A3 (en) | 2013-06-05 | 2024-12-25 | Bausch Health Ireland Limited | Ultra-pure agonists of guanylate cyclase c, method of making and using same |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer |
| US9718824B2 (en) | 2014-04-16 | 2017-08-01 | Signal Pharmaceuticals, Llc | Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof |
| US9737535B2 (en) | 2014-04-16 | 2017-08-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines |
| AU2015289929A1 (en) | 2014-07-14 | 2017-03-02 | Signal Pharmaceuticals, Llc | Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof |
| NZ629796A (en) | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
| BR112017003745A2 (pt) | 2014-08-29 | 2017-12-05 | Tes Pharma S R L | inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico |
| CN104387367A (zh) * | 2014-11-02 | 2015-03-04 | 湖南华腾制药有限公司 | 一种2位取代苯并咪唑衍生物的制备方法 |
| WO2018003962A1 (ja) | 2016-06-30 | 2018-01-04 | 国立研究開発法人理化学研究所 | 新規化合物又はその薬理学的に許容される塩 |
| TWI767945B (zh) | 2016-10-14 | 2022-06-21 | 義大利商Ｔｅｓ製藥（股份）責任有限公司 | α-胺基-β-羧基己二烯二酸半醛去羧酶之抑制劑 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| US10968232B2 (en) | 2016-12-20 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| 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 |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| WO2019131794A1 (ja) * | 2017-12-27 | 2019-07-04 | 公益財団法人がん研究会 | 抗がん剤 |
| EP3816160A4 (en) * | 2018-06-27 | 2022-03-16 | Reborna Biosciences, Inc. | PROPHYLACTIC OR THERAPEUTIC AGENT FOR SPINAL MUSCULAR ATROPHY |
| CN113302189B (zh) | 2018-11-20 | 2025-09-05 | Tes制药有限责任公司 | α-氨基-β-羧基己二烯二酸半醛去羧酶的抑制剂 |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| US11098029B2 (en) | 2019-02-13 | 2021-08-24 | Merck Sharp & Dohme Corp. | 5-alkyl pyrrolidine orexin receptor agonists |
| EP3923933A4 (en) | 2019-02-13 | 2022-08-17 | Merck Sharp & Dohme Corp. | PYRROLIDINOREXINE RECEPTOR AGONISTS |
| EP4010314B1 (en) | 2019-08-08 | 2024-02-28 | Merck Sharp & Dohme LLC | Heteroaryl pyrrolidine and piperidine orexin receptor agonists |
| EP3772513A1 (en) * | 2019-08-09 | 2021-02-10 | C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening | Shp2 inhibitors |
| CN116249697A (zh) | 2020-08-18 | 2023-06-09 | 默沙东有限责任公司 | 二环庚烷吡咯烷食欲素受体激动剂 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS55143980A (en) * | 1979-04-27 | 1980-11-10 | Dai Ichi Seiyaku Co Ltd | Anti-allergic preparation |
| WO1995028389A1 (en) * | 1994-04-15 | 1995-10-26 | Yamanouchi Pharmaceutical Co., Ltd. | Spiro compound and medicinal composition thereof |
| US5602024A (en) * | 1994-12-02 | 1997-02-11 | Synaptic Pharmaceutical Corporation | DNA encoding a hypothalamic atypical neuropeptide Y/peptide YY receptor (Y5) and uses thereof |
| ID29137A (id) * | 1998-07-27 | 2001-08-02 | Schering Corp | Ligan-ligan afinitas tinggi untuk reseptor nosiseptin orl-1 |
| DE69929235T2 (de) | 1998-11-10 | 2006-08-24 | Merck & Co., Inc. | Spiro-indole als y5-rezeptor antagonisten |
| TWI279402B (en) * | 1999-08-20 | 2007-04-21 | Banyu Pharma Co Ltd | Spiro compounds having NPY antagonistic activities and agents containing the same |
| AU7738100A (en) | 1999-09-30 | 2001-04-30 | Neurogen Corporation | Certain alkylene diamine-substituted pyrazolo(1,5,-a)-1,5-pyrimidines and pyrazolo(1,5-a)-1,3,5-triazines |
| CZ20021086A3 (cs) * | 1999-09-30 | 2002-10-16 | Neurogen Corporation | Alkylendiaminem substituované heterocykly |
| EP1263768A4 (en) * | 2000-01-28 | 2004-05-12 | Neurogen Corp | CHIMEAN NEUROPEPTID Y RECEPTORS |
| WO2001095856A2 (en) | 2000-06-15 | 2001-12-20 | Chaconne Nsi Co., Ltd. | Urea derivative useful as an anti-cancer agent and process for preparing same |
| MXPA03004245A (es) * | 2000-12-12 | 2003-09-22 | Neurogen Corp | Espiro[isobenzofuran-1,4'piperidin]-3-onas y 3h-espiroisobenzofuran-1,4'-piperidinas. |
| CA2403307A1 (en) | 2001-10-23 | 2003-04-23 | Neurogen Corporation | Substituted 2-cyclohexyl-4-phenyl-1h-imidazole derivatives |
-
2001
- 2001-12-11 MX MXPA03004245A patent/MXPA03004245A/es active IP Right Grant
- 2001-12-11 DE DE60115092T patent/DE60115092T2/de not_active Expired - Fee Related
- 2001-12-11 US US10/415,457 patent/US20050033048A1/en not_active Abandoned
- 2001-12-11 AU AU2002220276A patent/AU2002220276A1/en not_active Abandoned
- 2001-12-11 AT AT01270536T patent/ATE310004T1/de not_active IP Right Cessation
- 2001-12-11 BR BR0116113-0A patent/BR0116113A/pt not_active IP Right Cessation
- 2001-12-11 WO PCT/US2001/047863 patent/WO2002048152A2/en not_active Ceased
- 2001-12-11 JP JP2002549683A patent/JP2004520299A/ja active Pending
- 2001-12-11 EP EP01270536A patent/EP1347982B1/en not_active Expired - Lifetime
- 2001-12-11 ES ES01270536T patent/ES2249384T3/es not_active Expired - Lifetime
- 2001-12-11 US US10/013,846 patent/US6566367B2/en not_active Expired - Fee Related
-
2003
- 2003-04-09 US US10/410,648 patent/US6943199B2/en not_active Expired - Fee Related
-
2005
- 2005-07-18 US US11/183,615 patent/US20060040964A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2004520299A5 (enExample) | ||
| ES2974985T3 (es) | Inhibidores de FGFR y métodos de uso de los mismos | |
| US6387894B1 (en) | Use of CRF antagonists and renin-angiotensin system inhibitors | |
| JP4923146B2 (ja) | 合成トリテルペノイドおよび疾患の治療における使用方法 | |
| TWI716371B (zh) | 經1,3-噻唑-2-基取代之苯甲醯胺 | |
| CA2052884C (en) | Angiotensin 11 antagonists in the treatment of hyperuricemia | |
| CN102595896B (zh) | 提高低氧诱导因子-1α的稳定性的方法 | |
| CN120247875A (zh) | 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法 | |
| CN105517548B (zh) | 用于治疗过度增生性病症的mek抑制剂和erk抑制剂的组合 | |
| US12485169B2 (en) | Compounds | |
| WO2006022428A1 (ja) | 糖尿病治療剤 | |
| CN118084904A (zh) | 苯甲酰胺化合物 | |
| US20020091128A1 (en) | Combination of gaba agonists and sorbitol dehydrogenase inhibitors | |
| KR970001322A (ko) | 당뇨병 저해제로서의 치환 n-[인돌-2-카보닐]-글리신아미드 및 유도체 | |
| AU2006222060B2 (en) | Roflumilast for the treatment of diabetes mellitus | |
| CN107922388A (zh) | 用于抑制shp2活性的化合物和组合物 | |
| CA2232191A1 (en) | Inhibition of tumor necrosis factor alpha | |
| US20040192694A1 (en) | Use of COX-2 inhibitors as gastroprokinetics | |
| WO2017157792A1 (en) | Combinations of copanlisib | |
| RU2313345C2 (ru) | Комбинации, содержащие ингибитор трансдукции сигнала и производное эпотилона | |
| TW202341982A (zh) | Ｃｄｋ２抑制劑及其用途 | |
| JP2003521511A (ja) | 便秘のためのｃｏｘ−２阻害剤の使用 | |
| US20250127790A1 (en) | Combination therapy using vps34 inhibitors | |
| US20120129895A1 (en) | Methods of treatment | |
| US11684672B2 (en) | Combinations of copanlisib with anti-PD-1 antibody |