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1. 发明申请

US20040204375A1 Gene delivery compounds 审中-公开
标题翻译：基因递送化合物
公开(公告)号：US20040204375A1
公开(公告)日：2004-10-14
申请号：US10476754
申请日：2003-11-03
发明人： Eric J Sorscher , Jeong S Hong , Jennifer E Harris , Kimberly V Curlee , Joseph A Maddry , William B Parker , William R Wand
IPC分类号： A61K048/00 , A61K031/7076 , A61K031/15
CPC分类号： C07D213/53 , A61K31/15 , A61K31/7076 , A61K45/06 , A61K48/0008 , A61K2300/00
摘要： Compounds having the structure: 1 wherein R1, R2 and R3 are each independently a C0-12 substituent selected from the group consisting of: hydrogen, a heteroatom, alkyl, alkenyl, alkynyl, heteroatom substituted alkyl, heteroatom substituted alkenyl, heteroatom substituted alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl; where the heteroatom is selected from the group consisting of: N, O and S; and where (A) is a single or double bond between N and R3. Further the C0-12 substituent is linear, branched or cyclic and optionally includes a pendant moiety selected from the group consisting of: carbonyl, hydroxyl, carboxyl, amine, thiol, thioester, thioether, phosphate, alkoxy, aryl, arylalkyl, sulfonamide and alkyl halide. Further, compounds 6883, 6898, 6975, 7036, 7064 and 8496 are provided. A process is provided for activating gene transfer in a subject by administering a pharmaceutically effective amount of a gene transfer activating compound to a subject and delivering pharmaceutically effective amount of a vector containing a nucleic so that the nucleic acid is transcribed in a target cell of the subject. A process for activating gene transfer to a cell is provided. A kit for activating gene transfer is provided.
摘要翻译：具有以下结构的化合物：其中R1，R2和R3各自独立地为选自以下的C0-12取代基：氢，杂原子，烷基，烯基，炔基，杂原子取代的烷基，杂原子取代的烯基，杂原子取代的炔基，芳基，芳基烷基，芳基烯基，芳基炔基; 其中杂原子选自：N，O和S; 其中（A）是N和R3之间的单键或双键。此外，C0-12取代基是直链，支链或环状的，并且任选地包括选自羰基，羟基，羧基，胺，硫醇，硫酯，硫醚，磷酸酯，烷氧基，芳基，芳烷基，磺酰胺和烷基卤化物。此外，提供了化合物6883,6898,6975,7036,7064和8496。提供了通过向受试者施用药学有效量的基因转移活化化合物并递送药学有效量的含有核酸的载体以使得核酸被转录到靶细胞的靶细胞中来激活受试者中的基因转移的方法学科。提供了一种激活基因转移至细胞的方法。提供用于激活基因转移的试剂盒。

2. 发明申请

US20040110729A1 Primary N-hydroxylamines 审中-公开
公开(公告)号：US20040110729A1
公开(公告)日：2004-06-10
申请号：US10722820
申请日：2003-11-25
发明人： Bruce N. Ames , Hani Atamna
IPC分类号： A61K031/655 , A61K031/15 , A61K031/13
CPC分类号： A61K31/131 , A61K31/13 , A61K31/133 , A61K31/136 , A61K31/137 , A61K31/15 , A61K31/417 , A61K31/423 , A61K31/4406 , A61K31/4425 , A61K31/47
摘要： The invention provides pharmaceutical compositions comprising primary N-hydroxylamines and related therapeutic, prophylactic, diagnostic and screening methods. The pharmaceutical compositions generally comprise a pharmaceutical composition comprising an orally administrable effective unit solid dosage of a primary N-hydroxylamine or a pharmaceutically acceptable salt thereof and substantially free of a nitrone corresponding to the hydroxylamine.

3. 发明申请

US20040014807A1 Phenalenone derivatives, processes for preparation and use thereof 失效
标题翻译：萘烯酮衍生物，其制备方法和用途
公开(公告)号：US20040014807A1
公开(公告)日：2004-01-22
申请号：US10367545
申请日：2003-02-14
发明人： Laszlo Vertesy , Michael Kurz , Ziyu Li , Luigi Toti
IPC分类号： A61K031/343 , A61K031/15 , A61K031/277 , A61K031/122 , A61K031/135 , C07D307/93 , C07C255/40 , C07C251/44 , C07C050/10
CPC分类号： C07D307/92 , C12P7/22 , C12P17/04 , C12R1/80
摘要： The present invention provides novel phenalenone derivatives of formula (I) which are formed by the microorganism Penicillium herquei Bainer & Sartory, DSM 14142, during fermentation. A process for their preparation, their use as pharmaceutical compositions, and their use for the treatment or prophylaxis of bacterial infections, mycoses, oncoses and rheumatic diseases are also disclosed and claimed. 1
摘要翻译：本发明提供在发酵过程中由微生物青霉菌Bainer＆Sartory DSM 14142形成的新颖的式（I）的phenalenone衍生物。还公开并要求保护其制备方法，它们作为药物组合物的用途及其用于治疗或预防细菌感染，真菌病，肿瘤和风湿性疾病的用途。

4. 发明申请

US20030157037A1 Use of aryl oximes for the prophylaxis and/or treatment of erythema formation and/or inflammatory reaction of the skin 审中-公开
标题翻译：芳基肟用于预防和/或治疗皮肤红斑形成和/或炎症反应
公开(公告)号：US20030157037A1
公开(公告)日：2003-08-21
申请号：US10296059
申请日：2002-11-21
发明人： Joachim Bunger , Hansjurgen Driller , Michael Schwarz , Wolfgang Wohlrab
IPC分类号： A61K031/15 , A61K031/44 , A61K007/42
CPC分类号： A61Q17/04 , A61K8/40
摘要： The present invention relates to the use of at least one aryl oxime of Formula (I). 1 wherein: Y, Z represent independently from each other H, C1-18 alkyl, C2-18 alkenyl, C2-18 carboxy alkyl, C3-18 carboxy alkenyl or C2-18 alkanoyl; R represents C1-18 alkyl, C2-18 alkenyl, C3-8 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl or condensed systems; R1, R2, R3 and R4 represent independently from each other H, C1-12 alkyl, C2-12 alkenyl, C1-12 alkoxy, C3-8 cycloalkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, carboxy, hydroxy, chlorine, dialkyl amine or sulfonyl, for the prophylaxis and/or treatment of erythema formation and/or inflammation responses of the skin.
摘要翻译：本发明涉及式（I）的至少一种芳基肟的用途。其中：Y，Z彼此独立地表示H，C1-18烷基，C2-18烯基，C2-18羧基烷基，C3-18羧基烯基或C2-18烷酰基; R表示C1-18烷基，C2-18烯基，C3-8环烷基，芳基，芳烷基，杂芳基，杂芳烷基或稠合体系; R1，R2，R3和R4彼此独立地表示H，C1-12烷基，C2-12烯基，C1-12烷氧基，C3-8环烷氧基，芳基，芳氧基，芳烷基，杂芳基，杂芳烷基，羧基，羟基，氯，二烷基胺或磺酰基，用于预防和/或治疗皮肤的红斑形成和/或炎症反应。

5. 发明申请

US20020115617A1 Methods for the prevention and / or the treatment of glutamate cytotoxicity 有权
标题翻译：预防和/或治疗谷氨酸盐细胞毒性的方法
公开(公告)号：US20020115617A1
公开(公告)日：2002-08-22
申请号：US10051243
申请日：2002-01-22
发明人： Maurice Israel , Jordi Molgo , Christian Bloy , Cesar Mattei
IPC分类号： A61K031/704 , A61K031/175 , A61K031/15 , A61K031/16
CPC分类号： A61K31/12 , A61K31/175 , A61K31/70
摘要： The present invention relates to the use of beta-naphthoquinone derivatives, and salts thereof, for the prevention and/or the treatment of glutamate cytotoxicity. It further relates to the use of beta-naphthoquinone derivatives, and salts thereof, for preventing and/or treating glutamate induced neurological disorders. Additionally, it concerns the use of beta-naphthoguinone derivatives, and salts thereof, for making drugs exerting an inhibitory effect on the release of glutamate.
摘要翻译：本发明涉及β-萘醌衍生物及其盐在预防和/或治疗谷氨酸盐细胞毒性方面的用途。它还涉及β-萘醌衍生物及其盐在预防和/或治疗谷氨酸诱导的神经障碍中的用途。另外，它涉及使用β-萘醌酮衍生物及其盐来使药物对谷氨酸盐释放具有抑制作用。

6. 发明申请

US20040198716A1 Cysteine protease inhimbitors 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20040198716A1
公开(公告)日：2004-10-07
申请号：US10467105
申请日：2004-05-17
发明人： Dorit Arad , Arthur P Bollon , David C Young , Bradley W Poland , Andrew S Peek , Balin Shaw , Jyothi Vallurupalli
IPC分类号： A61K031/55 , A61K031/215 , A61K031/35 , A61K031/16 , A61K031/15
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。

7. 发明申请

US20030229146A1 Cyclopentenone derivatives for cancer therapy 失效
标题翻译：环戊烯酮衍生物用于癌症治疗
公开(公告)号：US20030229146A1
公开(公告)日：2003-12-11
申请号：US10309754
申请日：2002-12-04
申请人： DABUR RESEARCH FOUNDATION
发明人： Mukund K. Gurjar , Radhika D. Wakharkar , Gautam R. Desiraju , Ashwini Nangia , J. S. Yadav , Anand C. Burman , Rama Mukherjee , Hanumant Bapurao Borate , Srivari Chandrasekhar , Manu Jaggi , Anuo T. Singh , Kamal K. Kapoor , Sanjay Sarkhel , Kalapatapu V.V.M. Sairam
IPC分类号： A61K031/215 , A61K031/15 , A61K031/122 , C07C251/42 , C07C067/02
CPC分类号： C07C49/753 , C07C49/747 , C07C69/013 , C07C205/45 , C07C251/44 , C07C251/66 , C07C2601/10 , C07F7/1804
摘要： The invention relates to the use of derivatives of cyclopentenone for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of derivatives of cyclopentenone for the inhibition and/or prevention of cancer of the colon, pancreas, larynx, ovary, duodenum, kidney, oral cavity, prostate, lung, endothelial cells and leukemias
摘要翻译：本发明涉及环戊烯酮衍生物用于抑制或预防癌细胞生长或增殖的用途，以及含有这些化合物的治疗组合物的用途。本发明更具体地涉及环戊烯酮衍生物在结肠，胰腺，喉，卵巢，十二指肠，肾，口腔，前列腺，肺，内皮细胞和白血病的抑制和/或预防中的用途

8. 发明申请

US20030176470A1 Topical composition containing at least one aryl oxime, and method for the preparation thereof 审中-公开
标题翻译：含有至少一种芳基肟的局部组合物及其制备方法
公开(公告)号：US20030176470A1
公开(公告)日：2003-09-18
申请号：US10296173
申请日：2002-11-22
发明人： Joachim Bunger , Jutta zur Lage , Michael Schwarz
IPC分类号： A61K031/44 , A61K031/40 , A61K031/15 , A61K031/22
CPC分类号： A61K8/375 , A61K8/39 , A61K8/40 , A61Q19/00
摘要： The present invention relates to a topical composition, comprising (c) at least one aryl oxime of the Formula (I) and (d) at least one emulsifier, 1 wherein: Y, Z represent independently from each other H, C1-18 alkyl, C2-18 alkenyl, C2-18 carboxy alkyl, C3-18 carboxy alkenyl or C2-18 alkanoyl; R represents C1-18 alkyl, C2-18 alkenyl, C3-8 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl or condensed systems; R1, R2, R3 and R4 represent independently from each other H, C1-12 alkyl, C2-12 alkenyl, C1-12 alkoxy, C3-8 cycloalkoxy, aryl, aryloxy, aralkyl, heteroaryl, heteroaralkyl, carboxy, hydroxy, chlorine, dialkyl amine or sulfonyl, wherein the component (b) is selected from the group consisting of an ester, the carboxylic acid residue of which is derived from C5-C16 acids and the hydroxyl residue of which is derived from monomers, dimers or trimers of lactic acid or one of its salts or a polyglycerin of 2 to 10 molecules of glycerin whereby 1 to 3 moles of carboxylic acid are present per mole of polyglycerin. Furthermore, the present invention relates to a process for the preparation of said topical composition as well as the use of said topical composition.
摘要翻译：本发明涉及局部组合物，其包含（c）至少一种式（I）和（d）的芳基肟至少一种乳化剂，其中：Y，Z彼此独立地表示H，C 1-18烷基， C2-18烯基，C2-18羧基烷基，C3-18羧基烯基或C2-18烷酰基; R表示C1-18烷基，C2-18烯基，C3-8环烷基，芳基，芳烷基，杂芳基，杂芳烷基或稠合体系; R1，R2，R3和R4彼此独立地表示H，C1-12烷基，C2-12烯基，C1-12烷氧基，C3-8环烷氧基，芳基，芳氧基，芳烷基，杂芳基，杂芳烷基，羧基，羟基，氯，二烷基胺或磺酰基，其中组分（b）选自酯，其羧酸残基衍生自C5-C16酸，其羟基残基衍生自乳酸的单体，二聚体或三聚体酸或其一种盐或2至10分子甘油的聚甘油，其中每摩尔聚甘油存在1至3摩尔羧酸。此外，本发明涉及制备所述局部组合物的方法以及所述局部组合物的用途。

9. 发明申请

US20030083357A1 Oxime derivatives for the treatment of dyslipidemia and hypercholesteremia 审中-公开
标题翻译：肟衍生物用于治疗血脂异常和高胆固醇血症
公开(公告)号：US20030083357A1
公开(公告)日：2003-05-01
申请号：US10224288
申请日：2002-08-19
发明人： Magnus Pfahl , Catherine Tachdjian , Hussien A. Al-Shamma
IPC分类号： C07D213/54 , A61K031/44 , A61K031/40 , A61K031/15 , A61K031/165
CPC分类号： C07D213/64 , C07C251/48 , C07C2602/10 , C07D213/48 , C07D213/74 , C07D215/227 , C07D241/42 , C07D241/44 , C07D307/79 , C07D317/58
摘要： The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
摘要翻译：本发明涉及式（I）化合物，其可用于治疗疾病，例如代谢紊乱，血脂异常和/或高舒适心律失常：

10. 发明申请

US20030083326A1 Dihydroxyphenyl derivatives for hepatoprotection and treatment of liver diseases 失效
标题翻译：用于肝保护和治疗肝脏疾病的二羟基苯基衍生物
公开(公告)号：US20030083326A1
公开(公告)日：2003-05-01
申请号：US10114007
申请日：2002-04-01
申请人： Choongwae Pharm. Co., Ltd.
发明人： Sung-Hwan Moon , Hea-Jin Choi , Su-Jin Lee , Jea-Uk Chung , Jong-Ryul Ha , Kwang-Won Jeong , Se-Woong Oh
IPC分类号： A61K031/54 , A61K031/445 , A61K031/426 , A61K031/4025 , A61K031/15
CPC分类号： A61K31/445 , A61K31/15 , A61K31/4025 , A61K31/426 , A61K31/54
摘要： The present invention relates to a pharmaceutical composition for the hepatoprotection and treatment of liver diseases comprising as an active ingredient a dihydroxyphenyl derivative represented by the following formula (1), pharmaceutically acceptable acid addition salt or stereochemical isomer thereof together with a pharmaceutically acceptable inert carrier: 1 in which in which A, B, D and E are defined as described in the specification.
摘要翻译：本发明涉及肝保护和治疗肝病的药物组合物，其包含作为活性成分的由下式（1）表示的二羟基苯基衍生物，其药学上可接受的酸加成盐或其立体化学异构体以及药学上可接受的惰性载体：其中A，B，D和E的定义如说明书中所述。

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