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1. 发明授权

US4440903A Dihaloisocyanide derivatives of polymers for coupling nucleophiles 失效
标题翻译：用于偶联亲核体的聚合物的二卤代吖啶衍生物
公开(公告)号：US4440903A
公开(公告)日：1984-04-03
申请号：US921055
申请日：1978-06-30
申请人： Leon Golstein , Mordechai Sokolovsky , Amihay Freeman
发明人： Leon Golstein , Mordechai Sokolovsky , Amihay Freeman
IPC分类号： C08G12/40 , C08G63/685 , C08G63/91 , C08G85/00 , C12N11/08 , C07C143/00 , C07G7/00 , C12N11/06
CPC分类号： C08G63/91 , C08G12/40 , C08G63/685 , C08G85/004 , C12N11/08 , Y10S525/921
摘要： The present invention relates to novel key intermediates for the production of biologically active compounds coupled to polymers, of the general formula P--NCX.sub.2, wherein X designates a halogen atom selected from chlorine and bromine, and wherein P designates the polymer backbone of a polymer of the polyamide, polyester and ureaformaldehyde type. The invention further relates to compounds obtained by the reaction of the above compound P--NCX.sub.2 with a bifunctional or polyfunctional nucleophile. Suitable nucleophiles are hydrazides of dicarboxylic acids and amongst these there may be mentioned polyacrylamides partially substituted with acylhydrazide groups; polyfunctional amines selected from alkylamines, aralkylamines, arylamines and macromolecular compounds containing amino groups. The key intermediate PNCX.sub.2 may be coupled directly to biologically active macromolecules and amongst the preferred compounds of this type there are the various biologically active proteins and enzymes. The coupling of the biologically active macromolecules may also be effected via hydrophilic polymer moieties first grafted onto the polymer P via said dihaloisocyanide groups.
摘要翻译：本发明涉及用于生产与通式为P-NCX2的聚合物偶联的生物活性化合物的新型关键中间体，其中X表示选自氯和溴的卤素原子，其中P表示聚合物的聚合物主链聚酰胺，聚酯和脲甲醛型。本发明还涉及通过上述化合物P-NCX2与双官能或多官能亲核试剂的反应获得的化合物。合适的亲核试剂是二羧酸的酰肼，其中可以提及部分被酰基酰肼基团取代的聚丙烯酰胺; 选自烷基胺，芳烷基胺，芳基胺和含有氨基的高分子化合物的多官能胺。关键的中间体PNCX2可以直接与生物活性大分子偶联，并且在这种类型的优选化合物中存在各种生物活性蛋白质和酶。生物活性大分子的偶联也可以通过首先通过所述二卤代吖啶基接枝到聚合物P上的亲水性聚合物部分来实现。

2. 发明授权

US3970597A Novel substituted polyamides and process for producing them 失效
标题翻译：新型取代聚酰胺及其制备方法
公开(公告)号：US3970597A
公开(公告)日：1976-07-20
申请号：US476320
申请日：1974-06-04
申请人： Mordechai Sokolovsky , Amihay Freeman , Leon Goldstein
发明人： Mordechai Sokolovsky , Amihay Freeman , Leon Goldstein
IPC分类号： C08G69/48 , C08G69/50 , C08G18/00
CPC分类号： C08G69/48
摘要： Novel substituted polyamides of the general formula ##EQU1## wherein A and B, which may be identical or different, are the hydrocarbon backbone groups of the formula --(CH.sub.2).sub.n --, where n is an integer, R.sub.2 and R.sub.3 are the residues of an aldehyde R.sub.2 --CHO or of an isocyanide R.sub.3 --N.tbd.C, where R.sub.2 and R.sub.3 are aliphatic, aromatic or heterocyclic residues of the respective aldehyde or isocyanide, or where R.sub.3 is a chromophoric moiety. R.sub.2 and R.sub.3 can be substituted, and amongst the possible substituents there may be R.sub.3 designating --(CH.sub.2).sub.n --NHCO--CHR.sub.2 --N(CO)(R.sub.4)--X, where R.sub.4 is the residue of a monocarboxylic or dicarboxylic acid and X is the lysyl residue of a protein, which may be biologically active, or the residue of a low-molecular weight compound containing a primary amine moiety. Preferred polyamides are various types of nylons. Amongst proteins chemically bound to the polyamide there may be mentioned enzymes, antibodies and peptide hormones. When R.sub.3 is a chromophoric moiety, the product is a chemically dyed polyamide. The invention relates also to a process for the production of such novel substituted polyamides.
摘要翻译：通式-CONH-A-CONH-B-CO-NA-CONH-B-CONH-A- | CH-R2 | CO-NH-R3的新型取代聚酰胺其中A和B可以相同或不同，是式 - （CH 2）n - 的烃主链基团，其中n是整数，R 2和R 3是醛R 2 -CHO或异氰酸酯R 3 -N N BOND C的残基，其中R 2和R 3是脂族基，相应醛或异氰化物的芳族或杂环残基，或其中R3是发色部分。 R2和R3可以被取代，并且在可能的取代基中可以有R3表示 - （CH 2）n -NHCO-CHR 2 -N（CO）（R 4）-X，其中R 4是一元羧酸或二羧酸的残基，X 是可能是生物活性的蛋白质的赖氨酰残基，或含有伯胺部分的低分子量化合物的残基。优选的聚酰胺是各种类型的尼龙。与聚酰胺化学结合的蛋白质中，可以提及酶，抗体和肽激素。当R3是发色部分时，产物是化学染色的聚酰胺。本发明还涉及生产这种新型取代的聚酰胺的方法。

3. 发明授权

US4303786A Isonitrile derivatives of macromolecules containing hydroxyl groups 失效
标题翻译：含有羟基的大分子的异腈衍生物
公开(公告)号：US4303786A
公开(公告)日：1981-12-01
申请号：US929229
申请日：1978-07-31
申请人： Leon Goldstein , Amihay Freeman , Mordechai Sokolovsky
发明人： Leon Goldstein , Amihay Freeman , Mordechai Sokolovsky
IPC分类号： C08B15/06 , C08B37/00 , C12N11/08 , C12N11/10 , C08B37/02 , C08B11/155 , C08B31/08
CPC分类号： C08B37/00 , C08B15/06 , C12N11/08 , C12N11/10
摘要： The present invention relates to novel isocyano derivatives of linear or cross-linked, natural or synthetic macromolecules, the derivatives being of the general formula P--O--Q--NC, wherein P is the macromolecular backbone, the oxygen atom is part of the hydroxy group, Q is a group --(CH.sub.2).sub.n --wherein n is an integer of at least 3 carbon atoms, and up to about 20 carbon atoms, or Q is an aralkyl group, to a process for preparing such derivatives and to a process of linking to same biologically active proteins and to the products thus obtained.
摘要翻译：本发明涉及线型或交联天然或合成大分子的新型异氰酸衍生物，其衍生物为通式POQ-NC，其中P为高分子主链，氧原子为羟基的一部分，Q为一个 - （CH 2）n - ，其中n是至少3个碳原子的整数，以及至多约20个碳原子，或Q是一个芳烷基，用于制备这种衍生物的方法和连接到其上的方法生物活性蛋白质和由此获得的产物。

4. 发明授权

US5284867A NMDA-blocking pharmaceutical compositions 失效
标题翻译： NMDA阻断药物组合物
公开(公告)号：US5284867A
公开(公告)日：1994-02-08
申请号：US865088
申请日：1992-04-08
申请人： Yoel Kloog , Jeffrey J. Feigenbaum , Raphael Mechoulam , Mordechai Sokolovsky , Simon Benita
发明人： Yoel Kloog , Jeffrey J. Feigenbaum , Raphael Mechoulam , Mordechai Sokolovsky , Simon Benita
IPC分类号： A61K31/35 , C07D311/80 , C07D405/06
CPC分类号： A61K31/35 , C07D311/80 , C07D405/06
摘要： The use of a compound of the formula: ##STR1## having the (3S,4S) configuration, and which is essentially free of the (3R,4R) enantiomer, wherein A--B designates a 1(2) or a 6(1) double bond, R designates --CH.sub.3 or --CH.sub.2 OH, R.sup.1 designates a hydrogen atom or a lower acyl group, and R.sup.2 designates (A) a straight-chained or branched C.sub.6-12 alkyl radical; or (B) a group --O--R.sup.3, in which R.sup.3 is a straight-chained or branched C.sub.5-9 alkyl radical or a straight-chained or branched alkyl radical substituted at the terminal carbon atom by a phenyl group in the manufacture of a medicament for reducing or preventing glutamate neurotoxicity. Some of the above compounds are novel, and their preparation is described. Also described is a method of treating acute injuries to the central nervous system associated with excitatory amino acid neurotoxicity, a method of treating chronic degenerative disease associated with gradual selective neuronal loss and a method of treating poisonings affecting the central nervous system by administering a pharmaceutical composition containing the above compound.
摘要翻译：使用具有（3S，4S）构型的下式的化合物：（IMA），其基本上不含（3R，4R）对映体，其中AB表示1（2）或6（ 1）双键，R表示-CH 3或-CH 2 OH，R 1表示氢原子或低级酰基，R 2表示（A）直链或支链C 6-12烷基; 或（B）基团-O-R3，其中R3是直链或支链的C5-9烷基或在末端碳原子被苯基取代的直链或支链烷基，用于减少或预防谷氨酸神经毒性的药物。上述化合物中的一些是新颖的，并且描述了它们的制备方法。还描述了治疗与兴奋性氨基酸神经毒性相关的中枢神经系统的急性损伤的方法，治疗与逐渐选择性神经元丧失相关的慢性退行性疾病的方法和通过施用药物组合物治疗影响中枢神经系统的中毒的方法含有上述化合物。

5. 发明授权

US4994446A Drug system 失效
标题翻译：药物系统
公开(公告)号：US4994446A
公开(公告)日：1991-02-19
申请号：US293136
申请日：1989-01-03
申请人： Mordechai Sokolovsky , Yoel Kloog
发明人： Mordechai Sokolovsky , Yoel Kloog
IPC分类号： A61K31/66
CPC分类号： A61K31/66
摘要： The invention relates to a drug system for the treatment and alleviation of the symptoms of epilepsy; as anticonvulsant agent, and for the prevention or alleviation of brain damage due to strokes. The drug system comprises as active ingredient a compound such as MK-801, phencyclidine or as thienyl-cyclohexyl-piperidine (TCP), which is administered in such a manner that it encounters and binds to the N-methyl-D-aspartate (NMDA) receptor channels. This is in the presence of glutamate or glycine, or similarly acting amino-acid, which is either present in the patient, or which can be administered separately. The effective drug can be effectively locked in the receptor channels by means of a glutamate antagonist, such as AP-5.
摘要翻译：本发明涉及用于治疗和缓解癫痫症状的药物系统; 作为抗惊厥剂，并用于预防或减轻由于中风引起的脑损伤。药物系统包含作为活性成分的化合物如MK-801，苯环利定或噻吩基 - 环己基 - 哌啶（TCP），其以这样的方式施用，即其遇到并结合N-甲基-D-天冬氨酸（NMDA ）受体通道。这是存在谷氨酸或甘氨酸或类似作用的氨基酸，其存在于患者体内，或可分开施用。有效药物可以通过谷氨酸拮抗剂如AP-5有效地锁定在受体通道中。

6. 发明授权

US6096740A Dexanabinol derivatives and their use as neuroprotective pharmaceutical compositions 失效
标题翻译：德西那诺衍生物及其作为神经保护药物组合物的用途
公开(公告)号：US6096740A
公开(公告)日：2000-08-01
申请号：US11814
申请日：1998-09-28
申请人： Raphael Mechoulam , Emil Pop , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
发明人： Raphael Mechoulam , Emil Pop , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
IPC分类号： C07D311/80 , C07D405/06 , A61K31/352 , A61K31/496 , C07D295/037 , C07D453/04
CPC分类号： C07D405/06 , C07D311/80
摘要： The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow. ##STR1##
摘要翻译： PCT No.PCT / US95 / 01470 Sec。 371日期：1998年9月28日 102（e）1998年9月28日PCT提交1995年2月6日PCT公布。出版物WO95 / 20958 日期：1995年8月10日本发明涉及用于预防或减轻神经毒性的药物组合物。所述药物组合物包含具有（3S，4S）构型的如下文所定义的通式（I）的DELTA 6-四氢大麻酚（THC）型化合物的立体有择（+）对映异构体作为其活性成分。

7. 发明授权

US5521215A NMDA-blocking pharmaceuticals 失效
标题翻译： NMDA阻断药物
公开(公告)号：US5521215A
公开(公告)日：1996-05-28
申请号：US192886
申请日：1994-02-07
申请人： Raphael Mechoulam , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
发明人： Raphael Mechoulam , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
IPC分类号： A61K31/35 , A61K31/352 , A61P25/00 , A61P25/08 , C07D311/80 , C07D405/04 , C07D405/06 , C07D405/12
CPC分类号： C07D405/06 , A61K31/35 , C07D311/80
摘要： Pharmaceutical compositions are described for preventing neurotoxicity, crising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of .DELTA..sup.6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain chronic degenerative diseases characterized by gradual neuronal loss.
摘要翻译：描述了用于预防神经毒性的药物组合物，其包含具有（3S，4S）构型的DELTA 6四氢大麻酚型化合物的立体特异性（+）对映异构体作为活性成分。组合物特别有效地减轻甚至预防由于中枢神经系统的急性损伤引起的神经毒性，包括机械创伤，心脏骤停或中风或中毒可能发生的受损或减少的血液供应。它们也有效治疗某些以逐渐神经元损失为特征的慢性退行性疾病。

8. 发明授权

US3997543A Process for preparing quinuclidine enantiomers 失效
标题翻译：制备奎宁环对映异构体的方法
公开(公告)号：US3997543A
公开(公告)日：1976-12-14
申请号：US569282
申请日：1975-04-18
申请人： Mordechai Sokolovsky , Moshe Rehavi , Saul Maayani
发明人： Mordechai Sokolovsky , Moshe Rehavi , Saul Maayani
IPC分类号： C07D453/02 , C12P17/18 , C12P41/00 , C07D211/42
CPC分类号： C07D453/02 , C12P17/182 , C12P41/004
摘要： A new composition of matter, (+) 3-acetoxy- quinuclidine and its salts, ophthalmic compositions comprising this compound or any of its physiologically acceptable salts in a suitable carrier such as a phosphate buffer, and a process of preparation of the active ingredients, which comprises esterifying quinuclidinol so as to obtain racemic 3-lower-alkoxy quinuclidine, subjecting same to enzymatic hydrolysis by a cholinesterase so as to selectively hydrolyze the (-) isomer, separating the unchanged (+) lower-alkoxy quinuclidine, hydrolyzing the latter and esterifying it to the desired compound. Amongst various homolophes the preferred compound is (+)3-acetoxy quinuclidine as this is pharmaceutically the most potent one.
摘要翻译：一种新的物质组合物，（+）3-乙酰氧基 - 奎宁环及其盐，在合适的载体如磷酸盐缓冲液中包含该化合物或其任何生理学上可接受的盐的眼用组合物，以及制备活性成分的方法，其包括酯化奎宁环醇以获得外消旋的3-低级烷氧基奎宁环，通过胆碱酯酶进行酶水解，从而选择性地水解（ - ）异构体，分离未改变的（+）低级烷氧基奎宁环，水解后者和将其酯化成所需化合物。在各种均聚物中，优选的化合物是（+）3-乙酰氧基奎宁环，因为这是药物中最有效的。

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