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1. 发明授权

US07560591B2 Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 失效
标题翻译：具有抗炎和免疫抑制活性的苯甲脒衍生物
公开(公告)号：US07560591B2
公开(公告)日：2009-07-14
申请号：US12112299
申请日：2008-04-30
申请人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
发明人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
IPC分类号： C07C335/16 , A61K31/17
CPC分类号： C07D213/40 , C07C257/14 , C07C279/18 , C07C279/36 , C07C335/20 , C07C2601/14 , C07C2603/74 , C07D209/14 , C07D209/40 , C07D277/48
摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “—A—NH—” group.
摘要翻译：可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳的烷基原子和氨基，未取代或被硝基或甲基取代，R 2独立地选自氢，具有1至4个碳原子的烷基，甲氧基，乙氧基，丙氧基，单 - ，双 - 或具有5至12个碳原子的三环环烷烃残基，未被取代或被甲基，甲氧基，羟基，氨基或卤素基团取代的金刚烷基，芳基，萘基或杂环基，R3和R4独立地选自氢和烷基具有1至3个碳原子的基团，R 5表示独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n为0至6的整数，并且脒基为t 他相对于“-A-NH-”组的对位或间位。

2. 发明申请

US20080207764A1 Novel Benzamidine Derivatives Having Anti-Inflammatory and Immunosuppressive Activity 失效
标题翻译：具有抗炎和免疫抑制活性的新型苯甲脒衍生物
公开(公告)号：US20080207764A1
公开(公告)日：2008-08-28
申请号：US12112299
申请日：2008-04-30
申请人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
发明人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Claudio Rovati
IPC分类号： A61K31/155 , C07C257/10
CPC分类号： C07D213/40 , C07C257/14 , C07C279/18 , C07C279/36 , C07C335/20 , C07C2601/14 , C07C2603/74 , C07D209/14 , C07D209/40 , C07D277/48
摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH-” group.
摘要翻译：可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳原子的烷基和未被取代或被硝基或甲基取代的氨基，R 2独立地选自氢，具有1至4个碳的烷基原子，甲氧基，乙氧基，丙氧基，具有5至12个碳原子的单环，双环或三环环烷烃残基，金刚烷基，芳基，萘基或杂环基，未取代或被甲基，甲氧基，羟基，氨基或卤素基团，R 3和R 4独立地选自氢和具有1至3个碳原子的烷基，R 5，代表独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n是a 整数为0至6，脒基为相对于“-A-NH-”基的对位或间位。

3. 发明申请

US20070135523A1 Novel benzamidine derivatives having anti-inflammatory and immunosuppressive activity 审中-公开
标题翻译：具有抗炎和免疫抑制活性的新型苯甲脒衍生物
公开(公告)号：US20070135523A1
公开(公告)日：2007-06-14
申请号：US11652675
申请日：2007-01-12
申请人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Rovati
发明人： Francesco Makovec , Simona Zanzola , Roberto Artusi , Lucio Rovati
IPC分类号： A61K31/165 , A61K31/16 , C07C275/42
CPC分类号： C07D213/40 , C07C257/14 , C07C279/18 , C07C279/36 , C07C335/20 , C07C2601/14 , C07C2603/74 , C07D209/14 , C07D209/40 , C07D277/48
摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH—” group.
摘要翻译：可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳原子的烷基和未被取代或被硝基或甲基取代的氨基，R 2独立地选自氢，具有1至4个碳的烷基原子，甲氧基，乙氧基，丙氧基，具有5至12个碳原子的单环，双环或三环环烷烃残基，金刚烷基，芳基，萘基或杂环基，未取代或被甲基，甲氧基，羟基，氨基或卤素基团，R 3和R 4独立地选自氢和具有1至3个碳原子的烷基，R 5，代表独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n是a 整数为0至6，脒基为相对于“-A-NH-”基的对位或间位。

4. 发明授权

US5744607A Basic derivatives of glutamic acid and aspartic acid as gastrin or cholecystokinin antagonists 失效
标题翻译：谷氨酸和天冬氨酸作为胃泌素或胆囊收缩素拮抗剂的基本衍生物
公开(公告)号：US5744607A
公开(公告)日：1998-04-28
申请号：US733568
申请日：1996-10-18
申请人： Francesco Makovec , Lucio C. Rovati , Luigi A. Rovati
发明人： Francesco Makovec , Lucio C. Rovati , Luigi A. Rovati
IPC分类号： C07D295/12 , A61K31/40 , A61K31/435 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P13/02 , A61P13/06 , A61P15/00 , A61P25/00 , A61P25/22 , A61P27/02 , A61P27/12 , A61P43/00 , C07C237/22 , C07D207/09 , C07D207/14 , C07D215/54 , C07D217/06 , C07D221/20 , C07D295/13 , C07D295/18 , C07D295/185 , C07D401/12 , C07D405/12 , C07D453/02 , C07D209/54 , C07D401/06
CPC分类号： C07D295/185 , C07C237/22 , C07D207/14 , C07D295/13 , C07D453/02 , C07C2103/74
摘要： The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.
摘要翻译：本发明涉及由式（I）表示的谷氨酸和天冬氨酸衍生物：由未取代的，单取代或二取代的苯基，未取代的，单取代或二取代的苯基氨基，2（β），和杂环，单环和二环基团; R2选自杂环螺基，氨基烷基金刚烷基，烷基氨基，C4-C10环烷基氨基和二环氨基（缩合）; R3是H，CH3或C2H5; A是具有1至4个碳原子的键或直链或支链亚烷基; W是叔氨基或杂环基; 并且r为1或2.化合物对胃泌素和缩胆囊素具有有效的拮抗作用，可用于治疗与胃泌素，胆囊收缩素或与其相关的其它生物活性多肽的生理水平不平衡相关的疾病。

5. 发明授权

US5723494A Derivatives of glutamic and aspartic acids, a method of preparing them, and their use as drugs for enhancing memory and learning 失效
标题翻译：谷氨酸和天冬氨酸的衍生物，其制备方法及其作为增强记忆和学习药物的用途
公开(公告)号：US5723494A
公开(公告)日：1998-03-03
申请号：US513964
申请日：1995-09-11
申请人： Francesco Makovec , Walter Peris , Lucio C. Rovati , Luigi A. Rovati
发明人： Francesco Makovec , Walter Peris , Lucio C. Rovati , Luigi A. Rovati
IPC分类号： C07D295/14 , A61K31/195 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/24 , A61P25/26 , A61P25/28 , C07C231/12 , C07C237/06 , C07C237/22 , C07C237/24 , C07D209/02 , C07D217/06 , C07D221/20 , C07D295/185 , A61K31/16
CPC分类号： C07D221/20 , C07C237/06 , C07C237/22 , C07C237/24 , C07D209/02 , C07D217/06 , C07D295/185 , C07C2101/08 , C07C2101/14 , C07C2101/18 , C07C2102/28 , C07C2102/42 , C07C2103/74
摘要： Compounds represented by general formula (I) and (II), in which r is 1 or 2, R.sub.2 and R.sub.3 are selected independently from H, CH.sub.3, C.sub.2 H.sub.5 and CHO, provided that R.sub.2 and R.sub.3 are not simultaneously CHO, and in which R.sub.1 is selected from: an aminoalkyl adamantyl group, a monocyclic aminoalkyl group, a dicyclic aminospiro group, a dicyclic amino group (orthofused), a dicyclic amino group, and azacycloalkyl group, an azadicyclic group (orthofused), a dicyclic azaspiro group, and azadicyclic group, and azacycloalkyl group, and a linear or branched aminoalkyl group.
摘要翻译： PCT No.PCT / EP94 / 00604 Sec。 371 1995年9月11日第 102（e）日期1995年9月11日PCT 1994年3月2日PCT公布。公开号WO94 / 20454 1994年9月15日由通式（I）和（II）表示的化合物，其中r为1或2，R2和R3独立地选自H，CH3，C2H5和CHO，条件是R2和R3不同时为CHO ，其中R1选自：氨基烷基金刚烷基，单环氨基烷基，二环氨基螺旋基，二环氨基（orthofused），二环氨基和氮杂环烷基，氮杂双环基（orthofused），二环氮杂螺环基和氮杂双环基，氮杂环烷基和直链或支链氨基烷基。

6. 发明授权

US5602179A Optically-active derivatives of (R) 5-pentylamino-5-oxopentanoic acid with antagonistic activity towards cholecystokinin and a method for their preparation 失效
标题翻译：具有拮抗胆囊收缩素活性的（R）5-戊基氨基-5-氧代戊酸的光学活性衍生物及其制备方法
公开(公告)号：US5602179A
公开(公告)日：1997-02-11
申请号：US352818
申请日：1994-12-01
申请人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
发明人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
IPC分类号： C07C231/00 , A61K31/195 , A61P1/00 , A61P25/00 , A61P25/08 , C07C231/02 , C07C231/18 , C07C233/12 , C07C233/83 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/22
CPC分类号： A61K31/195 , C07C231/02 , C07C233/12 , C07C233/83 , C07C237/00
摘要： There are described optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorophenyl and 3,4-dimethylphenyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.
摘要翻译：描述了具有对缩胆囊素的拮抗作用的（R）5-戊基氨基-5-氧代戊酸及其药学上可接受的盐的光学活性衍生物，并具有下式：其中R1选自第2组 - 萘基，3,4-二氯苯基和3,4-二甲基苯基，R 2是具有4个碳原子的戊基或烷氧基烷基，其中中心手性基团上的取代基（在式（I）中用星号表示），具有R（直肠）构象。

7. 发明授权

US4978683A Proglumide and pharmaceutical compositions containing it for use in the treatment of neoplastic affections 失效
标题翻译：含有它的药物组合物和药物组合物用于治疗肿瘤性感染
公开(公告)号：US4978683A
公开(公告)日：1990-12-18
申请号：US900152
申请日：1986-08-13
申请人： Angelo L. Rovati , Claudio L. Rovati , Francesco Makovec
发明人： Angelo L. Rovati , Claudio L. Rovati , Francesco Makovec
IPC分类号： A61K31/195 , A61K31/165 , A61P35/00
CPC分类号： A61K31/165
摘要： This inventions relates to a method of treating malignant tumors of the pancreatic, colic or gastric origin whose growth is increase by bioactive polypeptides comprising administering an anti-tumor effective amount of proglumide or pharmaceutical acceptables salt thereof to a patient afflicted with said malignant tumors.
摘要翻译： PCT No.PCT / EP85 / 00673 Sec。 371日期1986年8月13日 102（e）日期1986年8月13日PCT提交1985年12月5日PCT公布。出版物WO86 / 03968 日期1986年7月17日。本发明涉及一种治疗胰腺，绞痛或胃起源的恶性肿瘤的方法，其生长由生物活性多肽增加，包括向患者施用抗肿瘤有效量的γ-葡聚糖或其药物可接受的盐患有恶性肿瘤。

8. 发明授权

US4895856A Derivatives of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids with antagonistic activity towards cholecystokinin 失效
标题翻译：对胆囊收缩素具有拮抗作用的5-戊基氨基-5-氧代戊酸和4-戊基氨基-4-氧代丁酸的衍生物
公开(公告)号：US4895856A
公开(公告)日：1990-01-23
申请号：US280857
申请日：1988-12-07
申请人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
发明人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
IPC分类号： A61K31/195 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61P1/00 , A61P25/00 , A61P43/00 , C07C231/00 , C07C231/02 , C07C237/06 , C07C237/08 , C07C237/22 , C07D209/42 , C07D215/48 , C07D215/54 , C07D307/84 , C07D307/85 , C07D333/68 , C07D333/70
CPC分类号： C07D215/48 , C07D209/42 , C07D307/84 , C07D307/85 , C07D333/70
摘要： New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

9. 发明授权

US4826878A New derivatives of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids with antagonistic activity towards cholecystokinin 失效
标题翻译：对缩胆囊素具有拮抗作用的5-戊基氨基-5-氧代戊酸和4-戊基氨基-4-氧代丁酸的新衍生物
公开(公告)号：US4826878A
公开(公告)日：1989-05-02
申请号：US133844
申请日：1987-12-16
申请人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
发明人： Francesco Makovec , Rolando Chiste , Walter Peris , Luigi Rovati
IPC分类号： A61K31/195 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61P1/00 , A61P25/00 , A61P43/00 , C07C231/00 , C07C231/02 , C07C237/06 , C07C237/08 , C07C237/22 , C07D209/42 , C07D215/48 , C07D215/54 , C07D307/84 , C07D307/85 , C07D333/68 , C07D333/70 , C07C101/42
CPC分类号： C07D215/48 , C07D209/42 , C07D307/84 , C07D307/85 , C07D333/70
摘要： New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutasnoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl.The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

10. 发明授权

US4791215A Derivatives of glutamic acid and aspartic acid 失效
标题翻译：谷氨酸和天冬氨酸的衍生物
公开(公告)号：US4791215A
公开(公告)日：1988-12-13
申请号：US746065
申请日：1985-06-18
申请人： Luigi Rovati , Francesco Makovec , Rolando Chiste' , Paolo Senin
发明人： Luigi Rovati , Francesco Makovec , Rolando Chiste' , Paolo Senin
IPC分类号： A23K1/16 , A61K31/195 , A61K31/445 , A61K31/535 , C07C233/12 , C07C255/49 , C07C255/51 , C07C255/56 , C07D295/18 , C07D295/185 , C07D307/66 , C07D309/32 , C07C121/52 , A61K31/275
CPC分类号： C07D295/185 , C07C255/00 , C07D307/66 , C07D309/32
摘要： New derivatives of D,L-glutamic acid and D,L-aspartic acid are described having the formulae: ##STR1## in which n is equal to 1 or 2, R.sub.1 is a phenyl group mono-, di- or tri-substituted with linear or branched C.sub.1 -C.sub.4 alkyl groups, which may be the same or different, or with halogens, with a cyano group or a trifluoromethyl group, and in which R.sub.2 is selected from the group consisting of morpholino, piperidino and amino with one or two linear, branched or cyclic alkyl group substituents containing from 1 to 8 carbon atoms, which may be the same or different, or a pharmaceutically-acceptable salt thereof.The compounds have an antagonistic activity towards bioactive polypeptides and are useful particularly in the treatment of illnesses of the digestive system and the central nervous system, as pain killers, and for the treatment of anorexia and all those affections (for example tumours) in which exogenous or endogenous bioactive polypeptides are involved.
摘要翻译：描述了D，L-谷氨酸和D，L-天冬氨酸的新衍生物，其具有下式：其中n等于1或2，其中R 1是苯基单 - 可以相同或不同的直链或支链C 1 -C 4烷基二取代或三取代，或与卤素一起用氰基或三氟甲基取代，并且其中R2选自吗啉代，哌啶子基和氨基，其具有一个或两个含有1至8个碳原子的直链，支链或环状烷基取代基，其可以相同或不同，或其药学上可接受的盐。这些化合物对生物活性多肽具有拮抗作用，特别用于治疗消化系统和中枢神经系统的疾病，作为止痛药，以及用于治疗厌食症和所有这些感染（例如肿瘤），其中外源性或内源性生物活性多肽。

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