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1. 发明申请

WO2011057209A1 ACIDIC OPHTHALMIC FORMULATIONS 审中-公开
标题翻译：酸性眼科配方
公开(公告)号：WO2011057209A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/055862
申请日：2010-11-08
申请人： QLT, INC. , PATIL, Ghanshyam , LI, Weixing , SENKO, Marina
发明人： PATIL, Ghanshyam , LI, Weixing , SENKO, Marina
IPC分类号： A01N43/08 , A61K31/34
CPC分类号： A61K31/34 , A61K9/0048 , A61K47/36 , A61K47/38
摘要： The invention is directed to ophthalmic formulations formulated to be below physiological pH.
摘要翻译：本发明涉及配制成低于生理pH的眼用制剂。

2. 发明申请

WO2008103613A2 HYDROXYLAMINE COMPOUNDS AND METHODS OF THEIR USE 审中-公开
标题翻译：羟基喹啉化合物及其使用方法
公开(公告)号：WO2008103613A2
公开(公告)日：2008-08-28
申请号：PCT/US2008/054122
申请日：2008-02-15
申请人： OTHERA HOLDING, INC. , PATIL, Ghanshyam
发明人： PATIL, Ghanshyam
IPC分类号： C07D207/46 , C07D209/44 , C07D211/94 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/12 , C07D417/14 , A61K31/4535 , A61P17/18
CPC分类号： C07D211/94 , C07D207/46 , C07D209/44 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/12 , C07D417/14
摘要： The present disclosure provides compounds that include hydroxylamines of formula (I) or (II), pharmaceutical compositions, and methods for their use. The methods utilize hydroxylamine compounds and/or their pharmaceutical compositions for the treatment of angiogenesis, hepatitis, complement-mediated pathologies, drusen-mediated pathologies, macular degeneration and certain other ophthalmic conditions, inflammation, arthritis, and related diseases and for the inhibition of complement activation.
摘要翻译：本公开提供了包括式（I）或（II）的羟胺，药物组合物及其使用方法的化合物。该方法利用羟胺化合物和/或其药物组合物来治疗血管发生，肝炎，补体介导的病理学，玻璃疣介导的病理学，黄斑变性和某些其它眼科疾病，炎症，关节炎和相关疾病以及抑制补体激活。

3. 发明申请

WO2007100623A2 HYDROXYLAMINES AND DERIVATIVES FOR THE INHIBITION OF COMPLEMENT ACTIVATION 审中-公开
标题翻译：用于抑制补体活化的羟甲苯胺和衍生物
公开(公告)号：WO2007100623A2
公开(公告)日：2007-09-07
申请号：PCT/US2007/004658
申请日：2007-02-22
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
CPC分类号： A61K31/445
摘要： Methods for the inhibition of complement activation, for the treatment of complement-mediated pathologies, and for the treatment of drusen-mediated pathologies are disclosed. The methods utilize hydroxylamine compounds and ester derivatives thereof, administered to subjects in effective amounts.
摘要翻译：公开了用于抑制补体激活，用于治疗补体介导的病理学和治疗玻璃疣介导的病理学的方法。该方法利用有效量给予受试者的羟胺化合物及其酯衍生物。

4. 发明申请

WO2005051328A2 AMELIORATION OF MACULAR DEGENERATION AND OTHER OPHTHALMIC DISEASES 审中-公开
标题翻译：黄斑变性和其他眼部疾病的改善
公开(公告)号：WO2005051328A2
公开(公告)日：2005-06-09
申请号：PCT/US2004/039719
申请日：2004-11-22
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
IPC分类号： A61K
CPC分类号： A61K31/13 , A61K31/42 , A61K31/445
摘要： Methods for the treatment or prevention of a number of ocular diseases or disorders are disclosed. In particular, methods are disclosed for the amelioration of macular degeneration, diabetic retinophaty and other retinopathies, as well as uveitis, presbyopia, dry eye, glaucoma, blepharitis and rosacea of the eye. The methods comprise administration of a compositions comprising an ophthalmologically acceptable carrier or diluent and a hydoxylamine compound in a therapeutically sufficient amount to prevent, retard the development or reduce the symptoms of one or more of the ophthalmic conditions.
摘要翻译：公开了用于治疗或预防许多眼部疾病或病症的方法。具体而言，公开了用于改善黄斑变性，糖尿病性视网膜病和其他视网膜病以及眼睛的葡萄膜炎，老花眼，干眼症，青光眼，眼睑炎和红斑痤疮的方法。所述方法包括施用包含眼科学上可接受的载体或稀释剂和羟基胺化合物的组合物，治疗足够量以防止，延缓一种或多种眼科病症的发展或减轻症状。

5. 发明申请

WO2006127592A2 AMELIORATION OF VITRECTOMY-INDUCED CATARACTS 审中-公开
标题翻译：诱导诱导的CATARACTS的调节
公开(公告)号：WO2006127592A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/019721
申请日：2006-05-22
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
CPC分类号： A61K31/133 , A61K31/421 , A61K31/445
摘要： Methods to prevent, inhibit, or slow the development of vitrectomy-induced cataracts are disclosed. The methods comprise administering to the eye of a subject a composition comprising an ophthalmologically acceptable carrier or diluent and at least one hydroxylamine compound in a therapeutically sufficient amount to prevent, inhibit, or slow the development of a vitrectomy- induced cataract in the subject to which the composition is administered.
摘要翻译：公开了预防，抑制或减缓玻璃体切割术诱导的白内障发展的方法。所述方法包括向受试者施用包含眼科学上可接受的载体或稀释剂和至少一种治疗上足够量的羟胺化合物的组合物以防止，抑制或减缓受试者中玻璃体切割术诱发的白内障发展，给予组合物。

6. 发明申请

WO2005115375A1 OCULOSELECTIVE DRUGS AND PRODRUGS 审中-公开
标题翻译： OCULOSELECTIVE DRUGS和PRODRUGS
公开(公告)号：WO2005115375A1
公开(公告)日：2005-12-08
申请号：PCT/US2005/018350
申请日：2005-05-24
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
IPC分类号： A61K31/24
CPC分类号： A61K31/195 , A61K31/215 , A61K31/24 , A61K31/34 , A61K31/401 , A61K31/445 , A61K31/537 , C07C219/14 , C07C237/08 , C07D307/24 , Y02P20/55
摘要： Compounds of the following formula are disclosed: wherein R 1 and R 2 are each independently H, W, or a phenoxyl protecting group; and R 4 is H or W, provided that at least one of R 1 , R 2 , and R 4 is W; R 3 is hydrogen, straight chain or branched C 1 -C 10 alkyl, cycloalkyl, amino, C 1 -C 10 alkoxy, -NHC(=O)Ra, or -C(=O)N(H)R a ; R a is alkyl, aryl, or heterocyclyl; Z is -0-, -O(C=O)-, or NH(C=O)-, wherein when Z is -0-, R 5 is H, straight chain or branched C 1 -C 10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C 1 -C 10 alkyl, CI-Clo alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolsdinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with CI-Clo alkyl, C 1 -C 10 alkoxy, or halo; and W is:, wherein each R 6 is independently H, straight chain or branched C 1 -C 10 alkyl, or straight chain or branched C l -C 10 alkoxyalkyl; and R 7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is -O(C=O)-, R 5 is straight chain or branched C 1 -C 10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C 1 -C 10 alkyl, CI-CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C l -C 10 alkyl, C 1 -C 10 alkoxy, or halo; and W is: , wherein each R6 is independently H, straight chain or branched CI-C to alkyl, or straight chain or branched C,-C to alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is-NH(C=O)-, R5 is straight chain or branched C 1 -C 10 alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C 1 -C 10 alkyl, CI-CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, &oxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C 1 -C 10 alkyl, C 1 -C 10 alkoxy, or halo; and W is: ; wherein each R6 is independently H, straight chain or branched C1 -C to alkyl, or straight chain or branched C,-Clo alkoxyalkyl. Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions, are also disclosed.
摘要翻译：公开了下式的化合物：其中R 1和R 2各自独立地为H，W或苯氧基保护基; R 4为H或W，条件是R 1，R 2和R 4中的至少一个为W; R 3是氢，直链或支链C 1 -C 10烷基，环烷基，氨基，C 1 -C 10烷氧基，-NHC（= O）R a或-C（= O）N（H）R a; R a是烷基，芳基或杂环基; Z是-O - ， - O（C = O） - 或NH（C = O） - ，其中当Z是-O-时，R 5是H，直链或支链C 1 -C 10烷基，环烷基，被至少一个直链或支链C 1 -C 10烷基，C 1 -C 6烷氧基烷基，氨基，苄基，四氢呋喃基，二氢呋喃基，呋喃基，吗啉基，哌啶基，四氢吡喃基，二氧戊环基，2,2-二甲基二氧戊环基，二恶烷基，吡咯基，吡咯烷基，苯基或被C 1-6烷基取代的苯基，C 1 -C 10烷氧基或卤素; W为：其中每个R 6独立地为H，直链或支链C 1 -C 10烷基，或直链或支链C 1 -C 10烷氧基烷基; 和R 7是烷基，环烷基，芳基或芳烷基; 并且当Z为-O（C = O） - 时，R 5为直链或支链C 1 -C 10烷基，环烷基，被至少一个直链或支链C 1 -C 10烷基取代的环烷基，C 1 -C 10烷氧基烷基，氨基二氢呋喃基，吡咯烷基，四氢恶唑基，二氢恶唑基，苯基或被C 1 -C 10烷基取代的苯基，C 1 -C 10烷氧基，C 1 -C 10烷氧基，或卤素; 且W为：其中每个R 6独立地为H，直链或支链C 1 -C 8烷基或直链或支链C 1 -C 3烷氧基烷基; 并且R 7是烷基，环烷基，芳基或芳烷基; 并且当Z是-NH（C = O） - 时，R 5是直链或支链C 1 -C 10烷基，环烷基，被至少一个直链或支链C 1 -C 10烷基取代的环烷基，C 1 -C 10烷氧基烷基，氨基，苄基，四氢呋喃基，二氢呋喃基，呋喃基，吗啉基，哌啶基，四氢吡喃基，氧杂环戊烷基，2,2-二甲基二氧戊环基，二恶烷基，吡咯基，吡咯烷基，四氢恶唑基，二氢恶唑基，苯基或被C1-C10烷基，C1-C10烷氧基或卤素取代的苯基。 W是：其中每个R 6独立地为H，直链或支链C 1 -C烷基或直链或支链C 1 -C 4烷氧基烷基。还公开了制备化合物的方法，包含该化合物的药物组合物，以及通过施用药物组合物治疗患者的方法。

7. 发明申请

WO2008101195A3 DRUG RESISTANCE REVERSAL IN NEOPLASTIC DISEASE 审中-公开
公开(公告)号：WO2008101195A3
公开(公告)日：2008-08-21
申请号：PCT/US2008/054135
申请日：2008-02-15
申请人： OTHERA HOLDING, INC. , PATIL, Ghanshyam , MOUSA, Shaker A.
发明人： PATIL, Ghanshyam , MOUSA, Shaker A.
IPC分类号： A61K31/445 , A61P27/00 , A61P35/00 , A61P39/06
摘要： The present invention is directed to compounds, compositions, and methods for halting or reversing the effects of chemoresistance in neoplastic diseases. In particular the use of hydroxylamines is described.

8. 发明申请

WO2007100624A2 HYDROXYLAMINES AND DERIVATIVES FOR TREATMENT OF INFLAMMATORY CONDITIONS OF THE LIVER 审中-公开
标题翻译：用于治疗肝脏炎症状况的羟甲苯胺和衍生物
公开(公告)号：WO2007100624A2
公开(公告)日：2007-09-07
申请号：PCT/US2007/004659
申请日：2007-02-22
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
CPC分类号： A61K31/421 , A61K31/445 , Y02A50/463
摘要： Methods for the treatment and inhibition of hepatitis are disclosed. The methods utilize hydroxylamine compounds or ester derivatives thereof, administered to patient in an amount effective to treat or inhibit hepatitis.
摘要翻译：公开了治疗和抑制肝炎的方法。该方法利用羟胺化合物或其酯衍生物，以有效治疗或抑制肝炎的量施用于患者。

9. 发明申请

WO2007092741A3 HYDROXYLAMINES AND DERIVATIVES AS ANTI-ANGIOGENIC AGENTS 审中-公开
公开(公告)号：WO2007092741A3
公开(公告)日：2007-08-16
申请号：PCT/US2007/061484
申请日：2007-02-01
申请人： OTHERA HOLDINGS, INC. , MATIER, William L. , PATIL, Ghanshyam
发明人： MATIER, William L. , PATIL, Ghanshyam
IPC分类号： A61K31/445 , A01N43/40
摘要： The present disclosure provides compounds that inclue hydroxylamines and ester derivatives thereof and methods for using the same for the treatment of angiogenesis and related diseases.

10. 发明申请

WO2005055926A2 AMELIORATION OF CATARACTS, MACULAR DEGENERATION AND OTHER OPHTHALMIC DISEASES 审中-公开
标题翻译：食物调理，黄斑变性和其他眼底疾病
公开(公告)号：WO2005055926A2
公开(公告)日：2005-06-23
申请号：PCT/US2004/039716
申请日：2004-11-22
申请人： OTHERA PHARMACEUTICALS, INC. , MATIER, William, L. , PATIL, Ghanshyam
发明人： MATIER, William, L. , PATIL, Ghanshyam
IPC分类号： A61K
CPC分类号： A61K31/445 , A61K9/0048 , A61K9/0051 , A61K31/145 , A61K31/198 , A61K31/4525 , A61K38/063 , A61K45/06 , C07D211/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D487/04 , A61K2300/00
摘要： Ophthalmically acceptable compositions used in arresting the development of cataract, presbyopia, macular degeneration and other retinopathies, glaucoma, uveitis and various corneal disorders are disclosed. The compositions are also useful as a prophylactic treatment to prevent or delay development of age-related ocular disorders, which include cataracts, presbyopia, glaucoma and macular degeneration. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula where R 1 and R 2 are, independently, H or C 1 to C 3 alkyl ; R 3 and R 4 are, independently C 1 to C 3 alkyl; and where R 1 and R 2 , taken together, or R 3 and R 4 , taken together, or both may be cycloalkyl; R 5 is H, OH, or C 1 to C 6 alkyl ; R 6 is or C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl ; R 7 is C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl or where R 6 and R 7 , or R 5 , R 6 and R 7 , taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.
摘要翻译：公开了用于阻止白内障，老花眼，黄斑变性和其他视网膜病变，青光眼，葡萄膜炎和各种角膜疾病发展的眼科可接受的组合物。该组合物还可用作预防或延迟年龄相关性眼部疾病（包括白内障，老花眼，青光眼和黄斑变性）的预防性治疗。组合物包含药学上可接受的载体或稀释剂和至少一种具有下式的化合物：其中R 1和R 2独立地为H或C 1至C 3烷基; R3和R4独立地为C1至C3烷基; 并且其中R 1和R 2一起或者R 3和R 4一起或两者可以是环烷基; R5是H，OH或C1-C6烷基; R 6为或C 1至C 6烷基，烯基，炔基或取代的烷基或链烯基; R 7是C 1至C 6烷基，烯基，炔基或取代的烷基或链烯基，或其中R 6和R 7或R 5，R 6和R 7一起形成环中具有3至7个原子的碳环或杂环。

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