PE20040692A1 - Composiciones oftalmologicas de indazol como bloqueadores de los canales de potasio - Google Patents
Composiciones oftalmologicas de indazol como bloqueadores de los canales de potasioInfo
- Publication number
- PE20040692A1 PE20040692A1 PE2003001115A PE2003001115A PE20040692A1 PE 20040692 A1 PE20040692 A1 PE 20040692A1 PE 2003001115 A PE2003001115 A PE 2003001115A PE 2003001115 A PE2003001115 A PE 2003001115A PE 20040692 A1 PE20040692 A1 PE 20040692A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- indazol
- potassium channels
- blockers
- compounds
- Prior art date
Links
- 102000004257 Potassium Channel Human genes 0.000 title abstract 3
- 108020001213 potassium channel Proteins 0.000 title abstract 3
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical group C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 2
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 abstract 1
- 229930182837 (R)-adrenaline Natural products 0.000 abstract 1
- -1 2-HYDROXYETHYL Chemical class 0.000 abstract 1
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 abstract 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 abstract 1
- 208000010412 Glaucoma Diseases 0.000 abstract 1
- 108050004689 Inhibitor of carbonic anhydrases Proteins 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 210000001742 aqueous humor Anatomy 0.000 abstract 1
- 239000002876 beta blocker Substances 0.000 abstract 1
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 abstract 1
- 230000000903 blocking effect Effects 0.000 abstract 1
- 229960003679 brimonidine Drugs 0.000 abstract 1
- 239000011575 calcium Substances 0.000 abstract 1
- 229910052791 calcium Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229960005139 epinephrine Drugs 0.000 abstract 1
- 230000004410 intraocular pressure Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000012049 topical pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/65031—Five-membered rings having the nitrogen atoms in the positions 1 and 2
- C07F9/65038—Five-membered rings having the nitrogen atoms in the positions 1 and 2 condensed with carbocyclic rings or carbocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE INDAZOL DE FORMULA (I) DONDE R Y Ry SON INDEPENDIENTEMENTE H O ALQUIL(C1-C6); R2 ES H, ALQUIL(C1-C10), OH, ALQUENIL(C2-C6), -(CH2)nO(CH2)mOR, -(CH2)nALCOXI(C1-C6), -(CH2)nCICLOALQUILL(C3-C8), ENTRE OTROS; R3 ES H, ALQUIL(C1-C10), -(CH2)nCICLOALQUIL(C3-C8), -(CH2)nO(CH2)mOR, (CH2)nHETEROCICLIL(C3-C10), -(CH2)nCOOR, ENTRE OTROS; R4 Y R5 SON INDEPENDIENTEMENTE H, ALCOXI(C1-C6), OH, ALQUIL(C1-C6), COOR, SOqALQUIL(C1-C6), ENTRE OTROS; R6 ES H, ALQUIL(C1-C10), -(CH2)nARIL(C6-C10), -(CH2)nHETEROCICLIL(C3-C10), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-(3-{[6-(2-HIDROXIETIL)PIRIDINA-3-IL]CARBONIL}-6-METOXI-1H-INDAZOL-1-IL)-3,3-DIMETILBUTAN-2-ONA, DI-TER-BUTIL 4-{[1-(3,3-DIMETIL-2-OXOBUTIL)-6-METOXI-1-H-INDAZOL-3-IL]CARBONIL}HIDROXIETILBENCIL; ENTRE OTROS. ESTOS COMPUESTOS SON POTENTES BLOQUEADORES DE LOS CANALES DE POTASIO, ESPECIALMENTE DE LOS CANALES DE POTASIO ACTIVADOS POR CALCIO Y CON ALTA CONDUCTANCIA (MAXI-K), AL BLOQUEARLOS INHIBEN LA PRODUCCION DE HUMOR ACUOSO Y POR ELLO DISMINUYE LA PIO, POR LO QUE SON UTILES PARA EL TRATAMIENTO DE GLAUCOMA Y OTRAS ENFERMEDADES RELACIONADAS CON UNA ELEVADA PRESION INTRAOCULAR.TAMBIEN SE REFIERE A UNA COMPOSICION DEL COMPUESTO CON UNA FORMULACION TOPICA,Y CON OTRO AGENTE ACTIVO COMO UN BLOQUEADOR ß-ADRENERGICO COMO TIMOLOL, BETAXOLOL ENTRE OTROS, UN PARASIMPATICOMIMETICO COMO PILOCARPINA, UN SIMPATICOMIMETICO COMO EPINEFRINA, BRIMONIDINA, UN INHIBIDOR DE LA ANHIDRASA CARBONICA, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42480802P | 2002-11-08 | 2002-11-08 | |
| US50009103P | 2003-09-04 | 2003-09-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20040692A1 true PE20040692A1 (es) | 2004-10-08 |
Family
ID=32314559
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2003001115A PE20040692A1 (es) | 2002-11-08 | 2003-11-05 | Composiciones oftalmologicas de indazol como bloqueadores de los canales de potasio |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US7196082B2 (es) |
| EP (1) | EP1562909B1 (es) |
| JP (2) | JP4456072B2 (es) |
| KR (1) | KR20050072805A (es) |
| AR (1) | AR041991A1 (es) |
| AU (2) | AU2003286884A1 (es) |
| BR (1) | BR0316040A (es) |
| CA (1) | CA2505086C (es) |
| CL (1) | CL2003002293A1 (es) |
| DO (1) | DOP2003000747A (es) |
| EC (1) | ECSP055781A (es) |
| HR (1) | HRP20050409A2 (es) |
| IS (1) | IS7822A (es) |
| MA (1) | MA27497A1 (es) |
| MX (1) | MXPA05004889A (es) |
| NO (1) | NO20052751D0 (es) |
| NZ (1) | NZ539593A (es) |
| PE (1) | PE20040692A1 (es) |
| PL (1) | PL377172A1 (es) |
| RU (1) | RU2005117627A (es) |
| TW (1) | TWI250873B (es) |
| WO (2) | WO2004043932A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20040028469A (ko) | 2002-09-30 | 2004-04-03 | 엘지전자 주식회사 | 1 회 기록 가능한 광디스크의 디펙트 영역 관리방법 |
| US7135575B2 (en) * | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| KR20060090801A (ko) * | 2003-09-04 | 2006-08-16 | 머크 앤드 캄파니 인코포레이티드 | 고안압증 치료용 안용 조성물 |
| AU2005274972A1 (en) * | 2004-07-20 | 2006-02-23 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| EP1647549A1 (en) * | 2004-10-14 | 2006-04-19 | Laboratoire Theramex | Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents |
| SG175599A1 (en) * | 2006-01-31 | 2011-11-28 | Array Biopharma Inc | Kinase inhibitors and methods of use thereof |
| EP2004193A2 (en) * | 2006-03-13 | 2008-12-24 | Merck & Co., Inc. | Ophthalmic compositions for treating ocular hypertension |
| MX2008012482A (es) * | 2006-03-31 | 2008-10-10 | Abbott Lab | Compuestos de indazol. |
| WO2010051561A1 (en) * | 2008-11-03 | 2010-05-06 | Chemocentryx, Inc. | Compounds for the treatment of osteoporosis and cancers |
| JP5951625B2 (ja) | 2010-11-24 | 2016-07-13 | ザ・トラスティーズ・オブ・コランビア・ユニバーシティー・イン・ザ・シティー・オブ・ニューヨークＴｈｅ Ｔｒｕｓｔｅｅｓ Ｏｆ Ｃｏｌｕｍｂｉａ Ｕｎｉｖｅｒｓｉｔｙ Ｉｎ Ｔｈｅ Ｃｉｔｙ Ｏｆ Ｎｅｗ Ｙｏｒｋ | 加齢性黄斑変性症およびシュタルガルト病の処置のための非レチノイドｒｂｐ４アンタゴニスト |
| US9333202B2 (en) | 2012-05-01 | 2016-05-10 | The Trustees Of Columbia University In The City Of New York | Non-retinoid antagonists for treatment of age-related macular degeneration and stargardt disease |
| WO2014151936A1 (en) | 2013-03-14 | 2014-09-25 | The Trustees Of Columbia University In The City Of New York | Octahydropyrrolopyrroles, their preparation and use |
| US9938291B2 (en) | 2013-03-14 | 2018-04-10 | The Trustess Of Columbia University In The City Of New York | N-alkyl-2-phenoxyethanamines, their preparation and use |
| ES2705247T3 (es) | 2013-03-14 | 2019-03-22 | Univ Columbia | 4-fenilpiperidinas, su preparación y uso |
| EP2968303B1 (en) | 2013-03-14 | 2018-07-04 | The Trustees of Columbia University in the City of New York | Octahydrocyclopentapyrroles, their preparation and use |
| AU2015253232B2 (en) | 2014-04-30 | 2020-10-01 | The Trustees Of Columbia University In The City Of New York | Substituted 4-phenylpiperidines, their preparation and use |
| CN104211638A (zh) * | 2014-08-13 | 2014-12-17 | 李增 | 一种脂肪氨基取代的芸香碱类衍生物及其制备和作为抗阿尔兹海默症的药物中的应用 |
| WO2017123826A1 (en) | 2016-01-14 | 2017-07-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2534580A1 (fr) | 1982-10-13 | 1984-04-20 | Synthelabo | Derives de phenyl-1 piperidino-2 propanol, leur preparation, et medicaments qui les contiennent |
| US5151444B1 (en) | 1987-09-18 | 1999-07-06 | R Tech Ueno Ltd | Ocular hypotensive agents |
| AU3693789A (en) | 1988-05-10 | 1989-11-29 | Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab) | New ophthalmic preparation for treating glaucoma |
| ES2317964T5 (es) | 1988-09-06 | 2015-02-20 | Pfizer Health Ab | Derivado de prostaglandina-F2alfa para el tratamiento de glaucoma o hipertensión ocular |
| US5296504A (en) | 1988-09-06 | 1994-03-22 | Kabi Pharmacia | Prostaglandin derivatives for the treatment of glaucoma or ocular hypertension |
| US5352708A (en) | 1992-09-21 | 1994-10-04 | Allergan, Inc. | Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents |
| US5922773A (en) | 1992-12-04 | 1999-07-13 | The Children's Medical Center Corp. | Glaucoma treatment |
| FR2701026B1 (fr) | 1993-02-02 | 1995-03-31 | Adir | Nouveaux dérivés de l'indole, de l'indazole et du benzisoxazole, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
| JP3208210B2 (ja) * | 1993-03-17 | 2001-09-10 | 旭化成株式会社 | 結晶性芳香族ポリカーボネートプレポリマーの製造方法及び芳香族ポリカーボネートの製造方法 |
| EP0724443A4 (en) | 1993-06-08 | 1997-09-10 | Vide Pharmaceuticals | METHOD AND PREPARATIONS FOR LOWERING THE EYE PRESSURE |
| US5510383A (en) | 1993-08-03 | 1996-04-23 | Alcon Laboratories, Inc. | Use of cloprostenol, fluprostenol and their salts and esters to treat glaucoma and ocular hypertension |
| US5573758A (en) | 1995-04-28 | 1996-11-12 | Allergan | Method for reducing intraocular pressure in the mammalian eye by administration of potassium channel blockers |
| AP2001002304A0 (en) * | 1996-05-03 | 2001-12-31 | Pfizer | Substituted indazole derivatives and related compounds |
| US5925342A (en) | 1996-11-13 | 1999-07-20 | Allergan | Method for reducing intraocular pressure in the mammalian eye by administration of potassium channel blockers |
| GB2321455A (en) * | 1997-01-24 | 1998-07-29 | Norsk Hydro As | Lipophilic derivatives of biologically active compounds |
| EP1114816A4 (en) | 1998-09-14 | 2002-09-04 | Ono Pharmaceutical Co | SUBSTITUTED PHENYL-PROSTAGLANDIN E DERIVATIVES- $ g (V) AND MEDICINAL PRODUCTS CONTAINING THEM AS ACTIVE INGREDIENT |
| AP2002002555A0 (en) | 1999-12-22 | 2002-06-30 | Pfizer Prod Inc | EP4 Receptor selective agonists in the treatment of osteoporosis. |
| JP2003520245A (ja) | 2000-01-18 | 2003-07-02 | 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科組成物 |
| AU2001219180B2 (en) | 2000-03-17 | 2005-04-07 | Alcon, Inc. | 5-hydroxy indazole derivatives for treating glaucoma |
| US6956036B1 (en) * | 2000-03-17 | 2005-10-18 | Alcon, Inc. | 6-hydroxy-indazole derivatives for treating glaucoma |
| AU2001216072A1 (en) | 2000-03-17 | 2001-10-03 | Alcon, Inc. | 6-hydroxy-indazole derivatives for treating glaucoma |
| EP1186287A1 (en) | 2000-03-31 | 2002-03-13 | Toray Industries, Inc. | Hair growth or hair formation controlling agents |
| WO2002024647A1 (en) | 2000-09-21 | 2002-03-28 | Ono Pharmaceutical Co., Ltd. | Ep4 receptor agonists containing 8-azaprostaglandin derivatives as the active ingredient |
| DK1339678T3 (da) | 2000-11-27 | 2008-02-04 | Pfizer Prod Inc | Selektive agonister til EP4-receptor til behandling af osteoporose |
| FR2827861B1 (fr) | 2001-07-27 | 2004-04-02 | Aventis Pharma Sa | Derives des indazoles ou des indoles, leur utilisation en medecine humaine et plus particulierement en cancerologie |
-
2003
- 2003-10-14 US US10/684,990 patent/US7196082B2/en not_active Expired - Lifetime
- 2003-11-03 TW TW092130678A patent/TWI250873B/zh not_active IP Right Cessation
- 2003-11-04 PL PL377172A patent/PL377172A1/pl not_active Application Discontinuation
- 2003-11-04 MX MXPA05004889A patent/MXPA05004889A/es unknown
- 2003-11-04 NZ NZ539593A patent/NZ539593A/en unknown
- 2003-11-04 WO PCT/US2003/035078 patent/WO2004043932A1/en not_active Ceased
- 2003-11-04 CA CA002505086A patent/CA2505086C/en not_active Expired - Fee Related
- 2003-11-04 JP JP2005507086A patent/JP4456072B2/ja not_active Expired - Fee Related
- 2003-11-04 AR ARP030104032A patent/AR041991A1/es not_active Application Discontinuation
- 2003-11-04 KR KR1020057008142A patent/KR20050072805A/ko not_active Ceased
- 2003-11-04 BR BR0316040-8A patent/BR0316040A/pt not_active IP Right Cessation
- 2003-11-04 AU AU2003286884A patent/AU2003286884A1/en not_active Abandoned
- 2003-11-04 AU AU2003287506A patent/AU2003287506B8/en not_active Ceased
- 2003-11-04 RU RU2005117627/04A patent/RU2005117627A/ru not_active Application Discontinuation
- 2003-11-04 HR HR20050409A patent/HRP20050409A2/hr not_active Application Discontinuation
- 2003-11-04 EP EP03781747A patent/EP1562909B1/en not_active Expired - Lifetime
- 2003-11-04 WO PCT/US2003/035080 patent/WO2004043933A1/en not_active Ceased
- 2003-11-05 PE PE2003001115A patent/PE20040692A1/es not_active Application Discontinuation
- 2003-11-07 CL CL200302293A patent/CL2003002293A1/es unknown
- 2003-11-07 DO DO2003000747A patent/DOP2003000747A/es unknown
-
2005
- 2005-04-25 IS IS7822A patent/IS7822A/is unknown
- 2005-05-06 EC EC2005005781A patent/ECSP055781A/es unknown
- 2005-06-07 MA MA28316A patent/MA27497A1/fr unknown
- 2005-06-07 NO NO20052751A patent/NO20052751D0/no unknown
-
2006
- 2006-12-19 US US11/641,212 patent/US7547720B2/en not_active Expired - Lifetime
-
2009
- 2009-08-24 JP JP2009192691A patent/JP5061293B2/ja not_active Expired - Fee Related
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