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31. 发明申请

WO1995023158A1 TRANSGENIC ANIMAL ASSAY SYSTEM FOR ANTI-CHOLINESTERASE SUBSTANCES 审中-公开
标题翻译：用于抗胆碱酯酶物质的转基因动物测定系统
公开(公告)号：WO1995023158A1
公开(公告)日：1995-08-31
申请号：PCT/US1995002806
申请日：1995-02-28
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KOHN, Kenneth, I.
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KOHN, Kenneth, I. , SOREQ, Hermona , ZAKUT, Haim , SHANI, Moshe
IPC分类号： C07H17/00
CPC分类号： C12N15/8509 , A01K67/0278 , A01K2207/15 , A01K2217/00 , A01K2217/05 , A01K2217/072 , A01K2227/105 , A01K2227/50 , A01K2267/03 , A01K2267/0356 , C12N9/18 , C12Q1/46
摘要： The present invention relates to novel alternative forms of human acetylcholinesterase (AChE) and nucleotide sequences encoding the same. The genes encoding the novel forms of human AChE have been identified in various malignant tumor cells. In a further aspect, the invention relates to a transgenic animal assay system for evaluating efficacy of drugs against cholinergic proteins, prior to or in the course of therapeutic treatment. Transgenic animals, preferably developing tadpole of Xenopus or mice which express human AChE, are used. The transgenic animal assay system is also useful for evaluating the toxicity of substances which potentially block human AChE (e.g. organophosphorous compounds).
摘要翻译：本发明涉及人乙酰胆碱酯酶（AChE）的新型替代形式及其编码的核苷酸序列。已经在各种恶性肿瘤细胞中鉴定了编码人类AChE的新型形式的基因。在另一方面，本发明涉及用于在治疗治疗之前或治疗过程中评价药物对胆碱能蛋白的功效的转基因动物测定系统。使用转基因动物，优选发育表达人AChE的非洲爪蟾的t us或小鼠。转基因动物测定系统也可用于评估潜在阻断人类AChE（例如有机磷化合物）的物质的毒性。

32. 发明申请

WO1995019169A2 TREATMENT OF PLATELET DERIVED GROWTH FACTOR RELATED DISORDERS SUCH AS CANCERS USING INHIBITORS OF PLATELET DERIVED GROWTH RECEPTOR 审中-公开
标题翻译：治疗板片衍生生长因子相关疾病如使用平板衍生生长受体的抑制剂
公开(公告)号：WO1995019169A2
公开(公告)日：1995-07-20
申请号：PCT/US1995000363
申请日：1995-01-06
申请人： SUGEN, INC. , BIOSIGNAL LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V. , REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： SUGEN, INC. , BIOSIGNAL LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V. , REGENTS OF THE UNIVERSITY OF CALIFORNIA , HIRTH, Klaus, Peter , SCHWARTZ, Donna, Pruess , MANN, Elaina , SHAWVER, Laura, Kay , KERI, Gyorgy , SZEKELY, Istvan , BAJOR, Tamas , HAIMICHAEL, Janis , ORFI, Laszlo , LEVITZKI, Alex , GAZIT, Aviv , ULLRICH, Axel , LAMMERS, Reiner , KABBINAVAR, Fairooz, F. , SLAMON, Dennis, J. , TANG, Cho, Peng
IPC分类号： A61K31/42
CPC分类号： C07D231/38 , A61K9/0019 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K31/70 , A61K33/24 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity of other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see Figure 1A), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。以下描述特征化合物A10（参见图1A）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

33. 发明申请

WO1995014464A1 SSI TYRPHOSTINS AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： SSI TYRPHOSTINS和药物组合物
公开(公告)号：WO1995014464A1
公开(公告)日：1995-06-01
申请号：PCT/US1994013535
申请日：1994-11-23
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KUPOT-HOLIM HEALTH INSURANCE INSTITUTE OF THE GENERAL FEDERATION OF LABOUR IN ERETZ-ISRAEL , LEVITZKI, Alexander , NOVOGRODSKY, Abraham , GAZIT, Aviv
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KUPOT-HOLIM HEALTH INSURANCE INSTITUTE OF THE GENERAL FEDERATION OF LABOUR IN ERETZ-ISRAEL
IPC分类号： A61K31/165
CPC分类号： A61K31/275
摘要： SSI thyrphostins are useful in preventing LPS induced toxicity, TNF alpha induced toxicity, LPS induced increases in TNF alpha levels, nitric oxide production, and the treatment of septic shock and various immune disorders. Featured are novel compounds and pharmaceutical compositions, both of which may be used in the methods of prevention and/or treatment described herein, as well as methods for making the novel compounds.
摘要翻译： SSI thyrphostins可用于预防LPS诱导的毒性，TNFα诱导的毒性，LPS诱导的TNFα水平升高，一氧化氮产生以及脓毒性休克和各种免疫疾病的治疗。特征是新颖的化合物和药物组合物，它们都可用于本文所述的预防和/或治疗方法，以及制备新化合物的方法。

34. 发明申请

WO1995012384A1 SELF-EMULSIBLE FORMULATION FORMING AN OIL-IN-WATER EMULSION 审中-公开
标题翻译：自制可塑性成型水性乳液
公开(公告)号：WO1995012384A1
公开(公告)日：1995-05-11
申请号：PCT/FR1994001239
申请日：1994-10-25
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , BENITA, Simon , KLEINSTERN, Jackie , GERSHANIK, Tatyana
IPC分类号： A61K09/107
CPC分类号： A61K9/1075
摘要： The self-emulsible oil formulation (SEOF) contains an oil component and a surfactant. The SEOF is characterized in that the oil component contains an oil vector and a cationic lipid and, optionally, a lipophilic oily fatty alcohol. The oil-in-water emulsion which is formed by the mixing of the SEOF has oily droplets which are positively charged.
摘要翻译：自乳油配方（SEOF）含有油组分和表面活性剂。 SEOF的特征在于油组分含有油载体和阳离子脂质，以及任选的亲油性油性脂肪醇。通过混合SEOF形成的水包油乳液具有带正电荷的油滴。

35. 发明申请

WO1995001956A1 DERIVATIVES OF VALPROIC AND 2-VALPROENOIC ACID AMIDES AND USE AS ANTICONVULSANTS 审中-公开
标题翻译：戊二酸和二恶唑酸的衍生物和用作抗生素
公开(公告)号：WO1995001956A1
公开(公告)日：1995-01-19
申请号：PCT/US1994007498
申请日：1994-07-06
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , TEVA PHARMACEUTICAL INDUSTRIE, LTD. , BIALER, Meir , HADAD, Salim , HERZIG, Jacob , STERLING, Jeff , LERNER, David , SHIRVAN, Mitchell
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , TEVA PHARMACEUTICAL INDUSTRIE, LTD.
IPC分类号： C07C237/12
CPC分类号： C07C233/49 , C07C233/47 , C07C237/22 , C07C255/29
摘要： A compound having structure (I), wherein A is X or Y, X is (a), Y is (b); R1, R2, R3, R4 and R5 are each independently hydrogen, a C1-C6 alkyl group, an aralkyl group, or an aryl group; and n is 0, 1, 2, or 3. Also provided are a compound containing a 2-valproenoic moiety, pharmaceutical compositions comprising these compounds, and methods of using them for the effective treatment of epilepsy and other neurological disorders.
摘要翻译：具有结构（I）的化合物，其中A是X或Y，X是（a），Y是（b）; R1，R2，R3，R4和R5各自独立地为氢，C1-C6烷基，芳烷基或芳基; 并且n为0,1,2或3.还提供含有2-戊烯基部分的化合物，包含这些化合物的药物组合物，及其用于有效治疗癫痫和其它神经障碍的方法。

36. 发明申请

WO1998029444A1 BROAD SPECTRUM PYROGENIC EXOTOXINS ANTAGONISTS AND VACCINES 审中-公开
标题翻译：广谱光谱外源毒素拮抗剂和疫苗
公开(公告)号：WO1998029444A1
公开(公告)日：1998-07-09
申请号：PCT/IL1997000438
申请日：1997-12-30
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KAEMPFER, Raymond , ARAD, Gila
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
IPC分类号： C07K14/31
CPC分类号： C07K14/31 , A61K39/00 , G01N33/56938 , G01N33/56944
摘要： The invention relates to peptides comprising an amino acid sequence substantially homologous to the amino sequence of a fragment of a pyrogenic exotoxin, and functional derivatives of said peptides, capable of eliciting protective immunity against toxic shock induced by a pyrogenic exotoxin or by a mixture of pyrogenic exotoxins. Preferred peptides comprise an amino acid sequence substantially homologous to the amino sequence of a fragment of Staphylococcal aureus enterotoxin B (SEB). The invention also relates to broad spectrum pharmaceutical compositions for the treatment or short term prophylaxis of toxin-mediated activation of T cells, comprising as active ingredient at least one peptide according to the invention or derivative thereof, and to broad spectrum vaccines for conferring long term immunity against toxic shock induced by at least one pyrogenic exotoxin are provided. The vaccines comprising as active ingredient at least one peptide according to the invention, or derivative thereof.
摘要翻译：本发明涉及包含与热原性外毒素片段的氨基序列基本上同源的氨基酸序列的氨基酸序列和所述肽的功能衍生物的肽，其能够引起针对由致热原外毒素引起的毒性休克的保护性免疫，或由热原性外毒素混合物外毒素。优选的肽包含与金黄色葡萄球菌肠毒素B（SEB）的片段的氨基序列基本同源的氨基酸序列。本发明还涉及用于治疗或短期预防毒素介导的T细胞活化的广谱药物组合物，其包含作为活性成分的至少一种根据本发明的肽或其衍生物，以及用于赋予长期的广谱疫苗提供了由至少一种致热外毒素引起的毒性休克的免疫力。包含至少一种根据本发明的肽或其衍生物作为活性成分的疫苗。

37. 发明申请

WO1998027055A1 AMINOINDAN DERIVATIVES 审中-公开
标题翻译：氨基衍生物
公开(公告)号：WO1998027055A1
公开(公告)日：1998-06-25
申请号：PCT/US1997024155
申请日：1997-12-18
申请人： TEVA PHARMACEUTICAL INDUSTRIES, LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. , CHOREV, Michael , GOREN, Tamar , HERZIG, Yacov , STERLING, Jeffrey , WEINSTOCK-ROSIN, Marta , YOUDIM, Moussa, B., H.
发明人： TEVA PHARMACEUTICAL INDUSTRIES, LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD.
IPC分类号： C07C271/42
CPC分类号： C07C271/56 , C07C271/24 , C07C271/44 , C07C271/58 , C07C333/04 , C07C2601/14 , C07C2602/08 , C07C2602/10
摘要： This invention is directed to compounds of formula (I) wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen or C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementias such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及式（I）的化合物，其中当a为0时，b为1或2; 当a为1时，b为1，m为0-3，X为O或S，Y为卤素，R1为氢或C1-4烷基，R2为氢，C1-4烷基或任选取代的炔丙基，R3为和R 4各自独立地为氢，C 1-8烷基，C 6-12芳基，各自任选取代的C 6-12芳烷基。本发明还涉及这些化合物用于治疗抑郁症，注意力缺陷障碍（ADD），注意力缺陷和多动症（ADHD），图雷特氏综合征，阿尔茨海默病和其他痴呆症如老年性痴呆，帕金森氏型痴呆，血管性痴呆和路易体痴呆。本发明进一步涉及包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

38. 发明申请

WO1998022091A1 PHARMACEUTICAL PREPARATIONS FOR THE CONTROLLED RELEASE OF 'beta'-LACTAM ANTIBIOTICS 审中-公开
标题翻译：用于控制释放β-LACTAM抗生素的药物制剂
公开(公告)号：WO1998022091A1
公开(公告)日：1998-05-28
申请号：PCT/IL1997000368
申请日：1997-11-13
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , KATZHENDLER, Ifat , HOFFMAN, Amnon , FRIEDMAN, Michael
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
IPC分类号： A61K09/10
CPC分类号： A61K31/545 , A61K9/2027 , A61K9/205 , A61K9/2054 , A61K31/43 , A61K2300/00
摘要： The present invention relates to a pharmaceutical controlled-release oral drug delivery system comprising as active ingredient at least one beta -lactam antibiotic agent, having a specific absorption site in the small intestine in combination with a polymeric matrix, optionally further containing additional pharmaceutically acceptable constituents, wherein at least 50 % of the beta -lactam antibiotic agent are released from the matrix within from about 3 to about 4 hours from oral administration and the remainder of the pharmaceutical agent is released at a controlled rate. The drug delivery system according to the invention optionally further comprises a beta -lactamase inhibitor, preferably in combination with amoxicillin and/or amoxicillin trihydrate as the active ingredient. The polymeric matrix of the pharmaceutical controlled-release oral drug delivery system of the invention may be of hydrophilic and/or hydrophobic nature and the delivery system may further comprise pharmaceutically acceptable additive. The pharmaceutical controlled-release oral drug delivery system of the invention is preferably in dosage unit form.
摘要翻译：本发明涉及药物控释口服药物递送系统，其包含至少一种β-内酰胺抗生素作为活性成分，其在小肠中具有与聚合物基质组合的特异性吸收部位，任选地还含有另外的药学上可接受的成分，其中至少50％的β-内酰胺抗生素试剂在口服给药约3至约4小时内从基质释放，并且药物的其余部分以受控的速率释放。根据本发明的药物递送系统任选地还包含β-内酰胺酶抑制剂，优选与阿莫西林和/或阿莫西林三水合物作为活性成分组合。本发明的药物控释口服药物递送系统的聚合物基质可具有亲水性和/或疏水性质，并且递送系统还可包含药学上可接受的添加剂。本发明的药物控释口服药物递送系统优选为剂量单位形式。

39. 发明申请

WO1998008380A1 SLOW RELEASE FORMULATIONS OF PESTICIDES 审中-公开
标题翻译：农药缓释配方
公开(公告)号：WO1998008380A1
公开(公告)日：1998-03-05
申请号：PCT/IL1997000277
申请日：1997-08-18
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MARGULIES, Gulia +hf , RUBIN, Baruch , EL-NAHHAL, Yasser , NIR, Shlomo
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , MARGULIES, Gulia +hf , MARGULIES, Leon +di
IPC分类号： A01N25/08
CPC分类号： A01N25/08
摘要： Slow-Release agrochemical formulations for the prevention of leaching and contamination of soil and ground water. The agrochemicals are organic compounds with non-ionic and non-polar molecular structures, which are adsorbed to clays whose surface properties have been transformed from hydrophilic to organophilic by previous adsorption of an organic cation, usually of quaternary ammonium structure, having at least one benzyl group attached to the ammonium nitrogen atom. The intermolecular interactions on the clay surface result in a reduction of the solubility in water of the agrochemical, preventing its leaching in the field.
摘要翻译：缓释农药配方，防止土壤和地下水的浸出和污染。农业化学品是具有非离子和非极性分子结构的有机化合物，其被吸附到粘土上，其粘土通过先前吸附有机阳离子（通常为季铵结构）而具有至少一个苄基基团连接到铵氮原子上。粘土表面上的分子间相互作用导致农药在水中的溶解度降低，防止其在现场的浸出。

40. 发明申请

WO1998006391A1 PHARMACEUTICAL COMPOSITIONS COMPRISING TYRPHOSTINS 审中-公开
标题翻译：包含TYRPHOSTINS的药物组合物
公开(公告)号：WO1998006391A1
公开(公告)日：1998-02-19
申请号：PCT/IL1997000276
申请日：1997-08-14
申请人： MOR-RESEARCH APPLICATIONS LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , NOVOGRODSKY, Abraham , LEVITZKI, Alexander , GAZIT, Aviv
发明人： MOR-RESEARCH APPLICATIONS LTD. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
IPC分类号： A61K31/275
CPC分类号： A61K31/415 , A61K31/277 , A61K31/427 , A61K31/4406
摘要： Compounds useful for countering undesired toxic effects to cells, tissues or organs having formula (I) wherein: Ar is a group of formulae (i) or (ii), n is O or, when Ar has formula (i) above, then n may also be 1, R is CN, -C(S)NH2, -C(O)NHR3 or, when R1 is 4-NO2 and R2 is H or 3-OH, then R may also be a group of formulae (iii), (iv), (v), (vi) where R3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl; R1 and R2 are each independently H, OH, NO2 or, when R is CN, also CH3, F, or CF3, provided that both R1 and R2 are not simultaneously H.
摘要翻译：用于对抗具有式（I）的细胞，组织或器官的不期望的毒性作用的化合物，其中：Ar是式（i）或（ii）的基团，n是O或当Ar具有上述式（i）时，则n 也可以是1，R是CN，-C（S）NH 2，-C（O）NHR 3，或者当R 1是4-NO 2且R 2是H或3-OH时，R也可以是式），（iv），（v），（vi）其中R3是H，苯基，苯基（低级烷基）或吡啶基甲基; R 1和R 2各自独立地为H，OH，NO 2，或当R为CN时，R 3，F或CF 3，只要R 1和R 2不同时为H.

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