AR046890A1 - [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. - Google Patents
[1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma.Info
- Publication number
- AR046890A1 AR046890A1 ARP040104648A ARP040104648A AR046890A1 AR 046890 A1 AR046890 A1 AR 046890A1 AR P040104648 A ARP040104648 A AR P040104648A AR P040104648 A ARP040104648 A AR P040104648A AR 046890 A1 AR046890 A1 AR 046890A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- alkoxy
- hydrogen
- thiomorpholine
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se describen [1,4]oxazino[2,3-g]indazoles para reducir la presión intraocular y tratar el glaucoma. Reivindicación 1: Un método para disminuir y/o controlar la presión intraocular en un ojo de un paciente que lo necesita, que comprende la administración al paciente de una cantidad eficaz para uso farmacéutico de un compuesto de fórmula (1), en la cual: R1 y R2 son independientemente hidrógeno, alquilo C1-4; R3 se selecciona de hidrógeno, alquilo C1-4, o bien R2 y R3 juntos pueden completar un anillo de pirrolidina o piperidina, que puede estar sustituido con alquilo C1-4; R4 es hidrógeno, halógeno, alquilo C1-4; R5 y R6 se seleccionan independientemente de hidrógeno, halógeno, alquilo C1-6, alquiltio C1-6, alquilsulfonilo C1- 6, alquilsulfóxido C1-6, nitrilo o alquilo C1-6 sustituido con halógeno; R7 y R8 se seleccionan de hidrógeno, C=OR9, alquilo C1-6, alquilo C1-6 sustituido con hidroxilo, alcoxi C1-6, NR12R13, CO2H, CO2alquilo C1-6, C(=O)NR12R13, S(O)mNR12R13, o un anillo heterocíclico de 5 o 6 miembros, saturado o insaturado, que puede contener de 1-4 heteroátomos seleccionados entre N, O o S y puede estar no sustituido o sustituido con alquilo C1-4; R9 se selecciona de hidroxilo, alcoxi C1-6, NR14R15, alquilo C1-6 o alquilo C2-6 sustituido con hidroxilo, alcoxi C1-6, NR12R13, CO2H, CO2alquilo C1-6, S(O)mNR12R13, halógeno y un anillo heterocíclico seleccionado entre pirrolidin-2-ilo, imidazo-2-ilo, imidazo-4-ilo, morfolin-3-ilo, oxazolilo, isoxazolilo, tiazolilo o tetrazolilo, que puede estar no sustituido o sustituido con alquilo C1-4; R12 y R13 se seleccionan independientemente de hidrógeno, alquilo C1-6, alquilo C2-6 sustituido con hidroxilo, alcoxi C1-6 o halógeno, o bien R12, R13 y el átomo de nitrógeno interviniente, pueden formar, en conjunto, un anillo heterocíclico seleccionado entre morfolina, tiomorfolina, tiomorfolina 1-óxido, tiomorfolina 1,1-dióxido, azetidina, pirrolidina, piperidina, piperazina, no sustituida o sustituida con alquilo C1-4, o alquilo C1-4 sustituido con hidroxi o alcoxi C1-4; R14 y R15 se seleccionan independientemente de hidrógeno, alquilo C1-6, hidroxilo, alcoxi C1-6, alquilo C2-6 sustituido con hidroxilo, alcoxi C1-6, halógeno y un anillo heterocíclico seleccionado entre pirrolidin-2-ilo, imidazo-2-ilo, imidazo-4-ilo, morfolin-3-ilo, oxazolilo, isoxazolilo, tiazolilo o tetrazolilo, que puede estar no sustituido o sustituido con alquilo C1-4; o bien R14 y R15 y el átomo de nitrógeno interviniente, pueden formar, en conjunto, un anillo heterocíclico seleccionado entre morfolina, tiomorfolina, tiomorfolina 1-óxido, tiomorfolina 1,1-dióxido, azetidina, pirrolidina, piperidina, piperazina, no sustituido o sustituido con alquilo C1-4 o alquilo C1-4 sustituido con hidroxi o alcoxi C1-4; A es N o CH; X e Y son N o C; siempre que X e Y no sean iguales; y los enlaces indicados en guiones denotan un enlace simple o doble adecuadamente asignado; o su sal, solvato o profármaco aceptable para uso farmacéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US52950703P | 2003-12-15 | 2003-12-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR046890A1 true AR046890A1 (es) | 2005-12-28 |
Family
ID=34699996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040104648A AR046890A1 (es) | 2003-12-15 | 2004-12-14 | [1,4] oxazino [2,3-g] indazoles sustituidos para el tratamiento del glaucoma. |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US6989445B2 (es) |
| AR (1) | AR046890A1 (es) |
| TW (1) | TW200520760A (es) |
| WO (1) | WO2005058911A2 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US7273889B2 (en) * | 2002-09-25 | 2007-09-25 | Innovative Drug Delivery Systems, Inc. | NMDA receptor antagonist formulation with reduced neurotoxicity |
| US7476687B2 (en) * | 2003-11-26 | 2009-01-13 | Alcon, Inc. | Substituted furo[2,3-g]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 |
| US7338972B1 (en) * | 2003-12-15 | 2008-03-04 | Alcon, Inc. | Substituted 1-alkylamino-1H-indazoles for the treatment of glaucoma |
| TW200744567A (en) * | 2005-09-23 | 2007-12-16 | Alcon Inc | Phenylethylamine analogs and their use for treating glaucoma |
| US20070293475A1 (en) * | 2006-06-20 | 2007-12-20 | Alcon Manufacturing Ltd. | Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma |
| US20110293549A1 (en) | 2009-02-03 | 2011-12-01 | Athena Cosmetics, Inc. | Composition, method and kit for enhancing hair |
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| WO2004054572A2 (en) | 2002-12-13 | 2004-07-01 | Alcon, Inc. | Novel benzopyran analogs and their use for the treatment of glaucoma |
| BR0317665A (pt) | 2002-12-23 | 2005-11-29 | Alcon Inc | 1-alquil-3-aminoindazóis |
| CN101809250A (zh) | 2007-07-31 | 2010-08-18 | 圣胡安煤矿公司 | 在采矿应用和用于输送矿石的设备中使用泡沫来增加对气流的阻碍 |
-
2004
- 2004-12-14 WO PCT/US2004/041735 patent/WO2005058911A2/en active Application Filing
- 2004-12-14 AR ARP040104648A patent/AR046890A1/es unknown
- 2004-12-14 US US11/011,804 patent/US6989445B2/en not_active Expired - Fee Related
- 2004-12-14 TW TW093138738A patent/TW200520760A/zh unknown
-
2005
- 2005-07-13 US US11/180,186 patent/US7268131B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| TW200520760A (en) | 2005-07-01 |
| US7268131B2 (en) | 2007-09-11 |
| WO2005058911A2 (en) | 2005-06-30 |
| WO2005058911A3 (en) | 2005-08-25 |
| US6989445B2 (en) | 2006-01-24 |
| US20050277636A1 (en) | 2005-12-15 |
| US20050130960A1 (en) | 2005-06-16 |
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