JP2003535821A5 - - Google Patents
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- Publication number
- JP2003535821A5 JP2003535821A5 JP2001568911A JP2001568911A JP2003535821A5 JP 2003535821 A5 JP2003535821 A5 JP 2003535821A5 JP 2001568911 A JP2001568911 A JP 2001568911A JP 2001568911 A JP2001568911 A JP 2001568911A JP 2003535821 A5 JP2003535821 A5 JP 2003535821A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- halogen
- substituted
- indazol
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 82
- 229910052739 hydrogen Inorganic materials 0.000 claims 52
- 239000001257 hydrogen Substances 0.000 claims 52
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 150000002431 hydrogen Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000004432 carbon atoms Chemical group C* 0.000 claims 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 201000002674 obstructive nephropathy Diseases 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 229940079593 drugs Drugs 0.000 claims 3
- 229910052698 phosphorus Inorganic materials 0.000 claims 3
- YALUWNWLPFRZCR-UHFFFAOYSA-N 3-(2-aminopropyl)-1-methylindazol-5-ol Chemical compound C1=C(O)C=C2C(CC(N)C)=NN(C)C2=C1 YALUWNWLPFRZCR-UHFFFAOYSA-N 0.000 claims 2
- MUVNPHDJNYIOQP-UHFFFAOYSA-N 3-(2-aminopropyl)-2H-indazol-5-ol Chemical compound C1=C(O)C=C2C(CC(N)C)=NNC2=C1 MUVNPHDJNYIOQP-UHFFFAOYSA-N 0.000 claims 2
- RVEXITQCEKUGFA-UHFFFAOYSA-N 3-(2-aminopropyl)-6-fluoro-1-methylindazol-5-ol Chemical compound FC1=C(O)C=C2C(CC(N)C)=NN(C)C2=C1 RVEXITQCEKUGFA-UHFFFAOYSA-N 0.000 claims 2
- ZNYROIPGZTXHCH-UHFFFAOYSA-N 3-(2-aminopropyl)-6-fluoro-2H-indazol-5-ol Chemical compound FC1=C(O)C=C2C(CC(N)C)=NNC2=C1 ZNYROIPGZTXHCH-UHFFFAOYSA-N 0.000 claims 2
- NVOVVQZEWRKFOQ-UHFFFAOYSA-N 3-(2-aminopropyl)-7-methyl-2H-indazol-5-ol Chemical compound C1=C(O)C=C2C(CC(N)C)=NNC2=C1C NVOVVQZEWRKFOQ-UHFFFAOYSA-N 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 208000001953 Hypotension Diseases 0.000 claims 2
- QPBRBJGSIDXXNB-UHFFFAOYSA-N [3-(2-aminopropyl)-2H-indazol-5-yl] 2,2-dimethylpropanoate Chemical compound C1=C(OC(=O)C(C)(C)C)C=C2C(CC(N)C)=NNC2=C1 QPBRBJGSIDXXNB-UHFFFAOYSA-N 0.000 claims 2
- LIRGIBHYEVBULM-UHFFFAOYSA-N [3-(2-aminopropyl)-2H-indazol-5-yl] 2-methylpropanoate Chemical compound C1=C(OC(=O)C(C)C)C=C2C(CC(N)C)=NNC2=C1 LIRGIBHYEVBULM-UHFFFAOYSA-N 0.000 claims 2
- RTUVYRWSYDAWLA-UHFFFAOYSA-N [3-(2-aminopropyl)-2H-indazol-5-yl] 4-(diethylamino)-4-oxobutanoate Chemical compound CCN(CC)C(=O)CCC(=O)OC1=CC=C2NN=C(CC(C)N)C2=C1 RTUVYRWSYDAWLA-UHFFFAOYSA-N 0.000 claims 2
- UZIBJOVSEWVLOL-UHFFFAOYSA-N [3-(2-aminopropyl)-2H-indazol-5-yl] cyclopropanecarboxylate Chemical compound C1=C2C(CC(N)C)=NNC2=CC=C1OC(=O)C1CC1 UZIBJOVSEWVLOL-UHFFFAOYSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 230000003042 antagnostic Effects 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 239000002876 beta blocker Substances 0.000 claims 2
- 239000003954 decarboxylase inhibitor Substances 0.000 claims 2
- 230000004406 elevated intraocular pressure Effects 0.000 claims 2
- 230000001077 hypotensive Effects 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000003547 miosis Effects 0.000 claims 2
- 239000003604 miotic agent Substances 0.000 claims 2
- 230000000051 modifying Effects 0.000 claims 2
- 239000004090 neuroprotective agent Substances 0.000 claims 2
- 230000004493 normal intraocular pressure Effects 0.000 claims 2
- 150000003180 prostaglandins Chemical class 0.000 claims 2
- TVHAZVBUYQMHBC-VLRWBWIZSA-N (E)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-(3-oxodecyl)cyclopentyl]hept-5-enoic acid Chemical compound CCCCCCCC(=O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C\CCCC(O)=O TVHAZVBUYQMHBC-VLRWBWIZSA-N 0.000 claims 1
- TWBNMYSKRDRHAT-RCWTXCDDSA-N (S)-timolol hemihydrate Chemical compound O.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1.CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1 TWBNMYSKRDRHAT-RCWTXCDDSA-N 0.000 claims 1
- NQJNCNUFJIFXEG-UHFFFAOYSA-N 1-(5-methoxy-2H-indazol-3-yl)propan-2-amine Chemical compound COC1=CC=C2NN=C(CC(C)N)C2=C1 NQJNCNUFJIFXEG-UHFFFAOYSA-N 0.000 claims 1
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 claims 1
- IEJXVRYNEISIKR-UHFFFAOYSA-N Apraclonidine Chemical compound ClC1=CC(N)=CC(Cl)=C1NC1=NCCN1 IEJXVRYNEISIKR-UHFFFAOYSA-N 0.000 claims 1
- NWIUTZDMDHAVTP-UHFFFAOYSA-N Betaxolol Chemical compound C1=CC(OCC(O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-UHFFFAOYSA-N 0.000 claims 1
- AQOKCDNYWBIDND-FTOWTWDKSA-N Bimatoprost Chemical compound CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-FTOWTWDKSA-N 0.000 claims 1
- HCRKCZRJWPKOAR-JTQLQIEISA-N Brinzolamide Chemical compound CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 HCRKCZRJWPKOAR-JTQLQIEISA-N 0.000 claims 1
- 229960001222 Carteolol Drugs 0.000 claims 1
- LWAFSWPYPHEXKX-UHFFFAOYSA-N Carteolol Chemical compound N1C(=O)CCC2=C1C=CC=C2OCC(O)CNC(C)(C)C LWAFSWPYPHEXKX-UHFFFAOYSA-N 0.000 claims 1
- GGUSQTSTQSHJAH-UHFFFAOYSA-N Eliprodil Chemical compound C=1C=C(Cl)C=CC=1C(O)CN(CC1)CCC1CC1=CC=C(F)C=C1 GGUSQTSTQSHJAH-UHFFFAOYSA-N 0.000 claims 1
- 229950005455 Eliprodil Drugs 0.000 claims 1
- UCTWMZQNUQWSLP-VIFPVBQESA-N Epinephrine Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims 1
- 229940095437 Iopidine Drugs 0.000 claims 1
- GGXICVAJURFBLW-CEYXHVGTSA-N Latanoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 claims 1
- 229960004771 Levobetaxolol Drugs 0.000 claims 1
- NWIUTZDMDHAVTP-KRWDZBQOSA-N Levobetaxolol Chemical compound C1=CC(OC[C@@H](O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-KRWDZBQOSA-N 0.000 claims 1
- IXHBTMCLRNMKHZ-LBPRGKRZSA-N Levobunolol Chemical compound O=C1CCCC2=C1C=CC=C2OC[C@@H](O)CNC(C)(C)C IXHBTMCLRNMKHZ-LBPRGKRZSA-N 0.000 claims 1
- 229960000831 Levobunolol Drugs 0.000 claims 1
- 229940112534 Lumigan Drugs 0.000 claims 1
- OMCPLEZZPVJJIS-UHFFFAOYSA-N Nipradilol Chemical compound C1C(O[N+]([O-])=O)COC2=C1C=CC=C2OCC(O)CNC(C)C OMCPLEZZPVJJIS-UHFFFAOYSA-N 0.000 claims 1
- 229950000754 Nipradilol Drugs 0.000 claims 1
- QCHFTSOMWOSFHM-WPRPVWTQSA-N Pilopine HS Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 claims 1
- AQHHHDLHHXJYJD-UHFFFAOYSA-N Proprasylyt Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims 1
- MKPLKVHSHYCHOC-AHTXBMBWSA-N Travoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC=CC(C(F)(F)F)=C1 MKPLKVHSHYCHOC-AHTXBMBWSA-N 0.000 claims 1
- 229960004317 UNOPROSTONE Drugs 0.000 claims 1
- 229960004324 betaxolol Drugs 0.000 claims 1
- 229960002470 bimatoprost Drugs 0.000 claims 1
- 229960003679 brimonidine Drugs 0.000 claims 1
- 229960000722 brinzolamide Drugs 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- IAVUPMFITXYVAF-XPUUQOCRSA-N dorzolamide Chemical compound CCN[C@H]1C[C@H](C)S(=O)(=O)C2=C1C=C(S(N)(=O)=O)S2 IAVUPMFITXYVAF-XPUUQOCRSA-N 0.000 claims 1
- 229960003933 dorzolamide Drugs 0.000 claims 1
- 229960005139 epinephrine Drugs 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 229960001160 latanoprost Drugs 0.000 claims 1
- 229960001416 pilocarpine Drugs 0.000 claims 1
- 229960003712 propranolol Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229960004605 timolol Drugs 0.000 claims 1
- 229960002368 travoprost Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19028300P | 2000-03-17 | 2000-03-17 | |
| US60/190,283 | 2000-03-17 | ||
| PCT/US2000/031143 WO2001070701A1 (en) | 2000-03-17 | 2000-11-14 | 5-hydroxy indazole derivatives for treating glaucoma |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003535821A JP2003535821A (ja) | 2003-12-02 |
| JP2003535821A5 true JP2003535821A5 (ru) | 2005-07-28 |
Family
ID=22700701
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001568911A Pending JP2003535821A (ja) | 2000-03-17 | 2000-11-14 | 緑内障を治療するための５−ヒドロキシインダゾール誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP1268439A1 (ru) |
| JP (1) | JP2003535821A (ru) |
| KR (1) | KR20030095183A (ru) |
| CN (1) | CN1450995A (ru) |
| AR (1) | AR026708A1 (ru) |
| AU (2) | AU1918001A (ru) |
| BR (1) | BR0017163A (ru) |
| CA (1) | CA2401959A1 (ru) |
| MX (1) | MXPA02008825A (ru) |
| PL (1) | PL365422A1 (ru) |
| WO (1) | WO2001070701A1 (ru) |
| ZA (1) | ZA200206853B (ru) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6960579B1 (en) | 1998-05-19 | 2005-11-01 | Alcon Manufacturing, Ltd. | Serotonergic 5HT7 receptor compounds for treating ocular and CNS disorders |
| DE60209486T2 (de) | 2001-06-01 | 2006-08-03 | Alcon Inc. | Pyranoindazole und ihre verwendung in der glaukombehandlung |
| TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| US7196082B2 (en) * | 2002-11-08 | 2007-03-27 | Merck & Co. Inc. | Ophthalmic compositions for treating ocular hypertension |
| CN100384827C (zh) * | 2002-11-08 | 2008-04-30 | 默克公司 | 用于治疗高眼压症的眼用组合物 |
| JP2006510742A (ja) * | 2002-11-08 | 2006-03-30 | メルク エンド カムパニー インコーポレーテッド | 高眼圧治療用眼科組成物 |
| CA2506204A1 (en) | 2002-12-13 | 2004-07-01 | Alcon, Inc. | Novel benzopyran analogs and their use for the treatment of glaucoma |
| JP2004262812A (ja) * | 2003-02-28 | 2004-09-24 | Rohto Pharmaceut Co Ltd | 眼圧低下剤 |
| JP2007504236A (ja) * | 2003-09-04 | 2007-03-01 | メルク エンド カムパニー インコーポレーテッド | 高眼圧症を治療するための眼用組成物 |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| US7338972B1 (en) | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| WO2005058911A2 (en) | 2003-12-15 | 2005-06-30 | Alcon, Inc. | Substituted [1,4]oxazino[2,3-g]indazoles for the treatment of glaucoma |
| ATE460415T1 (de) | 2004-11-29 | 2010-03-15 | Warner Lambert Co | Therapeutische pyrazoloä3,4-büpyridine und - indazole |
| WO2006062839A1 (en) | 2004-12-08 | 2006-06-15 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| KR100972921B1 (ko) * | 2009-12-02 | 2010-07-28 | 제이케이이앤씨 주식회사 | 회전 격판식 선회류 세정 및 탈취장치 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2680366B1 (fr) * | 1991-08-13 | 1995-01-20 | Adir | Nouveaux derives d'arylethylamines, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent. |
| WO1999059499A2 (en) * | 1998-05-19 | 1999-11-25 | Alcon Laboratories, Inc. | Serotonergic 5ht7 receptor compounds for treating ocular and cns disorders |
| GB9819020D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds III |
| US6664286B1 (en) * | 1998-09-18 | 2003-12-16 | Alcon Manufacturing, Ltd. | Serotonergic 5ht2 agonists for treating glaucoma |
-
2000
- 2000-11-14 BR BR0017163-8A patent/BR0017163A/pt not_active IP Right Cessation
- 2000-11-14 MX MXPA02008825A patent/MXPA02008825A/es unknown
- 2000-11-14 WO PCT/US2000/031143 patent/WO2001070701A1/en not_active Application Discontinuation
- 2000-11-14 PL PL00365422A patent/PL365422A1/xx not_active Application Discontinuation
- 2000-11-14 CA CA002401959A patent/CA2401959A1/en not_active Abandoned
- 2000-11-14 CN CN00819348A patent/CN1450995A/zh active Pending
- 2000-11-14 AU AU1918001A patent/AU1918001A/xx active Pending
- 2000-11-14 EP EP00982109A patent/EP1268439A1/en not_active Withdrawn
- 2000-11-14 AU AU2001219180A patent/AU2001219180B2/en not_active Ceased
- 2000-11-14 KR KR1020027011862A patent/KR20030095183A/ko not_active Application Discontinuation
- 2000-11-14 JP JP2001568911A patent/JP2003535821A/ja active Pending
- 2000-12-01 AR ARP000106395A patent/AR026708A1/es unknown
-
2002
- 2002-08-27 ZA ZA200206853A patent/ZA200206853B/en unknown
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