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1. 发明授权

US4636490A Novel peptidic derivatives inhibiting gastric secretion, process for preparing them and drugs containing them 失效
标题翻译：抑制胃分泌的新型肽衍生物，其制备方法和含有它们的药物
公开(公告)号：US4636490A
公开(公告)日：1987-01-13
申请号：US597427
申请日：1984-04-06
申请人： Jean Martinez , Jean-Pierre Bali , Bertrand Castro , Dino Nisato , Henri Demarne
发明人： Jean Martinez , Jean-Pierre Bali , Bertrand Castro , Dino Nisato , Henri Demarne
IPC分类号： A61K38/22 , A61K38/00 , A61P1/00 , C07K7/06 , C07K14/595 , A61K37/43
CPC分类号： C07K14/595 , A61K38/00
摘要： The invention relates to peptides of general formula:R--A--Gly--Trp--B--Asp--NH.sub.2 (I)in which:Asp NH.sub.2 represents the amide in .alpha. position of the aspartic acid of formula: ##STR1## R represents hydrogen, a protector group of the terminal amine function such as t.butyloxy carbonyl (BOC), benzyloxy carbonyl (Z), lower alkanoyl,A designates:either tyrosine, tyrosine-O-sulfate, threonine or methionine;or a dipeptide selected from: --Ala--TYR--, --TYR--Thr--, --TYR Met--, TYR designating either of the 2 amino-acids tyrosine or tyrosine-O-sulfate;or a tripeptide selected from: --Glu--Ala--TYR--, Asp--TYR--Thr--, --Asp--TYR--MET--;or a tetrapeptide selected from: --Glu--Glu--Ala--TYR--, --Gln Asp--TYR--Thr--, --Arg--ASP--TYR--Met--;or a pentapeptide selected from: --Glu--Glu--Glu--Ala--TYR--, --Pyr--Gln--Asp--TYR--Thr--, --Asp--Arg--Asp--TYR--Met;B designates methionine, leucine or norleucine.
摘要翻译：本发明涉及通式为：RA-Gly-Trp-B-Asp-NH 2（I）的肽，其中：Asp NH 2表示式中天冬氨酸的α位置的酰胺：R表示氢，保护基末端胺官能团如叔丁氧基羰基（BOC），苄氧基羰基（Z），低级烷酰基，A表示：酪氨酸，酪氨酸-O-硫酸盐，苏氨酸或甲硫氨酸; 或选自以下的二肽：-Ala-TYR-，-TYR-Thr-，-TYR Met-，TYR，其指定2个氨基酸酪氨酸或酪氨酸-O-硫酸盐中的任一个; 或选自以下的三肽：-Glu-Ala-TYR-，Asp-TYR-Thr-，-Asp-TYR-MET-; 或选自以下的四肽：-Glu-Glu-Ala-TYR-，-Gln Asp-TYR-Thr-，-Arg-ASP-TYR-Met-; 或选自以下的五肽：-Glu-Glu-Glu-Ala-TYR-，-Pyr-Gln-Asp-TYR-Thr-，-Asp-Arg-Asp-TYR-Met; B表示甲硫氨酸，亮氨酸或正亮氨酸。

2. 发明授权

US4687759A Tripeptide and tetrapeptide esters which inhibit gastric secretion, process for their preparation and pharmaceutical compositions in which they are present 失效
标题翻译：抑制胃分泌的三肽和四肽酯，其制备方法及其存在的药物组合物
公开(公告)号：US4687759A
公开(公告)日：1987-08-18
申请号：US808959
申请日：1985-12-16
申请人： Jean Martinez , Jean-Pierre Bali , Richard Magous , Bertrand Castro , Henri Demarne
发明人： Jean Martinez , Jean-Pierre Bali , Richard Magous , Bertrand Castro , Henri Demarne
IPC分类号： C07K5/08 , A61K38/00 , A61P1/00 , C07K5/097 , C07K5/10 , C07K14/575 , A61K37/43
CPC分类号： C07K5/0821 , Y02P20/55
摘要： The invention relates to the peptides of the formula: ##STR1## in which: R represents hydrogen or a protecting group for the terminal amine group, such as t-butoxycarbonyl (Boc), benzyloxycarbonyl (Z) or lower alkanoyl;X.sub.1 represents either beta-Ala or a direct bond between R and the terminal amine group of the amino acid TRP;TRP denotes either the L isomer or the D isomer of tryptophan;X.sub.2 represents L-leucine, L-methionine or L-norleucine; andY denotes hydrogen, a halogen atom (preferably fluorine or chlorine), a trifluoromethyl group, a cyano group or a nitro group.These peptides inhibit gastric secretion.
摘要翻译：本发明涉及下式的肽：其中：R表示氢或末端胺基的保护基，如叔丁氧基羰基（Boc），苄氧羰基（Z）或低级烷酰基; X1表示β-Ala或R与氨基酸TRP的末端胺基之间的直接键; TRP表示色氨酸的L异构体或D异构体; X2表示L-亮氨酸，L-甲硫氨酸或L-正亮氨酸; Y表示氢，卤素原子（优选氟或氯），三氟甲基，氰基或硝基。这些肽抑制胃分泌。

3. 发明授权

US4687760A Reduced peptides which inhibit gastric secretion, process for their preparation and pharmaceutical compositions in which they are present 失效
标题翻译：抑制胃分泌的减少肽，其制备方法及其存在的药物组合物
公开(公告)号：US4687760A
公开(公告)日：1987-08-18
申请号：US809131
申请日：1985-12-16
申请人： Jean Martinez , Jean-Pierre Bali , Richard Magous , Bertrand Castro , Henri Demarne
发明人： Jean Martinez , Jean-Pierre Bali , Richard Magous , Bertrand Castro , Henri Demarne
IPC分类号： C07K1/113 , A61K38/00 , A61P1/00 , C07K5/06 , C07K5/072 , A61K37/43 , C07K5/02 , C07K5/08 , C07K5/10
CPC分类号： C07K5/06113 , Y02P20/55
摘要： The invention relates to the peptides of the formula: ##STR1## in which: R.sub.1 represents hydrogen or a protecting group for the amine group, such as t-butoxycarbonyl, benzyloxycarbonyl or lower alkanoyl groups;X represents beta-alanine glycine or a direct bond between R.sub.1 and the amine group; andR.sub.2 represents a group chosen from: ##STR2## corresponding to the side chains of the natural amino acid leucine, methionine and norleucine.These peptides inhibit gastric secretion.
摘要翻译：本发明涉及下式的肽：其中：R1代表氢或胺基的保护基，如叔丁氧基羰基，苄氧基羰基或低级烷酰基; X表示β-丙氨酸甘氨酸或R1与胺基之间的直接键; 并且R 2表示选自对应于天然氨基酸亮氨酸，甲硫氨酸和正亮氨酸的侧链的。这些肽抑制胃分泌。

4. 发明授权

US4694015A Pharmaceutical or veterinary compositions containing thiosulfonate derivatives 失效
标题翻译：含有硫代磺酸衍生物的药物或兽药组合物
公开(公告)号：US4694015A
公开(公告)日：1987-09-15
申请号：US797486
申请日：1985-11-13
申请人： Bernard Sebille , Yves Beuzard , Henri Demarne
发明人： Bernard Sebille , Yves Beuzard , Henri Demarne
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/433 , A61K31/47 , A61P7/00 , A61P33/00 , A61P33/02 , C07D215/36 , C07D233/84 , C07D235/28 , C07D263/58 , C07D277/16 , C07D277/40 , C07D285/12 , C07D285/125
CPC分类号： C07D263/58 , C07D215/36 , C07D233/84 , C07D235/28 , C07D277/16 , C07D285/125
摘要： The invention relates to pharmaceutical or veterinary compositions for initing the malformation or destruction of red blood corpuscules due to a genetic modification of haemoglobin or to parasites, compositions comprising, as active ingredient, at least one thiosulfonate derivative of general formula:R--S--SO.sub.2 --R.sub.1in which R represents a 1-methyl-imidazol-2-yl, 1H-benzimidazol-2-yl or benzoxazol-2-yl radical and R.sub.1 represents a lower alkyl, (hydroxy) lower alkyl, lower alkanoyl, phenyl, (lower alkyl) phenyl, (hydroxy lower alkyl) phenyl, (lower alkanoyl) phenyl or quinolin-8-yl radical.The compositions in question can be used in the treatment of drepanocytosis, malaria and babebiosis.
摘要翻译：本发明涉及用于抑制由于血红蛋白或寄生虫的遗传修饰导致的红血球的畸形或破坏的药物或兽用组合物，所述组合物包含作为活性成分的至少一种通式为RS-SO 2 -R 1的硫代磺酸酯衍生物其中R表示1-甲基 - 咪唑-2-基，1H-苯并咪唑-2-基或苯并恶唑-2-基，R 1表示低级烷基，（羟基）低级烷基，低级烷酰基，苯基，（低级烷基）苯基，（羟基低级烷基）苯基，（低级烷酰基）苯基或喹啉-8-基。所述组合物可用于治疗脱发细胞增多症，疟疾和巴比血病。

5. 发明授权

US4587245A Method of treating neuropsychic disturbances by benzodiazepine derivatives and composition therefor 失效
标题翻译：用苯并二氮杂衍生物治疗神经功能紊乱的方法及其组成
公开(公告)号：US4587245A
公开(公告)日：1986-05-06
申请号：US695557
申请日：1985-01-28
申请人： Henri Demarne , Andre Hallot
发明人： Henri Demarne , Andre Hallot
IPC分类号： A61K31/495 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P21/02 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/26 , C07D243/16 , C07D243/18 , C07D243/24 , C07D243/26 , C07D243/28
CPC分类号： C07D243/24
摘要： Benzodiazepines of formula ##STR1## wherein R3 is methyl or ethyl and R4 is chlorine or fluorine are useful therapeutic agents for the treatment of neuropsychic disturbances.
摘要翻译：其中R3是甲基或乙基，R4是氯或氟的式“IMAGE”的苯二氮卓类是用于治疗神经障碍的有用的治疗剂。

6. 发明授权

US4696937A Thiosulfonate derivatives for inhibiting malformation or destruction of red blood corpuscules 失效
标题翻译：用于抑制红细胞畸形或破坏的硫代磺酸衍生物
公开(公告)号：US4696937A
公开(公告)日：1987-09-29
申请号：US797521
申请日：1985-11-13
申请人： Bernard Sebille , Yves Beuzard , Henri Demarne
发明人： Bernard Sebille , Yves Beuzard , Henri Demarne
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/433 , A61K31/47 , A61P7/00 , A61P33/00 , A61P33/02 , C07D215/36 , C07D233/84 , C07D235/28 , C07D263/58 , C07D277/16 , C07D277/40 , C07D285/12 , C07D285/125 , C07D401/12
CPC分类号： C07D263/58 , C07D215/36 , C07D233/84 , C07D235/28 , C07D277/16 , C07D285/125
摘要： The invention relates to novel thiosulfonate derivatives of general formu a:R--S--SO.sub.2 --R.sub.1in which R represents a 1H-imidazol-2-yl, quinolin-2-yl, 5-amino-1,3,4-thiadizol-2-yl or 4,5-dihydro-thiazol-2-yl radical and R.sub.1 represents a lower alkyl, (hydroxy)lower alkyl, phenyl, (lower alkyl) phenyl, (hydroxy lower alkyl) phenyl, (lower alkanoyl) phenyl or quinolin-8-yl radical.The thiosulfonate derivatives in question exert an inhibitory action with respect to the malformation or destruction of red blood corpuscules due to a genetic modification of haemoglobin or to parasites and can, therefore, be used in the treatment of drepanocytosis, malaria and babebiosis.
摘要翻译：本发明涉及通式为RS-SO 2 -R 1的新型硫代磺酸衍生物，其中R代表1H-咪唑-2-基，喹啉-2-基，5-氨基-1,3,4-噻二唑-2-基或羟基低级烷基，苯基，（低级烷基）苯基，（羟基低级烷基）苯基，（低级烷酰基）苯基或喹啉-8 环基所述的硫代磺酸衍生物由于血红蛋白或寄生虫的遗传修饰而对红血球的畸形或破坏产生抑制作用，因此可用于治疗脱发细胞增多症，疟疾和巴比血症。

7. 发明授权

US4581168A 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：US4581168A
公开(公告)日：1986-04-08
申请号：US580287
申请日：1984-02-17
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 , C07C103/52
CPC分类号： C07K7/06 , C07K14/60 , C07K5/06043 , C07K5/06069 , C07K5/06086 , C07K5/06095 , 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：本发明涉及液相和中间肽中hpGRF（somatocrinin）的合成，其包括： - 一个接一个接合并按照GRF序列的顺序，其中：（a）侧酸功能的天冬氨酸和谷氨酸以及赖氨酸的侧胺官能团由Boc组脱保护条件下稳定的保护基团保护，（b）精氨酸的胍功能受到质子化保护，（c）N - 末端氨基酸被Boc基团保护在胺上; - 通过用三氟乙酸水解选择性地在延伸期通过肽从N末端胺除去基团Boc，所述偶联在非质子极性溶剂中进行，在序列结束时，通过在0.1至1M甲磺酸或三氟甲磺酸三氟乙酸溶液中水解除去所有的保护基团。

8. 发明授权

US4404217A 3-Indolyl alkylene amino propanols and cardiovascular compositions thereof 失效
标题翻译： 3-吲哚基亚烷基氨基丙醇及其心血管组合物
公开(公告)号：US4404217A
公开(公告)日：1983-09-13
申请号：US178550
申请日：1980-08-15
申请人： Henri Demarne , Jean Wagnon
发明人： Henri Demarne , Jean Wagnon
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P9/00 , C07D209/14 , C07D209/16 , C07D209/12
CPC分类号： C07D209/14 , C07D209/16
摘要： The present invention relates to the chemical products of general formula: ##STR1## in which R.sub.1 and R.sub.2 designate hydrogen; halogen, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 designate hydrogen, alkyl, alkoxy, halogen, nitro, acyl, alkylthio, alkylsulfinyl, alkylsulfonyl, a (CH.sub.2).sub.n COOR, (CH.sub.2).sub.2 CONHR, (CH.sub.2).sub.n NHCOOR or (CH.sub.2).sub.n NHCOR group; or R.sub.3 and R.sub.4 together form a heterocycle bonded to the benzene cycle; X.sub.1 is hydrogen, alkyl, hydroxymethyl or COOR and X.sub.2 is hydrogen or methyl; and to the pharmaceutically acceptable salts of said products. It also relates to a process for preparing said products and to the drugs active in particular on the cardiovascular system, containing at least one of said products.
摘要翻译：本发明涉及以下通式的化学产物：其中R 1和R 2表示氢; 卤素，低级烷基或低级烷氧基; R 3和R 4表示氢，烷基，烷氧基，卤素，硝基，酰基，烷硫基，烷基亚磺酰基，烷基磺酰基，（CH 2）n COOR，（CH 2）2 CONHR，（CH 2）n NHCOOR或（CH 2）n NHCOR基团; 或R3和R4一起形成键合到苯环上的杂环; X1是氢，烷基，羟甲基或COOR，X2是氢或甲基; 以及所述产品的药学上可接受的盐。它还涉及制备所述产品和特别是在心血管系统上活性的药物的方法，其含有至少一种所述产品。

9. 发明授权

US4302601A Aromatic ketones having cardiovascular activity 失效
标题翻译：具有心血管活性的芳香酮
公开(公告)号：US4302601A
公开(公告)日：1981-11-24
申请号：US129730
申请日：1980-03-12
申请人： Henri Demarne
发明人： Henri Demarne
IPC分类号： A61K31/135 , A61P9/12 , A61P25/02 , C07C67/00 , C07C213/00 , C07C217/36 , C07D263/06 , C07D303/22 , C07D498/08 , C07C93/06
CPC分类号： C07D303/22
摘要： The present invention relates to phenoxypropane having the formula ##STR1## in which R.sup.1 and R.sup.2 are like or unlike and each is an alkyl group having 1-4 carbon atoms, R.sup.3 is hydrogen or an alkyl group having 1-4 carbon atoms, R.sup.4 is a halogen atom, preferably fluorine, chlorine or bromine, including their optical isomers and also their addition salts with acids.These compounds are of therapeutic value in the treatment of cardiovascular conditions.The invention also relates to methods of synthesis of these products including a synthesis which involves the production, as a intermediate of an 8-aza-4,9-dioxa-2,3-benzo-bicyclo-[4,2,1]-octane having the formula ##STR2## in which R.sup.1 and R.sup.4 are as above defined.
摘要翻译：本发明涉及具有式“IMAGE”的苯氧基丙烷，其中R1和R2是相同或不同的，并且各自是具有1-4个碳原子的烷基，R3是氢或具有1-4个碳原子的烷基，R4是卤素原子，优选氟，氯或溴，包括它们的光学异构体，以及它们与酸的加成盐。这些化合物在治疗心血管疾病方面具有治疗价值。本发明还涉及这些产物的合成方法，包括涉及生产8-氮杂-4,9-二氧杂-2,3-苯并 - 双环[4,2,1] - 四氢 - 具有式“IMAGE”的辛烷，其中R 1和R 4如上所定义。

10. 发明授权

US4252825A Compositions for treatment of cardiovascular conditions associated with overproduction of catecholamines 失效
标题翻译：用于治疗与儿茶酚胺过量产生相关的心血管疾病的组合物
公开(公告)号：US4252825A
公开(公告)日：1981-02-24
申请号：US1314
申请日：1979-01-05
申请人： Henri Demarne
发明人： Henri Demarne
IPC分类号： A61K31/135 , A61P9/12 , A61P25/02 , C07C67/00 , C07C213/00 , C07C217/36 , C07D263/06 , C07D303/22 , C07D498/08
CPC分类号： C07D303/22
摘要： Compositions having therapeutic value in the treatment of cardiovascular conditions associated with the overproduction of catecholamines include as the active ingredient 5-fluoro-2-(2-hydroxy-3-tertiary butyl-amino-propoxy) butyrophenone-, its optical isomers and non-toxic acid addition salts.
摘要翻译：在治疗与儿茶酚胺过量生成相关的心血管病症中具有治疗价值的组合物包括作为活性成分的5-氟-2-（2-羟基-3-叔丁基 - 氨基 - 丙氧基）丁酰苯酮，其旋光异构体和非 - 有毒的酸加成盐。

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