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51. 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。

52. 发明授权

US4179467A Dopamine hydroxylase inhibiting 2-amino-cyclopent-1-ene-1-thiocarboxylic acid-disulfides 失效
标题翻译：多巴胺羟化酶抑制2-氨基 - 环戊-1-烯-1-硫代羧酸二硫化物
公开(公告)号：US4179467A
公开(公告)日：1979-12-18
申请号：US865429
申请日：1977-12-29
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bella Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/13 , C07C87/02
CPC分类号： C10M1/08
摘要： New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the formula, ##STR1## wherein R is a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, or a C.sub.3-8 cycloalkyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the formula, ##STR2## wherein R is as defined above. The compounds of the formula (I) exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in therapy.
摘要翻译：新的2-氨基 - 环戊-1-烯 - 硫代羧酸 - 二硫化物，其中R是具有任选C 1-4烷氧基的C 1-6烷基，羟基，羧基和/或氨基取代基，C 2-4链烯基或C 3-8环烷基，是通过将下式所示的2-氨基环戊-1-烯二硫代羧酸，其中R如上定义。式（I）化合物发挥多巴胺-β-羟化酶抑制作用，可用于治疗。

53. 发明授权

US4089856A 1-Ethyl-1-(alkoxycarbonylethyl)-octahydro-indolo[2,3-a]quinolizines 失效
标题翻译： 1-乙基-1-（烷氧基羰基乙基） - 八氢 - 吲哚并[{2,3-a {9 quinolizines
公开(公告)号：US4089856A
公开(公告)日：1978-05-16
申请号：US699084
申请日：1976-06-23
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/04 , A61K31/435 , A61P9/06 , A61P9/08 , A61P9/12 , C07D471/14 , C07D459/00
CPC分类号： C07D471/14
摘要： Racemic and optically active 1-alkyl-1,2,3,4,6,7,12,12b-octahydro-indolo[2,3-a]quinolizines of vasodilatory and haemodynamic effect are disclosed.
摘要翻译：公开了血管扩张和血液动力学作用的外消旋和光学活性的1-烷基-1,2,3,4,6,7,12,12b-八氢 - 吲哚并[2,3-a]喹嗪。

54. 发明授权

US4057551A Indolo[2,3-a]quinolizines 失效
标题翻译：吲哚并[8-2,3-a {9 quinolizines
公开(公告)号：US4057551A
公开(公告)日：1977-11-08
申请号：US614240
申请日：1975-09-17
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/04 , A61K31/437 , C07D471/14 , C07D471/02 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R stands for an alkyl group, have been prepared by reducing a compound of the general formula (II) ##STR2## wherein R stands for alkyl, B stands for H.sub.2 O or an X.sup.- anion derived from an acid, and if B is an X.sup.- anion, A represents hydrogen, whereas if B is H.sub.2 O, A represents an electron pair. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R代表烷基的化合物是通过还原通式（II）的化合物（II）制备的，其中R代表烷基，B 代表H 2 O或衍生自酸的X阴离子，如果B是X-阴离子，则A表示氢，而如果B是H 2 O，则A表示电子对。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

55. 发明授权

US4057550A Nitrogen-containing polycyclic compounds 失效
标题翻译：含氮多环化合物
公开(公告)号：US4057550A
公开(公告)日：1977-11-08
申请号：US614239
申请日：1975-09-17
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/06 , A61K31/435 , A61K31/4375 , A61K31/439 , A61P9/08 , C07D461/00 , C07D471/02 , C07D455/02
CPC分类号： C07D461/00 , Y10S514/929
摘要： New compounds of the general formula (I) ##STR1## wherein R.sub.1 stands for alkyl and R.sub.2 stands for carboxy, a functional carboxy derivative or a group convertible into carboxy group or a functional derivative thereof, have been prepared by reducing a compound of the general formula ##STR2## wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- represents an anion derived from an acid, and optionally subjecting the obtained compound to hydrolysis. If desired, the racemic compounds of the general formula (I) can be resolved to yield the corresponding optically active isomers. The free bases of the general formula (I) can be converted into their pharmaceutically acceptable salts, or the salts can be treated with an alkaline agent to yield the free bases.The compounds of the general formula (I) can be used in the therapy primarily as vasodilatating agents.
摘要翻译：通式（I）的新化合物其中R1代表烷基，R2代表羧基，官能羧基衍生物或可转化成羧基的基团或其官能衍生物，通过还原化合物通式（II）其中R 1和R 2各自具有与上述相同的含义，并且X代表由酸衍生的阴离子，并且任选地使得到的化合物进行水解。如果需要，可以拆分通式（I）的外消旋化合物，得到相应的旋光异构体。通式（I）的游离碱可以转化为其药学上可接受的盐，或者盐可以用碱剂处理以产生游离碱。

56. 发明授权

US4048322A Bronchially effective xanthene-9-carboxylates 失效
标题翻译：支气管有效的呫吨-9-羧酸盐
公开(公告)号：US4048322A
公开(公告)日：1977-09-13
申请号：US673135
申请日：1976-04-02
申请人： Egon Karpati , Laszlo Szporny , Mihaly Bartok , Jozsef Czombos , Karoly Felfoldi , Marta Laszlavik , Ferenc Notheisz
发明人： Egon Karpati , Laszlo Szporny , Mihaly Bartok , Jozsef Czombos , Karoly Felfoldi , Marta Laszlavik , Ferenc Notheisz
IPC分类号： C07D311/90 , A61K31/35 , A61K31/352 , A61K31/40 , A61P11/14 , A61P25/02 , C07D295/13 , C07D311/82 , C07D311/84
CPC分类号： C07D295/13 , C07D311/84
摘要： The invention relates to new xanthene-9-carboxylates of the formula (I), ##STR1## wherein R.sub.1 and R.sub.3 are the same or different and each can represent a lower alkyl group,R.sub.2 is a lower alkyl group or a group of the formula (VI), ##STR2## WHEREIN M IS AN INTEGER OF 2 TO 5, OR R.sub.1 and R.sub.2 form, together with the adjacent nitrogen atom, a five- or six-membered heterocyclic group, and n and m each represent integers of 2 to 5, or salts thereof. These compounds possess cholinolytic and bronchospasmolytic effects and are completely devoid of harmful side-effects. Thus these compounds can be used to great advantage in therapy. The new compounds of the formula (I) or their salts can be prepared by reacting a diaminoalcohol of the formula (III), ##STR3## wherein R.sub.2 is lower alkyl or a group of formula -(CH.sub.2).sub.m -OH, with a reactive derivative of xanthene-9-carboxylic acid, and, if desired, converting the obtained product into its salt.
摘要翻译：本发明涉及式（I）的新的呫吨-9-羧酸盐，其中R1和R3相同或不同并且各自表示低级烷基，R2是低级烷基或基团式（VI），（VI），其中M为2至5的整数，或R 1和R 2与相邻的氮原子一起形成五元或六元杂环基，n和m 各自表示2至5的整数，或其盐。这些化合物具有胆固醇和支气管痉挛的作用，完全没有有害的副作用。因此，这些化合物可用于治疗中的极大优势。式（I）的新化合物或其盐可以通过使式（III），（III）的二氨基醇与其中R 2为低级烷基或式 - （CH 2）m -OH的基团反应制备，与呫吨-9-羧酸的反应性衍生物反应，如果需要，将得到的产物转化成其盐。

57. 发明授权

US4044012A Indolo-quinolizidine derivatives 失效
标题翻译：吲哚 - 喹嗪啶衍生物
公开(公告)号：US4044012A
公开(公告)日：1977-08-23
申请号：US670243
申请日：1976-03-25
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/14 , C07D459/00
CPC分类号： C07D471/14 , Y10S514/929
摘要： New compounds of the formula ##STR1## are provided wherein R.sub.1 is hydrogen, and R.sub.2 stands for an alkyl group and optically active enanthiomers and pharmaceutically acceptable salts thereof.
摘要翻译：提供新的式“IMAGE”化合物，其中R 1是氢，R 2代表烷基和光学活性的对映异构体及其药学上可接受的盐。

58. 发明授权

US5494909A Substituted oxazinoisoquinoline derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：取代的恶嗪基异喹啉衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5494909A
公开(公告)日：1996-02-27
申请号：US244736
申请日：1994-07-20
申请人： Jen Kobor , Laszlo Lazar , Imre Huber , Judit Arva , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Gabor Bernath , Ferenc Fulop
发明人： Jen Kobor , Laszlo Lazar , Imre Huber , Judit Arva , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Gabor Bernath , Ferenc Fulop
IPC分类号： A61K31/535 , A61P3/00 , A61P9/08 , A61P9/10 , A61P25/28 , C07D217/06 , C07D498/04 , A61K31/47 , C07D265/14
CPC分类号： C07D498/04
摘要： New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.
摘要翻译： PCT No.PCT / HU92 / 00053 Sec。 371日期：1994年7月20日 102（e）日期1994年7月20日PCT提交1992年12月11日PCT公布。公开号WO93 / 12118 （I）其中R 1是氢，C 1至C 4烷基，苯基或苯基的式（I）公开了具有抑制哺乳动物脑中钙摄取的能力的新化合物。 C1至C4烷基; R2和R3中的一个是C1-C4烷氧基，另一个是在芳核中被C1-C4烷基任选取代的苯基-C 1至C 4烷氧基; 并且R 4是任选地被芳族核中的C 1 -C 4烷基取代的苯基，或它们的溶剂化物，单独的光学活性和几何异构体，这些异构体的混合物，以及其药学上可接受的酸加成盐。式（I）的化合物能够抑制钙对脑细胞的吸收并对低压缺氧具有保护作用。

59. 发明授权

US5225416A 1,2,3,6-tetrahydropyridine derivatives useful for improving cerebral blood circulation 失效
标题翻译：用于改善脑血管循环的1,2,3,6-四氢吡啶衍生物
公开(公告)号：US5225416A
公开(公告)日：1993-07-06
申请号：US805861
申请日：1991-12-10
申请人： Tibor Gizur , Kalman Harsanyi , Attila Csehi , Aniko Demeter nee Szabo , Ferenc Trischler , Eva Vajda , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo
发明人： Tibor Gizur , Kalman Harsanyi , Attila Csehi , Aniko Demeter nee Szabo , Ferenc Trischler , Eva Vajda , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo
IPC分类号： A61K31/435 , A61P9/00 , C07D211/70
CPC分类号： C07D211/70
摘要： The present invention relates to novel 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) ##STR1## wherein R stands for hydrogen or an alkyl group,X stands for an unsubstituted phenyl or benzyl group or for a phenyl or benzyl group substituted with a halogen atom,Y stands for hydrogen or halogen or a trifluoro-methyl groupas well as enantiomers acid addition salts thereof.The invention further extends to pharmaceutical compositions containing said compounds as active ingredient mainly for improving cerebral blood circulation and antihypoxic activity. The 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) are prepared by treating an oxo derivative of the general formula (II) ##STR2## wherein R, X and Y are as given above in an organic solvent by a reducing agent and reacting the obtained 1,2,3,6-tetrahydropyridine derivative of the general formula (I), wherein R, X and Y are as given above, with a mineral or organic acid and converting the same, if desired, to an acid addition salt.

60. 发明授权

US5096902A Heterocyclic compounds containing nitrogen and sulfur, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：含有氮和硫的杂环化合物，含有它们的药物组合物及其制备方法
公开(公告)号：US5096902A
公开(公告)日：1992-03-17
申请号：US509473
申请日：1990-04-12
申请人： Karoly Nador , Pal Scheiber , nee Szelecsenyi; Erzsebet Andrasi , Bela Molnar , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmay
发明人： Karoly Nador , Pal Scheiber , nee Szelecsenyi; Erzsebet Andrasi , Bela Molnar , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Dora Groo , Istvan Laszlovszky , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmay
IPC分类号： A61K31/425 , A61K31/426 , A61K31/445 , A61K31/54 , A61P9/10 , A61P25/28 , C07D277/04 , C07D277/06 , C07D279/06 , C07D283/02 , C07D417/06
CPC分类号： C07D417/06 , C07D277/04 , C07D277/06 , C07D279/06
摘要： The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g. the senile dementia, Alzheimer's disease or disturbances of the cognitive function.

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