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1. 发明授权

US6121241A Anticoagulant peptide aldehyde derivatives 失效
标题翻译：抗凝血肽醛衍生物
公开(公告)号：US6121241A
公开(公告)日：2000-09-19
申请号：US11001
申请日：1999-04-02
申请人： Sandor Bajusz , Attila Juhasz , Eva Barabas , Andras Feher , Gabriella Szabo , Erzsebet Szell nee Hasenohrl , Iren Veghelyi nee Fauszt , Emilia Lavich nee Oszko , Eva Kaszas , Jozsef Lango , Imre Moravcsik , Agnes Szeker nee Peszeky , Zsuzsanna Taschler nee Pasztor , Gabor Toth , Zsuzsanna Mohai nee Nagy , Anna Maria Szalkay nee Hollosi , Klara Makk nee Ocskay
发明人： Sandor Bajusz , Attila Juhasz , Eva Barabas , Andras Feher , Gabriella Szabo , Erzsebet Szell nee Hasenohrl , Iren Veghelyi nee Fauszt , Emilia Lavich nee Oszko , Eva Kaszas , Jozsef Lango , Imre Moravcsik , Agnes Szeker nee Peszeky , Zsuzsanna Taschler nee Pasztor , Gabor Toth , Zsuzsanna Mohai nee Nagy , Anna Maria Szalkay nee Hollosi , Klara Makk nee Ocskay
IPC分类号： C07D207/16 , A61K38/05 , C07K5/00
CPC分类号： C07D207/16 , Y10S514/822
摘要： This invention relates to peptide aldehyde derivatives of formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represent a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents an L-prolyl residue and Arg represents an L-arginyl residue, their acid-additon salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) of the invention have therapeutic, particularly anticoagulant, antiplatelet and antithrombotic properties.
摘要翻译： PCT No.PCT / HU97 / 00027 Sec。一九九九年四月二日 102（e）1999年4月2日PCT 1997年6月5日PCT公布。第WO97 / 46523号公报日期1997年12月11日本发明涉及式（I）的肽醛衍生物：D-Xaa-Pro-Arg-H，其中Xaa表示2-环庚基-2-羟基乙酰基或2-环戊基-2-羟基乙酰基，Pro 代表L-脯氨酰残基，Arg表示L-精氨酰残基，它们与有机或无机酸形成的酸加成盐和含有它们的药物组合物。本发明式（I）的化合物具有治疗性，特别是抗凝血，抗血小板和抗血栓形成的特性。

2. 发明授权

US5760235A Anticoagulant peptide derivatives and pharmaceutical compositions containing the same as well as a process for preparation thereof 失效
标题翻译：抗凝血肽衍生物和含有其的药物组合物及其制备方法
公开(公告)号：US5760235A
公开(公告)日：1998-06-02
申请号：US740009
申请日：1996-10-23
申请人： Sandor Bajusz , Daniel Bagdy , Eva Barabas , Andras Feher , Gabriella Szabo , Gyorgyne Szell , Belane Veghelyi , Gyula Horvath , Attila Juhasz , Janosne Lavich , Laszlone Mohai , Imre Moravcsik , Gaborne Szeker , Istvan Pallagi , Katalin Palne Aranyosi
发明人： Sandor Bajusz , Daniel Bagdy , Eva Barabas , Andras Feher , Gabriella Szabo , Gyorgyne Szell , Belane Veghelyi , Gyula Horvath , Attila Juhasz , Janosne Lavich , Laszlone Mohai , Imre Moravcsik , Gaborne Szeker , Istvan Pallagi , Katalin Palne Aranyosi
IPC分类号： A61K38/00 , A61P7/02 , C07D207/16 , C07D211/60 , C07D405/06 , C07K1/06 , C07K5/06 , C07K5/078 , A61K38/05
CPC分类号： C07D405/06 , C07D207/16 , C07D211/60
摘要： This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.
摘要翻译： PCT No.PCT / HU93 / 00013 Sec。 371日期1994年12月5日第 102（e）日期1994年12月5日PCT提交1993年3月4日PCT公布。出版物WO93 / 18060 PCT 日本公开专利文献1日本公开专利文献1日本公开专利文献1日本公开专利文献1：日本专利公开公报发明内容本发明涉及通式（I）A-Xaa-Arg-H的新型肽衍生物，其中A表示D-或L-异色满-1-羰基，D-或L-异色满-3 - 羰基，此外还有通式为D-或DL-A'-CH（OH）-CO的酰基，其中A'代表苯基，苄基，1-萘基，1-萘基甲基，2-萘基，2 - 萘基甲基，9-芴基，二苯甲基，环己基，环己基甲基，2-吡啶基，3-吡啶基或4-吡啶基，Xaa表示L-脯氨酰基或L-哌啶酸残基，Arg表示L-精氨酸残基，它们与有机或无机酸形成的酸加成盐和含有它们的药物组合物。此外，本发明涉及一种制备它们的方法。本发明的化合物具有有价值的治疗，特别是抗凝血剂的性质。

3. 发明授权

US06593300B1 (3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta 失效
标题翻译：（3R）-3-氨基-4-羧基丁醛衍生物抑制白细胞介素-1 /β的释放
公开(公告)号：US06593300B1
公开(公告)日：2003-07-15
申请号：US09423006
申请日：2000-02-07
申请人： Sandor Bajusz , Iren Veghelyi , Klara Nemeth , Eva Barabas , Attila Juhasz , Jozsef Lango , Emilia Lavich , Zsuzsanna Mohai , Imre Moravcsik , Zsuzsanna Taschler , Gabor Toth
发明人： Sandor Bajusz , Iren Veghelyi , Klara Nemeth , Eva Barabas , Attila Juhasz , Jozsef Lango , Emilia Lavich , Zsuzsanna Mohai , Imre Moravcsik , Zsuzsanna Taschler , Gabor Toth
IPC分类号： A61K3800
CPC分类号： C07K7/02 , A61K38/00 , C07K5/0202
摘要： The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n=0, an &agr;-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an &agr;-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an &agr;-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q2-Q4 represent an acyl group selected from the following &agr;-hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1&bgr; converting enzyme.
摘要翻译：本发明涉及通式（I）的新的（3R）-3-氨基-4-羧基丁醛衍生物，其中X代表C1-4烷氧基羰基，任意取代的苯基 - （C 1-2烷氧基） - 羰基， 4烷基羰基或任选取代的苯基 - （C 1-3烷基） - 羰基，n表示1或0，Y表示在n = 1的情况下，通式Y4-Y3-Y2-Y1的四肽，三肽通式Y3-Y2-Y1或通式Y2-Y1的二肽或通式Y1的氨基酸残基，或在n = 0的情况下，通式为Q4-Y3-Y2的α-羟基酰基三肽 -Y1，通式为Q3-Y2-Y1的α-羟酰基二肽或通式为Q2-Y1的α-羟基酰基 - 酰基残基; 其中Y 1 -Y 4表示选自以下L-或D-氨基酸的残基：丙氨酸，异亮氨酸，环己基 - 甘氨酸，苯丙氨酸，谷氨酰胺，组氨酸，异亮氨酸，亮氨酸，赖氨酸，甲硫氨酸，哌可酸，脯氨酸，酪氨酸和缬氨酸; 和Q 2 -Q 4表示选自以下R或S构型的α-羟基酸的酰基：2-环庚基-2-羟基 - 乙酸，2-环己基-2-羟基乙酸，3-环己基乳酸，3-苯基乳酸，2-羟基-3-甲基丁酸，2-羟基-3-甲基戊酸，扁桃酸或乳酸，以及与有机或无机碱形成的盐，以及含有它们的药物组合物。本发明通式（I）的化合物是白细胞介素-1β转换酶的有价值的抑制剂。

4. 发明授权

US5241063A Process for the preparation of steroids bearing 17.alpha.-hydroxy-20-oxopregnane side chain 失效
标题翻译：制备支链17（ALPHA） - 羟基-20-氧化二苯胺侧链的方法
公开(公告)号：US5241063A
公开(公告)日：1993-08-31
申请号：US717823
申请日：1991-06-19
申请人： Andras Toro , Gabor Ambrus , Istvan Pallagi , Nandor Makk , Gyula Horvath , Ferenc Szederkenyi , Eva Ilkoy , Antonia Jekkel , Imre Moravcsik , Kalman Konczol
发明人： Andras Toro , Gabor Ambrus , Istvan Pallagi , Nandor Makk , Gyula Horvath , Ferenc Szederkenyi , Eva Ilkoy , Antonia Jekkel , Imre Moravcsik , Kalman Konczol
IPC分类号： C07J7/00 , C07J21/00
CPC分类号： C07J7/0045 , C07J21/00
摘要： The invention relates to a novel process for the preparation of 17 .alpha.-hydroxy-20-oxopregnane derivatives of the general formula (I), ##STR1## wherein R.sub.1 means a hydroxy or an oxo group; andthe dotted lines optionally represent one or more additional valence bond(s), with the proviso that the dotted line in the 4-position and the dotted line in the 5-position cannot each simultaneously be an additional valence bond from steroids having 23,24-dinor-17(20)-dehydrocholan-22-oic -22-oic acid structure.According to the process of the invention a steroid derivative having 23,24-dinorcholan-22-oic acid structure, containing a double bond in 17(20)-position, is transformed to 17.alpha., 20-epoxy-23,24-dinorcholanoic acid, the latter is converted to a reactive acid derivative, which is then reacted with a salt-containing azide ion to yield a 17.alpha., 20-epoxy-23,24-dinorcholanoic acyl azide derivative and the azide obtained is reacted with a mineral or organic acid in an aqueous medium.
摘要翻译：本发明涉及制备通式（I）的17α-羟基-20-氧代孕烷衍生物的新方法，其中R1表示羟基或氧代基; 并且虚线可选地表示一个或多个另外的价键，条件是4-位中的虚线和5-位的虚线不能同时作为具有23的类固醇的另外的价键， 24-二酮-17（20） - 脱氢胆烷-22-酸-22-酸结构。根据本发明的方法，在17（20） - 位中含有双键的具有23,24-二肌醇二十二酸结构的类固醇衍生物转化为17α，20-环氧-23,24-二肉桂酸酸，后者转化为反应性酸衍生物，然后与含盐的叠氮化物离子反应，得到17α，20-环氧-23,24-二牛油酰基叠氮化物衍生物，所得叠氮化物与矿物质反应或有机酸。

5. 发明授权

US5204343A 5H-benzodiazepin derivative 失效
标题翻译： 5H-苯并咪唑衍生物
公开(公告)号：US5204343A
公开(公告)日：1993-04-20
申请号：US776771
申请日：1991-10-17
申请人： Ferenc Andrasi , Peter Botka , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gyula Horvath , Jeno Korosi , Imre Moravcsik , Marta Rusz nee Patfalusi , Eva Tomori nee Joszt , Gabor Zolyomi
发明人： Ferenc Andrasi , Peter Botka , Katalin Goldschmidt nee Horvath , Tamas Hamori , Gyula Horvath , Jeno Korosi , Imre Moravcsik , Marta Rusz nee Patfalusi , Eva Tomori nee Joszt , Gabor Zolyomi
IPC分类号： A61K31/55 , A61P25/20 , A61P25/24 , A61P25/26 , C07D243/02 , C07D243/04
CPC分类号： C07D243/02
摘要： The invention relates to the new 1-(3-chlorophenyl)-4-hydroxymethyl-7,8-dimethoxy-5H-2,3-benzodiazepine of formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof, furthermore to a process for preparing these compounds.The compounds according to the invention possess valuable anxiolytic, antiaggressive and antidepressant effects and have at the same time favorable acute toxicity values, so they can be used to advantage in therapy.
摘要翻译：本发明涉及式（I）的新的1-（3-氯苯基）-4-羟甲基-7,8-二甲氧基-5H-2,3-苯并二氮杂及其药学上可接受的酸加成盐，此外涉及制备这些化合物的方法。根据本发明的化合物具有有价值的抗焦虑，抗侵袭和抗抑郁作用，同时具有有利的急性毒性值，因此它们可用于治疗中的优势。

6. 发明授权

US5112815A 9.alpha.-hydroxy-3-oxo-4,24(25)-stigmastadien-26-oic acid derivatives, a process for preparing same and pharmaceutical compositions containing same 失效
标题翻译： 9（ALPHA）-HYDROXY-3-OXO-4,24（25）-STIGMASTADIEN-26-酸性衍生物，其制备方法和含有其的药物组合物
公开(公告)号：US5112815A
公开(公告)日：1992-05-12
申请号：US635623
申请日：1991-02-17
申请人： Gabor Ambrus , Andrea Maderspach , Antalne Jekkel , Andras Javor , Eva Ilkoy , Gyorgy Hajos , Laszlo Szporny , Jozsef Nagy , Gyula Horvath , Imre Moravcsik
发明人： Gabor Ambrus , Andrea Maderspach , Antalne Jekkel , Andras Javor , Eva Ilkoy , Gyorgy Hajos , Laszlo Szporny , Jozsef Nagy , Gyula Horvath , Imre Moravcsik
IPC分类号： A61K31/565 , A61K31/575 , C07J1/00 , C07J9/00 , C12P33/00
CPC分类号： C07J9/005
摘要： The invention relates to novel 9.alpha.-hydroxy-3-oxo-4,24(25)-stigmastadien-26-oic acid derivatives of the formula (I), ##STR1## wherein M stands for hydrogen, C.sub.1-4 alkyl or a pharmaceutically accteptable cation to a process for repairing these compounds and to compositions containing said compounds which exert an anti-hypercholesteremic effect.
摘要翻译： PCT No.PCT / HU90 / 00033 Sec。 371日期：1991年2月17日 102（e）日期1991年2月17日PCT提交1990年5月10日PCT公布。出版物WO90 / 13559 1990年11月15日，本发明涉及式（I）的新型9α-羟基-3-氧代-4,24（25） - 蓖麻醇二异戊酸衍生物，其中M 代表氢，C 1-4烷基或药学上可接受的阳离子，用于修复这些化合物的方法和含有发挥抗高胆固醇作用的所述化合物的组合物。

7. 发明授权

US5004695A Microbiological process for preparing 9.alpha.-hydroxy-4-androstene-3,17-dione 失效
标题翻译：制备9α-羟基-4-雄甾烯-3,17-二酮的微生物过程
公开(公告)号：US5004695A
公开(公告)日：1991-04-02
申请号：US116872
申请日：1987-11-05
申请人： Antonia Jekkel nee Bokany , Karoly Albrecht , Gabor Ambrus , Tibor Lang , Istvan M. Szabo , Eva Ilkoy , Kalman Konczol , Imre Moravcsik , Gabor Hantos , Emilia Simonovits , Zsuzsanna Lengyel nee Szemenyei , Zsuzesanna Vida , Eva Csajagi
发明人： Antonia Jekkel nee Bokany , Karoly Albrecht , Gabor Ambrus , Tibor Lang , Istvan M. Szabo , Eva Ilkoy , Kalman Konczol , Imre Moravcsik , Gabor Hantos , Emilia Simonovits , Zsuzsanna Lengyel nee Szemenyei , Zsuzesanna Vida , Eva Csajagi
IPC分类号： C12N1/20 , C12P33/00 , C12P33/16 , C12R1/32
CPC分类号： C12P33/005 , Y10S435/863
摘要： The invention relates to a process for the production of 9.alpha.-hydroxy-4-androstene-3,17-dione from natural sterols of plant or animal origin or from mixtures thereof by the submerged aerobic fermentation of an enzyme-deficient, sterol-de-grading microorganism in a nutrient medium containing utilizable carbon and nitrogen sources as well as mineral salts, and by isolating the product formed, which comprises transforming the sterol or sterol mixture with the culture of a 1,2-steroid-dehydrogenase deficient strain of new Mycobacterium roseum species which is able to degrade the side-chain of natural sterols, preferably with Mycobacterium roseum sp. nov. 1108/1 deposited at the National Collection of Agricultural and Industrial Microorganisms, Budapest, Hungary under the number NCAIM B (P) 000339, and by isolating and purifying the 9.alpha.-hydroxy-4-androstene-3,17-dione obtained.
摘要翻译：本发明涉及一种由植物或动物来源的天然甾醇生产9α-羟基-4-雄甾烯-3,17-二酮的方法或其混合物，其通过潜在的需氧发酵酶缺陷型固醇在含有可利用的碳源和氮源以及无机盐的营养培养基中分解微生物，并通过分离形成的产物，其包括用新型的1,2-类固醇 - 脱氢酶缺陷菌株的培养物转化固醇或固醇混合物能够降解天然甾醇侧链的玫瑰花分枝杆菌物种，优选用玫瑰红分枝杆菌分枝杆菌。 nov。 1108/1，保藏在匈牙利布达佩斯国家农业和工业微生物收集库，编号为NCAIM B（P）000339，并通过分离和纯化得到的9α-羟基-4-雄甾烯-3,17-二酮。

8. 发明授权

US5639751A N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders 失效
标题翻译：用于治疗急性和慢性神经变性疾病的N-酰基-2,3-苯并二氮杂衍生物
公开(公告)号：US5639751A
公开(公告)日：1997-06-17
申请号：US477801
申请日：1995-06-07
申请人： Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Sandor Farkas , Katalin Goldschmidt , Tamas Hamori , Jeno Korosi , Imre Moravcsik , Istvan Tarnawa
发明人： Ferenc Andrasi , Pal Berzsenyi , Peter Botka , Sandor Farkas , Katalin Goldschmidt , Tamas Hamori , Jeno Korosi , Imre Moravcsik , Istvan Tarnawa
IPC分类号： C07D491/04 , A61K31/55 , A61K31/44
CPC分类号： C07D491/04
摘要： The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I)R stands for a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group, or by one or more halogen(s); or R is a benzoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; or R is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.1 means hydrogen; or R.sup.1 is absent when a double bond exists between the N(3) and C(4) atoms;R.sup.2 means a C.sub.1-3 alkyl group; orR.sup.1 and R.sup.2 together stand for a methylene group and no double bond is present between the N(3) and C(4) atoms;R.sup.3 means hydrogen or a C.sub.1-4 alkanoyl group;R.sup.4 represents hydrogen; a C.sub.1-6 alkanoyl group optionally substituted by a methoxy, cyano, carboxyl, amino, C.sub.1-4 alkylamino, di(C.sub.1-4 alkyl)amino, pyrrolidino, phthalimido or phenyl group or by one or more halogen(s); as well as a benzoyl, palmitoyl, cyclopropanecarbonyl, C.sub.1-5 alkylcarbamoyl or phenylcarbamoyl group; andthe dotted lines represent valence bonds optionally being present, with the proviso that no double bond exists between the N(3) and C(4) atoms when both R.sup.3 and R.sup.4 stand for hydrogen.The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.
摘要翻译：本发明涉及通式（I）的新型N-酰基-2,3-苯并二氮杂萘衍生物，其立体异构体和酸加成盐，含有它们的药物组合物及其制备方法。在通式（I）中，R代表任选被甲氧基，氰基，羧基，氨基，C 1-4烷基氨基，二（C 1-4烷基）氨基，吡咯烷子基，邻苯二甲酰亚胺基或苯基取代的C 1-6烷酰基，或通过一个或多个卤素; 或R是苯甲酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 或者当N（3）和C（4）原子之间存在双键时，R不存在; R1表示氢; 当N（3）和C（4）原子之间存在双键时，R1不存在; R2表示C1-3烷基; 或者R 1和R 2一起代表亚甲基，N（3）和C（4）原子之间不存在双键; R3表示氢或C1-4烷酰基; R4代表氢; 任选被甲氧基，氰基，羧基，氨基，C1-4烷基氨基，二（C1-4烷基）氨基，吡咯烷子基，苯二甲酰亚氨基或苯基或一个或多个卤素取代的C 1-6烷酰基; 以及苯甲酰基，棕榈酰基，环丙烷羰基，C 1-5烷基氨基甲酰基或苯基氨基甲酰基; 并且虚线表示任选存在的价键，条件是当R3和R4均代表氢时，N（3）和C（4）原子之间不存在双键。通式（I）的化合物具有有价值的中枢神经系统作用，特别是肌肉松弛剂，抗惊厥和神经保护作用。因此，它们可用于治疗中枢神经系统起源的各种疾病。

9. 发明授权

US5604223A N acyl 2 3 benzodiazepine derivatives pharmaceutical compositions containing them and process for preparing same 失效
标题翻译： N-酰基2,3-苯并二氮杂衍生物含有它们的药物组合物及其制备方法
公开(公告)号：US5604223A
公开(公告)日：1997-02-18
申请号：US423032
申请日：1995-03-21
申请人： Ferenc Andr asi , P al Berzsenyi , P eter Botka , S andor Farkas , Katalin Goldschmidt , Tam as H amori , Jen o K or osi , Imre Moravcsik , Istv an Tarnawa
发明人： Ferenc Andr asi , P al Berzsenyi , P eter Botka , S andor Farkas , Katalin Goldschmidt , Tam as H amori , Jen o K or osi , Imre Moravcsik , Istv an Tarnawa
IPC分类号： A61K31/55 , A61K20060101 , A61K31/00 , A61K31/335 , A61K31/395 , A61K31/551 , A61P9/08 , A61P9/10 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/28 , C07D20060101 , C07D243/00 , C07D243/02 , C07D247/00 , C07D317/00 , C07D317/08 , C07D317/44 , C07D491/00 , C07D491/04 , C07D491/056 , C07D493/04
CPC分类号： C07D491/04
摘要： The invention relates to novel N-acyl-2,3-benzodiazepine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I), defined in this specification, a more complete description of the compounds may be found.The compounds of the general formula (I) possess valuable central nervous system effects, particularly muscle-relaxant, anticonvulsive and neuroprotective action. Thus, they may be useful for the treatment of various diseases of central nervous system origin.
摘要翻译：本发明涉及通式（I）的新型N-酰基-2,3-苯并二氮杂衍生物，其立体异构体和酸加成盐，含有它们的药物组合物及其制备方法。在本说明书中定义的通式（I）中，可以找到更完整的化合物的描述。通式（I）的化合物具有有价值的中枢神经系统作用，特别是肌肉松弛剂，抗惊厥和神经保护作用。因此，它们可用于治疗中枢神经系统起源的各种疾病。

10. 发明授权

US5552299A Plasmids and process for producing recombinant desulphatohirudin HV-1 peptides 失效
标题翻译：重组脱硫水蛭素HV-1肽的质粒和方法
公开(公告)号：US5552299A
公开(公告)日：1996-09-03
申请号：US44506
申请日：1993-04-09
申请人： Istv an Ott , Tibor Klupp , Istv an Moln ar , Andr as Patthy , Istv an Barta , Zsuzsa Bark o n ee T oth , G abor Ambrus , J anos Sal at , Anik o Tegdes , Imre Moravcsik , Cecilia Egy ud , K arnly Albrecht , K alm an K oncz ol , Attila Vincze , Eva Barab as , Gy orgy M at e , Gy orgy B. Kiss , P eter Kiss , K alm an P olya , J anos Erdei , Eva Guly as , Erika Zilahi
发明人： Istv an Ott , Tibor Klupp , Istv an Moln ar , Andr as Patthy , Istv an Barta , Zsuzsa Bark o n ee T oth , G abor Ambrus , J anos Sal at , Anik o Tegdes , Imre Moravcsik , Cecilia Egy ud , K arnly Albrecht , K alm an K oncz ol , Attila Vincze , Eva Barab as , Gy orgy M at e , Gy orgy B. Kiss , P eter Kiss , K alm an P olya , J anos Erdei , Eva Guly as , Erika Zilahi
IPC分类号： A61K38/00 , C07K14/815 , C12N15/15 , C12N15/76 , C12P21/06 , C12N1/19 , C12N15/81
CPC分类号： C07K14/815 , C12N15/76 , A61K38/00 , C07K2319/00
摘要： The present invention relates to a process for producing recombinant desulphatohirudin by means of culturing microorganisms.Concerning the codon usage of microorganisms the synthesized nucleotide sequences were joined downstream of and in reading frame with isolated promoters and signal sequences, subsequently the expression/secretion cassettes comprising the foregoing elements were inserted into plasmid DNAs allowing the cultivation of cells under selective culture conditions. E. coli, Saccharomyces and Streptomyces species were transformed with the said recombinant plasmids to biosynthesize the thrombin inhibitor desulphatohirudin HV-1 which was then isolated and identified.The thus-produced desulphatohirudin can be used to inhibit blood coagulation.
摘要翻译：本发明涉及通过培养微生物生产重组脱硫水蛭素的方法。关于微生物的密码子使用，合成的核苷酸序列在分离的启动子和信号序列的下游和阅读框架中连接，随后将包含上述元件的表达/分泌盒插入质粒DNA中，允许在选择性培养条件下培养细胞。用所述重组质粒转化大肠杆菌，酵母属和链霉菌物种，以生物合成凝血酶抑制剂脱硫水蛭素HV-1，然后分离鉴定。由此产生的脱硫水蛭素可用于抑制血液凝固。

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