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51. 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。

52. 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。

53. 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。

54. 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.

55. 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.

56. 发明授权

US4424223A Polycyclic compounds containing a double bond in the D-ring pharmaceutical compositions containing them, and methods of treating psoriasis with them 失效
标题翻译：在含有它们的D环药物组合物中含有双键的多环化合物，以及用它们治疗牛皮癣的方法
公开(公告)号：US4424223A
公开(公告)日：1984-01-03
申请号：US345630
申请日：1982-02-04
申请人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Tibor Keve , Bela Zsadon , Gyorgy Fekete , Csaba Lorincz , Janos Galambos , Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： A61K31/435 , A61K31/475 , A61P17/00 , A61P17/16 , A61P43/00 , C07D461/00
CPC分类号： C07D461/00 , Y10S514/863
摘要： The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.
摘要翻译：本发明涉及式（I）的新的17,18-脱氢阿朴氨酚-3'，4'，5'-三甲氧基 - 苯甲酸酯及其酸加成盐。根据本发明的另一方面，提供了制备这些新化合物的方法。本发明的另一方面是用于治疗牛皮癣的药物组合物。

57. 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。

58. 发明授权

US4328231A Method of treating psoriasis 失效
标题翻译：治疗牛皮癣的方法
公开(公告)号：US4328231A
公开(公告)日：1982-05-04
申请号：US172169
申请日：1980-07-25
申请人： Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
发明人： Maria Zajer nee Balazs , Lilla Forgach , Egon Karpati , Arpad Kiraly , Gyongyver Kiraly nee Soos , Laszlo Szporny , Bela Rosdy
IPC分类号： C07D461/00 , A61K31/435 , A61K31/475 , A61K31/58 , A61P17/00 , A61P43/00 , C12N9/99
CPC分类号： A61K31/475 , A61K31/58 , Y10S514/863
摘要： Skin diseases such as psoriasis in a human patient can be treated by topically or parenterally administering a dermatological composition containing a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen andR.sub.2 is the group --COOCH.sub.3, --CONH.sub.2 or --CONHNH.sub.2 ; orR.sub.1 is methoxy andR.sub.2 is a group ##STR2##
摘要翻译：可以通过局部或胃肠外施用含有下式化合物的皮肤病学组合物治疗皮肤疾病如牛皮癣：其中R 1是氢，R 2是基团-COOCH 3，-CONH 2 + L或-CONHNH 2 ; 或R 1为甲氧基，R 2为基团

59. 发明授权

US4283401A Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy 失效
标题翻译：制备11-溴 - 长春胺酸酯衍生物的方法及其在保护动物免受脑缺氧的作用
公开(公告)号：US4283401A
公开(公告)日：1981-08-11
申请号：US56647
申请日：1979-07-11
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
IPC分类号： C07D461/00 , C07D471/22 , A61K31/55 , C07D459/00
CPC分类号： C07D461/00
摘要： A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.All the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.
摘要翻译：一种用于制备通式为“IMAGE”的11-溴 - 长春胺酸酯的新方法，其中R 1和R 2各自独立地为C 1-6烷基独立地包括如下步骤：将1-烷基-1-烷氧基羰基乙基其中R 2如上所定义，R 3表示C 1-6烷基，与溴化剂反应，并用碱处理所得到的溴代衍生物的异构体混合物或处理环A中未取代的相应的14-氧代-E-均 - 异丁苯与溴化剂并亚硝化所得的通式为“IMAGE”的11-溴-14-氧代-E-均 - 胡烷，其中R2如上定义，然后将所得的11-溴代-14-氧代-15-羟基亚氨基-E-高硼烷进行脱氧亚胺化处理，并用在通式为R 1 OH的醇中用碱获得的14,15-二氧代衍生物进行脱氧，其中R1如上定义。所有的中间产物都是新颖的，并且对脑缺氧具有治疗保护作用。

60. 发明授权

US4278682A Vasodilating method of treatment using a indolo-quinolizine-monoester, diester or nitrile 失效
标题翻译：使用吲哚 - 喹诺酮单酯，二酯或腈的血管扩张治疗方法
公开(公告)号：US4278682A
公开(公告)日：1981-07-14
申请号：US26345
申请日：1979-04-02
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： C07D455/02 , A61K31/435 , A61K31/439 , A61P9/08 , C07D471/14 , A61K31/445
CPC分类号： C07D471/14 , Y10S514/929
摘要： Vasodilating octahydro-indolo[2,3-a]quinolizine derivatives of the formula ##STR1## wherein Q is hydrogen or an A--CH.sub.2 --CH.sub.2 -- group and A is cyano or --COOR, wherein R is C.sub.1-6 alkyl.
摘要翻译：其中Q为氢或A-CH2-CH2-基团且A为氰基或-COOR的式为“IMAGE”的血管扩张型八氢 - 吲哚并[2,3-a]喹嗪衍生物，其中R为C1-6烷基。

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