公开(公告)号：US4397856A

公开(公告)日：1983-08-09

申请号：US262952

申请日：1981-05-12

申请人： Andre Allais ,  Francois Clemence ,  Roger Deraedt ,  Odile Lemartret

发明人： Andre Allais ,  Francois Clemence ,  Roger Deraedt ,  Odile Lemartret

IPC分类号： A61K31/47 ,  A61P25/04 ,  A61P29/00 ,  C07C237/04 ,  C07C237/22 ,  C07D215/56 ,  C07D233/88 ,  C07D263/48 ,  C07D265/16 ,  C07D265/22 ,  C07D277/20 ,  C07D277/46 ,  C07D277/82 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D265/22 ,  C07D215/56 ,  C07D233/88 ,  C07D263/48 ,  C07D277/46

摘要： Novel compounds of the formula ##STR1## wherein X is in the 5,6,7 or 8 position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 O--, CF.sub.3 S-- and CF.sub.3 --, R.sub.1 ' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 ' is selected from the group consisting of hydrogen or an optionally unsaturated ring able to contain one or more heteroatoms of the group consisting of --S--, --O-- and --N-- optionally substituted with one or more members of the group consisting of (a) halogens, (b) alkyl of 1 to 4 carbon atoms optionally substituted with NH.sub.2, --NHAlK or --N---(AlK).sub.2 and AlK is alkyl of 1 to 3 carbon atoms, (c) phenyl, (d) alkoxy of 1 to 4 carbon atoms, (e) --OH, (f) --CF.sub.3 and (g) --NO.sub.2 or R.sub.1 ' together with the nitrogen atom to which they are attached form an optionally unsaturated ring, the said ring then being connected to the nitrogen atom by a double bond, R.sub.3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and halogen, R.sub.5 is a halogen with the proviso that R.sub.3, R.sub.4 and R.sub.5 can not all be fluorine and R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and an acyl of an organic carboxylic acid of 2 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and their salts with non-toxic, pharmaceutically acceptable bases having a remarkable analgesic activity, a very weak anti-inflammatory activity and a good tolerance by the gastrointestinal system and their preparation and their intermediates.

摘要翻译： 新颖的式（Ⅰ）化合物，其中X为5,6,7或8位，选自氢，卤素，1至5个碳原子的烷基，1至4个碳原子的烷氧基 ，CF 3 O-，CF 3 S-和CF 3 - ，R''选自氢和1至4个碳原子的烷基，R 2'选自氢或任选不饱和的环，其能够含有一个或多个 任选被一个或多个由（a）卤素，（b）任选被NH 2取代的1至4个碳原子的烷基取代的-S-，-O-和 - NHAlK或-N - （AlK）2，AlK是1至3个碳原子的烷基，（c）苯基，（d）1-4个碳原子的烷氧基，（e）-OH，（f）-CF3和（ g）-NO 2或R 1'与它们所连接的氮原子一起形成任选的不饱和环，然后所述环通过双键与氮原子连接，R 3选自组 氢，卤素和1至4个碳原子的烷基，R4选自氢和卤素，R5是卤素，条件是R3，R4和R5不能全部是氟，R6选自 由氢，1-8个碳原子的烷基和2至8个碳原子的有机羧酸的酰基及其无毒的药学上可接受的酸加成盐和它们的盐与无毒的药学上可接受的碱组成的组，其具有 显着的止痛活性，非常弱的抗炎活性和良好的耐胃肠系统及其制备及其中间体。

公开(公告)号：US4337353A

公开(公告)日：1982-06-29

申请号：US875323

申请日：1978-02-06

申请人： Andre Allais ,  Francois Clemence ,  Jean Meier ,  Roger Deraedt

发明人： Andre Allais ,  Francois Clemence ,  Jean Meier ,  Roger Deraedt

IPC分类号： C07C59/76 ,  C07C45/41 ,  C07C51/00 ,  C07C51/08 ,  C07C51/09 ,  C07C59/84 ,  C07C59/88 ,  C07C59/90 ,  C07C67/00

CPC分类号： C07C59/90 ,  C07C45/41 ,  C07C59/84 ,  C07C59/88

摘要： Novel carboxylic acids of the formula ##STR1## wherein Z is an aliphatic hydrocarbon chain selected from the group consisting of --(CH.sub.2).sub.n -- and --CH.dbd.CH--(CH.sub.2).sub.n-2 -- where the double bond may be at any point in the chain, n is an integer from 5 to 10 and X, X.sub.1, X.sub.2 and X.sub.3 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkylthio of 1 to 5 carbon atoms, CF.sub.3 --, CF.sub.3 O-- and CF.sub.3 S-- and their non-toxic, pharmaceutically acceptable organic and inorganic salts and esters having analgesic and anti-inflammatory activity and their preparation.

摘要翻译： 式（Ⅰ）的新型羧酸，其中Z是选自 - （CH 2）n - 和-CH = CH-（CH 2）n-2-的脂族烃链，其中双键可以是任何 n为5至10的整数，X，X 1，X 2和X 3分别选自氢，卤素，1至5个碳原子的烷基，1至5个碳原子的烷氧基，烷硫基 1至5个碳原子，CF 3 - ，CF 3 O-和CF 3 S-及其无毒的药学上可接受的有镇痛和抗炎活性的有机和无机盐和酯及其制备。

公开(公告)号：US4294845A

公开(公告)日：1981-10-13

申请号：US34431

申请日：1979-04-30

申请人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

发明人： Daniel Humbert ,  Francois Clemence ,  Michele Dagnaux

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P3/04 ,  A61P9/00 ,  C07C39/367 ,  C07D319/08

CPC分类号： C07D319/08 ,  C07C39/367

摘要： Novel racemic mixtures or optically active isomers of 1,3-benzodioxins of the formula ##STR1## wherein R.sub.1 ' is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, --NH.sub.4, aluminum, non-toxic, pharmaceutically acceptable amines, alkyl of 1 to 5 carbon atoms, 2,3-dihydroxypropanyl, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl and dialkylaminoalkyl with alkyls of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and phenyl and R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen and halogen, and the non-toxic, pharmaceutically acceptable acid addition salts where R.sub.1 ' is dialkylaminoalkyl, with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously having hypolipemic activity and their preparation.

摘要翻译： 下式的1,3-苯并二恶英的新型外消旋混合物或光学活性异构体其中R1'选自氢，碱金属，碱土金属，-NH4，铝，无毒，药学上可接受的 胺，1至5个碳原子的烷基，2,3-二羟基丙酰基，（2,2-二甲基-1,3-二氧戊环-4-基）甲基和具有1至4个碳原子的烷基的二烷基氨基烷基，R2选自 由氢和1至5个碳原子的烷基组成的组，R3选自氢，1至5个碳原子的烷基和苯基，R4和R5分别选自氢和卤素，和 无毒，药学上可接受的酸加成盐，其中R1'是二烷基氨基烷基，条件是R2和R3不同时具有降血脂活性及其制备。

公开(公告)号：US4172137A

公开(公告)日：1979-10-23

申请号：US820098

申请日：1977-07-29

申请人： Francois Clemence ,  Robert Fournex

发明人： Francois Clemence ,  Robert Fournex

IPC分类号： C07D277/20 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  A61K31/425

CPC分类号： C07D277/20 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30

摘要： Novel 5-thiazole-alkylamines of the formula ##STR1## wherein R is alkyl of 1 to 6 carbon atoms and n is a whole number of 2 to 7 and their non-toxic, pharmaceutically acceptable acid addition salts having marked antilipolytic activity.

摘要翻译： 新的式（I）的5-噻唑 - 烷基胺其中R是1至6个碳原子的烷基，n是2至7的整数，以及它们具有显着的抗水解活性的无毒的药学上可接受的酸加成盐。

公开(公告)号：US4159986A

公开(公告)日：1979-07-03

申请号：US610110

申请日：1975-09-04

申请人： Francois Clemence ,  Odile Le Martret

发明人： Francois Clemence ,  Odile Le Martret

IPC分类号： C07D333/22 ,  C07D333/24 ,  A01N9/00

CPC分类号： C07D333/24 ,  C07D333/22

摘要： Novel thiophene-acetic acid derivatives of the formulae ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of lower alkyl of 1 to 4 carbon atoms and hydrogen and R.sub.2 is selected from the group consisting of hydrogen, lower alkyl of 1 to 7 carbon atoms and optionally substituted with at least one hydroxy group or an oxygen atoms-containing heterocycle,di-lower alkylamino-lower alkyl, N-heterocyclic alkyl, alkali metals, alkaline earth metals, aluminum and --H,NH (lower alkyl).sub.2 and Ar is selected from the group consisting of phenyl, optionally substituted with at least one member of the group consisting of halogen, trihalogenomethyl, lower alkyl, lower alkoxy and carboxyl, cyclohexyl, thienyl, furyl, tetrahydrofuryl and pyridyl, and in formula II, ArCO is attached to one of the positions .alpha. to the sulfur atom, which compounds have analgesic and anti-inflammatory activity and their preparations.

摘要翻译： 式（I）＆lt; IMAGE＆gt; II的新型噻吩 - 乙酸衍生物，其中R选自氢和1至4个碳原子的烷基，R 1选自1至 4个碳原子和氢，R2选自氢，1至7个碳原子的低级烷基，任选被至少一个羟基或含氧原子的杂环取代，二低级烷基氨基 - 低级烷基，N - 杂环烷基，碱金属，碱土金属，铝和-H，NH（低级烷基）2和Ar选自苯基，任选被至少一个由卤素，三卤甲基，低级 烷基，低级烷氧基和羧基，环己基，噻吩基，呋喃基，四氢呋喃基和吡啶基，并且在式II中，ArCO与硫原子的α位置连接，该化合物具有镇痛和抗炎活性， 准备工作

公开(公告)号：US4045567A

公开(公告)日：1977-08-30

申请号：US662122

申请日：1976-02-27

申请人： Francois Clemence ,  Odile Le Martret

发明人： Francois Clemence ,  Odile Le Martret

IPC分类号： A61K31/425

CPC分类号： A61K31/425

摘要： Hypolipemiant compositions comprising an effective amount of at least one 2-alkyl-5-thiazole-carboxylic acid derivative of the formula ##STR1## wherein R is hydrogen, an alkali metal, ammonium, the monovalent residue of an organic base or a substituted or unsubstituted alkyl and where R'.sub.1 is a linear alkyl of 1 to 12 carbon atoms, and a major amount of a pharmaceutical carrier; as well as the method of reducing the amount of sanguine lipids in warm-blooded animals utilizing the above-hypolipemiant compositions.

摘要翻译： 包含有效量的至少一种下式的2-烷基-5-噻唑 - 羧酸衍生物，其中R是氢，碱金属，铵，有机碱的一价残基或取代或未取代的低分子量组合物 烷基，其中R'1是1至12个碳原子的直链烷基，和主要量的药物载体; 以及利用上述降血脂组合物减少温血动物中血糖量的方法。