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1. 发明申请

WO2007146953A3 COMPOSITIONS AND METHODS FOR SIRNA INHIBITION OF ANGIOGENESIS 审中-公开
标题翻译：用于SIRNA抑制血管生成的组合物和方法
公开(公告)号：WO2007146953A3
公开(公告)日：2008-03-06
申请号：PCT/US2007071029
申请日：2007-06-12
申请人： EXEGENICS INC D B A OPKO HEALT , REICH SAMUEL JOTHAM
发明人： REICH SAMUEL JOTHAM
IPC分类号： A61K31/7105 , A61K31/713 , C12N15/11 , C12N15/113
CPC分类号： C12N15/1137 , C12N15/111 , C12N15/1136 , C12N2310/111 , C12N2310/14 , C12N2320/31
摘要： Embodiments of methods of using siRNAs targeting VEGF including an siRNA defined by SEQ ID NO: 77 and SEQ ID NO: 78 to stabilize visual acuity in a subject, to inhibit choroidal neovascularization lesions, to treat age-related macular degeneration, to treat diabetic macular edema, and to decrease foveal thickness in subjects are disclosed. Additionally, methods of treating age-related macular degeneration and diabetic macular edema by administering combinatorial therapy comprising an siRNA targeting VEGF and a non-siRNA VEGF antagonist are described.
摘要翻译：使用靶向VEGF的siRNA的方法的实施方案，包括由SEQ ID NO：77和SEQ ID NO：78定义的siRNA，以稳定受试者的视力，抑制脉络膜新生血管形成病变，治疗年龄相关性黄斑变性，治疗糖尿病性黄斑公开了水肿，并减少受试者的中心凹厚度。另外，描述了通过包括靶向VEGF和非siRNA VEGF拮抗剂的siRNA的组合疗法治疗年龄相关性黄斑变性和糖尿病性黄斑水肿的方法。

2. 发明申请

WO2007146953A2 COMPOSITIONS AND METHODS FOR SIRNA INHIBITION OF ANGIOGENESIS 审中-公开
标题翻译：用于SIRNA抑制血管生成的组合物和方法
公开(公告)号：WO2007146953A2
公开(公告)日：2007-12-21
申请号：PCT/US2007071029
申请日：2007-06-12
申请人： EXEGENICS INC D B A OPKO HEALT , REICH SAMUEL JOTHAM
发明人： REICH SAMUEL JOTHAM
IPC分类号： C12N15/11 , C12N15/113
CPC分类号： C12N15/1137 , C12N15/111 , C12N15/1136 , C12N2310/111 , C12N2310/14 , C12N2320/31
摘要： Embodiments of methods of using siRNAs targeting VEGF including an siRNA defined by SEQ ID NO: 77 and SEQ ID NO: 78 to stabilize visual acuity in a subject, to inhibit choroidal neovascularization lesions, to treat age-related macular degeneration, to treat diabetic macular edema, and to decrease foveal thickness in subjects are disclosed. Additionally, methods of treating age-related macular degeneration and diabetic macular edema by administering combinatorial therapy comprising an siRNA targeting VEGF and a non-siRNA VEGF antagonist are described.
摘要翻译：使用靶向VEGF的siRNA的方法的实施方案，包括由SEQ ID NO：77和SEQ ID NO：78定义的siRNA，以稳定受试者的视力，抑制脉络膜新生血管形成病变，治疗年龄相关性黄斑变性，治疗糖尿病性黄斑公开了水肿，并减少受试者的中心凹厚度。另外，描述了通过包括靶向VEGF和非siRNA VEGF拮抗剂的siRNA的组合疗法治疗年龄相关性黄斑变性和糖尿病性黄斑水肿的方法。

3. 发明专利

DK2029746T3 Sammensætninger og fremgangsmåder til siRNA-hæmning af angiogenese 未知
公开(公告)号：DK2029746T3
公开(公告)日：2012-10-08
申请号：DK07812121
申请日：2007-06-12
申请人： EXEGENICS INC D B A OPKO HEALTH INC
发明人： REICH SAMUEL JOTHAM
IPC分类号： C12N15/113 , A61K31/713 , C12N15/11

4. 发明专利

CA2634286A1 COMPOSITIONS AND METHODS FOR REGULATING COMPLEMENT SYSTEM 未知
公开(公告)号：CA2634286A1
公开(公告)日：2007-08-09
申请号：CA2634286
申请日：2006-12-22
申请人： EXEGENICS INC D B A OPKO HEALT
发明人： REICH SAMUEL JOTHAM , DEJNEKA NADINE
IPC分类号： A61K31/713 , A61K48/00 , C07H21/02 , C12N15/113 , C12N15/12
摘要： An isolated siRNA is provided for modulating the human complement pathway by reducing the expression or production of one or more complement pathway protein(s) and uses for such siRNAs for treating diseases including ocular disease and macular degeneration related disease. The invention also includes compositions mediating the modulation of the complement pathway including siRNA designed to cause the RNAi-mediated degradation of complement pathway proteins.

5. 发明专利

IL152110D0 EXPRESSION SYSTEM FOR EFFICIENTLY PRODUCING CLINICALLY EFFECTIVE LYSOSOMAL ENZYMES (GLUCOCEREBROSIDASE) 未知
公开(公告)号：IL152110D0
公开(公告)日：2003-07-31
申请号：IL15211001
申请日：2001-04-06
申请人： EXEGENICS INC
IPC分类号： C12N9/24 , C12N
摘要： The invention as described herein relates to the efficient production of recombinant, clinically effective lysosomal enzymes using a transformed insect cell expression system. For example, to create the expression system of the invention, any insect cell can be transfected with a plasmid comprised of a gene encoding the human glucocerebrosidase gene and genetic elements that enhance its expression. The insect cell transfected with the plasmid encoding glucocerebrosidase secretes synthesized glucocere-brosidase into its growth media. The recombinantly produced clinically effective glucocerebrosidase produced by the insect cell expression system can be used to treat Gaucher's disease.

6. 发明申请

WO2004012506A2 ANTIMICROBIAL COMPOUNDS 审中-公开
标题翻译：抗微生物化合物
公开(公告)号：WO2004012506A2
公开(公告)日：2004-02-12
申请号：PCT/US2003/019788
申请日：2003-06-23
申请人： EXEGENICS, INC. , ARAD, Dorit , AV-GAY, Yossef
发明人： ARAD, Dorit , AV-GAY, Yossef
IPC分类号： A01N
CPC分类号： A01N37/44 , A01N37/52 , A01N47/44
摘要： Novel anti-microbial compounds are disclosed. Representative antimicrobial compounds have the following chemical structure: (F) wherein the Q-A grouping can be at the ortho, meta or para position; A is selected from the group consisting of CH 2 , O, S, SO, SO 2i NH, and NR wherein R is selected from the group consisting of C1-C7 alkyls, aralkyls having a C 1 -C 3 alkyl chain, and C 3 -C 7 cycloalkyls; Q is a ω-unsubstituted or ω-substituted basic nitrogen connected through a linker to A, wherein the basic nitrogen is selected from the group consisting of i) an unsubstituted or substituted amine, amidine, or guanidine, wherein substitutions on the amine, amidine, and guanidine groups, other than A can be one or more C 1 -C 6 alkyl, acyl, aminoacyl (urea), aminothioacyl (thiourea), and aryl or aralkyl unsubstituted or substituted with C 1 -C 3 alkoxy, -NR 2 , -NHCOR, halogen (from one to three substitutions), -NO 2i or -OH, wherein R is as defined above and wherein R2 is selected from the group consisting of hydrogen, aryl, saturated and unsaturated C1-C6 alkyl or aralkyl singly or in combination; or ii) contained in a heterocyclic ring including but not limited to pyrrole, pyrrolidine, oxazole, thiazole, pyridine, piperidine, morpholine or imidazole; wherein Q linked to A has a configuration selected from the group consisting of i) a saturated or unsaturated alkyl of one to eight carbons which can be unsubstituted or substituted with one or more C 1 -C 6 alkyl, C1-C 3 alkoxy, C 1 -C 6 alkyl-S-, C 1 -C 6 alkyl-SO-, or C 1 -C 6 alkyl-S02-, ii) an alkyl chain containing an aromatic ring selected from the group consisting of -0-alkyl-aryl, -0-alkyl-aryl-alkyl, and -0-aryl-alkyl, iii) an alkyl forming five and six membered rings which can be unsubstituted or substituted with C 1 -C 7 alkyl, C 1 -C 3 alkoxy, C 3 -C 7 cycloalkyls, or aralkyls having a C 1 -C 3 alkyl chain, unsubstituted or substituted with C 1 -C 3 alkoxy, -NR 2 , -NHCOR, halogen (from one to three substitutions), -NO 2 , or -OH, wherein R and R 2 are as defined above, iv) when Q is amine, amidine or guanidine, an alkyl chain which incorporates the basic nitrogen of Q into a five or six membered ring, v) an unsubstituted or substituted bicyclic aralkyl including but not limited to biphenyls, diphenyl ethers, and diphenylthio ethers; vi) linker A and core benzene ring together forming a substituted naphthyl which can contain one to two nitrogens; J m are aromatic substituents together or in combination, including but not limited to ethers, halogens, CF 3 , C 1 -C 6 alkyl, carboxylic acids, esters, amides, substituted heteroatom ethers including but not limited to sulfides, sulfoxides, and sulfones, -NH 2 , -NHR, or -NR 2 , wherein R and R 2 are as defined above, and wherein m is 1-3; (CZ) n is selected from the group consisting of a C 1 -C 4 alkyl, wherein Z is independently selected from the group consisting of hydrogen, aryl, saturated and unsaturated C 1 -C 6 alkyl or aralkyl singly or in combination, and wherein n = 0 to 4; R 3 is selected from the group consisting of hydrogen, C 1 -C 7 alkyl, aralkyl, substituted and unsubstituted alkoxymethyl, tetrahydropyranyl, or tetrahydrofuranyl, and wherein the C=NOR 3 stereochemistry can be E or Z ; G is selected from the group consisting of hydrogen, aryl, saturated and unsaturated C 1 -C 6 alkyl or aralkyl; Y is the linker connecting NG to L which can be i) a saturated or unsaturated alkyl chain of 2-8 carbons, ii) an alkyl chain containing an aromatic ring selected from the group consisting of -0-alkyl-aryl, -0-alkyl-aryl-alkyl, and -0-aryl-alkyl, iii) an alkyl forming five and six membered rings which can be unsubstituted or substituted with C1-C7 alkyl, C 1 -C 3 alkoxy, C 3 -C 7 cycloalkyls, or aralkyls having a C 1 -C 3 alkyl chain, unsubstituted or substituted with C 1 -C 3 alkoxy, -NR 2 , -NHCOR, halogen (from one to three substitutions), NO 2 , or -OH, wherein R and R 2 are as defined above, or iv) when L is amine, amidine, or guanidine, an alkyl chain which incorporates the basic nitrogen of L into a five or six membered ring, and L is an unsubstituted or substituted basic nitrogen connected through linker Y to NG, wherein the basic nitrogen can be: i) an unsubstituted or substituted amine, amidine, or guanidine, wherein substitutions on the amine, amidine, and guanidine groups, other than Y can be C 1 -C 6 alkyl, acyl, aminoacyl (urea), aminothioacyl (thiourea), or aryl or aralkyl unsubstituted or substituted with C 1 -C 3 alkoxy, -NR 2 , -NHCOR, halogen (from one to three substitutions), -NO 2 , or -OH, wherein R and R 2 are as defined above, or ii) contained in a heterocyclic ring including but not limited to pyrrole, pyrrolidine, oxazole, thiazole, pyridine, piperidine, morpholine or imidazole, provided that when n is 1; A is O; m=2; J is selected from the group consisting of halogens, CF 3 , esters and C1 - C 4 alkyls and are at the 3 and 5 positions; T is =NOH; and Q and L are independently selected from the group consisting of amine, amidine, guanidine, piperazine, piperidine, and 1 H -imidazol-2-ylamino attached to A at the carbon at the 4 position or 1 H imidazol-2-ylamino attached to Y at the carbon at the 4 position, respectively, then Q-A cannot be in the para position.
摘要翻译：公开了新的抗微生物化合物。代表性的抗微生物化合物具有以下化学结构：（F）其中Q-A基团可以在邻位，间位或对位; A选自CH 2，O，S，SO，SO 2 NH和NR，其中R选自C 1 -C 7烷基，具有C 1 -C 3烷基链的芳烷基和C 3 -C 7环烷基; Q是通过接头与A连接的ω-未取代的或ω-取代的碱式氮，其中碱性氮选自i）未取代或取代的胺，脒或胍，其中取代胺，脒和除A之外的胍基可以是一个或多个C 1 -C 6烷基，酰基，氨酰基（脲），氨基硫代酰基（硫脲）和未被取代或被C 1 -C 3烷氧基，-NR 2，-NHCOR，卤素取代的芳基或芳烷基（1至3个取代），-NO 2或-OH，其中R如上所定义，其中R 2选自氢，芳基，饱和和不饱和的C 1 -C 6烷基或芳烷基单独或组合; 或ii）包含在包括但不限于吡咯，吡咯烷，恶唑，噻唑，吡啶，哌啶，吗啉或咪唑的杂环中; 其中与A连接的Q具有选自以下的构型：i）1至8个碳原子的饱和或不饱和烷基，其可以是未取代的或被一个或多个C 1 -C 6烷基，C 1 -C 3烷氧基，C 1 -C 6烷基 -S-，C 1 -C 6烷基-SO-或C 1 -C 6烷基-SO 2 - ，ii）含有选自-O-烷基 - 芳基，-O-烷基 - 芳基 - 烷基和-O-芳基 - 烷基，iii）形成五元和六元环的烷基，其可以是未取代的或被C 1 -C 7烷基，C 1 -C 3烷氧基，C 3 -C 7环烷基或具有C 1 -C 3烷基的芳烷基链，未取代或被C 1 -C 3烷氧基取代，-NR 2，-NHCOR，卤素（1至3个取代），-NO 2或-OH，其中R和R 2如上定义，iv）当Q为胺时，或胍，其将Q的碱性氮结合成五元或六元环的烷基链，v）未取代或取代的双环芳烷基，包括但不限于联苯，二苯基乙和二苯硫醚; vi）连接体A和核心苯环一起形成可含有一至两个氮原子的取代萘基; 包括但不限于醚，卤素，CF 3，C 1 -C 6烷基，羧酸，酯，酰胺，取代的杂原子醚，包括但不限于硫化物，亚砜和砜，芳族取代基，-NH 2， -NHR或-NR2，其中R和R2如上所定义，并且其中m为1-3; （CZ）n选自C 1 -C 4烷基，其中Z独立选择

7. 发明申请

WO2003087127A3 ANTIMICROBIAL COMPOUNDS AGAINST STAPHYLOCOCCI, MYCOBACTERIA, AND OTHER INFECTIOUS AGENTS 审中-公开
公开(公告)号：WO2003087127A3
公开(公告)日：2003-10-23
申请号：PCT/US2003/010780
申请日：2003-04-07
申请人： EXEGENICS INC. , ARAD, Dorit , AV-GAY, Yossef
发明人： ARAD, Dorit , AV-GAY, Yossef
IPC分类号： A61K31/13
摘要： Novel antimicrobial compounds effective against mycobacteria, staphylococci, and other infectious agents are disclosed. Representative antimicrobial compounds have the following chemical structure: Wherein: (Formula I), M and L independently can be hydrogen, halogen, -CF 3 , -OMe (Me=methyl), -OR 4 wherein R 4 is selected from the group consisting of alkyls of 2-4 carbons, or R 5 wherein R 5 is selected from the group consisting of alkyls of 1-4 carbons; T can be O, S or NR 6 wherein R 6 is selected from the group consisting of hydrogen or alkyls of 1-4 carbons which are straight or branched; Q can be CH 2 , CHR 7 , S, O, NH, or NR 7 wherein R 7 is selected from the group consisting of hydrogen or alkyls of 1-4 carbons which are straight or branched; Y can be N, O or S; R 1 is an aminoalkyl with or without substitution and R 3 is either an amidinoalkyl or guanidinoalkyl with or without substitution; R 1 is either an amidinoalkyl or guanidinoalkyl with or without substitution and R 3 is an aminoalkyl with or without substitution; or both R 1 and R 3 are either an amidinoalkyl or guanidinoalkyl with or without substitution; and R 2 is selected from the group consisting of -OH, -OG, -NMe 2 , -NHCONH 2 , -NHCSNH 2 , -NH 2 , and -NH-G, wherein G is as defined in R 1 above and in all of which the C=N~R 2 stereochemistry can be E or Z , and acid salts thereof.

8. 发明申请

WO2007146953A8 COMPOSITIONS AND METHODS FOR SIRNA INHIBITION OF ANGIOGENESIS 审中-公开
公开(公告)号：WO2007146953A8
公开(公告)日：2007-12-21
申请号：PCT/US2007/071029
申请日：2007-06-12
申请人： EXEGENICS, INC., D/B/A OPKO HEALTH, INC. , REICH, Samuel, Jotham
发明人： REICH, Samuel, Jotham
IPC分类号： C12N15/11 , A61K31/7105 , A61K31/713
摘要： Embodiments of methods of using siRNAs targeting VEGF including an siRNA defined by SEQ ID NO: 77 and SEQ ID NO: 78 to stabilize visual acuity in a subject, to inhibit choroidal neovascularization lesions, to treat age-related macular degeneration, to treat diabetic macular edema, and to decrease foveal thickness in subjects are disclosed. Additionally, methods of treating age-related macular degeneration and diabetic macular edema by administering combinatorial therapy comprising an siRNA targeting VEGF and a non-siRNA VEGF antagonist are described.

9. 发明申请

WO2002076939A2 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：WO2002076939A2
公开(公告)日：2002-10-03
申请号：PCT/US2002/003785
申请日：2002-02-05
申请人： EXEGENICS INC. , ARAD, Dorit , BOLLON, Arthur, P. , YOUNG, David, G. , PEEK, Andrew, S. , POLAND, Bradley, W. , SHAW, Bailin , VALLURUPALLI, Jyothi
发明人： ARAD, Dorit , BOLLON, Arthur, P. , YOUNG, David, G. , PEEK, Andrew, S. , POLAND, Bradley, W. , SHAW, Bailin , VALLURUPALLI, Jyothi
IPC分类号： C07D
CPC分类号： C07D213/53 , C07C49/86 , C07C50/32 , C07C50/38 , C07C225/30 , C07C233/31 , C07C233/76 , C07C251/20 , C07C251/24 , C07C251/48 , C07C251/86 , C07C271/12 , C07C271/28 , C07C271/64 , C07C309/44 , C07C317/24 , C07C323/22 , C07C2601/14 , C07C2602/10 , C07C2603/74 , C07D211/90 , C07D213/90 , C07D215/233 , C07D215/24 , C07D215/50 , C07D221/14 , C07D223/16 , C07D239/56 , C07D241/44 , C07D263/57 , C07D307/54 , C07D307/88 , C07D333/38 , C07D417/04 , C07D471/04 , C07F15/02
摘要： Compounds having quinone and quinone analogs useful for pharmaceutical preparations have now been found which inhibit cysteine proteases, in particular, caspases and 3C-cysteine proteases. The cysteine protease inhibitors of the present invention can be identified by their mode of action in disrupting the ability of cysteine proteases and, in particular, caspases to cleave a peptide chain. These compounds are useful in inhibiting cysteine protease or cysteine protease-like proteins and for treating infections diseases or physiopathological diseases or disorders attributed to the presence of excessive or insufficient levels of cysteine proteases.
摘要翻译：现已发现可用于药物制剂的醌和醌类似物的化合物抑制半胱氨酸蛋白酶，特别是胱天蛋白酶和3C-半胱氨酸蛋白酶。本发明的半胱氨酸蛋白酶抑制剂可以通过它们的作用模式来破坏半胱氨酸蛋白酶，特别是胱天蛋白酶切割肽链的能力。这些化合物可用于抑制半胱氨酸蛋白酶或半胱氨酸蛋白酶样蛋白，并用于治疗由于半胱氨酸蛋白酶过多或不足的存在引起的感染疾病或病理病理学疾病或病症。

10. 发明专利

IL195803D0 COMPOSITIONS AND METHODS FOR SIRNA INHIBITION OF ANGIOGENESIS 未知
公开(公告)号：IL195803D0
公开(公告)日：2011-08-01
申请号：IL19580308
申请日：2008-12-08
申请人： EXEGENICS INC D B A OPKO HEALTH INC
IPC分类号： C12N15/11 , C12N15/113
摘要： Embodiments of methods of using siRNAs targeting VEGF including an siRNA defined by SEQ ID NO: 77 and SEQ ID NO: 78 to stablize visual acuity in a subject, to inhibit choroidal neovascularization lesions, to treat age-related ;macular degeneration, to treat diabetic macular edema, and to decrease foveal thickness in subjects are disclosed. Additionally, methods of treating age-related macular degeneration and diabetic macular edema by administering combinatorial therapy comprising an siRNA targeting VEGF and a non-siRNA VEGF antagonist are described.

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