公开(公告)号：US4048313A

公开(公告)日：1977-09-13

申请号：US540032

申请日：1975-01-09

Applicant: Michel Vincent ,  Georges Remond ,  Xavier Pascaud ,  Jean-Claude Poignant

Inventor： Michel Vincent ,  Georges Remond ,  Xavier Pascaud ,  Jean-Claude Poignant

IPC: C07D295/22 ,  A61K31/535 ,  A61K31/5375 ,  A61P1/00 ,  A61P1/04 ,  A61P21/02 ,  A61P25/00 ,  C07C67/00 ,  C07C301/00 ,  C07C303/38 ,  C07C303/40 ,  C07C311/46 ,  C07D211/60 ,  C07D295/26 ,  C07D295/00

CPC classification number: C07D295/26 ,  C07D211/60 ,  Y10S514/872 ,  Y10S514/926 ,  Y10S514/927

Abstract: This application relates to benzenesulphonamides and more specifically to 1-acylamino 2- alcoxy or alcenyloxy 5-morpholinylsulfonyl benzenes and their salts with a mineral or organic acid. It also relates to processes for producing these compounds.The disclosed compounds are useful for stimulating gastric evacuation while inhibiting emisis and gastric secretion in warm-blooded animals.

Abstract translation: 本申请涉及苯磺酰胺，更具体地涉及1-酰氨基2-烷氧基或烯丙氧基-5-吗啉基磺酰基苯及其与矿物或有机酸的盐。 它还涉及生产这些化合物的方法。

公开(公告)号：US4148912A

公开(公告)日：1979-04-10

申请号：US442351

申请日：1974-02-14

Applicant: Michel Vincent ,  Georges Remond ,  Xavier Pascaud

Inventor： Michel Vincent ,  Georges Remond ,  Xavier Pascaud

IPC: C07F5/06 ,  C07F9/94 ,  A61K31/295 ,  A61K31/195 ,  A61K31/205 ,  A61K31/29

CPC classification number: C07F5/069 ,  C07F9/94

Abstract: The present application relates to pharmaceutical compositions incorporating as active ingredient p.chlorohippuric acid or one of its mineral or organic base addition salts.The pharmaceutical compositions are those adapted for parenteral or oral administration. They may include another active ingredient.The present application also extends to therapeutic methods for using the said pharmaceutical compositions namely for protecting the gastric mucosa from acid hypersecretion, ulcers from therapeutic origin and for protecting the liver from toxic aggressions.

Abstract translation: 本申请涉及作为活性成分掺入氯丙酸或其矿物或有机碱加成盐之一的药物组合物。

公开(公告)号：US5565429A

公开(公告)日：1996-10-15

申请号：US439233

申请日：1995-05-11

Applicant: Michel Vincent ,  Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Yolande Herve ,  Emmanuel Canet ,  Michel Lonchampt

Inventor： Michel Vincent ,  Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Yolande Herve ,  Emmanuel Canet ,  Michel Lonchampt

IPC: A61K38/00 ,  A61P29/00 ,  C07K1/10 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/087 ,  C07K5/09 ,  C07K14/81 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

CPC classification number: C07K5/06191 ,  A61K38/00

Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 represents an unsubstituted or substituted alkyl,R.sub.2 represents an unsubstituted or substituted alkyl,A represents, with the nitrogen and carbon atoms to which it is attached, a nitrogenous mono- or polycyclic structure, andB represent any one of the radicals a through j as defined in the description, and medicaments containing the same, are useful as human leucocyte elastase inhibitors.

Abstract translation: 式（I）的化合物：其中：R 1表示未取代或取代的烷基，R 2表示未取代或取代的烷基，A表示与其连接的氮和碳原子， 或多环结构，B表示说明书中定义的基团a至j中的任一个，含有该基团的药物可用作人白细胞弹性蛋白酶抑制剂。

公开(公告)号：US4959372A

公开(公告)日：1990-09-25

申请号：US237497

申请日：1988-08-26

Applicant: Michel Vincent ,  Georges Remond ,  Michel Laubie

Inventor： Michel Vincent ,  Georges Remond ,  Michel Laubie

IPC: C07D453/02 ,  A61K31/435 ,  A61K38/00 ,  A61P1/16 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P25/04 ,  A61P27/02 ,  A61P29/00 ,  A61P43/00 ,  C07K5/02

CPC classification number: C07K5/0222 ,  A61K38/00

Abstract: Compounds of formula (I): ##STR1## in which E denotes a lower alkyl group, or preferably a hydrogen atom, and their addition salts with a pharmaceutically acceptable acid or base, the preparation thereof and pharmaceutical compositions containing them.

Abstract translation: 式（I）化合物：其中E表示低级烷基，优选氢原子，及其与药学上可接受的酸或碱的加成盐，其制备方法和含有它们的药物组合物。

公开(公告)号：US4914214A

公开(公告)日：1990-04-03

申请号：US245446

申请日：1988-09-16

Applicant: Michel Vincent ,  Jean Baliarda ,  Bernard Marchand ,  Georges Remond

Inventor： Michel Vincent ,  Jean Baliarda ,  Bernard Marchand ,  Georges Remond

IPC: C07D209/42 ,  A61K38/00 ,  B01J23/00 ,  B01J23/40 ,  B01J23/755 ,  C07B31/00 ,  C07B53/00 ,  C07B61/00 ,  C07C67/00 ,  C07C227/00 ,  C07C227/18 ,  C07C227/32 ,  C07C229/16 ,  C07K1/02 ,  C07K5/02 ,  C07K5/06 ,  C07K14/81

CPC classification number: C07K5/0222 ,  A61K38/00

Abstract: Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring.The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.

Abstract translation: 在保护羧基后，（2S，3aS，7aS）-2-羧基全氢吲哚与N - [（S）-1-乙酯基] - （S） - 丙氨酸缩合的培养基工业合成方法，产物 由缩合得到的杂环进行羧基负载脱保护。 （2S，3aS，7aS）-2-羧基全氢吲哚和N - [（S）-1-甲乙氧基丁基] - （S） - 丙氨酸本身分别在2-羧基吲哚和L-丙氨酸的良好条件下得到， 工业规模。

公开(公告)号：US4720484A

公开(公告)日：1988-01-19

申请号：US933093

申请日：1986-11-20

Applicant: Michel Vincent ,  Georges Remond ,  Claude Cudennec

Inventor： Michel Vincent ,  Georges Remond ,  Claude Cudennec

IPC: C07K5/10 ,  A61K38/00 ,  A61P35/00 ,  A61P37/04 ,  C07D209/42 ,  C07K5/103 ,  C07K5/107 ,  C07K5/11 ,  C07K5/113 ,  C07K5/117 ,  C07K16/00 ,  A61K37/02

CPC classification number: C07K5/1013 ,  C07K5/1008 ,  C07K5/101 ,  C07K5/1016 ,  C07K5/1019 ,  C07K5/1021 ,  C07K5/1024

Abstract: The invention relates to tetrapeptide derivatives of the general formula ##STR1## in which R represents a hydrogen atom, a straight-chain or branched alkyl radical containing from 1 to 5 carbon atoms, optionally substituted by a hydroxy, amino, mercapto, methylthio, methylsulphoxide, carboxy or guanidino group, or a benzyl or indol-3-ylmethyl radical optionally substituted by a hydroxy group,R.sub.1 represents a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, ##STR2## represents a nitrogenous polycyclic structure, the enantiomers, epimers and diastereoisomers thereof, as well as to the pharmaceutically acceptable acid or base addition salts thereof.

Abstract translation: 本发明涉及通式为“IMAGE”的四肽衍生物，其中R表示氢原子，含有1至5个碳原子的直链或支链烷基，任选被羟基，氨基，巯基，甲硫基，甲基亚砜 ，羧基或胍基，或任选被羟基取代的苄基或吲哚-3-基甲基，R1表示氢原子或含有1至4个碳原子的烷基，表示含氮多环结构， 对映异构体，差向异构体和非对映异构体，以及其药学上可接受的酸或碱加成盐。

公开(公告)号：US4288453A

公开(公告)日：1981-09-08

申请号：US949571

申请日：1978-10-10

Applicant: Michel Vincent ,  Jacques Duhault ,  Michelle Boullanger ,  Georges Remond

Inventor： Michel Vincent ,  Jacques Duhault ,  Michelle Boullanger ,  Georges Remond

IPC: C07C323/52 ,  A61K31/10 ,  A61K31/19 ,  C07C29/70 ,  C07C41/01 ,  C07C41/26 ,  C07C43/03 ,  C07C43/23 ,  C07C45/00 ,  C07C45/71 ,  C07C59/125 ,  C07C59/66 ,  C07C59/68 ,  C07C69/66 ,  C07C69/708 ,  C07C319/14 ,  C07D207/32 ,  C07D207/333 ,  C07D295/08 ,  C07D295/096 ,  C07D295/185 ,  C07D307/42 ,  C07D333/16 ,  C07C53/134

CPC classification number: C07D207/333 ,  C07C29/70 ,  C07C29/705 ,  C07C323/00 ,  C07C41/26 ,  C07C45/004 ,  C07C45/71 ,  C07C59/68 ,  C07D295/096 ,  C07D295/185 ,  C07D333/16

Abstract: There are now described some novel alpha-[1-aryl-2,2,2-trifluoroethoxy (or-ethylthio)]alkanoic acids that are useful for reducing triglycerides and cholesterol levels in the blood of animals. The percentage reduction in test rats has been observed to be from 20 to 65 for triglycerides and from 15 to 50 for cholesterol. A representative compound of the invention is alpha-(2,2,2-trifluoro-1-phenyl-1-ethoxy)butyric acid. Most of the compounds have an LD.sub.50 greater than 800 mg/kg, intraperitoneally, in male mice.A method of use, compositions, and a process for synthesis are also described.

Abstract translation: 现在描述了一些可用于降低动物血液中甘油三酯和胆固醇水平的新型α-[1-芳基-2,2,2-三氟乙氧基（或 - 乙硫基）]链烷酸。 对于甘油三酸酯，测试大鼠的百分比降低已被观察到为20至65，对于胆固醇为15至50。 本发明的代表性化合物是α-（2,2,2-三氟-1-苯基-1-乙氧基）丁酸。 大多数化合物在雄性小鼠中腹膜内具有大于800mg / kg的LD50。 还描述了使用方法，组合物和合成方法。

公开(公告)号：US4246267A

公开(公告)日：1981-01-20

申请号：US948536

申请日：1978-10-04

Applicant: Michel Vincent ,  Georges Remond ,  Michel Laubie

Inventor： Michel Vincent ,  Georges Remond ,  Michel Laubie

IPC: A61K31/4433 ,  A61K31/445 ,  A61K31/4468 ,  A61P9/12 ,  C07D211/58 ,  C07D333/34 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07C321/00 ,  C07D211/58 ,  C07D333/34

Abstract: This invention relates to 4-aminopiperidines and more precisely to 4-aminopiperidines the nitrogen atom of the piperidine ring is substituted with an aryl lower alkyl side-chain.This invention also relates to processes for producing the same.This invention further extends to pharmaceutical compositions and to the method of using the same.

Abstract translation: 本发明涉及4-氨基哌啶，更准确地说涉及4-氨基哌啶，哌啶环的氮原子被芳基低级烷基侧链取代。 本发明还涉及其制造方法。 本发明进一步延伸至药物组合物及其使用方法。

公开(公告)号：US4166117A

公开(公告)日：1979-08-28

申请号：US814482

申请日：1977-07-11

Applicant: Michel Vincent ,  Georges Remond ,  Michel Laubie

Inventor： Michel Vincent ,  Georges Remond ,  Michel Laubie

IPC: C07C69/65 ,  A61K31/505 ,  A61K31/517 ,  A61P9/12 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D239/90 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D491/10 ,  C07D491/113 ,  C07D455/02

CPC classification number: C07D491/10 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74

Abstract: This invention relates to novel quinazolinones, the nitrogen of which is bound to 4-amino piperidinyl-1 structures.This invention also relates to processes for producing these compounds.They have interesting pharmacological properties which make them useful in human or veterinary medicine for treating hypertension.

公开(公告)号：US4954640A

公开(公告)日：1990-09-04

申请号：US462797

申请日：1990-01-10

Applicant: Michel Vincent ,  Jean Baliarda ,  Bernard Marchand ,  Georges Remond

Inventor： Michel Vincent ,  Jean Baliarda ,  Bernard Marchand ,  Georges Remond

IPC: C07B61/00 ,  C07C211/27 ,  C07D209/42 ,  C07K1/02 ,  C07K5/02 ,  C07K5/06

CPC classification number: C07K5/0222 ,  C07D209/42

Abstract: Process for the industrial synthesis of (2S,3 7aS)-2-carboxyperhydroindole by reduction of 2-carboxindole or of one of its esters to (R,S)-2-carboxyindo or of one of its esters which, after saponification, converted into the acid, the S isomer cf (R,S)-2-carboxyindoline being obtained by precipitation from the mixture of the two (R) and (S) isomers, in the presence of (+) methylbenzylamine, (S)-2-carboxyindoline being in its turn subjected to catalytic hydrogenation to give (2S, 3aS,7aS)-2-carboxyperhydroindole, after separation of (2S,3aR,7aR) isomer by crystallization.Application to the synthesis of carboxyalkyl d peptides capable of being employed in therapeutics.