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1. 发明授权

US5252558A Pentapeptide having specific inhibiting effect on epidermal cell proliferation, the salts thereof, pharmaceutical compositions comprising the same and a process for the preparation of the pentapeptide and the pharmaceutical compositions 失效
标题翻译：对表皮细胞增殖具有特异性抑制作用的五肽，其盐，包含其的药物组合物和制备五肽和药物组合物的方法
公开(公告)号：US5252558A
公开(公告)日：1993-10-12
申请号：US750330
申请日：1991-08-27
申请人： Andras Balazs , Tamas Szirtes , Istva Schon , Lajos Kisfaludy, deceased
发明人： Andras Balazs , Tamas Szirtes , Istva Schon , Lajos Kisfaludy, deceased
IPC分类号： A61K38/00 , A61P43/00 , C07K1/06 , C07K7/06 , A61K37/02
CPC分类号： C07K7/06 , A61K38/00 , Y10S930/32
摘要： The present invention relates to novel pentapeptide of formulaXaa Glu Asp Ser Gly (SEQ ID NO: 1)wherein Xaa is pyro-alpha-aminoadipic acid, having specific inhibiting effect on epidermal cell proliferation, salts thereof, pharmaceutical compositions comprising the same and a method for the treatment of mammals for inhibiting the epidermal cell proliferation by administering the novel pentapeptide. The invention also covers a process for the preparation of both the pentapeptide and the pharmaceutical composition.

2. 发明授权

US4386073A Tripeptides acting on the central nervous system and a process for the preparation thereof 失效
标题翻译：作用于中枢神经系统的三肽及其制备方法
公开(公告)号：US4386073A
公开(公告)日：1983-05-31
申请号：US163830
申请日：1980-06-27
申请人： Lajos Kisfaludy , Tamas Szirtes , Lajos Balaspiri , Eva Palosi , Laszlo Szporny , Adam Sarkadi
发明人： Lajos Kisfaludy , Tamas Szirtes , Lajos Balaspiri , Eva Palosi , Laszlo Szporny , Adam Sarkadi
IPC分类号： C07K5/08 , A61K38/00 , A61K38/04 , A61K38/06 , A61P5/12 , A61P25/00 , A61P25/26 , C07K1/02 , C07K1/06 , C07K1/08 , C07K1/113 , C07K5/06 , C07K5/078 , C07K5/087 , C07K5/097 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0825 , C07K5/06043 , C07K5/06052 , C07K5/06147 , C07K5/06173 , C07K5/0821 , A61K38/00
摘要： The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),X--Y--W--NH.sub.2 (I)whereinX is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group,Y is L-leucyl, L-norvalyl or L-histidyl group, andW is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, orthe W-NH.sub.2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.
摘要翻译：本发明涉及作用于中枢神经系统并对应于通式（I）的XYW-NH 2（I）的新肽衍生物，其中X是L-焦谷氨酰基，D-焦谷氨酰基，L-2-酮 - 咪唑烷-4 羰基，L-6-酮基哌啶基，L-噻唑烷-4-羰基，L-脯氨酰基或正十二烷基，Y是L-亮氨酰，L-缬氨酰或L-组氨酰基，W是L-脯氨酰基，D- 脯氨酰基，L-噻唑烷-4-羰基，L-哌啶基，L-高辛基，L-亮氨酰基，L-异亮氨酰基，L-甲硫氨酰基或D-哌啶基，或W-NH 2基团代表吡咯烷基或哌啶基，条件是，如果X是L-焦谷氨酰基，Y是L-组氨酰基，则W不是L-脯氨酰基，和其药学上可接受的复合物。这些化合物通过肽化学中常用的方法制备。

3. 发明授权

US5008246A Novel peptides suppressing the function of the immune system, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：抑制免疫系统功能的新肽，含有它们的药物组合物及其制备方法
公开(公告)号：US5008246A
公开(公告)日：1991-04-16
申请号：US365457
申请日：1989-06-13
申请人： Istvan Schon , Olga Nyeki , Lajos Kisfaludy, deceased , Laszlo Denes , Gyorgy Hajos , Laszlo Szporny
发明人： Istvan Schon , Olga Nyeki , Lajos Kisfaludy, deceased , Laszlo Denes , Gyorgy Hajos , Laszlo Szporny
IPC分类号： A61K38/00 , A61P37/06 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/037 , C07K5/068 , C07K5/08 , C07K5/09 , C07K5/10 , C07K5/11
CPC分类号： C07K5/0817 , C07K5/06086 , C07K5/0815 , C07K5/1019 , A61K38/00
摘要： The invention relates to novel peptides and their acid addition salts, suppressing the function of the immune system, pharmaceutical compositions containing these peptides as well as to a process for preparing these peptides and compositions. The peptides are represented by formulae (1) to (16): ##STR1## The novel peptides are useful for the therapy of diseases where a decrease in the activity of the immune system is desirable.

4. 发明授权

US4672054A Process for the preparation of angiotensin-II analogues substituted in the 1-, 5- and 8- positions 失效
标题翻译：用于制备在1-，5-和8-位取代的血管紧张素-II类似物的方法
公开(公告)号：US4672054A
公开(公告)日：1987-06-09
申请号：US761596
申请日：1985-08-01
申请人： Olga Nyeki nee Kuprina , Lajos Kisfaludy , Katalin Szeberenyi nee Szalay , Gabor Makara , Bertalan Varga , Egon Karpati , Laszlo Szporny
发明人： Olga Nyeki nee Kuprina , Lajos Kisfaludy , Katalin Szeberenyi nee Szalay , Gabor Makara , Bertalan Varga , Egon Karpati , Laszlo Szporny
IPC分类号： A61K38/00 , C07K1/113 , C07K7/14 , C07K14/81 , A61K37/24
CPC分类号： C07K7/14 , A61K38/00
摘要： The invention relates to octapeptides of the formulaX-Arg-Val-Tyr-Y-His-Pro-W (I)whereinX is a sarcosyl, lactoyl or hydroxyacetyl radical,Y is cyclopentylglycyl or cyclohexylglycyl, andW is an alanine radical or lactic acid radicalhaving angiotensine-II antagonistic activity.
摘要翻译：本发明涉及式X-Arg-Val-Tyr-Y-His-Pro-W（I）的八肽，其中X是肌氨酰基，乳酰基或羟基乙酰基，Y是环戊基甘氨酰或环己基甘氨酰，W是丙氨酸基或具有血管紧张素II拮抗作用的乳酸根。

5. 发明授权

US4530964A Pharmaceutically active copolymers, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：药物活性共聚物，其制备方法和含有它们的药物组合物
公开(公告)号：US4530964A
公开(公告)日：1985-07-23
申请号：US478468
申请日：1983-03-24
申请人： Raymund Machovich , Miklos Nagy , Judit Gyorgyi nee Edelenyi , Istvan Horvath , Miklos Low , Katalin Csomor , Egon Karpati , Laszlo Szporny , Lajos Kisfaludy
发明人： Raymund Machovich , Miklos Nagy , Judit Gyorgyi nee Edelenyi , Istvan Horvath , Miklos Low , Katalin Csomor , Egon Karpati , Laszlo Szporny , Lajos Kisfaludy
IPC分类号： C08F16/00 , A61K31/78 , A61K31/795 , A61L33/06 , A61P7/02 , C08F8/44 , C08F16/02 , C08F20/00 , C08F216/00 , C08F216/06 , C08F220/00 , C08F220/04 , C08F228/00 , C08F228/02
CPC分类号： C08F228/00 , A61K31/78 , A61K31/795 , A61L33/064 , C08F220/04
摘要： The invention relates to new, pharmaceutically active copolymers with heparin-like activity, pharmaceutically acceptable salts thereof and a process for their preparation. The new copolymers comprise the units of the formula I ##STR1## wherein X stands for hydrogen or methyl and Y is hydrogen, units of the formula III ##STR2## optionally units of the formula II ##STR3## wherein Z' is hydrogen, and chain terminating units, formed from the units of the formulae I, III and optionally II under the conditions of copolymerization, in a statistical arrangement, and the pharmaceutically acceptable salts thereof, which contain, in addition to the above chain-members, units of the formulae IV and/or V ##STR4## wherein A is a cation/ satisfactorily replace the organogenic heparin, or give a synergistic combination with that,
摘要翻译：本发明涉及具有肝素样活性的新的药物活性共聚物及其药学上可接受的盐及其制备方法。新的共聚物包含式I的单元/ I /其中X代表氢或甲基，Y是氢，式III的单元/ III /任选的式II单元/ IMAGE /其中Z'为氢，以及由式I，III和任选II的单元在统计学排列的共聚条件下形成的链终止单元及其药学上可接受的盐，除了上述链成员，式IV和/或V的单元/ IV / / V /其中A

6. 发明授权

US4260595A Pharmaceutical compositions and process for the preparation of same 失效
标题翻译：药物组合物及其制备方法
公开(公告)号：US4260595A
公开(公告)日：1981-04-07
申请号：US950579
申请日：1978-10-12
申请人： Karoly Lapis , Bela Szende , Andreas Jeney , Laszlo Kopper , Karoly Simon , Erno Tyihak , Lajos Kisfaludy , Lajos Kovacs , Gyorgy Dobo
发明人： Karoly Lapis , Bela Szende , Andreas Jeney , Laszlo Kopper , Karoly Simon , Erno Tyihak , Lajos Kisfaludy , Lajos Kovacs , Gyorgy Dobo
IPC分类号： A61K31/195 , A61K31/475 , A61K31/675 , A61K31/66
CPC分类号： A61K31/475 , A61K31/195 , A61K31/675 , Y10S514/922
摘要： There are disclosed pharmaceutical compositions comprising at least one cytostatic agent and N.sup..epsilon. -trimethylthyllysin or a pharmaceutically acceptable salt thereof, optionally in association with conventional pharmaceutical carriers and other additives.The new compositions possess a reduced toxicity compared with the cytostatic agents administered alone.
摘要翻译：公开了包含至少一种细胞生长抑制剂和Nε-三甲基乙基溶素或其药学上可接受的盐，任选地与常规药物载体和其它添加剂相关的药物组合物。与单独施用的细胞生长抑制剂相比，新组合物的毒性降低。

7. 发明授权

US4329341A 5-Phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones, and pharmaceutical compositions containing them 失效
标题翻译： 5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-和含有它们的药物组合物
公开(公告)号：US4329341A
公开(公告)日：1982-05-11
申请号：US178679
申请日：1980-11-26
申请人： Julianna Rochricht , Lajos Kisfaludy , Marton Kajtar , Eva Palosi , Laszlo Szporny
发明人： Julianna Rochricht , Lajos Kisfaludy , Marton Kajtar , Eva Palosi , Laszlo Szporny
IPC分类号： C07D243/24 , A61K31/55
CPC分类号： C07D243/24
摘要： The invention relates to new optically active or racemic 5-phenyl-1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen, halogen, trifluoromethyl or a nitro group;R.sup.2 stands for hydrogen or alkyl having 1 to 6 carbon atoms;R.sup.3 represents a group conventionally attached to the --CH(NH.sub.2)--COOH group of the known optically active or racemic .alpha.-amino-acids, preferably an optionally substituted lower alkyl group;R.sup.4 is hydrogen, chlorocarbonyl or carbamoyl; andX is hydrogen, halogen or trifluoromethyl, with the proviso that if in the racemic compounds R.sup.4 stands for hydrogen R.sup.3 is other than alkyl having 1 to 6 carbon atoms, in which the centers of asymmetry in the 3- and 5-positions have the same absolute configuration, and pharmaceutically acceptable acid addition salts thereof, and a process for their preparation. The new compounds show valuable enzyme inducing activity and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.
摘要翻译：本发明涉及通式（I）的新的光学活性或外消旋的5-苯基-1,3,4,5-四氢-2H-1,4-苯并二氮杂-2-酮衍生物，其中R 1 代表氢，卤素，三氟甲基或硝基; R2代表氢或具有1至6个碳原子的烷基; R3表示通常与已知光学活性或外消旋的α-氨基酸的-CH（NH 2）-COOH基团连接的基团，优选任选取代的低级烷基; R4是氢，氯代羰基或氨基甲酰基; 并且X是氢，卤素或三氟甲基，条件是如果在外消旋化合物中R4代表氢，R3不是具有1至6个碳原子的烷基，其中3-和5-位的不对称中心具有相同的绝对构型及其药学上可接受的酸加成盐及其制备方法。新化合物显示有价值的酶诱导活性，因此可用作药物组合物的活性成分，其也在本发明的范围内。

8. 发明授权

US4209442A Angiotensin II analogs and process for the preparation thereof 失效
标题翻译：血管紧张素II类似物及其制备方法
公开(公告)号：US4209442A
公开(公告)日：1980-06-24
申请号：US923663
申请日：1978-07-11
申请人： Lajos Kisfaludy , Gyorgyne Nyeki nee Olga Kuprina , Laszlone Szirmai nee Maria Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
发明人： Lajos Kisfaludy , Gyorgyne Nyeki nee Olga Kuprina , Laszlone Szirmai nee Maria Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
IPC分类号： A61K38/00 , A61K38/22 , A61P9/12 , A61P43/00 , B02C13/22 , B02C21/00 , C07K1/113 , C07K7/14 , C07C103/52 , A61K37/00
CPC分类号： C07K7/14 , A61K38/00
摘要： Novel Angiotensin II peptides of the formula:X-Arg-Val-Tyr-Ile-His-Pio-Ywhere X is hydroxyacetyl or .alpha.-hydroxypropyl and Y is leucyl, isoleucyl, alanyl or threonyl or an acid addition salt or a complex thereof are disclosed and a process for the preparation thereof are disclosed having the ability to lower renal hypertension.
摘要翻译：新型的式：X-Arg-Val-Tyr-Ile-His-Pio-Y的血管紧张素II肽，其中X是羟乙酰或α-羟丙基，Y是亮氨酰，异亮氨酰，丙氨酰或苏氨酰或其酸加成盐或其复合物并且公开了其制备方法，其具有降低肾性高血压的能力。

9. 发明授权

US4179433A Angiotensin II antagonist peptides containing an alpha-aminooxyacid in the position-1 失效
标题翻译：血管紧张素II拮抗剂肽在第1位含有α-氨氧基酸
公开(公告)号：US4179433A
公开(公告)日：1979-12-18
申请号：US923681
申请日：1978-07-11
申请人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Maria Skirmai nee Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
发明人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Maria Skirmai nee Sarkozi , Egon Karpati , Katalin Gidai , Laszlo Szporny
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61P43/00 , C07C231/00 , C07K7/14 , C07C103/52 , A61K37/00
CPC分类号： C07K7/14 , A61K38/00
摘要： Angiotensin II analog of the formula IX-Arg-Val-Tyr-Ile-His-Pro-Y (I)whereinX is a radical derived from an aliphatic .alpha.-aminooxy-carboxylic acid andY is a radical derived from an aliphatic .alpha.-amino-carboxylic acid,and acid addition salts and complexes thereof with antagonistic properties useful in the diagnosis and treatment of hypertensions depending on renin.
摘要翻译：式I X-Arg-Val-Tyr-Ile-His-Pro-Y（I）的血管紧张素II类似物，其中X是衍生自脂族α-氨基氧基羧酸的基团，Y是衍生自脂族α - 氨基 - 羧酸及其具有拮抗性质的酸加成盐和复合物，其用于诊断和治疗依赖于肾素的高血压。

10. 发明授权

US4172130A .alpha.-AMINOACYL CONTAINING NEW PEPTIDES WITH GASTRIN EFFECTS AND A PROCESS FOR THE PREPARATION THEREOF 失效
标题翻译：含有GASTRIN效应的新型肽的60-氨基酸及其制备方法
公开(公告)号：US4172130A
公开(公告)日：1979-10-23
申请号：US865503
申请日：1977-12-29
申请人： Lajos Kisfaludy , Istvan Schon , Vince Varro , Laszlo Varga , Jozsef Nafradi
发明人： Lajos Kisfaludy , Istvan Schon , Vince Varro , Laszlo Varga , Jozsef Nafradi
IPC分类号： C07K5/10 , A61K38/00 , A61K38/08 , A61K38/22 , A61P1/00 , C07C53/15 , C07C291/04 , C07D207/40 , C07D207/404 , C07K1/08 , C07K1/107 , C07K1/113 , C07K5/117 , C07K7/02 , C07K7/06 , C07K14/575 , A61K37/00 , C07C103/52
CPC分类号： C07D207/404 , C07C291/04 , C07C53/15 , C07K5/1024 , A61K38/00
摘要： Peptides of the formula:A--Trp--B--Asp--Phe--NH--Ywherein A is tert.-butoxycarbonyl-aminooxy-acyl, benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl, or E-aminooxy-acyl, wherein E is benzoyl or straight-chain or branched C.sub.1-5 aliphatic acyl, B is methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl, and Y is hydrogen or carboxymethoxy, and pharmaceutically acceptable acid-addition salts or complexes thereof have gastric-acid secretion increasing effects.
摘要翻译：下式的肽：

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