公开(公告)号：US4092423A

公开(公告)日：1978-05-30

申请号：US723684

申请日：1976-09-16

Applicant: Charles Malen ,  Pierre Roger ,  Jean-Claude Poignant ,  Xavier Pascaud

Inventor： Charles Malen ,  Pierre Roger ,  Jean-Claude Poignant ,  Xavier Pascaud

IPC: C07D207/08 ,  C07D211/34 ,  C07D211/60 ,  C07D295/15 ,  C07D207/04 ,  A61K31/40

CPC classification number: C07D295/15 ,  C07D207/08 ,  C07D211/34 ,  C07D211/60

Abstract: This invention relates to ortho-alkoxy anilines having the amino group substituted with an amino lower alkyl carboxylic residue, as well as their physiologically-compatible acid-addition salts and their optically-active isomers.This invention also relates to processes for making the same in which an ortho-alkoxy aniline is reacted with a lower alkanoic acid or a functional derivative thereof.The compounds of the invention have therapeutical utility namely for the prevention or treatment of digestive disorders and gastric ulcers.

Abstract translation: 本发明涉及具有被氨基低级烷基羧酸残基取代的氨基的邻烷氧基苯胺，以及它们的生理上相容的酸加成盐及其光学活性异构体。

公开(公告)号：US4048321A

公开(公告)日：1977-09-13

申请号：US685756

申请日：1976-05-13

Applicant: Laszlo Beregi ,  Pierre Hugon ,  Xavier Pascaud ,  Jean-Claude Poignant

Inventor： Laszlo Beregi ,  Pierre Hugon ,  Xavier Pascaud ,  Jean-Claude Poignant

IPC: C07D209/44 ,  C07D209/52 ,  A61K31/40 ,  C07D207/12

CPC classification number: C07D209/52 ,  C07D209/44 ,  Y10S514/872

Abstract: Disubstituted azabicycloalkanes of the formula ##STR1## wherein: N IS 0, 1 OR 2R is saturated or unsaturated straight or branched (C.sub.1 -C.sub.5) aliphatic hydrocarbon, andX.sub.1, x.sub.2, x.sub.3, x.sub.4, x.sub.5, which are the same or different, are hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino or sulfamoyl.These compounds are used as medicine especially in the treatment of gastroduodenal ulcers, gastric hypersecretion, nauseous syndromes of central origin and hypertension.

Abstract translation: 下式的二取代氮杂双环烷烃其中：

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：US3970661A

公开(公告)日：1976-07-20

申请号：US465931

申请日：1974-05-01

Applicant: Gilbert Regnier ,  Roger Canevari ,  Xavier Pascaud

Inventor： Gilbert Regnier ,  Roger Canevari ,  Xavier Pascaud

IPC: C07D213/81 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/455 ,  A61K31/505 ,  A61K31/535 ,  A61P1/04 ,  A61P25/00 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D213/75

CPC classification number: C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  Y10S514/927

Abstract: Heterocyclic amides of the formula: ##SPC1##Wherein:X is N or CH;n is O or 1 andR is ##EQU1## or ##SPC2##Wherein:R.sub.1 is hydrogen or methyl,R.sub.2 and R.sub.3 which are the same, are lower alkyl or joined together, represent a polymethylenic chain from C.sub.4 to C.sub.7 optionally including an oxygen atom, andR' is saturated or unsaturated acyclic hydrocarbon radicals from C.sub.1 to C.sub.20, cycloalkyl from C.sub.3 to C.sub.7, Ar -- A-- or Ar ##EQU2## wherein: A is a single bond or a saturated or unsaturated acyclic hydrocarbon chain from C.sub.1 to C.sub.6 optionally including an oxygen atom, andAr and R" are aromatic, alkoxy aromatic, methlenedioxy aromatic or polymethylenedioxy aromatic.These compounds are used as medicine, especially in the treatment of gastric hypersecretion, gastroduodenal ulcers and central nervous system disorders.

Abstract translation: 下式的杂环酰胺：

公开(公告)号：US5034419A

公开(公告)日：1991-07-23

申请号：US484403

申请日：1990-02-26

Applicant: Gilbert G. Aubard ,  Alain P. Calvet ,  Jean-Pierre DeFaux ,  Claude J. Gouret ,  Agnes M. Grouhel ,  Henry L. Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud ,  Francois F. Roman ,  James P. Hudspeth ,  Yuan Lin

Inventor： Gilbert G. Aubard ,  Alain P. Calvet ,  Jean-Pierre DeFaux ,  Claude J. Gouret ,  Agnes M. Grouhel ,  Henry L. Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud ,  Francois F. Roman ,  James P. Hudspeth ,  Yuan Lin

IPC: A61K31/135 ,  A61P1/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07C57/42 ,  C07C57/58 ,  C07C67/00 ,  C07C209/00 ,  C07C211/27 ,  C07C211/28 ,  C07C211/29 ,  C07C217/58 ,  C07C217/62 ,  C07C217/64 ,  C07C233/03 ,  C07C233/05 ,  C07C233/08 ,  C07C233/12 ,  C07C233/13 ,  C07C233/21 ,  C07C241/00 ,  C07C255/24 ,  C07C255/30 ,  C07C255/42 ,  C07C265/06 ,  C07C265/08

CPC classification number: C07C265/08 ,  C07C211/28 ,  C07C211/29 ,  C07C217/58 ,  C07C217/62 ,  C07C233/03 ,  C07C233/05 ,  C07C233/12 ,  C07C233/13 ,  C07C233/21 ,  C07C255/42 ,  C07C2101/02 ,  C07C2101/04 ,  C07C2101/08 ,  Y10S514/925 ,  Y10S514/926 ,  Y10S514/927

Abstract: N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur,R2 is lower alkyl,R3 is hydrogen or lower alkyl,m has the value of 1 or 2,R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5,R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, andQ represents an ethylene-1,2-diyl group --CH.dbd.CH-- or a cyclopropane-1,2-diyl group ##STR2##

Abstract translation: 式I的N-环烷基烷基胺：其中：R 1是任选被卤素或低级烷基，卤代烷基或低级烷氧基单取代，二取代或三取代的苯基，或是具有5-7个链的芳族杂环基 成员，其中杂原子是氮，氧或硫，R2是低级烷基，R3是氢或低级烷基，m的值是1或2，R4是环烷基-CH（CH2）n，其中碳原子 可以携带基团Rx，它是低级烷基或苯基; 并且其中n具有2至5的值，R 5是苯基，其可以被卤素或低级烷氧基单取代，二取代或三取代，并且Q表示乙烯-1,2-二基-CH = CH - 或环丙烷-1,2-二基

公开(公告)号：US3972994A

公开(公告)日：1976-08-03

申请号：US525623

申请日：1974-11-20

Applicant: Laszlo Beregi ,  Pierre Hugon ,  Xavier Pascaud ,  Jean-Claude Poignant

Inventor： Laszlo Beregi ,  Pierre Hugon ,  Xavier Pascaud ,  Jean-Claude Poignant

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P1/08 ,  A61P9/12 ,  B01J21/00 ,  B01J25/00 ,  C07B61/00 ,  C07D209/44 ,  C07D209/52

CPC classification number: C07D209/44 ,  C07D209/52

Abstract: Disubstituted azabicycloalkanes of the formula ##SPC1##Wherein:n is 0, 1 or 2R is saturated or unsaturated straight or branched (C.sub.1 -C.sub.5) aliphatic hydrocarbon, andX.sub.1, x.sub.2, x.sub.3, x.sub.4, x.sub.5, which are the same or different, are hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, trifluoromethyl, nitro, amino or sulfamoyl.These compounds are used as medicine especially in the treatment of gastroduodenal ulcers, gastric hypersecretion, nauseous syndromes of central origin and hypertension.

Abstract translation: 下式的二取代的氮杂双环烷烃：

公开(公告)号：US5389686A

公开(公告)日：1995-02-14

申请号：US91691

申请日：1993-07-13

Applicant: Laurent Diop ,  Agnes Grouhel ,  Jean-Louis Junien ,  Annick Langlois ,  Xavier Pascaud

Inventor： Laurent Diop ,  Agnes Grouhel ,  Jean-Louis Junien ,  Annick Langlois ,  Xavier Pascaud

IPC: C07C217/48 ,  A61K31/135

CPC classification number: C07C217/48

Abstract: Process for the treatment of painful syndromes, especially local and/or visceral, consisting in the parenteral or topical administration of a therapeutically effective quantity of the (-) tartrate of (+)-(R)-1-[(3,4,5-trimethoxy)benzyloxymethyl]-1-phenyl-N,N-dimethyl-n-propylamine.

Abstract translation: 用于治疗疼痛综合征，特别是局部和/或内脏的方法，其组合在肠胃外或局部施用治疗有效量的（+） - （R）-1 - [（3,4,5-三甲基 - 5-三甲氧基）苄氧基甲基] -1-苯基-N，N-二甲基 - 正丙胺。

公开(公告)号：US5236947A

公开(公告)日：1993-08-17

申请号：US899712

申请日：1992-06-17

Applicant: Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

Inventor： Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

IPC: C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C217/72 ,  C07C225/16 ,  C07D317/28

CPC classification number: C07C225/16 ,  C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C217/72 ,  C07D317/28

Abstract: The present invention relates to propanamines of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted in an identical or different manner with halogen atoms, or lower alkyl, lower haloalkyl or lower alkoxy radicals;R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkyalkyl radical,R5 is a 5-to 7-membered cycloalkyl radical or a phenyl radical, andW represents a heterocycle .dbd.C[Q--(CH.sub.2).sub.n --Q] in which Q is an oxygen or sulfur atom and n is 2 or 3,and their acid addition salts with pharmaceutically acceptable acids. The invention also relates to antidiarrheal pharmaceutical compositions comprising the claimed propanamines.

Abstract translation: 本发明涉及通式（I）的丙胺，其中：R 1是任选地以与卤素原子相同或不同的方式单，二或三取代的苯基，或低级烷基低级卤代烷基 或低级烷氧基; R2是低级烷基，R3和R4是氢原子或低级烷基，低级烯基或低级环烷基，R5是5-至7-元环烷基或苯基，W表示杂环= C [ Q-（CH2）nQ]其中Q是氧或硫原子，n是2或3，以及它们与药学上可接受的酸的酸加成盐。 本发明还涉及包含所要求保护的丙胺的止泻药物组合物。

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：US5143938A

公开(公告)日：1992-09-01

申请号：US660873

申请日：1991-02-26

Applicant: Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

Inventor： Alain Calvet ,  Agnes Grouhel ,  Henri Jacobelli ,  Jean-Louis Junien ,  Xavier Pascaud

IPC: A61K31/135 ,  A61K31/335 ,  A61K31/357 ,  A61K31/385 ,  C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C215/30 ,  C07C217/72 ,  C07C225/16 ,  C07C225/18 ,  C07C323/29 ,  C07D317/28 ,  C07D339/06

CPC classification number: C07C225/16 ,  C07C205/04 ,  C07C205/09 ,  C07C205/32 ,  C07C205/45 ,  C07C217/72 ,  C07D317/28

Abstract: A compound which is a propanamine of general formula (I) ##STR1## in which: R1 is a phenyl radical optionally mono-, di- or trisubstituted,or is a 5- or 6-membered monocyclic heteroaryl radical in which the single heteroatom is nitrogen, oxygen or sulfur,R2 is a lower alkyl radical,R3 and R4 are a hydrogen atom or a lower alkyl, lower alkenyl or lower cycloalkylalkyl radical,or, together with the nitrogen atom to which they are attached, form a saturated 5- to 6-membered heterocycle comprising only one heteroatom,R5 is a 5- to 7-membered cycloalkyl radical, a phenyl radical or a 5- or 6-membered monocyclic heteroaryl radical,and W representsa group .dbd.CH--QH,or a heterocycle .dbd.C[Q--(CH2)n--Q],or a group .dbd.C.dbd.Q, in which groupsQ is an oxygen or sulfur atom,n has the value 2 or 3,W being .dbd.C.dbd.Q only when R3 and R4 are not both hydrogen, and their additions salts with pharmaceutically acceptable acids.A pharmaceutical composition comprising a compound of general formula (I) with the above definitions for the treatment of diarrheal states.

Abstract translation: 作为通式（I）的丙胺的化合物，其中：R 1是任选被一个，二或三取代的苯基，或是5或6元单环杂芳基，其中 单个杂原子是氮，氧或硫，R2是低级烷基，R3和R4是氢原子或低级烷基，低级烯基或低级环烷基烷基，或者与它们相连的氮原子一起形成 饱和的5至6元杂环，仅包含一个杂原子，R 5为5-至7-元环烷基，苯基或5-或6-元单环杂芳基，W表示基团= CH-QH， 或杂环= C [Q-（CH 2）nQ]或基团= C = Q，其中基团Q是氧或硫原子，n具有值2或3，W仅当R 3为 和R4不同时为氢，并且它们与药学上可接受的酸相加。 一种药物组合物，其包含具有上述定义用于治疗腹泻状态的通式（I）的化合物。