公开(公告)号：US4736034A

公开(公告)日：1988-04-05

申请号：US29086

申请日：1987-03-23

申请人： Lucien Nedelec ,  Patrick Fauveau ,  Gilles Hamon ,  Claude Oberlander

发明人： Lucien Nedelec ,  Patrick Fauveau ,  Gilles Hamon ,  Claude Oberlander

IPC分类号： C07D211/22 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P25/00 ,  A61P25/02 ,  C07D211/26 ,  C07D211/42 ,  C07D211/70 ,  C07D401/04

CPC分类号： C07D401/04 ,  C07D211/26

摘要： A compound selected from the group consisting of a compound of the formulae ##STR1## wherein R.sub.1 ' is selected from the group consisting of alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms, R' is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and phenyl alkyl of 7 to 12 carbon atoms optionally substituted with one or more members of the group consisting of alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, halogen and alkenyl of 3 to 5 carbon atoms and alkynyl of 3 to 5 carbon atoms with the proviso that the multiple bond is not between the carbons .alpha.- and .beta. to the nitrogen atom and B is a reversible secondary amine blocking group and their haloamines.

摘要翻译： 选自下列化合物的化合物：其中R 1'选自1至5个碳原子的烷氧基，苯氧基和7至9个碳原子的苯基烷氧基，R'选自式 由1至5个碳原子的烷基，4至7个碳原子的环烷基烷基和7至12个碳原子的苯基烷基任选被1至5个碳原子的烷基中的一个或多个成员所取代， 至5个碳原子，3至5个碳原子的卤素和烯基和3至5个碳原子的炔基，条件是多重键不在氮原子的α和β之间，而B是可逆的仲胺封闭 组及其卤胺。

公开(公告)号：US4694011A

公开(公告)日：1987-09-15

申请号：US838242

申请日：1986-03-10

申请人： Lucien Nedelec ,  Gilles Hamon ,  Patrick Fauveau ,  Claude Oberlander

发明人： Lucien Nedelec ,  Gilles Hamon ,  Patrick Fauveau ,  Claude Oberlander

IPC分类号： C07D211/22 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P25/00 ,  A61P25/02 ,  C07D211/26 ,  C07D211/42 ,  C07D211/70 ,  C07D401/04 ,  C07D209/34 ,  A61K31/40

CPC分类号： C07D401/04 ,  C07D211/26

摘要： Novel 7-hydroxy-indoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms and aralkyl of 7 to 12 carbon atoms optionally substituted by one or more members of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen and alkenyl and alkynyl of 3 to 5 carbon atoms with the multiple bond being other than between the carbons .alpha.- and .beta.- to the nitrogen atom, R.sub.1 is selected from the group consisting of --OH, alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having remarkable dopaminergic properties with few central effects and a novel process and novel intermediates for their preparation.

摘要翻译： 式VII的新型7-羟基 - 吲哚，其中R选自氢，1至5个碳原子的烷基，4至7个碳原子的环烷基烷基和7至12个碳原子的芳烷基，任选被 由1至5个碳原子的烷基和烷氧基组成的组中的一个或多个成员，具有3至5个碳原子的卤素和链烯基和炔基，多重键不同于与氮原子之间的α-和β-的碳原子， R1选自-OH，1至5个碳原子的烷氧基，7至9个碳原子的苯氧基和苯基烷氧基及其无毒的药学上可接受的酸加成盐，具有极少的中枢效应的显着的多巴胺能性质， 工艺和新型中间体的制备。

公开(公告)号：US4661482A

公开(公告)日：1987-04-28

申请号：US833347

申请日：1986-02-25

申请人： Lucien Nedelec ,  Patrick Fauveau ,  Gilles Hamon ,  Claude Oberlander

发明人： Lucien Nedelec ,  Patrick Fauveau ,  Gilles Hamon ,  Claude Oberlander

IPC分类号： A61K31/535 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  A61P5/00 ,  A61P7/00 ,  A61P9/12 ,  A61P25/00 ,  A61P25/28 ,  C07D265/36 ,  C07D498/04 ,  C07D265/34

CPC分类号： C07D265/36

摘要： Novel pyrazolobenzoxazines of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl or 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 5 carbon atoms with the proviso that the multiple bond is not between the carbon .alpha.- and .beta.- to the nitrogen atom, aralkyl of 7 to 12 carbon atoms and aralkyl of 7 to 12 carbon atoms substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, amino, -OH and halogen, X is selected from the group consisting of hydrogen and --CH.sub.2 --S--Alk, Alk is alkyl of 1 to 5 carbon atoms, the wavy line indicates the .alpha.- or .beta.-position and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic agonistic, hypotensive, antihypertensive and antianoxic properties and their preparation.

摘要翻译： 新颖的式（Ⅰ）的吡唑并苯并恶嗪其中R选自氢，1至5个碳原子的烷基，环烷基烷基或4至7个碳原子，3至5个碳原子的链烯基和炔基，条件是 多个键不在与氮原子的碳原子和β之间，7-12个碳原子的芳烷基和7至12个碳原子的芳烷基被至少一个由1至5个碳原子的烷基和烷氧基组成的组取代的芳烷基 碳原子，氨基，-OH和卤素，X选自氢和-CH 2 -S-Alk，Alk是1至5个碳原子的烷基，波浪线表示α或β位，它们的 具有多巴胺能激动，降血压，抗高血压和抗痉挛性质的无毒，药学上可接受的酸加成盐及其制备。

公开(公告)号：US4831043A

公开(公告)日：1989-05-16

申请号：US155303

申请日：1988-02-12

申请人： Patrick Fauveau ,  Lucien Nedelec ,  Constantin Agouridas ,  Gilles Hamon

发明人： Patrick Fauveau ,  Lucien Nedelec ,  Constantin Agouridas ,  Gilles Hamon

IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61K31/451 ,  A61P1/04 ,  A61P1/08 ,  A61P9/08 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D211/26 ,  C07D401/04

CPC分类号： C07D401/04 ,  C07D211/26

摘要： Novel benzimidazol-2-ones of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, alkenyl and alkynyl of 3 to 5 carbon atoms with the multiple bond not between the carbons .alpha.- and .beta.- to the nitrogen and aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of halogen and alkyl and alkoxy of 1 to 5 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, --OH, alkoxy of 1 to 5 carbon atoms, phenoxy and phenylalkoxy of 7 to 9 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having dopaminergic, antiulcerous, and antihypertensive and vasodilatatory activity.

摘要翻译： 式Ⅰ的新型苯并咪唑-2-酮其中R选自氢，1至5个碳原子的烷基，4至7个碳原子的环烷基烷基，3至5个碳原子的链烯基和炔基， 选择不是碳原子的碳原子和碳原子之间的碳原子数为7〜12个碳原子的碳原子和碳原子数为1〜5的烷基和烷氧基中的至少一个成员所取代的碳原子和R1之间的多重键， 由氢，-OH，1至5个碳原子的烷氧基，7至9个碳原子的苯氧基和苯基烷氧基组成的组，以及它们具有多巴胺能，抗溃疡和抗高血压和血管扩张活性的无毒的药学上可接受的酸加成盐。

公开(公告)号：US4493836A

公开(公告)日：1985-01-15

申请号：US493355

申请日：1983-05-10

申请人： Lucien Nedelec ,  Andre Pierdet ,  Patrick Fauveau

发明人： Lucien Nedelec ,  Andre Pierdet ,  Patrick Fauveau

IPC分类号： A61K31/535 ,  A61P9/12 ,  A61P43/00 ,  C07D209/00 ,  C07D209/90 ,  C07D265/00 ,  C07D498/06 ,  C07D498/04

CPC分类号： C07D209/90

摘要： Novel derivatives of 9-oxalysergic acid of the formula ##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 hydrogen, chlorine and bromine, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of --CH.sub.2 OH, alkylthiomethyl with 1 to 4 alkyl carbon atoms, --CH.sub.2 CN, --COOH, --COOAlk and ##STR2## Alk is alkyl of 1 to 5 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, R.sub.5 is alkyl of 1 to 5 carbon atoms or R.sub.4 and R.sub.5 together with the nitrogen form a saturated heterocycle optionally containing another heteroatom and their non-toxic, pharmaceutically acceptable acid addition salts having essentially dopaminergic agonist activity, inhibiting activity of prolactin secretion, serotoninergic activity and antihypertensive activity and their preparation.

摘要翻译： 其中R选自氢和1至4个碳原子的烷基，其中R选自氢，氯和溴，R2选自下列化学式的9-氧代戊酸的新型衍生物：其中R选自氢， 由氢，1-4个碳原子的烷基，7-12个碳原子的芳烷基和4-7个碳原子的环烷基烷基组成的组中，R3选自-CH2OH，具有1-4个烷基碳原子的烷硫基甲基 ，-CH 2 CN，-COOH，-COOAlk和Alk是1至5个碳原子的烷基，R 4选自氢和1至5个碳原子的烷基，R 5是1至5个碳原子的烷基 或R 4和R 5与氮一起形成任选地含有另外的杂原子的饱和杂环及其无毒的药学上可接受的酸加成盐，其具有基本上多巴胺能激动剂活性，抑制催乳素分泌的活性，血清素能活性和抗高血压 随行活动及其准备。

公开(公告)号：US4503053A

公开(公告)日：1985-03-05

申请号：US532740

申请日：1983-09-15

申请人： Lucien Nedelec ,  Jean-Claude Gasc ,  Patrick Fauveau

发明人： Lucien Nedelec ,  Jean-Claude Gasc ,  Patrick Fauveau

IPC分类号： A61K31/535 ,  A61P25/00 ,  A61P43/00 ,  C07D209/00 ,  C07D265/00 ,  C07D498/06

CPC分类号： C07D209/94 ,  C07D498/06

摘要： Novel C-homo-9-oxa-ergolines of the formula ##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 hydrogen, chlorine and bromine or taken with b forms .dbd.0, a and b form a carbon-carbon bond or a is hydrogen when R.sub.1 and b form .dbd.0, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, aralkyl of 7 to 12 carbon atoms and cycloalkylalkyl of 4 to 7 carbon atoms, R.sub.3 is selected from the group consisting of hydroxymethyl, alkylthiomethyl of 1 to 5 alkyl carbon atoms, cyanomethyl, carboxy optionally esterified with an aliphatic alcohol of 1 to 5 carbon atoms and ##STR2## R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.5 is alkyl of 1 to 4 carbon atoms or R.sub.4 and R.sub.5 taken with the nitrogen atom form a saturated heterocycle optionally containing a second heteroatom having dopaminergic agonist, serotoninergic and antihypertensive activity as well as prolactin secretion inhibition and antianoxic activities and their preparation and intermediates.

摘要翻译： 式（Ⅰ）的新型C-高-9-氧杂 - 麦角醇其中R选自氢和1至4个碳原子的烷基，R 1选自氢，氯和溴或 以b形式= 0取代，a和b形成碳 - 碳键，或者当R 1和b形成= 0时，a为氢，R 2选自氢，1至4个碳原子的烷基，7至 12个碳原子和4至7个碳原子的环烷基烷基，R 3选自羟甲基，1至5个烷基碳原子的烷基硫甲基，氰基甲基，任选被1至5个碳原子的脂族醇酯化的羧基， R4选自氢和1-4个碳原子的烷基，R5是1-4个碳原子的烷基或R4和R5与氮原子一起形成饱和杂环，任选地含有具有多巴胺能激动剂的第二个杂原子，5-羟色胺能 和抗高血压活动 以及催乳素分泌抑制和抗氧化活性及其制备和中间体。

公开(公告)号：US20060035820A1

公开(公告)日：2006-02-16

申请号：US11225627

申请日：2005-09-13

申请人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

发明人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

IPC分类号： A61K38/12 ,  C07K5/12

CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S930/27

摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b—C≡N radical or R1 and R2 together with the nitrogen which carries-them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear,. branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.

摘要翻译： 本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4， 氢或羟基R：代表线性。 支链或环状链T：氢，甲基，CH 2 CONH 2，CH 2C≡N，a（CH 2） / SUB 2）或（CH 2）2 N 2 O 2 N 2 O 2 N 2 N 2 O 2 X，卤素和烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH，Z：H，CH 3 。 式（I）化合物具有抗真菌性质。

公开(公告)号：US5141952A

公开(公告)日：1992-08-25

申请号：US716950

申请日：1991-06-18

申请人： Constantin Agouridas ,  Patrick Fauveau

发明人： Constantin Agouridas ,  Patrick Fauveau

IPC分类号： A61K31/35 ,  A61K31/351 ,  A61K31/445 ,  A61K39/39 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D211/18 ,  C07D211/60 ,  C07D211/78 ,  C07D309/08 ,  C07D309/10 ,  C07D309/28

CPC分类号： C07D309/10 ,  C07D211/18 ,  C07D211/60

摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein the dotted lines represent a possible endo or exo double bond, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms and ##STR2## R'.sub.2 is alkyl of 1 to 8 carbon atoms or aryl of 6 to 14 carbon atoms, X is --O-- or --NR--, R is selected from the group consisting of --OH, hydrogen, ##STR3## and --COOR', R' is hydrogen or alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and alkenyl and alkynyl of 2 to 8 carbon atoms, all optionally substituted with at least one halogen or --OH, with the proviso that if Y is --OH, X is not --NH-- and their non-toxic, pharmaceutically acceptable addition salts of acids or bases having antibacterial and immunological properties.

摘要翻译： 选自下式的化合物的化合物，其中虚线表示可能的内端或外双键，R 1和R 2分别选自氢，1至8个碳原子的烷基 2至8个碳原子的烯基和炔基，6至14个碳原子的芳基，7至18个碳原子的芳烷基和1至8个碳原子的烷基或6至14个碳原子的芳基， X是-O-或-NR-，R选自-OH，氢，IMA和-COOR'，R'是氢或1至8个碳原子的烷基，Y选自 由氢，1至8个碳原子的烷基和2至8个碳原子的烯基和炔基组成，全部任选被至少一个卤素或-OH取代，条件是如果Y是-OH，X不是-NH- 及其无毒，药学上可接受的具有抗菌和免疫学特性的酸或碱的加成盐。

公开(公告)号：US07192920B2

公开(公告)日：2007-03-20

申请号：US11225627

申请日：2005-09-13

申请人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

发明人： Patrick Fauveau ,  Stephen Hawser ,  Gilles Lebourg ,  Laurent Schio

IPC分类号： A61K38/12

CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S930/27

摘要： A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I): in which either R1: H or CH3 and R2: cyclohexyl substituted by an amine, a (CH2)b-C≡N radical or R1 and R2 together with the nitrogen which carries them form a ring with 3, 4 or 5 carbons optionally substituted by an amine R3: hydrogen, methyl or hydroxyl R4: hydrogen or hydroxyl R: represents a linear, branched or cyclic chain T: hydrogen, methyl, CH2CONH2, CH2C≡N, a (CH2)2NH2 or (CH2)2Nalk+X− radical, X halogen and alk alkyl Y: hydrogen, hydroxyl, halogen or OSO3H, W: H or OH, Z: H, CH3. The compounds of formula (I) have antifungal properties.

摘要翻译： 本发明的所有可能的异构体形式以及它们的混合物的主题是式（I）的化合物：其中R 1，H或CH 3 和R 2：被胺取代的环己基，（CH 2 H 2）bC≡N基或R 1和R 2， / SUB与携带它们的氮一起形成具有3,4或5个碳原子的环，任选被胺R 3取代：氢，甲基或羟基R 4： 氢或羟基R：表示直链，支链或环状的链T：氢，甲基，CH 2 CONH 2，CH 2C≡N （CH 2）2 NH 2或（CH 2 CH 2）2，或（CH 2）2 卤素，烷基Y：氢，羟基，卤素或OSO 3 H，W：H或OH， Z：H，CH 3。 式（I）化合物具有抗真菌性质。

公开(公告)号：US07160983B2

公开(公告)日：2007-01-09

申请号：US10666072

申请日：2003-09-19

申请人： Olivier Courtin ,  Patrick Fauveau ,  Astrid Markus ,  Dominique Melon Manguer ,  Jean-Marc Michel ,  Laurent Schio

发明人： Olivier Courtin ,  Patrick Fauveau ,  Astrid Markus ,  Dominique Melon Manguer ,  Jean-Marc Michel ,  Laurent Schio

IPC分类号： C07K7/50

CPC分类号： A01N43/90 ,  A61K38/00 ,  C07D487/18 ,  C07K7/56

摘要： Compound of the formula wherein R2 is —CH2—CH2—NH2, R3 is —CH3, R4 is —OH, R is Z is methyl and salts thereof which are useful as antifungal agents.

摘要翻译： 下式的化合物其中R 2是-CH 2 -CH 2 -NH 2，其中R 1，R 2， 3是-CH 3，R 4是-OH，R是Z是甲基，其盐可用作抗真菌剂。