JP2003528085A5 - - Google Patents
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- Publication number
- JP2003528085A5 JP2003528085A5 JP2001568912A JP2001568912A JP2003528085A5 JP 2003528085 A5 JP2003528085 A5 JP 2003528085A5 JP 2001568912 A JP2001568912 A JP 2001568912A JP 2001568912 A JP2001568912 A JP 2001568912A JP 2003528085 A5 JP2003528085 A5 JP 2003528085A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- halogen
- independently selected
- trifluoromethyl
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims 2
- IUIAMNBONBRMDM-WLHGVMLRSA-N 1-(2-aminopropyl)-3-methylindazol-6-ol (E)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.c1cc(O)cc2c1c(C)nn2CC(N)C IUIAMNBONBRMDM-WLHGVMLRSA-N 0.000 claims 2
- -1 C 1-6 alkylsulfoxyl Chemical group 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims 2
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 claims 1
- 229930182837 (R)-adrenaline Natural products 0.000 claims 1
- GGUSQTSTQSHJAH-FQEVSTJZSA-N (R)-eliprodil Chemical compound C([C@H](O)C=1C=CC(Cl)=CC=1)N(CC1)CCC1CC1=CC=C(F)C=C1 GGUSQTSTQSHJAH-FQEVSTJZSA-N 0.000 claims 1
- NWIUTZDMDHAVTP-KRWDZBQOSA-N (S)-betaxolol Chemical compound C1=CC(OC[C@@H](O)CNC(C)C)=CC=C1CCOCC1CC1 NWIUTZDMDHAVTP-KRWDZBQOSA-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
- PNHDUSKIMUKQDR-UHFFFAOYSA-N 1-(3-chloro-6-methoxyindazol-1-yl)propan-2-amine Chemical compound COC1=CC=C2C(Cl)=NN(CC(C)N)C2=C1 PNHDUSKIMUKQDR-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
- OMCPLEZZPVJJIS-UHFFFAOYSA-N Hypadil (TN) Chemical compound C1C(O[N+]([O-])=O)COC2=C1C=CC=C2OCC(O)CNC(C)C OMCPLEZZPVJJIS-UHFFFAOYSA-N 0.000 claims 1
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000003276 anti-hypertensive effect Effects 0.000 claims 1
- 229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 claims 1
- IEJXVRYNEISIKR-UHFFFAOYSA-N apraclonidine Chemical compound ClC1=CC(N)=CC(Cl)=C1NC1=NCCN1 IEJXVRYNEISIKR-UHFFFAOYSA-N 0.000 claims 1
- 239000002876 beta blocker Substances 0.000 claims 1
- 229940097320 beta blocking agent Drugs 0.000 claims 1
- 229960004324 betaxolol Drugs 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
- 229960003679 brimonidine Drugs 0.000 claims 1
- 229960000722 brinzolamide Drugs 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
- 239000003489 carbonate dehydratase inhibitor Substances 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
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003933 dorzolamide Drugs 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
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960005139 epinephrine Drugs 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229940095437 iopidine Drugs 0.000 claims 1
- 229960001160 latanoprost 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
- 229960000831 levobunolol Drugs 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
- 150000002632 lipids Chemical class 0.000 claims 1
- 230000003547 miosis Effects 0.000 claims 1
- 239000003604 miotic agent Substances 0.000 claims 1
- 239000004090 neuroprotective agent Substances 0.000 claims 1
- 229950000754 nipradilol Drugs 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229960001416 pilocarpine Drugs 0.000 claims 1
- 229960003712 propranolol Drugs 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229960004605 timolol Drugs 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 229960002368 travoprost Drugs 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
- TVHAZVBUYQMHBC-SNHXEXRGSA-N unoprostone Chemical compound CCCCCCCC(=O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(O)=O TVHAZVBUYQMHBC-SNHXEXRGSA-N 0.000 claims 1
- 229960004317 unoprostone Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19038000P | 2000-03-17 | 2000-03-17 | |
| US60/190,380 | 2000-03-17 | ||
| PCT/US2000/031247 WO2001070702A1 (en) | 2000-03-17 | 2000-11-14 | 6-hydroxy-indazole derivatives for treating glaucoma |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003528085A JP2003528085A (ja) | 2003-09-24 |
| JP2003528085A5 true JP2003528085A5 (https=) | 2005-12-22 |
Family
ID=22701093
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001568912A Withdrawn JP2003528085A (ja) | 2000-03-17 | 2000-11-14 | 緑内障治療のための６−ヒドロキシ・インダゾール誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1268438A1 (https=) |
| JP (1) | JP2003528085A (https=) |
| KR (1) | KR20030065304A (https=) |
| CN (1) | CN1450994A (https=) |
| AR (1) | AR032138A1 (https=) |
| AU (1) | AU2001216072A1 (https=) |
| BR (1) | BR0017157A (https=) |
| CA (1) | CA2402403A1 (https=) |
| GC (1) | GC0000155A (https=) |
| MX (1) | MXPA02008547A (https=) |
| PL (1) | PL358481A1 (https=) |
| TW (1) | TWI221839B (https=) |
| WO (1) | WO2001070702A1 (https=) |
| ZA (1) | ZA200206851B (https=) |
Families Citing this family (20)
| 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 |
| TW593302B (en) | 2001-12-20 | 2004-06-21 | Alcon Inc | Novel benzodifuranimidazoline and benzofuranimidazoline derivatives and their use for the treatment of glaucoma |
| AU2002360819A1 (en) * | 2001-12-28 | 2003-07-24 | Bayer Corporation | Cyclohexano- and cycloheptapyrazole derivative compounds, for use in diseases associated with the 5-ht2c receptor |
| AU2003287481B2 (en) | 2002-11-08 | 2009-04-23 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| 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 |
| US7053085B2 (en) | 2003-03-26 | 2006-05-30 | Merck & Co. Inc. | EP4 receptor agonist, compositions and methods thereof |
| BR0316775A (pt) | 2002-12-13 | 2005-11-01 | Alcon Inc | Novos análogos de benzopirano e seu uso para o tratamento de glaucoma |
| JP2004262812A (ja) * | 2003-02-28 | 2004-09-24 | Rohto Pharmaceut Co Ltd | 眼圧低下剤 |
| AU2004268012B2 (en) | 2003-09-02 | 2008-11-20 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| DE602004020079D1 (de) | 2003-09-04 | 2009-04-30 | Merck & Co Inc | Ophthalmische zusammensetzungen zur behandlung der okularen hypertonie |
| AU2004271978B2 (en) | 2003-09-04 | 2009-02-05 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| TW200520760A (en) | 2003-12-15 | 2005-07-01 | Alcon Inc | Substituted [1,4] oxazino [2,3-g] indazoles 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 |
| US7129257B1 (en) | 2003-12-15 | 2006-10-31 | Alcon, Inc. | Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma |
| CN1988903A (zh) | 2004-07-20 | 2007-06-27 | 默克公司 | 用于治疗高眼压症的眼用组合物 |
| ATE460415T1 (de) | 2004-11-29 | 2010-03-15 | Warner Lambert Co | Therapeutische pyrazoloä3,4-büpyridine und - indazole |
| US7425572B2 (en) | 2004-12-08 | 2008-09-16 | Alcon, Inc. | Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma |
| CN101704785B (zh) * | 2009-11-16 | 2012-02-29 | 东南大学 | 有机二羧酸和其盐及其制备方法 |
| CN105884687B (zh) * | 2016-04-14 | 2018-06-22 | 梯尔希（南京）药物研发有限公司 | 一种5-苄基苄达明的制备方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1301161A (zh) * | 1998-05-19 | 2001-06-27 | 艾尔科实验室公司 | 用于治疗眼睛和中枢神经系统障碍的血清素激活的5ht7受体化合物 |
| ATE247963T1 (de) * | 1998-05-26 | 2003-09-15 | Pfizer Prod Inc | Medikament zur behandlung von glaukoma und ischämischer retinopathie |
| GB9819032D0 (en) * | 1998-09-01 | 1998-10-28 | Cerebrus Ltd | Chemical compounds IV |
| CN1269484C (zh) * | 1998-09-18 | 2006-08-16 | 艾尔科实验室公司 | 用于治疗青光眼的5－羟色胺激活性激动剂 |
| GB9820767D0 (en) * | 1998-09-23 | 1998-11-18 | Cerebrus Ltd | Chemical compounds VIII |
-
2000
- 2000-11-14 BR BR0017157-3A patent/BR0017157A/pt not_active IP Right Cessation
- 2000-11-14 WO PCT/US2000/031247 patent/WO2001070702A1/en not_active Ceased
- 2000-11-14 KR KR1020027011867A patent/KR20030065304A/ko not_active Ceased
- 2000-11-14 PL PL00358481A patent/PL358481A1/xx not_active Application Discontinuation
- 2000-11-14 MX MXPA02008547A patent/MXPA02008547A/es unknown
- 2000-11-14 AU AU2001216072A patent/AU2001216072A1/en not_active Abandoned
- 2000-11-14 EP EP00978628A patent/EP1268438A1/en not_active Withdrawn
- 2000-11-14 JP JP2001568912A patent/JP2003528085A/ja not_active Withdrawn
- 2000-11-14 CA CA002402403A patent/CA2402403A1/en not_active Abandoned
- 2000-11-14 CN CN00819346A patent/CN1450994A/zh active Pending
- 2000-11-27 TW TW089125127A patent/TWI221839B/zh not_active IP Right Cessation
- 2000-12-01 AR ARP000106394A patent/AR032138A1/es not_active Application Discontinuation
- 2000-12-03 GC GCP20001082 patent/GC0000155A/xx active
-
2002
- 2002-08-27 ZA ZA200206851A patent/ZA200206851B/en unknown
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