公开(公告)号：US3903114A

公开(公告)日：1975-09-02

申请号：US40203073

申请日：1973-10-01

Applicant: ROUSSEL UCLAF

Inventor： LE MARTRET ODILE ,  CLEMENCE FRANCOIS

IPC: A61K31/38 ,  A61K31/381 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  C07D333/22 ,  C07D333/38

CPC classification number: C07D333/22

Abstract: Novel thiophene derivatives of the formula

WHEREIN R and R2 are individually selected from the group consisting of hydrogen and methyl with R2 being in the 3- or 4position of the thienyl ring, R1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms and X is selected from the group consisting of hydrogen, halogen, methyl, methoxy, CF3- and CF3O- in any position on the benzene ring, the compounds being in racemic or optically active form when R is methyl having anti-inflammatory and analgesic activity.

Abstract translation: 式WHEREIN R和R2的新型噻吩衍生物分别选自氢和甲基，R2在噻吩环的3-或4-位，R1选自氢和酰基， 1至18个碳原子的有机羧酸，X选自氢，卤素，甲基，甲氧基，CF3-和CF3O-在苯环上的任何位置，该化合物当R 是具有抗炎和止痛活性的甲基。

公开(公告)号：US3700677A

公开(公告)日：1972-10-24

申请号：US3700677D

申请日：1969-07-15

Applicant: ROUSSEL UCLAF

Inventor： CLEMENCE FRANCOIS ,  MARTRET ODILE LE

IPC: C07D277/32 ,  C07D277/56 ,  C07D491/04 ,  C07D91/32

CPC classification number: C07D491/04 ,  C07D277/56

Abstract: 5-THIAZOL CARBOXYLATES OF THE FORMULA WHEREIN R is an alkali-metal atom, the residue of an organic base or the alkyl radical of an aliphatic, arylaliphatic or alkylheterocyclic alcohol having hypolipemiant activity and their preparation.

Abstract translation: 其中R为碱金属原子的有机碱的残基或具有低活性活性的脂族，芳基脂族或烷基杂环醇的烷基的制备方法及其制备方法制备的5-噻唑羧酸酯。

公开(公告)号：US3925399A

公开(公告)日：1975-12-09

申请号：US46518874

申请日：1974-04-29

Applicant: ROUSSEL UCLAF

Inventor： CLEMENCE FRANCOIS ,  LE MARTRET ODILE

IPC: A61K31/425 ,  C07D277/56 ,  C07F5/06

Abstract: The basic aluminum salt of 2-n-propyl-5-thiazolecarboxylic acid having the formula

ITS PREPARATION, HYPOLIPEMIANT COMPOSITIONS CONTAINING THE SAME AND THERAPEUTIC METHODS TO TREAT HYPERLIPEMIA UTILIZING THE HYPOLIPEMIANT COMPOSITIONS.

Abstract translation: 具有式ITS的2-正丙基-5-噻唑甲酸的碱性铝盐，其含有其的高效组合物和治疗使用高效组合物的治疗方法。

公开(公告)号：US3644382A

公开(公告)日：1972-02-22

申请号：US3644382D

申请日：1969-03-18

Applicant: ROUSSEL UCLAF

Inventor： CLEMENCE FRANCOIS ,  MARTRET ODILE LE

IPC: C07D213/82 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18 ,  C07D307/68 ,  C07D333/38 ,  C07D49/38

CPC classification number: C07D213/82 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18 ,  C07D307/68 ,  C07D333/38

Abstract: BENZIMIDAZOLES OF THE FORMULA

1-(2-R-PHENYL),2-R1,5-X'',6-X-BENZMIDAZOLE

WHERIN X AND X'' MAY BE DIFFERENT AND ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, ALKYL, ALKOXY, TRIHALOMETHYL AND NITRO, R IS SELECTED FROM THE GROUP CONSISTING OF -COOH, -COOR'', AND

-CO-N(-A)-B

R'' IS SELECTED FROM THE GROUP CONSISTING OF ALIPHATIC AND HHDROXYLATED RESIDUE OF A GLYCOL, A AND B ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND OPTIONALLY SUBSTITUTED ALIPHATIC AND R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALIPHATIC HDROCARBON, UNSUBSTITUTED AND POLYSUBSTITUTED ARYL, ARYLALIPHATIC, A THIENYL, A B-PYRIDYL AND A FURYL WITH THE PROVISO THAT WHEN R1 IS PHENYL, X'' AND X ARE OTHER THAN HALOGEN, ALKOXY AND TRIFLUROMETHYL WHICH COMPOUNDS POSSESS ANTI-INFLAMMATORY AND ANTIVIRAL ACTIVITY AND A NOVEL PROCESS FOR THEIR PREPARATION.

公开(公告)号：US3882110A

公开(公告)日：1975-05-06

申请号：US43188174

申请日：1974-01-09

Applicant: ROUSSEL UCLAF

Inventor： CLEMENCE FRANCOIS ,  LE MARTRET ODILE

IPC: A61K31/425 ,  C07D277/56 ,  C07D91/32

CPC classification number: A61K31/425 ,  C07D277/56

Abstract: WHEREIN R has the above-assigned meaning and R''1 is a linear alkyl of 1 to 12 carbon atoms.

WHEREIN R is hydrogen, an alkali metal, ammonium, the monovalent residue of an organic amine base or a substituted or unsubstituted alkyl and R'' is a linear alkyl of 3 to 12 carbon atoms, and their preparation, and hypolipemiant compositions containing at least one 2-alkyl-5-thiazole carboxylic acid derivative of the formula

2-Alkyl-5-thiazole carboxylic acid derivatives of the formula

Abstract translation: 2-烷基-5-噻唑羧酸衍生物，式为WHEREIN R为氢，碱金属，铵，有机胺碱的单价残基或取代或未取代的烷基，R'为3至12碳的直链烷基 原子及其制备方法，以及含有至少一种下式WHEREIN R具有上述含义的2-烷基-5-噻唑羧酸衍生物的低胆固醇组合物，R'1是1至12个碳原子的直链烷基。

公开(公告)号：US3872124A

公开(公告)日：1975-03-18

申请号：US34028973

申请日：1973-03-12

Applicant: ROUSSEL UCLAF

Inventor： LE MARTRET ODILE ,  CLEMENCE FRANCOIS

IPC: C07D295/13 ,  A61K20060101 ,  A61K31/425 ,  A61K31/495 ,  C07D20060101 ,  C07D277/20 ,  C07D277/56 ,  C07D295/096 ,  C07D417/12 ,  C07D51/70

CPC classification number: C07D295/13 ,  C07D277/56

Abstract: Novel thiazolcarboxamides of the formula

D R A W I N G
WHEREIN R is selected from the group consisting of alkyl of 1 to 6 carbon atoms and phenyl, R1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, n is a whole number from 2 to 5 and X and X1 are individually selected from the group consisting of hydrogen, halogen, trifluoromethyl and alkyl, alkoxy and alkylthio of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having Alpha -adrenolytic activity and their preparation.

Abstract translation: 式WHEREIN R的新型噻唑甲酰胺选自1至6个碳原子的烷基和苯基，R 1选自氢和1至4个碳原子的烷基，n是从2到 5和X和X 1分别选自氢，卤素，三氟甲基和具有1至4个碳原子的烷基，烷氧基和烷硫基及其无毒的药学上可接受的具有α-脱水活性的酸加成盐及其制备。

公开(公告)号：US3668238A

公开(公告)日：1972-06-06

申请号：US3668238D

申请日：1968-09-25

Applicant: ROUSSEL UCLAF

Inventor： CLEMENCE FRANCOIS ,  MARTRET ODILE LE

IPC: C07D295/192 ,  C07C69/02

CPC classification number: C07D295/192

Abstract: WHEREIN R is selected from the group consisting of hydrogen, alkyl of one to seven carbon atoms and acyl of an organic carboxylic acid of one to 18 carbon atoms, R1 and R2 are selected from the group consisting of hydrogen, substituted and unsubstituted alkyl of one to seven carbon atoms, aryl and cycloalkyl and when taken together with the nitrogen atom form a heterocyclic which may contain another heteroatom, which products possess outstanding choleretic properties far superior to dehydrocholic acid. The invention also relates to a novel process and novel intermediate for the preparation of the said benzamides of Formula I.

An amide of 2-hydroxy-3-methoxy-5-allyl-benzoic acid of the formula

Abstract translation: 式WHEREIN R的2-羟基-3-甲氧基-5-烯丙基 - 苯甲酸的酰胺选自氢，1至7个碳原子的烷基和1至18个碳原子的有机羧酸的酰基 原子，R 1和R 2选自氢，取代和未取代的1至7个碳原子的烷基，芳基和环烷基，并且当与氮原子一起形成可含有另外杂原子的杂环时，该产物具有优异的胆固醇 性质远优于脱氢胆酸。 本发明还涉及用于制备所述式I的苯甲酰胺的新方法和新型中间体。