JP2016503797A - ペリ−カルビノール - Google Patents
ペリ−カルビノール Download PDFInfo
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- JP2016503797A JP2016503797A JP2015549717A JP2015549717A JP2016503797A JP 2016503797 A JP2016503797 A JP 2016503797A JP 2015549717 A JP2015549717 A JP 2015549717A JP 2015549717 A JP2015549717 A JP 2015549717A JP 2016503797 A JP2016503797 A JP 2016503797A
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- Prior art keywords
- compound
- alkyl
- independently
- compound according
- pharmaceutically acceptable
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- 150000001875 compounds Chemical class 0.000 claims abstract description 168
- 238000000034 method Methods 0.000 claims abstract description 39
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- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims abstract description 17
- 230000002207 retinal effect Effects 0.000 claims abstract description 17
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- 230000011506 response to oxidative stress Effects 0.000 claims abstract description 14
- 239000000203 mixture Substances 0.000 claims description 80
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- 125000001424 substituent group Chemical group 0.000 claims description 22
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 19
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 19
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- 229910052794 bromium Inorganic materials 0.000 claims description 16
- 125000004429 atom Chemical group 0.000 claims description 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 11
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
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- 125000005270 trialkylamine group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- DSDAICPXUXPBCC-MWDJDSKUSA-N trimethyl-β-cyclodextrin Chemical compound COC[C@H]([C@H]([C@@H]([C@H]1OC)OC)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COC)[C@H]([C@@H]([C@H]3OC)OC)O[C@H]3O[C@H](COC)[C@H]([C@@H]([C@H]3OC)OC)O[C@H]3O[C@H](COC)[C@H]([C@@H]([C@H]3OC)OC)O[C@H]3O[C@H](COC)[C@H]([C@@H]([C@H]3OC)OC)O3)[C@H](OC)[C@H]2OC)COC)O[C@@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@@H]3O[C@@H]1COC DSDAICPXUXPBCC-MWDJDSKUSA-N 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
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- 239000003981 vehicle Substances 0.000 description 1
- 230000004393 visual impairment Effects 0.000 description 1
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Images
Classifications
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
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| PCT/US2013/076592 WO2014100425A1 (en) | 2012-12-20 | 2013-12-19 | Peri-carbinols |
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| US7973025B2 (en) | 2005-05-26 | 2011-07-05 | Neuron Systems, Inc. | Compositions and methods of treating retinal disease |
| CA2782015C (en) | 2009-12-11 | 2020-08-25 | Neuron Systems, Inc. | Topical ophthalmic compositions and methods for the treatment of macular degeneration |
| GEP201706757B (en) | 2012-12-21 | 2017-10-25 | Alios Biopharma Inc | Substituted nucleosides, nucleotides and analogs thereof |
| CA2898631C (en) | 2013-01-23 | 2023-06-13 | Aldeyra Therapeutics, Inc. | Toxic aldehyde related diseases and treatment |
| RU2015126015A (ru) | 2013-01-25 | 2017-03-03 | Альдейра Терапьютикс, Инк. | Новые улавливатели в лечении макулодистрофии |
| CA2996183A1 (en) * | 2015-08-21 | 2017-03-02 | Aldeyra Therapeutics, Inc. | Deuterated compounds and uses thereof |
| KR20180073553A (ko) * | 2015-08-21 | 2018-07-02 | 알데이라 테라퓨틱스, 아이엔씨. | 알데히드 접합체 및 이의 용도 |
| KR20180116416A (ko) | 2016-02-28 | 2018-10-24 | 알데이라 테라퓨틱스, 아이엔씨. | 사이클로덱스트린으로의 알레르기성 안질환의 치료 |
| US11129823B2 (en) | 2016-05-09 | 2021-09-28 | Aldeyra Therapeutics, Inc. | Combination treatment of ocular inflammatory disorders and diseases |
| EP3500256A4 (en) * | 2016-08-22 | 2020-01-08 | Aldeyra Therapeutics, Inc. | ALDEHYDE TRAPPING COMPOUNDS AND USES THEREOF |
| JP7648117B2 (ja) | 2017-03-16 | 2025-03-18 | アルデイラ セラピューティクス， インコーポレイテッド | 多形化合物およびその使用 |
| CN111356451A (zh) | 2017-10-10 | 2020-06-30 | 奥尔德拉医疗公司 | 炎性病症的治疗 |
| CN112714762A (zh) | 2018-08-06 | 2021-04-27 | 奥尔德拉医疗公司 | 多晶型化合物及其用途 |
| CA3113462A1 (en) | 2018-09-25 | 2020-04-02 | Aldeyra Therapeutics, Inc. | Formulations of reproxalap for the treatment of dry eye disease |
| US11786518B2 (en) | 2019-03-26 | 2023-10-17 | Aldeyra Therapeutics, Inc. | Ophthalmic formulations and uses thereof |
| WO2020223685A1 (en) | 2019-05-02 | 2020-11-05 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| WO2020223717A1 (en) | 2019-05-02 | 2020-11-05 | Aldeyra Therapeutics, Inc. | Process for preparation of aldehyde scavenger and intermediates |
| WO2021231792A1 (en) | 2020-05-13 | 2021-11-18 | Aldeyra Therapeutics, Inc. | Pharmaceutical formulations and uses thereof |
| AU2021308209A1 (en) | 2020-07-16 | 2023-02-09 | Dermavant Sciences GmbH | Isoquinoline compounds and their use in treating ahr imbalance |
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| US2086186A (en) | 1933-10-10 | 1937-07-06 | Us Rubber Co | Treatment of rubber |
| SU509046A1 (ru) | 1975-02-21 | 1984-06-23 | Всесоюзный научно-исследовательский химико-фармацевтический институт им.Серго Орджоникидзе | Производные 2-карбэтокси-3-аминоиндола,про вл ющие противовоспалительную активность, и способ их получени |
| US4675332A (en) | 1984-12-10 | 1987-06-23 | Warner-Lambert Company | Acidic tetrazolyl substituted indole compounds and their use as antiallergy agents |
| GB8610981D0 (en) | 1986-05-06 | 1986-06-11 | Ici America Inc | Quinoline amides |
| CA2054339C (en) | 1990-11-02 | 2002-12-24 | Francesco G. Salituro | 3-amidoindolyl derivatives |
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| US6444221B1 (en) | 1992-06-30 | 2002-09-03 | Howard K. Shapiro | Methods of treating chronic inflammatory diseases using carbonyl trapping agents |
| US20050090553A1 (en) | 1992-06-30 | 2005-04-28 | Shapiro Howard K. | Compositions and method for treatment of chronic inflammatory diseases |
| US5472954A (en) | 1992-07-14 | 1995-12-05 | Cyclops H.F. | Cyclodextrin complexation |
| US5493027A (en) | 1993-01-22 | 1996-02-20 | Board Of Regents, The University Of Texas System | Anticonvulsive agents and uses thereof |
| US5597823A (en) | 1995-01-27 | 1997-01-28 | Abbott Laboratories | Tricyclic substituted hexahydrobenz [e]isoindole alpha-1 adrenergic antagonists |
| CA2261916A1 (en) | 1996-08-01 | 1998-02-12 | Dowelanco Llc | 4-substituted quinoline derivatives having fungicidal activity |
| AU8330898A (en) | 1997-05-02 | 1998-11-27 | Schering Aktiengesellschaft | Substituted heterocycles and their use in medicaments |
| KR20010041811A (ko) | 1998-03-12 | 2001-05-25 | 온토젠 코포레이션 | 단백질 티로신 포스파타제의 조절제 |
| US6498154B1 (en) | 1999-05-04 | 2002-12-24 | Wyeth | Cyclic regimens using quinazolinone and benzoxazine derivatives |
| WO2001041757A1 (en) | 1999-12-10 | 2001-06-14 | Senju Pharmaceutical Co., Ltd. | Cyclodextrin-containing pharmaceutical composition |
| FR2827599A1 (fr) | 2001-07-20 | 2003-01-24 | Neuro3D | Composes derives de quinoleine et quinoxaline,preparation et utilisations |
| US20060014786A1 (en) | 2002-05-17 | 2006-01-19 | Rajeev Raut | Opthalmic pharmaceutical compositions and methods for treating ocular inflammation |
| CA2451267A1 (en) | 2002-12-13 | 2004-06-13 | Warner-Lambert Company Llc | Pharmaceutical uses for alpha2delta ligands |
| US20040242704A1 (en) | 2003-03-14 | 2004-12-02 | University Of Washington, Techtransfer - Invention Licensing | Stabilized mutant opsin proteins |
| US20060111318A1 (en) | 2003-04-18 | 2006-05-25 | Advanced Medicine Research Institute | Agent for treating eye diseases |
| CA2527175A1 (en) | 2003-04-18 | 2004-10-28 | Advanced Medicine Research Institute | Remedies for diseases to be applied to eye |
| US7297709B2 (en) | 2003-05-22 | 2007-11-20 | Abbott Laboratories | Indazole, benzisoxazole, and benzisothiazole kinase inhibitors |
| EP1679308B1 (en) | 2003-10-15 | 2013-07-24 | Ube Industries, Ltd. | Novel indazole derivative |
| JP4975440B2 (ja) | 2003-11-20 | 2012-07-11 | オセラ・ホールディング・インコーポレイテッド | 黄斑変性およびその他の眼科疾患の改善 |
| US20050197292A1 (en) | 2004-01-30 | 2005-09-08 | Glennda Smithson | Compositions and methods for treating T-cell mediated pathological conditions |
| KR20060135819A (ko) | 2004-02-17 | 2006-12-29 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 황반변성을 포함하는 안과질환의 관리 |
| US20050234018A1 (en) | 2004-04-15 | 2005-10-20 | Allergan, Inc. | Drug delivery to the back of the eye |
| WO2006002473A1 (en) | 2004-07-02 | 2006-01-12 | Adelaide Research & Innovation Pty Ltd | Method of controlling damage mediated by alpha, beta-unsaturated aldehydes |
| US20070287716A1 (en) * | 2004-10-28 | 2007-12-13 | Hu Essa H | Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors |
| TW200640443A (en) | 2005-02-23 | 2006-12-01 | Alcon Inc | Methods for treating ocular angiogenesis, retinal edema, retinal ischemia, and diabetic retinopathy using selective RTK inhibitors |
| US7973025B2 (en) | 2005-05-26 | 2011-07-05 | Neuron Systems, Inc. | Compositions and methods of treating retinal disease |
| US20100144693A1 (en) * | 2006-04-14 | 2010-06-10 | Prana Biotechnology Limited | Method of treatment of age-related macular degeneration (amd) |
| EP2079699A1 (en) * | 2006-07-25 | 2009-07-22 | Envivo Pharmaceuticals, Inc. | Quinoline derivatives |
| CA2701116C (en) | 2007-10-05 | 2013-02-05 | Acucela Inc. | Alkoxy compounds for disease treatment |
| RU2011109190A (ru) | 2008-08-12 | 2012-09-20 | Сертрис Фармасьютикалз, Инк. (Us) | Бензоксазолы, бензтиазолы и родственные аналоги в качестве модуляторов сиртуина |
| WO2010133672A1 (en) | 2009-05-20 | 2010-11-25 | Clanotech Ab | Derivatives of quinoline-3-carboxylic acid and their medical use |
| EP2477594A4 (en) | 2009-07-15 | 2013-03-13 | Univ Vanderbilt | ISOKETAL CATCHER AND TREATMENT OF DISEASES WITH OXIDATIVE INJURY |
| EP2509596B1 (en) | 2009-12-08 | 2019-08-28 | Case Western Reserve University | Gamma aminoacids for treating ocular disorders |
| CA2782015C (en) | 2009-12-11 | 2020-08-25 | Neuron Systems, Inc. | Topical ophthalmic compositions and methods for the treatment of macular degeneration |
| ES2620606T3 (es) | 2011-01-12 | 2017-06-29 | Ventirx Pharmaceuticals, Inc. | Benzoazepinas sustituidas como moduladores de receptores tipo Toll |
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| RU2015126015A (ru) | 2013-01-25 | 2017-03-03 | Альдейра Терапьютикс, Инк. | Новые улавливатели в лечении макулодистрофии |
| EP3151818A4 (en) | 2014-06-04 | 2018-05-30 | Case Western Reserve University | Compositions and methods of treating diabetic retinopathy |
| US10363231B2 (en) | 2014-11-24 | 2019-07-30 | Case Western Reserve University | Compounds and methods of treating ocular disorders |
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- 2013-12-19 JP JP2015549717A patent/JP2016503797A/ja not_active Withdrawn
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Also Published As
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| EP2935220A4 (en) | 2016-04-27 |
| WO2014100425A1 (en) | 2014-06-26 |
| EP2935220A1 (en) | 2015-10-28 |
| US20150344432A1 (en) | 2015-12-03 |
| MX2015007916A (es) | 2016-04-07 |
| SG11201504859YA (en) | 2015-07-30 |
| KR20150118106A (ko) | 2015-10-21 |
| AU2013361314A1 (en) | 2015-07-02 |
| IL239178A0 (en) | 2015-07-30 |
| CN105073714A (zh) | 2015-11-18 |
| HK1217325A1 (zh) | 2017-01-06 |
| CL2015001754A1 (es) | 2015-11-06 |
| CA2896032A1 (en) | 2014-06-26 |
| US9604997B2 (en) | 2017-03-28 |
| RU2015120478A (ru) | 2017-01-25 |
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