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1. 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。

2. 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。

3. 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。

4. 发明授权

US4428938A Peptides affecting the immune regulation and a process for their preparation 失效
标题翻译：影响免疫调节的肽及其制备方法
公开(公告)号：US4428938A
公开(公告)日：1984-01-31
申请号：US387655
申请日：1982-06-11
申请人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Istvan Schon , Laszlo Denes , Julia Ember , Gyorgy Hajos , Laszlo Szporny , Bela Szende
发明人： Lajos Kisfaludy , Olga Nyeki nee Kuprina , Istvan Schon , Laszlo Denes , Julia Ember , Gyorgy Hajos , Laszlo Szporny , Bela Szende
IPC分类号： C07K5/08 , A61K38/00 , A61K38/07 , A61K38/22 , A61P37/00 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/12 , C07K1/113 , C07K5/09 , C07K5/10 , C07K5/103 , C07K5/11 , C07K5/117 , C07K7/06 , C07K14/575 , C07K14/66 , A61K37/00 , C07C103/52
CPC分类号： C07K5/0815 , C07K14/66 , C07K5/1008 , C07K5/1019 , C07K5/1024 , Y10S930/18
摘要： Peptides affecting the immune regulation selected from the following group:Arg-Lys-AspArg-Lys-Asp-ValArg-Lys-Asn-ValArg-Lys-Asu-ValArg-Lys-Ala-ValArg-Lys-Asp-AlaArg-Lys-Asp-IleArg-Lys-Glu-ValArg-Ala-Asp-ValArg-Asp-Lys-ValAla-Lys-Asp-ValLys-Arg-Asp-ValGlp-Arg-Lys-AspGlp-Arg-Lys-Asp-ValGlp-Arg-Lys-Asp-Val-Tyr and salts, amides lower alkyl esters and protected derivatives thereof.
摘要翻译： Arg-Lys-Asp Arg-Lys-Asp-Val Arg-Lys-Asn-Val Arg-Lys-Asu-Val Arg-Lys-Ala-Val Arg-Lys-Asp- Ala Arg-Lys-Asp-Ile Arg-Lys-Glu-Val Arg-Ala-Asp-Val Arg-Asp-Lys-Val Ala-Lys-Asp-Val Lys-Arg-Asp-Val Glp-Arg-Lys-Asp Glp-Arg-Lys-Asp-Val Glp-Arg-Lys-Asp-Val-Tyr和其盐，酰胺低级烷基酯及其被保护的衍生物。

5. 发明授权

US5041535A Antileukemic and immunostimulant peptides 失效
标题翻译：抗白血病和免疫刺激肽
公开(公告)号：US5041535A
公开(公告)日：1991-08-20
申请号：US123124
申请日：1987-11-20
申请人： Olga Nyeki nee Kuprina , Istvan Schon , Lajos Kisfaludy , Laszlo Denes , Gyorgy Hajos , Laszlo Szporny , Bela Szende , Karoly Lapis
发明人： Olga Nyeki nee Kuprina , Istvan Schon , Lajos Kisfaludy , Laszlo Denes , Gyorgy Hajos , Laszlo Szporny , Bela Szende , Karoly Lapis
IPC分类号： A61K38/00 , A61P35/02 , A61P37/04 , C07K1/06 , C07K1/113 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/09 , C07K5/097 , C07K5/10 , C07K5/11 , C07K5/113
CPC分类号： C07K5/06173 , C07K5/0815 , C07K5/0825 , C07K5/1019 , C07K5/1021 , A61K38/00
摘要： The new peptides of the Formulae(1) Glp-Lys-NH.sub.2(2) Glp-Glu-Lys-NH.sub.2(3) Arg-Lys-Glu-NH.sub.2(4) Arg-lys-Asp-NH.sub.2(5) Arg-Lys-Glu-OH(6) Arg-Lys-Gln-OH(7) Leu-Val-Ala-OH(8) Arg-Orn-Asp-Val-NH.sub.2(9) Arg-Orn-Asp-Val-OH(10) Lys-Glu-Lys-Lys-OH(11) Lys-Leu-Lys-Lys-OH(12) Lys-Asp-Leu-Lys-OH(13) Glu-Leu-Val-Ala-OH and(14) Leu-Pro-Ala-Gly-OHand acid addition salts thereof inhibit the proliferation of leukaemic cells and exhibit immunostimulant effect.
摘要翻译：式（1）的新肽Glp-Lys-NH2（2）Glp-Glu-Lys-NH2（3）Arg-Lys-Glu-NH2（4）Arg-lys-Asp-NH2（5）Arg-Lys -Glu-OH（6）Arg-Lys-Gln-OH（7）Leu-Val-Ala-OH（8）Arg-Orn-Asp-Val-NH2（9）Arg-Orn-Asp-Val-OH ）Lys-Glu-Lys-Lys-OH（11）Lys-Leu-Lys-Lys-OH（12）Lys-Asp-Leu-Lys-OH（13）Glu-Leu-Val-Ala-OH和（14） Leu-Pro-Ala-Gly-OH及其酸加成盐抑制白血病细胞的增殖并显示出免疫刺激作用。

6. 发明授权

US4200631A Treating mammalian subject sensitive to indomethacin ulcerogenisis 失效
标题翻译：治疗对吲哚美辛溃疡发生敏感的哺乳动物受试者
公开(公告)号：US4200631A
公开(公告)日：1980-04-29
申请号：US931910
申请日：1978-08-08
申请人： Elemer Ezer , Laszlo Szporny , Lilla Forgach , Eva Palosi , Eszter Cholnoky , Egon Karpati , Gyorgy Hajos , Gyozo Hortobagyi , Katalin Gidai
发明人： Elemer Ezer , Laszlo Szporny , Lilla Forgach , Eva Palosi , Eszter Cholnoky , Egon Karpati , Gyorgy Hajos , Gyozo Hortobagyi , Katalin Gidai
IPC分类号： A61K31/405 , A61K31/62
CPC分类号： A61K31/60
摘要： Ulcer production in animals is prevented during prolonged antiphlogistic treatment with ulcerogenic quantities of indomethacin by using it in a composition of 1 part of indomethacin to 7.5 to 25 parts, preferably 10 parts by weight of a salicylate. Indomethacin is the most potent ulcerating compound among approved non-steroid antiinflammatory agents.
摘要翻译：通过将其用于1份吲哚美辛组合物中的7.5〜25份，优选10份重量的水杨酸酯，在用溃疡性量的吲哚美辛进行长时间的消炎治疗期间，能够预防动物的溃疡生产。吲哚美辛是经批准的非类固醇抗炎药物中最有效的溃疡化合物。

7. 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

8. 发明授权

US4388304A Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof 失效
标题翻译：具有拮抗作用的血管紧张素-II类似物，其含有8位的酯基及其制备方法
公开(公告)号：US4388304A
公开(公告)日：1983-06-14
申请号：US225048
申请日：1981-01-14
申请人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
发明人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08 , A61K38/55 , A61P9/12 , C07K7/14 , A61K37/00 , C07C103/52
CPC分类号： C07K7/14 , A61K38/00 , Y02P20/55 , Y10S530/80
摘要： New octapeptides of the general formula (I),X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I)whereinX stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid,Y is the residue of an aliphatic amino acid, andA is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II),B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andA, X and Y are as defined above,are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex.The new compounds according to the invention possess angiotensin-II antagonizing effects, and can be used in the therapy to diagnose or treat hypertensive states.
摘要翻译：通式（I）的新八肽，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X代表N-甲基氨基酸的酰基或脂族 α-羟基或α-氨基氧基羧酸，Y是脂族氨基酸的残基，A是C 1-5烷基，使得通式（II）的保护的八肽衍生物的保护基， BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OA（II）其中B是通过酸解或催化氢化除去的基团，C是临时保护的基团 Arg部分的胍基，D为Tyr部分上芳香族羟基的临时保护基，E为His部分上咪唑基的临时保护基团，A，X和Y为如上所定义的，可以逐步地或单步地去除。如果需要，将通式（I）的化合物转化为其酸加成盐或药学上可接受的络合物。根据本发明的新化合物具有血管紧张素-II拮抗作用，可用于诊断或治疗高血压状态的治疗。

9. 发明授权

US4035370A Alkaloid esters 失效
标题翻译：生物碱类
公开(公告)号：US4035370A
公开(公告)日：1977-07-12
申请号：US645244
申请日：1975-12-29
申请人： Csaba Lorincz , Egon Karpati , Laszlo Szporny , Kalman Szasz , Lajos Kisfaludy
发明人： Csaba Lorincz , Egon Karpati , Laszlo Szporny , Kalman Szasz , Lajos Kisfaludy
IPC分类号： C07D461/00 , C07D459/00
CPC分类号： C07D461/00 , Y10S514/929
摘要： Vasodilatory eburnamine-type alkaloid esters of the formula (I) ##STR1## and salts and quaternary derivatives thereof, wherein X.about.Y REPRESENTS A =CH=CH- or ##STR2## R represents a C.sub.1-6 alkoxycarbonyl group optionally substituted with a hydroxy group or with a halogen atom, further an alkenyloxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl group or an acylated primary alcohol group, especially apovincaninic acid ethyl ester, have been prepared by various methods of esterification.
摘要翻译：式（I）的血管扩张性本burn胺型生物碱及其盐和季衍生物，其中X代表Y代表A = CH = CH-或R表示任选取代的C 1-6烷氧基羰基具有羟基或卤素原子，还通过各种酯化方法制备了链烯氧基羰基，芳氧基羰基，芳烷氧基羰基或酰化伯醇基，特别是亚氨基二乙酸乙酯。

10. 发明授权

US4330532A Angiotensin-II analogues with antagonizing effects, containing an .alpha.-hydroxycarboxylic acid residue in position 8, and a process for the preparation thereof 失效
标题翻译：在8位含有α-羟基羧酸残基的具有拮抗作用的血管紧张素-II类似物及其制备方法
公开(公告)号：US4330532A
公开(公告)日：1982-05-18
申请号：US222765
申请日：1981-01-06
申请人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
发明人： Olga Nyeki , Lajos Kisfaludy , Egon Karpati , Laszlo Szporny
IPC分类号： C07K7/06 , A61K38/08 , A61K38/55 , A61P43/00 , C07K7/14 , A61K37/00 , C07C103/52
CPC分类号： C07K7/14 , Y02P20/55
摘要： New angiotensin-II analogues of the general formula (I),X-Arg-Val-Tyr-Ile-His-Pro-Y-OA (I)whereinX stands for the acyl group of an N-methylamino acid, or the acyl group of an aliphatic .alpha.-aminooxy- or .alpha.-hydroxycarboxylic acid,Y is the residue of an aliphatic .alpha.-hydroxycarboxylic acid, andA is hydrogen or a C.sub.1-5 alkyl group,are prepared by removing the protecting groups of a protected octapeptide derivative of the general formula (II) or (III),B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OF (II)B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OA (III)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andF is a group for the protection of the terminal carboxy group, resistant to the effect of mild acids but removable by catalytic hydrogenolysis or upon treatment with a stronger acid.The new compounds of the invention can be applied to diagnose and differentiate hypertensions of various origin, and in the therapy to suppress hypertensions of renal origin, in the treatment of hypertensive crises, secondary cardiac insufficiency, etc.
摘要翻译：通式（I）的新型血管紧张素-II类似物，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X表示N-甲基氨基酸的酰基，或酰基脂肪族α-氨基氧基或α-羟基羧酸的基团，Y是脂肪族α-羟基羧酸的残基，A是氢或C 1-5烷基，是通过除去保护的八肽衍生物的保护基来制备的的通式（II）或（III）的BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OF（II）BX-Arg（C）-Val- Tyr（D）-Ile-His（E）-Pro-Y-OA（III）其中B是通过酸解或催化氢化除去的基团，C是用于临时保护Arg部分上胍基的基团，D 是用于临时保护Tyr部分上的芳族羟基的基团，E是His部分上咪唑基的临时保护基团，F是保护末端羧基的基团，耐受温和酸的作用b 通过催化氢解或用较强酸处理可以除去。本发明的新化合物可用于诊断和鉴别各种起因的高血压，以及用于抑制肾源性高血压，治疗高血压危象，继发性心脏功能不全等的治疗。

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