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1. 发明申请

US20070042935A1 Quinazolinone-derivatives and their use for preparation of pharmaceutical compositions having parp enzyme inhibitory effect 有权
标题翻译：喹唑啉酮衍生物及其制备具有酶抑制作用的药物组合物的用途
公开(公告)号：US20070042935A1
公开(公告)日：2007-02-22
申请号：US10554749
申请日：2004-04-30
申请人： Balazs Sumegi , Kalman Hideg , Tamas Kalai
发明人： Balazs Sumegi , Kalman Hideg , Tamas Kalai
IPC分类号： A61K31/00
CPC分类号： C07D401/04 , C07D239/95 , C07D401/06 , C07D401/12
摘要： The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.
摘要翻译：本发明的主题是抑制DNA修复酶，聚（ADP-核糖）聚合酶（PARP））的喹唑啉衍生物及其药学上可接受的通式（I）的盐，使其能够用于制备药物用于预防或治疗PARP抑制产生有益效果的疾病的组合物。在通式（I）中，R 1表示氢或通式（a）的基团; R 2代表a）氢或C 1-6烷基，如果R 1不是氢，和b）如果R' SUP> 1是氢，则R 2可以是通式（b），（c）或（d）的基团。本发明的主题还包括上述化合物的制备方法。

2. 发明申请

US20070072912A1 Alicyclic-amine-substituted 4-carboxamido-benzimidazoles as parp-inhibitors and antioxidants 审中-公开
标题翻译：脂环胺 - 胺取代的4-甲酰氨基 - 苯并咪唑作为对位抑制剂和抗氧化剂
公开(公告)号：US20070072912A1
公开(公告)日：2007-03-29
申请号：US10553937
申请日：2004-04-27
申请人： Kalman Hideg , Tamas Kalai , Balazs Sumegi
发明人： Kalman Hideg , Tamas Kalai , Balazs Sumegi
IPC分类号： A61K31/4439 , A61K31/4184 , C07D403/02
CPC分类号： C07D401/04 , C07D403/04 , C07D403/10 , C07D405/14 , C07D495/04
摘要： Compounds of the formula (I) and their pharmaceutically acceptable or technically applicable acid salts—where in the formula R1 represents hydrogen, C(1-4)alkyl or C(1-4)alkoxy R2 represents hydrogen, C(1-4)alkyl, carboxyl, C(1-4)alkoxycarbonyl, carboxamido, aryl or hetero-aryl R3 represents hydrogen, C(1-4)alkyl, aryl-methylene, or aryl, Y is a valency bond, a straight or branched chain C(1-4)alkene, a carbonyl-amino-C(1-4)alkene, or a —S—(CH2)m— group, where all alkene groups above may be spaced by an arylene group, n represents zero or the integer 1 m represents the integer 1, 2 or 3 Q represents hydrogen, hydroxyl or the oxygen radical (0) or together with the N atom of the adjacent ring forms a +N=O (oxoimmonium) group Z represents a single or double bond and their pharmaceutically acceptable or technically useful salts, processes for their preparation and their biological use as PARP inhibitors and antioxidants.
摘要翻译：式（I）化合物及其药学上可接受的或技术上可应用的酸盐 - 其中在式R 1表示氢，C 1-4（1-4） - 烷基或C （1-4）烷氧基R 2表示氢，C 1-4（1-4）烷基，羧基，C 1-4（1-4）烷氧基羰基，甲酰胺基，芳基或杂芳基R 3表示氢，C 1-4（1-4）烷基，芳基 - 亚甲基或芳基，Y是直链或支链C 1-4（1-4）烯烃，羰基 - 氨基-C 1-4（1-4） - 烯烃或-S-（CH 其中所有上述烯烃基团可以被亚芳基间隔开，n表示0或整数1m表示整数1,2或3个Q 表示氢，羟基或氧自由基（0）或与相邻环的N原子一起形成a + N = O（有机基元素）基团Z表示单键或双键及其药学上可接受或技术上有用的盐，准备 n及其生物用作PARP抑制剂和抗氧化剂。

3. 发明授权

US4897413A Alkyl diamine derivatives 失效
标题翻译：烷基二胺衍生物
公开(公告)号：US4897413A
公开(公告)日：1990-01-30
申请号：US109819
申请日：1987-10-16
申请人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
发明人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
IPC分类号： C07D207/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/505 , A61P9/06 , C07D207/16 , C07D207/22 , C07D207/32 , C07D207/335 , C07D207/46 , C07D401/00 , C07D401/12 , C07D403/00 , C07D403/12 , C07D405/00 , C07D405/12 , C07D409/00 , C07D409/12
CPC分类号： C07D207/335 , C07D207/22 , C07D207/46 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention refers to new diamines of the Formula I ##STR1## wherein stands for ##STR2## wherein A stands for C.sub.1-5 alkylene which can be substituted by hydroxyl,X stands for a single or double bond,R.sup.2 stands for aryl or heteroaryl optionally substituted by halogen, C.sub.1-4 alkoxy or acylamino,R.sup.3 stands for hydrogen or C.sub.1-4 alkyl,A.sup.1 stands for a single bond or C.sub.1-5 alkyl optionally substituted by hydroxyl or thioalkylene or oxyalkylene,R.sup.4 stands for a 5- or 6- membered aromatic or heteroaromatic ring which can be substituted by one or more hydroxyl, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy and/or halogen or methylenedioxy and the alkyl group can be unsaturated as well,Q stands for a 6-membered ring which can be partially hydrogenated, andR.sup.1 stands for C.sub.1-4 alkyl.The new compounds are antiarrhythmic agents.

4. 发明申请

US20120316203A1 Compositions and Methods for Inhibition of Cancers 审中-公开
标题翻译：抑制癌症的组合物和方法
公开(公告)号：US20120316203A1
公开(公告)日：2012-12-13
申请号：US13382545
申请日：2010-07-06
申请人： Periannan Kuppusamy , Kalman Hideg
发明人： Periannan Kuppusamy , Kalman Hideg
IPC分类号： A61K31/454 , C12N5/09 , A61P35/00 , C07D401/06
CPC分类号： A61K31/454
摘要： Methods and compositions for treating cancers, including ovarian cancers, are described. The compositions generally include a redox based curcumin derivative, diarylidenylpiperiden-4-one (DAP) having a hydroxylamine moiety attached thereto.
摘要翻译：描述了治疗癌症（包括卵巢癌）的方法和组合物。组合物通常包括氧化还原基的姜黄素衍生物，具有连接羟胺部分的二芳基亚基哌啶-4-酮（DAP）。

5. 发明授权

US4731376A 2-(-(2,2,5,5-tetramethyl-3-pyrrolin-3-carbonyl))-amino derivatives 失效
标题翻译： 2 - （ - （2,2,5,5-四甲基-3-吡咯啉-3-羰基）） - 氨基衍生物
公开(公告)号：US4731376A
公开(公告)日：1988-03-15
申请号：US898723
申请日：1986-08-14
申请人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
发明人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
IPC分类号： C07D207/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61P9/06 , C07D207/16 , C07D207/22 , C07D401/00 , C07D401/12 , C07D207/09 , C07D207/18
CPC分类号： C07D207/22 , C07D207/16
摘要： Compounds are disclosed of the formula (I) ##STR1## wherein A.sup.1 is a valence bond or a C.sub.1 to C.sub.5 straight or branched chain alkylene group unsubstituted or substituted by hydroxy or aminocarbonyl;B is a valence bond or a double bond;R.sup.3 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2 is a phenyl or phenoxy group unsubstituted or substituted by one or two C.sub.1 to C.sub.4 alkyl groups, C.sub.1 to C.sub.4 alkoxy groups, or halo substituents; or R.sup.2 is an amino group, a diphenylmethyl group, or an R.sup.4 --NH--CO-- group in whichR.sup.4 is 2,6-dimethyl-phenyl; or a pharmaceutically acceptable acid addition salt thereof. The compounds possess anti-arrhythmic activity and exert little or no hypotensive side effects.
摘要翻译： PCT No.PCT / HU84 / 00004 Sec。 371日期1984年9月20日 102（e）1984年9月20日PCT PCT 1月20日，PCT PCT。出版物WO84 / 02906 日期：1984年8月2日。公开了式（I）的化合物：其中A1是未取代或被羟基或氨基羰基取代的价键或C1至C5直链或支链亚烷基; B是价键或双键; R3是氢或C1-C4烷基; R2是未被取代或被一个或两个C1至C4烷基，C1至C4烷氧基或卤素取代基取代的苯基或苯氧基; 或R 2为氨基，二苯基甲基或R 4 -NH-CO-基，其中R 4为2,6-二甲基 - 苯基; 或其药学上可接受的酸加成盐。该化合物具有抗心律不齐活性，并且发挥很少或没有降压作用。

6. 发明授权

US4703056A New alkyl diamine derivatives 失效
标题翻译：新的烷基二胺衍生物
公开(公告)号：US4703056A
公开(公告)日：1987-10-27
申请号：US662298
申请日：1984-09-20
申请人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
发明人： Kalman Hideg , Olga H. Hankovszky , Laszlo Frank , Ilona Bodi , Jozsef Csak
IPC分类号： C07D207/00 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/505 , A61P9/06 , C07D207/16 , C07D207/22 , C07D207/32 , C07D207/335 , C07D207/46 , C07D401/00 , C07D401/12 , C07D403/00 , C07D403/12 , C07D405/00 , C07D405/12 , C07D409/00 , C07D409/12
CPC分类号： C07D207/335 , C07D207/22 , C07D207/46 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention relates to new anti-arrhythmic compounds of the formula (I) ##STR1## wherein A is C1 to C5 alkylene which can be substituted by hydroxyl;X is a single or a double bond; andQ is a 6-membered carbocyclic moiety fused to each of the adjacent carbonyl carbon atoms, and which is either fully hydrogenated, partially hydrogenated, or aromatic, or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译： PCT No.PCT / HU84 / 00005 Sec。 371日期1984年9月20日 102（e）1984年9月20日PCT PCT 1月23日，PCT PCT。公开号WO84 / 02907 日本1984年8月2日。本发明涉及式（I）的新型抗心律失常化合物，其中A为可被羟基取代的C1至C5亚烷基; X是单键或双键; 和Q是与每个相邻羰基碳原子稠合的6元碳环部分，并且其是完全氢化的，部分氢化的或芳族的，或其药学上可接受的酸加成盐。

7. 发明授权

US4017507A 2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt 失效
标题翻译： 2,3-二氢-7-氯噻唑并[8 3,2-a {9苯并咪唑和盐
公开(公告)号：US4017507A
公开(公告)日：1977-04-12
申请号：US637978
申请日：1975-12-05
申请人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
发明人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##STR2## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a=C-- group, orA stands for a group of the general formula (III), ##STR3## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##STR4## wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##STR5## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(ch.sub.2).sub.m --X VI.in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.
摘要翻译：通式（I）的新型三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表一个基团的通式（II），其中R 2表示氢或羟基，R 3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示一个通式（III），其中R 4和R 5各自代表氢，甲基，氯或硝基，通过反应通用化合物（IV）化合物（IV）制备其中A和n各自具有与上述定义相同的含有通式（Ⅴ）的化合物，其中X代表卤素，R6代表氢，R7代表通式（Ⅵ）的基团，（CH2）mX VI。

8. 发明授权

US3941788A Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US3941788A
公开(公告)日：1976-03-02
申请号：US463686
申请日：1974-04-24
申请人： Olga Hankovszky , Kalman Hideg , Sandor Pacsa
发明人： Olga Hankovszky , Kalman Hideg , Sandor Pacsa
IPC分类号： C07D235/04 , A01N43/52 , C07D487/04 , C07D239/06
CPC分类号： C07D487/04 , A01N43/52
摘要： New benzimidazole derivatives of the general formula (I) ##SPC1##and acid addition salts thereof, whereinR.sub.1 and R.sub.2 each represent hydrogen or methyl,R.sub.5 and R.sub.6 form together a valence bond and at the same time R.sub.3 and R.sub.4 form together a group of the general formula (II), ##EQU1## wherein n is equal to zero or one, or R.sub.4, R.sub.5 and R.sub.6 form together a group of the formula (III) ##EQU2## and at the same time R.sub.3 stands for benzyl group, were prepared by reacting a compound of the general formula (IV), ##SPC2##wherein R.sub.7 stands for hydrogen or benzyl group and R.sub.1, R.sub.2 and n each have the same meanings as defined above, or an acid addition salt thereof with epichlorohydrine optionally in the presence of a base.The new compounds of the general formula (I) and their acid addition salts inhibit the reproduction of viruses and can be used in therapy as antiviral agents.
摘要翻译：通式（I）的新的苯并咪唑衍生物及其酸加成盐，其中R 1和R 2各自表示氢或甲基，R 5和R 6一起形成价键，同时R 3和R 4一起形成通式（II），-CH 2 -CH-CH 2 -NH-（CH 2）n - （II）OH其中n等于零或一个，或者R 4，R 5和R 6一起形成式（III）= N -CH 2 -CH-CH 2 - |（III）OH，同时R3代表苄基，通过使通式（IV）的化合物与其中R 7，R 2，R 2， n各自具有与上述相同的含义，或其酸加成盐与任选在碱存在下的表氯醇。

9. 发明授权

US3932395A Tricyclic imidazole derivatives 失效
标题翻译：三环咪唑衍生物
公开(公告)号：US3932395A
公开(公告)日：1976-01-13
申请号：US473184
申请日：1974-05-24
申请人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
发明人： Kalman Hideg , Olga Hankovszky , Eva Palosi , Gyorgy Hajos , Laszlo Szporny
IPC分类号： C07D513/16 , C07D513/04 , C07D513/14 , C07D279/08 , C07D279/14
CPC分类号： C07D513/04 , C07D513/14 , Y10S514/916
摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.
摘要翻译：新的通式（I）的三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表通式（II ），-C = QC = Z- |（II）R2R3其中R2表示氢或羟基，R3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示通式（III）-CH = C-C = CH- |（III）R4R5其中R4和R5各自表示氢，甲基，氯或硝基，通过反应通用化合物（IV）的化合物制备，其中A和n各自具有与上述相同的含义，与通式（V）的化合物，X-CH 2 -CH-CH 2 ||（V）R 6 R 7，其中X代表卤素，R6代表氢，R7 代表通式（VI）， - （CH 2）m X（VI）的基团，其中m和X各自具有与上述相同的含义，或者R6和R7一起代表氧。任选地在碱的存在下进行反应。通式（I）的化合物可以转化成它们的酸加成盐。

10. 发明授权

US08722707B1 Compositions and methods for inhibition of smooth muscle cell proliferation and neointimal hyperplasia 有权
标题翻译：抑制平滑肌细胞增殖和新生内膜增生的组合物和方法
公开(公告)号：US08722707B1
公开(公告)日：2014-05-13
申请号：US12831170
申请日：2010-07-06
申请人： Periannan Kuppusamy , Kalman Hideg , Karuppaiyah Selvendiran
发明人： Periannan Kuppusamy , Kalman Hideg , Karuppaiyah Selvendiran
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： A61K31/381 , A61K9/0019
摘要： Compositions and methods for treating post angioplasty restenosis, arteriosclerosis, and/or smooth muscle cell proliferation and/or neointimal hyperplasia in vascular tissues, and at least one composition of a redox based curcumin derivative, DAP-F(p) and a pharmaceutically acceptable carrier, are described.
摘要翻译：用于治疗血管成形术再狭窄，动脉硬化和/或血管组织中的平滑肌细胞增殖和/或内膜增生的组合物和方法，以及至少一种基于氧化还原的姜黄素衍生物DAP-F（p）和药学上可接受的载体的组合物，被描述。

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