AU2018348174A1 - Treatment of inflammatory disorders - Google Patents
Treatment of inflammatory disorders Download PDFInfo
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- AU2018348174A1 AU2018348174A1 AU2018348174A AU2018348174A AU2018348174A1 AU 2018348174 A1 AU2018348174 A1 AU 2018348174A1 AU 2018348174 A AU2018348174 A AU 2018348174A AU 2018348174 A AU2018348174 A AU 2018348174A AU 2018348174 A1 AU2018348174 A1 AU 2018348174A1
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| US62/644,263 | 2018-03-16 | ||
| PCT/US2018/055310 WO2019075136A1 (en) | 2017-10-10 | 2018-10-10 | TREATMENT OF INFLAMMATORY DISORDERS |
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Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006249866B2 (en) | 2005-05-26 | 2011-10-13 | Aldeyra Therapeutics, Inc. | Compositions and methods of treating retinal disease |
| WO2011072141A1 (en) | 2009-12-11 | 2011-06-16 | Neuron Systems, Inc. | Compositions and methods for the treatment of macular degeneration |
| CN117045653A (zh) | 2013-01-23 | 2023-11-14 | 奥尔德拉医疗公司 | 与毒性醛相关的疾病和治疗 |
| US10550085B2 (en) | 2015-08-21 | 2020-02-04 | Aldeyra Therapeutics, Inc. | Deuterated compounds and uses thereof |
| CA3022665A1 (en) | 2016-05-09 | 2017-11-16 | Aldeyra Therapeutics, Inc. | Combination treatment of ocular inflammatory disorders and diseases |
| WO2019075136A1 (en) | 2017-10-10 | 2019-04-18 | Aldeyra Therapeutics, Inc. | TREATMENT OF INFLAMMATORY DISORDERS |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| AU2019319740A1 (en) | 2018-08-06 | 2021-03-25 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| EP3856478A4 (en) | 2018-09-25 | 2022-06-08 | Aldeyra Therapeutics, Inc. | FORMULATIONS FOR THE TREATMENT OF DRY EYE |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| MX2021007140A (es) * | 2018-12-18 | 2021-11-03 | Medshine Discovery Inc | Compuesto para usarse en enfermedades de la retina. |
| US11786518B2 (en) | 2019-03-26 | 2023-10-17 | Aldeyra Therapeutics, Inc. | Ophthalmic formulations and uses thereof |
| WO2020223717A1 (en) | 2019-05-02 | 2020-11-05 | Aldeyra Therapeutics, Inc. | Process for preparation of aldehyde scavenger and intermediates |
| JP2022530967A (ja) | 2019-05-02 | 2022-07-05 | 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 |
| PH12022500002A1 (en) | 2019-06-28 | 2023-04-03 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| WO2021011868A1 (en) | 2019-07-17 | 2021-01-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2021119159A1 (en) | 2019-12-10 | 2021-06-17 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| KR20220145325A (ko) | 2019-12-17 | 2022-10-28 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
| US20230149383A1 (en) * | 2020-04-13 | 2023-05-18 | Aldeyra Therapeutics, Inc. | Quinoline compounds for treating lung, liver, and kidney diseases, disorders, or conditions |
| WO2021222366A1 (en) * | 2020-04-28 | 2021-11-04 | Kymera Therapeutics, Inc. | Irak inhibitors and uses thereof |
| WO2021231792A1 (en) | 2020-05-13 | 2021-11-18 | Aldeyra Therapeutics, Inc. | Pharmaceutical formulations and uses thereof |
| CN115702144A (zh) * | 2020-06-17 | 2023-02-14 | 南京明德新药研发有限公司 | 氨基吡啶类化合物 |
| US11753377B2 (en) * | 2020-06-17 | 2023-09-12 | Zhuhai United Laboratories Co., Ltd. | Crystal form of 2-methyl-2-propanol and amino-substituted aryl compound |
| MX2023003583A (es) * | 2020-09-28 | 2023-04-04 | Zhuhai United Laboratories Co Ltd | Forma cristalina del compuesto de piridinilfenilo y metodo de preparacion del mismo. |
| EP4273150A4 (en) * | 2020-12-29 | 2024-04-24 | The National Institutes of Pharmaceutical R&D Co., Ltd | TRICYCLIC COMPOUND AND PRODUCTION PROCESS THEREOF AND MEDICAL USE THEREOF |
| CN116867758A (zh) | 2020-12-30 | 2023-10-10 | 凯麦拉医疗公司 | Irak降解剂和其用途 |
| WO2022232110A1 (en) * | 2021-04-26 | 2022-11-03 | Jem Therapeutics Pbc | Method of treatment for autophagy diseases by administration of dexibuprofen and use of dexibuprofen for preparation of a medicament for same |
| AU2022303386A1 (en) * | 2021-07-02 | 2023-12-14 | Aldeyra Therapeutics, Inc. | Heterocyclic aldehyde trapping compounds and uses thereof |
| CA3243560A1 (en) | 2022-01-31 | 2023-08-03 | Kymera Therapeutics, Inc. | Iraqi Degradation Agents and Their Uses |
| KR20250111213A (ko) * | 2022-11-26 | 2025-07-22 | 주하이 유나이티드 라보라토리즈 컴퍼니 리미티드 | 피리딘 페닐 화합물을 포함하는 안과용 제형, 이의 제조 방법, 및 이의 용도 |
| CN120424003A (zh) * | 2024-02-02 | 2025-08-05 | 深圳新锐基因科技有限公司 | 一种基于ai设计的活性醛类物质抑制剂及其应用 |
Family Cites Families (141)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2086186A (en) | 1933-10-10 | 1937-07-06 | Us Rubber Co | Treatment of rubber |
| SU50906A1 (ru) | 1935-12-20 | 1936-11-30 | А.И. Бурляев | Веретено дл пр дильных машин |
| GB1435721A (en) | 1972-05-18 | 1976-05-12 | Lilly Industries Ltd | Benzoxazole derivatives |
| JPS6192592A (ja) | 1984-10-12 | 1986-05-10 | Norin Suisansyo Shokuhin Sogo Kenkyusho | 分岐サイクロデキストリンの製造方法 |
| 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 |
| NZ225045A (en) | 1987-07-01 | 1990-06-26 | Janssen Pharmaceutica Nv | Antiviral pharmaceutical compositions containing cyclodextrin and an antiviral agent |
| US5002935A (en) | 1987-12-30 | 1991-03-26 | University Of Florida | Improvements in redox systems for brain-targeted drug delivery |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| BR9106193A (pt) | 1990-10-22 | 1993-03-23 | Bausch & Lomb | Metodo e composicao para limpar lentes de contato |
| AU641052B2 (en) | 1990-11-02 | 1993-09-09 | Aventisub Ii Inc. | 3-amidoindolyl derivatives |
| US5668117A (en) | 1991-02-22 | 1997-09-16 | Shapiro; Howard K. | Methods of treating neurological diseases and etiologically related symptomology using carbonyl trapping agents in combination with previously known medicaments |
| 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 |
| TW401300B (en) | 1992-12-25 | 2000-08-11 | Senju Pharma Co | Antiallergic composition for ophthalmic or nasal use |
| US5493027A (en) | 1993-01-22 | 1996-02-20 | Board Of Regents, The University Of Texas System | Anticonvulsive agents and uses thereof |
| US5767109A (en) | 1993-10-20 | 1998-06-16 | Sanchez; Robert A. | Complexing urushiols |
| US5576311A (en) | 1994-11-30 | 1996-11-19 | Pharmos Corporation | Cyclodextrins as suspending agents for pharmaceutical suspensions |
| JP3297969B2 (ja) | 1994-12-26 | 2002-07-02 | ライオン株式会社 | 点眼剤 |
| US5597823A (en) | 1995-01-27 | 1997-01-28 | Abbott Laboratories | Tricyclic substituted hexahydrobenz [e]isoindole alpha-1 adrenergic antagonists |
| JP3736916B2 (ja) | 1996-02-19 | 2006-01-18 | 株式会社サンコンタクトレンズ | 含水性ソフトコンタクトレンズの消毒用組成物とその用途 |
| US6107300A (en) | 1996-03-27 | 2000-08-22 | Dupont Pharmaceuticals | Arylamino fused pyrimidines |
| KR20000029694A (ko) | 1996-08-01 | 2000-05-25 | 케네쓰 엘. 로에르트셔 | 살진균활성을갖는4-치환된퀴놀린유도체 |
| BR9710808A (pt) * | 1996-08-06 | 1999-08-17 | Pfizer | Derivados biciclicos 6,6 ou 6,7 contendo pirito ou pirimido substitu¡dos |
| US6191127B1 (en) | 1997-05-02 | 2001-02-20 | Schering Aktiengesellschaft | Substituted heterocycles and their use in medicaments |
| GB2327672A (en) | 1997-07-23 | 1999-02-03 | Merck & Co Inc | 4-(1,2,3,4-Tetrahydro-1,8-naphthyridin-7-yl)butanoyl-glycyl-3(S)-quinolin-3-yl-beta-alanine |
| US6245769B1 (en) * | 1997-09-02 | 2001-06-12 | Dupont Pharmaceuticals Company | Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders |
| WO1999046237A1 (en) | 1998-03-12 | 1999-09-16 | Novo Nordisk A/S | Modulators of protein tyrosine phosphatases |
| US6498154B1 (en) | 1999-05-04 | 2002-12-24 | Wyeth | Cyclic regimens using quinazolinone and benzoxazine derivatives |
| US6358948B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| US6515010B1 (en) | 1999-11-15 | 2003-02-04 | Smithkline Beecham Corporation | Carvedilol methanesulfonate |
| AU1735001A (en) | 1999-12-10 | 2001-06-18 | Senju Pharmaceutical Co., Ltd. | Cyclodextrin-containing pharmaceutical composition |
| US6569879B2 (en) | 2000-02-18 | 2003-05-27 | Merck & Co., Inc. | Aryloxyacetic acids for diabetes and lipid disorders |
| JP4748289B2 (ja) | 2000-06-23 | 2011-08-17 | ライオン株式会社 | 点眼剤、眼科用組成物及び吸着抑制方法 |
| FR2827599A1 (fr) | 2001-07-20 | 2003-01-24 | Neuro3D | Composes derives de quinoleine et quinoxaline,preparation et utilisations |
| UA83620C2 (ru) | 2001-12-05 | 2008-08-11 | Уайт | Замещенные бензоксазолы и их аналоги как эстрогенные агенты |
| 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 |
| US20040198828A1 (en) | 2003-01-17 | 2004-10-07 | Abelson Mark B. | Combinational use of long-acting and short-acting anti-histamines for ocular allergies |
| EP3326623A1 (en) | 2003-03-14 | 2018-05-30 | University of Washington | Retinoid replacements and opsin agonists and methods for the use thereof |
| EP1621199B8 (en) | 2003-04-18 | 2011-01-19 | Advanced Medicine Research Institute | Remedies for diseases to be applied to eye |
| US20060111318A1 (en) | 2003-04-18 | 2006-05-25 | Advanced Medicine Research Institute | Agent for treating eye diseases |
| US20040235892A1 (en) | 2003-05-22 | 2004-11-25 | Yujia Dai | Indazole and benzisoxazole kinase inhibitors |
| US7297709B2 (en) | 2003-05-22 | 2007-11-20 | Abbott Laboratories | Indazole, benzisoxazole, and benzisothiazole kinase inhibitors |
| US7083803B2 (en) | 2003-09-19 | 2006-08-01 | Advanced Ocular Systems Limited | Ocular solutions |
| JP2005132834A (ja) | 2003-10-09 | 2005-05-26 | Kyowa Hakko Kogyo Co Ltd | キノリン誘導体 |
| EP1679308B1 (en) | 2003-10-15 | 2013-07-24 | Ube Industries, Ltd. | Novel indazole derivative |
| CA2543644A1 (en) | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| CA2546042A1 (en) | 2003-11-20 | 2005-06-09 | Othera Pharmaceuticals, Inc. | Amelioration of macular degeneration and other ophthalmic diseases |
| US20050197292A1 (en) | 2004-01-30 | 2005-09-08 | Glennda Smithson | Compositions and methods for treating T-cell mediated pathological conditions |
| US20080176952A1 (en) | 2004-02-17 | 2008-07-24 | Rando Robert R | Management of Ophthalmologic Disorders, Including Macular Degeneration |
| US20050234018A1 (en) | 2004-04-15 | 2005-10-20 | Allergan, Inc. | Drug delivery to the back of the eye |
| JP2006008568A (ja) | 2004-06-24 | 2006-01-12 | Cyclochem:Kk | IgE抗体抑制剤および食品 |
| WO2006002473A1 (en) | 2004-07-02 | 2006-01-12 | Adelaide Research & Innovation Pty Ltd | Method of controlling damage mediated by alpha, beta-unsaturated aldehydes |
| FR2875409B1 (fr) | 2004-09-17 | 2010-05-07 | Sanofi Aventis | Composition pharmaceutique comprenant une dispersion solide a matrice polymere comprenant une phase continue de polydextrose et une phase continue d'un polymere autre que du polydextrose |
| US20070287716A1 (en) | 2004-10-28 | 2007-12-13 | Hu Essa H | Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors |
| EP1844768A1 (en) | 2005-01-19 | 2007-10-17 | Dainippon Sumitomo Pharma Co., Ltd. | Aromatic sulfone compound as aldosterone receptor modulator |
| 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 |
| EP1893174A2 (en) | 2005-05-10 | 2008-03-05 | Cytophil, Inc. | Injectable hydrogels and methods of making and using same |
| AU2006249866B2 (en) | 2005-05-26 | 2011-10-13 | Aldeyra Therapeutics, Inc. | Compositions and methods of treating retinal disease |
| EP1967186B1 (en) | 2005-12-27 | 2015-03-11 | Lion Corporation | Composition for soft contact lens and adsorption suppressing method |
| US7842312B2 (en) | 2005-12-29 | 2010-11-30 | Cordis Corporation | Polymeric compositions comprising therapeutic agents in crystalline phases, and methods of forming the same |
| US20070297981A1 (en) | 2006-01-25 | 2007-12-27 | Ousler George W Iii | Formulations and methods for treating dry eye |
| US20070203216A1 (en) * | 2006-02-14 | 2007-08-30 | Bjarke Ebert | Method of treating inflammatory diseases |
| JP4466875B2 (ja) | 2006-04-05 | 2010-05-26 | ライオン株式会社 | ソフトコンタクトレンズ用点眼剤 |
| CN101534826A (zh) | 2006-04-14 | 2009-09-16 | 普拉纳生物技术有限公司 | 治疗与年龄相关的黄斑变性(amd)的方法 |
| JP5194218B2 (ja) | 2006-06-05 | 2013-05-08 | 株式会社メニコンネクト | 含水性コンタクトレンズの保存方法ならびに該保存方法により保存された含水性コンタクトレンズ |
| JP2009544631A (ja) | 2006-07-25 | 2009-12-17 | エンビボ ファーマシューティカルズ インコーポレイテッド | キノリン誘導体 |
| CA2660703A1 (en) | 2006-08-14 | 2008-02-21 | Schering Corporation | Salts of 5-(1(s)-amino-2-hydroxyethyl)-n-[(2,4-difluorophenyl)-methyl]-2-[8-methoxy-2-(trifluoromethyl)-5-quinoline]-4-oxazolecarboxamide |
| US20080069878A1 (en) | 2006-08-31 | 2008-03-20 | Gopi Venkatesh | Drug Delivery Systems Comprising Solid Solutions of Weakly Basic Drugs |
| US8158609B1 (en) | 2006-11-02 | 2012-04-17 | Novartis Ag | Use of cyclodextrins as an active ingredient for treating dry AMD and solubilizing drusen |
| US20080241256A1 (en) | 2007-03-30 | 2008-10-02 | Liisa Kuhn | Targeted active agent delivery system based on calcium phosphate nanoparticles |
| US20090118503A1 (en) | 2007-06-20 | 2009-05-07 | Kevin Sprott | Faah inhibitors |
| CN103553945B (zh) | 2007-10-05 | 2015-01-07 | 奥克塞拉有限公司 | 用于治疗疾病的烷氧基化合物 |
| WO2009102418A1 (en) | 2008-02-11 | 2009-08-20 | University Of Washington | Methods for the treatment and prevention of age-related retinal dysfunction |
| AU2009282076A1 (en) | 2008-08-12 | 2010-02-18 | Sirtris Pharmaceuticals, Inc. | Benzoxazoles, benzthiazoles and related analogs as sirtuin modulators |
| JP5773877B2 (ja) | 2008-10-22 | 2015-09-02 | アキュセラ インコーポレイテッド | 眼の疾患及び障害を治療する化合物 |
| JP2012508215A (ja) | 2008-11-11 | 2012-04-05 | ノバルティス アーゲー | 有機化合物 |
| CA2754996A1 (en) | 2009-03-17 | 2010-09-23 | Aciex Therapeutics, Inc. | Ophthalmic formulations of ketotifen and methods of use |
| WO2010133672A1 (en) | 2009-05-20 | 2010-11-25 | Clanotech Ab | Derivatives of quinoline-3-carboxylic acid and their medical use |
| MX2011013061A (es) | 2009-06-05 | 2012-02-28 | Aciex Therapeutics Inc | Formulaciones oftalmicas de fluticasona y metodos de uso. |
| WO2010148351A1 (en) | 2009-06-18 | 2010-12-23 | Cylene Pharmaceuticals, Inc. | Rhodanines and related heterocycles as kinase inhibitors |
| WO2011008202A1 (en) | 2009-07-15 | 2011-01-20 | Vanderbilt University | Isoketal scavengers and mitigation of disorders involving oxidative injury |
| TWI492769B (zh) | 2009-09-23 | 2015-07-21 | Alcon Res Ltd | 可注射的水性眼用組成物及其使用之方法 |
| ES2758554T3 (es) | 2009-12-08 | 2020-05-05 | Univ Case Western Reserve | Aminoácidos gama para tratamiento de trastornos oculares |
| WO2011072141A1 (en) | 2009-12-11 | 2011-06-16 | Neuron Systems, Inc. | Compositions and methods for the treatment of macular degeneration |
| JPWO2011078204A1 (ja) | 2009-12-24 | 2013-05-09 | 浜理薬品工業株式会社 | 高脂血症の予防または治療剤、および抗疲労剤 |
| WO2011106729A2 (en) | 2010-02-26 | 2011-09-01 | Xenon Pharmaceuticals Inc. | Pharmaceutical compositions of spiro-oxindole compound for topical administration and their use as therapeutic agents |
| WO2011116066A1 (en) | 2010-03-17 | 2011-09-22 | Concert Pharmaceuticals, Inc. | Derivatives of dimethylcurcumin |
| KR20130138770A (ko) | 2010-09-01 | 2013-12-19 | 아레나 파마슈티칼스, 인크. | 광학적으로 활성 산을 갖는 로르카세린의 염 |
| EP3208263A1 (en) | 2011-01-12 | 2017-08-23 | VentiRx Pharmaceuticals, Inc. | Substituted benzoazepines as toll-like receptor modulators |
| US10463687B2 (en) | 2011-01-20 | 2019-11-05 | Cornell University | Treatments for retinal disorders |
| US9302013B2 (en) | 2011-01-31 | 2016-04-05 | Termira Ab | Active principle for mitigating undesired medical conditions |
| TWI544922B (zh) | 2011-05-19 | 2016-08-11 | 愛爾康研究有限公司 | 高濃度歐羅派特錠(olopatadine)眼用組成物 |
| HK1202064A1 (en) | 2011-10-13 | 2015-09-18 | 托马斯.盖德克 | Topical formulations of chemerin c15 peptides for the treatment of dermatological conditions |
| US20130190500A1 (en) | 2011-12-12 | 2013-07-25 | Neuron Systems, Inc. | Process to prepare 6-chloro-3-amino-2-(2-hydroxypropyl)-1-azanaphthalene |
| US20130165419A1 (en) | 2011-12-21 | 2013-06-27 | Insite Vision Incorporated | Combination anti-inflammatory ophthalmic compositions |
| MX367879B (es) | 2012-08-01 | 2019-09-10 | Lewis And Clark Pharmaceuticals Inc | N-alquil 2-(disustituido)alquiladenosin-5-uronamidas como agonistas a2a. |
| MX373894B (es) | 2012-11-08 | 2020-07-09 | Clearside Biomedical Inc | Métodos y dispositivos para el tratamiento de trastornos oculares en sujetos humanos. |
| AU2013361314A1 (en) | 2012-12-20 | 2015-07-02 | Aldeyra Therapeutics, Inc. | Peri-carbinols |
| NZ709620A (en) | 2013-01-23 | 2020-07-31 | Semnur Pharmaceuticals Inc | Pharmaceutical formulation comprising an insoluble corticosteroid and a soluble corticosteroid |
| CN117045653A (zh) | 2013-01-23 | 2023-11-14 | 奥尔德拉医疗公司 | 与毒性醛相关的疾病和治疗 |
| US10111862B2 (en) | 2013-01-25 | 2018-10-30 | Aldeyra Therapeutics, Inc. | Traps in the treatment of macular degeneration |
| TWI643853B (zh) | 2013-02-27 | 2018-12-11 | 阿爾米雷爾有限公司 | 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類 |
| US9713330B1 (en) | 2013-03-15 | 2017-07-25 | Deuteria Agrochemicals, Llc | Deuterium-enriched aldehydes |
| US20160151410A1 (en) | 2013-07-02 | 2016-06-02 | The Trustees Of Columbia University In The City Of New York | Clearance of bioactive lipids from membrane structures by cyclodextrins |
| US10272106B2 (en) | 2014-06-04 | 2019-04-30 | Case Western Reserve University | Compositions and methods of treating diabetic retinopathy |
| WO2015198350A1 (en) | 2014-06-25 | 2015-12-30 | Synergia Bio Sciences Private Limited | A pharmaceutical oil-in-water nano-emulsion |
| RU2016141135A (ru) | 2014-07-29 | 2018-08-28 | Терапьютиксмд, Инк. | Трансдермальный крем |
| NO2721710T3 (https=) * | 2014-08-21 | 2018-03-31 | ||
| AU2015312134A1 (en) | 2014-09-02 | 2017-03-23 | Bhupinder Singh | Deuterated or a non-deuterated molecule and pharmaceutical formulations |
| TW201628622A (zh) | 2014-11-17 | 2016-08-16 | 製藥公司 | Tlr抑制劑與布魯頓氏(bruton's)酪胺酸激酶抑制劑之組合 |
| US10363231B2 (en) | 2014-11-24 | 2019-07-30 | Case Western Reserve University | Compounds and methods of treating ocular disorders |
| CN113307805A (zh) | 2015-04-15 | 2021-08-27 | 百济神州有限公司 | B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 |
| KR20180073553A (ko) | 2015-08-21 | 2018-07-02 | 알데이라 테라퓨틱스, 아이엔씨. | 알데히드 접합체 및 이의 용도 |
| US10550085B2 (en) | 2015-08-21 | 2020-02-04 | Aldeyra Therapeutics, Inc. | Deuterated compounds and uses thereof |
| KR20180116416A (ko) | 2016-02-28 | 2018-10-24 | 알데이라 테라퓨틱스, 아이엔씨. | 사이클로덱스트린으로의 알레르기성 안질환의 치료 |
| CA3022665A1 (en) | 2016-05-09 | 2017-11-16 | Aldeyra Therapeutics, Inc. | Combination treatment of ocular inflammatory disorders and diseases |
| EP3463277A4 (en) | 2016-06-06 | 2020-01-01 | GDD Therapeutics, LLC | FORMULATIONS FOR SUBSTITUTED 3-PYRROLIDINES, COMPOSITIONS THEREFOR AND USES THEREOF |
| WO2018039192A1 (en) * | 2016-08-22 | 2018-03-01 | Aldeyra Therapeutics, Inc. | Aldehyde trapping compounds and uses thereof |
| CA3032609A1 (en) | 2016-08-22 | 2018-03-01 | Aldeyra Therapeutics, Inc. | Aldehyde trapping compounds and methods of use thereof |
| US11510931B2 (en) | 2016-09-28 | 2022-11-29 | Medicon Pharmaceuticals, Inc. | Compositions and methods for treating ophthalmic conditions |
| ES2887008T3 (es) | 2016-10-05 | 2021-12-21 | Mitobridge Inc | Formas cristalinas y de sal de compuestos agonistas del PPAR |
| CA3054811A1 (en) | 2017-03-16 | 2018-09-20 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| WO2019075136A1 (en) | 2017-10-10 | 2019-04-18 | Aldeyra Therapeutics, Inc. | TREATMENT OF INFLAMMATORY DISORDERS |
| WO2020018498A1 (en) | 2018-07-16 | 2020-01-23 | Aldeyra Therapeutics, Inc. | Cyclodextrin formulations |
| WO2020028820A1 (en) * | 2018-08-03 | 2020-02-06 | Aldeyra Therapeutics, Inc. | Topical compositions and methods of preparation and use |
| AU2019319740A1 (en) | 2018-08-06 | 2021-03-25 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
| EP3856478A4 (en) | 2018-09-25 | 2022-06-08 | Aldeyra Therapeutics, Inc. | FORMULATIONS FOR THE TREATMENT OF DRY EYE |
| WO2020072621A1 (en) | 2018-10-02 | 2020-04-09 | Aldeyra Therapeutics, Inc. | Contact lens solutions and kits |
| WO2020118045A1 (en) | 2018-12-05 | 2020-06-11 | Aldeyra Therapeutics, Inc. | Injectable formulations |
| US11786518B2 (en) | 2019-03-26 | 2023-10-17 | Aldeyra Therapeutics, Inc. | Ophthalmic formulations and uses thereof |
| WO2020223717A1 (en) | 2019-05-02 | 2020-11-05 | Aldeyra Therapeutics, Inc. | Process for preparation of aldehyde scavenger and intermediates |
| JP2022530967A (ja) | 2019-05-02 | 2022-07-05 | 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 |
| US20230131929A1 (en) | 2020-03-24 | 2023-04-27 | Aldeyra Therapeutics, Inc. | Quinoline compounds for treating respiratory disorders and viral infections |
| US20230149383A1 (en) | 2020-04-13 | 2023-05-18 | Aldeyra Therapeutics, Inc. | Quinoline compounds for treating lung, liver, and kidney diseases, disorders, or conditions |
| WO2021231792A1 (en) | 2020-05-13 | 2021-11-18 | Aldeyra Therapeutics, Inc. | Pharmaceutical formulations and uses thereof |
| WO2021248031A1 (en) | 2020-06-04 | 2021-12-09 | Aldeyra Therapeutics, Inc. | Dry eye disease biomarkers and their use for treatment |
| WO2022150580A1 (en) | 2021-01-07 | 2022-07-14 | Aldeyra Therapeutics, Inc. | Treatment of dry eye disease |
| US20220211691A1 (en) | 2021-01-07 | 2022-07-07 | Aldeyra Therapeutics, Inc. | Treatment of dry eye disease |
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2018
- 2018-10-10 WO PCT/US2018/055310 patent/WO2019075136A1/en not_active Ceased
- 2018-10-10 EP EP18865612.8A patent/EP3694500A4/en not_active Withdrawn
- 2018-10-10 CN CN201880073697.1A patent/CN111356451A/zh active Pending
- 2018-10-10 MX MX2020003425A patent/MX2020003425A/es unknown
- 2018-10-10 US US16/157,069 patent/US11040039B2/en active Active
- 2018-10-10 AU AU2018348174A patent/AU2018348174A1/en not_active Abandoned
- 2018-10-10 JP JP2020520127A patent/JP7311162B2/ja active Active
- 2018-10-10 CA CA3077362A patent/CA3077362A1/en active Pending
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2020
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2023
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| WO2019075136A1 (en) | 2019-04-18 |
| US11583529B2 (en) | 2023-02-21 |
| CN111356451A (zh) | 2020-06-30 |
| US20190105322A1 (en) | 2019-04-11 |
| JP7311162B2 (ja) | 2023-07-19 |
| EP3694500A1 (en) | 2020-08-19 |
| US20230293527A1 (en) | 2023-09-21 |
| US20210353628A1 (en) | 2021-11-18 |
| JP2020536896A (ja) | 2020-12-17 |
| CA3077362A1 (en) | 2019-04-18 |
| US11040039B2 (en) | 2021-06-22 |
| IL273693A (en) | 2020-05-31 |
| JP2023115307A (ja) | 2023-08-18 |
| MX2020003425A (es) | 2020-07-29 |
| US20230248727A1 (en) | 2023-08-10 |
| EP3694500A4 (en) | 2021-06-30 |
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