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1. 发明授权

US5288855A Extracellular form of the human fibroblast growth factor receptor 失效
标题翻译：人成纤维细胞生长因子受体的细胞外形式
公开(公告)号：US5288855A
公开(公告)日：1994-02-22
申请号：US997133
申请日：1992-12-28
申请人： Laura Bergonzoni , Guy Mazue , Antonella Isacchi , Romeo Roncucci , Paolo Sarmientos
发明人： Laura Bergonzoni , Guy Mazue , Antonella Isacchi , Romeo Roncucci , Paolo Sarmientos
IPC分类号： A61K38/00 , A61K47/48 , C07K14/71 , C12P21/06 , A01N37/18 , A61K37/24 , C07K3/00
CPC分类号： C07K14/71 , A61K47/48269 , A61K38/00
摘要： The present invention provides a polypeptide which is capable of binding specifically human basic fibroblast growth factor and human acidic fibroblast growth factor, a DNA sequence which encodes the polypeptide of the invention and a vector which incorporates a DNA sequence of the invention and which is capable, when provided in a transformed host, of expressing the polypeptide of the invention encoded by the DNA sequence. A host transformed with such a vector forms part of the invention also.
摘要翻译：本发明提供能够特异性结合人碱性成纤维细胞生长因子和人酸性成纤维细胞生长因子的多肽，编码本发明多肽的DNA序列和含有本发明DNA序列的载体，当提供在转化的宿主中时，表达由DNA序列编码的本发明的多肽。用这种载体转化的宿主也构成了本发明的一部分。

2. 发明授权

US5236957A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译：取代（α-氨基）氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5236957A
公开(公告)日：1993-08-17
申请号：US646596
申请日：1991-01-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

3. 发明授权

US4474977A Amino-alcohol derivatives 失效
标题翻译：氨基醇衍生物
公开(公告)号：US4474977A
公开(公告)日：1984-10-02
申请号：US901223
申请日：1978-04-28
申请人： Georges Lambelin , Romeo Roncucci , Joseph Roba , Claude Gillet , Michel Snyers
发明人： Georges Lambelin , Romeo Roncucci , Joseph Roba , Claude Gillet , Michel Snyers
IPC分类号： A61K31/135 , A61K31/215 , A61P3/06 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/20 , C07C45/71 , C07C67/00 , C07C219/22 , C07C225/16 , C07C313/00 , C07C323/32 , C07C69/76
CPC分类号： C07C323/32 , C07C45/71 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： The new amino-alcohol derivatives according to the invention have the formula: ##STR1## wherein: (a) R.sub.1 is hydrogen, an alkylthio C.sub.1 -C.sub.5 radical, a cycloalkylthio C.sub.5 -C.sub.6 radical, an alkoxy C.sub.1 -C.sub.5 radical, a cycloalkyloxy C.sub.5 -C.sub.6 radical, an alkyl C.sub.1 -C.sub.5 radical, a cycloalkyl C.sub.5 -C.sub.6 radical or a halogen atom;(b) R.sub.2 is a lower alkyl C.sub.1 -C.sub.3 radical;(c) R.sub.3 is an alkyl C.sub.1 -C.sub.18 radical, substituted or not, an alkenyl C.sub.6 -C.sub.18 radical substituted or not, a cycloalkyl C.sub.5 -C.sub.9 radical;(d) R.sub.4 is an acyl group having the formula: ##STR2## in which R.sub.5 represents an alkyl C.sub.1 -C.sub.10 substituted or not, an alkenyl C.sub.2 -C.sub.4, a cycloalkyl C.sub.3 -C.sub.8, a phenyl substituted or not or a cinnamyl radical, R.sub.4 being hydrogen if R.sub.1 is hydrogen, an alkyl, alkoxy, cycloalkoxy or cycloalkyl radical or a halogen atom.
摘要翻译：根据本发明的新的氨基醇衍生物具有下式：其中：（a）R 1是氢，烷硫基C 1 -C 5基，环烷硫基C 5 -C 6基，烷氧基C 1 -C 5基，环烷氧基C5-C6基，烷基C1-C5基，环烷基C5-C6基或卤原子; （b）R2是低级烷基C1-C3基; （c）R3是烷基C1-C18基团，取代或不取代或不取代环烷基C5-C9基团的烯基C6-C18基团; （d）R4是具有下式的酰基：其中R 5表示被取代或未被取代的C 1 -C 10烷基，烯基C 2 -C 4，环烷基C 3 -C 8，被取代或未取代的苯基或肉桂基，如果R 1是氢，烷基，烷氧基，环烷氧基或环烷基或卤素原子，则R4是氢。

4. 发明申请

US20050095685A1 Anti-hirudin polyclonal antibodies and their use for the identification, immunopurification and quantitative determination of hirudin 审中-公开
标题翻译：抗水蛭素多克隆抗体及其用于水蛭素鉴定，免疫纯化和定量测定的应用
公开(公告)号：US20050095685A1
公开(公告)日：2005-05-05
申请号：US10767200
申请日：2004-01-30
申请人： Antonio Molinari , Marco Gerna , Carla Giorgetti , Jacqueline Lansen , Romeo Roncucci
发明人： Antonio Molinari , Marco Gerna , Carla Giorgetti , Jacqueline Lansen , Romeo Roncucci
IPC分类号： C07K14/815 , C07K16/38 , C07K16/18 , C12P21/04
CPC分类号： C07K16/38 , C07K14/815 , Y10S530/855
摘要： A method of producing an immunogen comprising polymerizing a hirudin and/or a hirudin-like protein is provided. A method of producing an antibody specific for a hirudin or a hirudin-like protein is also provided.
摘要翻译：提供一种产生包含聚合水蛭素和/或水蛭素样蛋白质的免疫原的方法。还提供了产生对水蛭素或水蛭素样蛋白质特异性抗体的方法。

5. 发明授权

US5502079A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
公开(公告)号：US5502079A
公开(公告)日：1996-03-26
申请号：US343853
申请日：1994-11-17
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32 , A61K31/165
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

6. 发明授权

US4704450A Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides 失效
标题翻译：液相中的hpGRF（somatocrinin）和中间体肽的合成
公开(公告)号：US4704450A
公开(公告)日：1987-11-03
申请号：US807691
申请日：1985-12-11
申请人： Joseph Diaz , Henri Demarne , Romeo Roncucci , Paul-Henry Schmelck
发明人： Joseph Diaz , Henri Demarne , Romeo Roncucci , Paul-Henry Schmelck
IPC分类号： A61K38/00 , C07K5/062 , C07K5/068 , C07K5/072 , C07K5/083 , C07K5/107 , C07K5/113 , C07K7/06 , C07K14/60 , C07K7/10 , C07K5/08 , C07K5/10
CPC分类号： C07K7/06 , C07K14/60 , C07K5/06043 , C07K5/06069 , C07K5/06104 , C07K5/06113 , C07K5/0804 , C07K5/1016 , C07K5/1021 , A61K38/00 , Y10S930/12
摘要： The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
摘要翻译：本发明涉及在液相和中间肽中合成hpGRF（somatocrinin），其包括：一个接一个地并按照GRF序列顺序偶联其中：（a）侧酸功能的赖氨酸的天冬氨酸和谷氨酸和侧胺的功能受到Boc组脱保护条件稳定的保护基保护，（b）精氨酸的胍官能团被质子化保护，（c）N- 末端氨基酸被Boc保护在胺上; 通过用三氟乙酸水解，选择性地从氨基末端胺中除去基团Boc的延伸相，所述偶联在非质子极性溶剂中进行，并且在序列结束时通过水解将所有保护基团除去帮助0.1至1M甲磺酸或三氟甲磺酸在三氟乙酸中的溶液。

7. 发明授权

US4501747A Certain amide derivatives of 2-guanidino-thiazoles and compositions containing same 失效
标题翻译： 2-胍基 - 噻唑的某些酰胺衍生物和含有它们的组合物
公开(公告)号：US4501747A
公开(公告)日：1985-02-26
申请号：US489723
申请日：1983-04-29
申请人： Dino Nisato , Sergio Boveri , Romeo Roncucci , Paolo Carminati
发明人： Dino Nisato , Sergio Boveri , Romeo Roncucci , Paolo Carminati
IPC分类号： C07D277/48 , C07D417/12 , C07D411/12 , C07D263/28
CPC分类号： C07D417/12 , C07D277/48
摘要： Amides acting as histamine H.sub.2 receptors antagonists, of formula ##STR1## wherein X represents a N.fwdarw.O or C-NH-A-B group in which A is CO or SO.sub.2 and B is alkyl, phenyl, pyridyl, pyridyl 1-oxide, pyrazinyl or thienyl; their salts; process for their preparation by reacting 2-(2-guanidinothiazol-4-ylmethylthio)ethylamine with a derivative of formula ##STR2## and optional salification; and pharmaceutical compositions containing same.
摘要翻译：作为组胺H 2受体拮抗剂的酰胺，其中X代表N-或O-C-NH-AB基团，其中A是CO或SO2，B是烷基，苯基，吡啶基，吡啶基1-氧化物，吡嗪基或噻吩基; 他们的盐 2-（2-胍基噻唑-4-基甲硫基）乙胺与式“IMAGE”的衍生物反应制备方法和任选的成盐方法; 和含有它们的药物组合物。

8. 发明授权

US06719975B1 Anti-hirudin polyclonal antibodies and their use for the identification, immunopurification and quantitative determination of hirudin 失效
标题翻译：抗水蛭素多克隆抗体及其用于水蛭素鉴定，免疫纯化和定量测定的应用
公开(公告)号：US06719975B1
公开(公告)日：2004-04-13
申请号：US08603182
申请日：1996-02-20
申请人： Antonio Molinari , Marco Gerna , Carla Giorgetti , Jacqueline Lansen , Romeo Roncucci
发明人： Antonio Molinari , Marco Gerna , Carla Giorgetti , Jacqueline Lansen , Romeo Roncucci
IPC分类号： A61K3900
CPC分类号： C07K16/38 , C07K14/815 , Y10S530/855
摘要： A method of making antibodies to hirudin by immunizing with an immunogenic composition containing polymerized hirudin monomers in the absence of carrier protein is taught.
摘要翻译：教导了在不存在载体蛋白的情况下用含有聚合水蛭素单体的免疫原性组合物免疫水蛭素抗体的方法。

9. 发明授权

US5391577A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译： N-苯基烷基取代的α-氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5391577A
公开(公告)日：1995-02-21
申请号：US065888
申请日：1993-05-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32 , A61K31/165
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.
摘要翻译：式（I）的N-苯基烷基取代的α-氨基甲酰胺衍生物其中R为C1-C8烷基，C3-C8环烷基，呋喃基，噻吩基，吡啶基或未取代或取代的苯基; A是 - （CH 2）m - 或 - （CH 2）p -X-（CH 2）q-基，其中X是-O - ， - S-或-NR 4 - ; R1，R2，R3，R'3，R4，n，m，p和q如本文所定义; 并且R 5和R 6各自独立地为氢或C 1 -C 6烷基，并且其药学上可接受的盐在中枢神经系统上具有活性，可用作抗癫痫药，抗帕金森综合征，神经保护药，抗抑郁药，抗痉挛药和/或哺乳动物催眠药。

10. 发明授权

US4639468A Derivatives of glycinamide, their preparation and their use 失效
标题翻译：甘氨酰胺的衍生物，其制备及其用途
公开(公告)号：US4639468A
公开(公告)日：1987-01-27
申请号：US768185
申请日：1985-08-23
申请人： Romeo Roncucci , Claude L. Gillet , Alexis H. Cordi , Mark A. Martens , Joseph L. Roba , Paul J. Niebes , Georges E. Lambelin , William R. Van Dorsser
发明人： Romeo Roncucci , Claude L. Gillet , Alexis H. Cordi , Mark A. Martens , Joseph L. Roba , Paul J. Niebes , Georges E. Lambelin , William R. Van Dorsser
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/205 , C07C233/00 , C07C233/12 , C07C233/30 , C07C237/00 , C07C271/06 , C07C271/22
CPC分类号： C07C255/00 , C07C271/22
摘要： A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.sub.6, a benzoyl group, a linear or ramified alkoxycarbonyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8, a carboxamidomethyl group,R.sub.2 represents hydrogen, a linear or ramified alkyl C.sub.1, C.sub.2, C.sub.3, a phenyl group,R.sub.3 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8, a phenyl group, optionally substituted by a halogen atom, such as fluorine, chlorine or bromine,R.sub.4 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7 or C.sub.8 as well as salts of these derivatives with non toxic and pharmaceutically usable acids.
摘要翻译：通式I的甘氨酰胺衍生物：其中：R是直链或支链烷基C5-C18，直链或支链烯基C5，C6，C7，C8，C9，C10，C11，C12 C13，C14，C15，C16，C17或C18，直链或支链炔基C4-C10，线性或分枝酰基C4-C18，被苯氧基取代的直链或支链烷基C1-C10，由羟基自由基，乙酰氧基，羧基，直链或分支的烷氧羰基C1-C4，羰基，羧醛基，缩醛或鲸蜡基，一个或多个苯基，被一个或多个被卤素原子如氟，氯或溴取代的苯基，R 1表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7，C8，C9或C10，线性或分支酰基C 1 -C 6，苯甲酰基，直链或支链烷氧基羰基C1，C2，C3，C4，C5，C6，C7或C8，羧酰胺基甲基，R2表示氢，线性或柱塞烷基C1，C2，C3，苯基，R3表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7或C8，任选被卤素原子取代的苯基，作为氟，氯或溴，R 4表示氢，直链或支链烷基C1，C2，C3，C4，C5，C6，C7或C8，以及这些衍生物与无毒和可药用酸的盐。

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