公开(公告)号：US5746840A

公开(公告)日：1998-05-05

申请号：US827204

申请日：1997-03-28

申请人： Albert Louis Anna Willemsens ,  Walter Louis Antoine Verstappen ,  Alex Herman Copmans ,  Anna Maria Jozefa Vandendriessche ,  Alfons Gaston Maria De Knaep ,  Marc Gaston Venet

发明人： Albert Louis Anna Willemsens ,  Walter Louis Antoine Verstappen ,  Alex Herman Copmans ,  Anna Maria Jozefa Vandendriessche ,  Alfons Gaston Maria De Knaep ,  Marc Gaston Venet

IPC分类号： C07B57/00 ,  C07D249/18 ,  C07D403/06 ,  C07D521/00

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/18

摘要： A process for preparing (+)-6-�(4-chlorophenyl)(1H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole comprising the resolution of (.+-.)-6-!(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-�(4-chlorophenyl)(H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole.

摘要翻译： 制备（+） - 6 - [（4-氯苯基）（1 + E，H + EE-1,2,4-三唑-1-基）甲基] -1-甲基-1- H + EE-苯并三唑包括（+/-） - 6 - ]（4-氯苯基） - 肼基甲基）-1-甲基-1E'，非H + EE-苯并三唑的拆分，并将合适的对映体纯的肼中间体转化为 （+） - 6 - [（4-氯苯基）（+ E，H + EE-1,2,4-三唑-1-基）甲基] -1-甲基-1E，H + EE-苯并三唑 。

公开(公告)号：US08329714B2

公开(公告)日：2012-12-11

申请号：US11669587

申请日：2007-01-31

申请人： Marc Gaston Venet ,  Patrick René Angibaud ,  David William End

发明人： Marc Gaston Venet ,  Patrick René Angibaud ,  David William End

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D491/00

CPC分类号： C07D487/14 ,  C07D487/04

摘要： (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer.

公开(公告)号：US07579352B2

公开(公告)日：2009-08-25

申请号：US11926699

申请日：2007-10-29

申请人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

发明人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4196 ,  C07D403/02 ,  C07D401/06 ,  C07D401/02 ,  C07D249/08

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/61 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中X代表O，S或NR 3; R 1表示氢，羟基，C 1-6烷基或芳基; R2表示氢; 任选取代的C 1-12烷基; C 3-7环烷基; C2-8烯基; 芳基; Het1; R 3表示氢，任选取代的C 1-6烷基，芳基，Het 1; R4代表氢; 羟基; 巯基 C 1-6烷氧基; C 1-6烷硫基; 芳氧基 芳硫基; Het1-oxy; Het1-硫代 任选取代的C 1-12烷基; 任选取代的C 2-8烯基; 任选取代的C 2-8炔基; 任选取代的C 3-7环烷基; 任选取代的C 5-7环烯基; 芳基; Het1; 或-Alk-NR 3 R 5（i）或-NR 3 R 5（ii）其中Alk表示C 1-6烷二基; 并且R 5表示氢，C 1-6烷基，芳基，Het 1，（芳基或Het 1）C 1-6烷基，（芳基或Het 1）羰基或（芳基或Het 1）C 1-6烷氧基羰基; 芳基表示任选取代的茚满基，茚基，萘基，5,6,7,8-四氢-2-萘基或苯基; Het是三唑基; 且Het1表示任选取代的单环或双环杂环; 具有视黄酸模拟活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US20080114009A1

公开(公告)日：2008-05-15

申请号：US11926741

申请日：2007-10-29

申请人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  David William End

发明人： Marc Gaston Venet ,  Patrick Rene Angibaud ,  David William End

IPC分类号： A61K31/519 ,  C07D487/14 ,  A61P35/00

CPC分类号： C07D487/14 ,  C07D487/04

摘要： (−)-5-(3-Chlorophenyl)-α-(4-chlorophenyl)-α-(1-methyl-1H-imidazol-5-yl)tetrazolo-[1,5-a]quinazoline-7-methanamine and its pharmaceutically acceptable acid addition salts, and the use of such compounds in medicine especially for the treatment of cancer

摘要翻译： （ - ） - 5-（3-氯苯基）-α-（4-氯苯基）-α-（1-甲基-1H-咪唑-5-基）四唑并[1,5-a]喹唑啉-7-甲胺和 其药学上可接受的酸加成盐，以及这些化合物在医药中的用途，特别是用于治疗癌症

公开(公告)号：US07196094B2

公开(公告)日：2007-03-27

申请号：US10381361

申请日：2001-09-18

申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Laurence Anne Mevellec

发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Laurence Anne Mevellec

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/395

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1—Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括新的式（I）化合物，

公开(公告)号：US07179825B2

公开(公告)日：2007-02-20

申请号：US11081393

申请日：2005-03-16

申请人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

发明人： Dominique Mabire ,  Christophe Denis Adelinet ,  Imré Christian Csoka ,  Marc Gaston Venet

IPC分类号： C07D213/02 ,  A61K31/44

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D233/61 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het represents an optionally substituted unsaturated heterocycle; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：US07173040B2

公开(公告)日：2007-02-06

申请号：US10381556

申请日：2001-09-18

申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Ashis Kumar Saha ,  Laurence Anne Mevellec

发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Ashis Kumar Saha ,  Laurence Anne Mevellec

IPC分类号： C07D403/06 ,  A61K31/47 ,  C07D215/227

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明包括式（I）化合物：其中r，s，t，Y 1 -Y 2，R 1，R 2， R 2，R 3，R 4，R 5，R 6和R 6， SUP> 7限定含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：US06894046B2

公开(公告)日：2005-05-17

申请号：US09812731

申请日：2001-03-19

申请人： Eddy Jean Edgard Freyne ,  Jean Fernand Armand Lacrampe ,  Frederik Dirk Deroose ,  Marc Gaston Venet

发明人： Eddy Jean Edgard Freyne ,  Jean Fernand Armand Lacrampe ,  Frederik Dirk Deroose ,  Marc Gaston Venet

IPC分类号： C07D253/06 ,  A61K31/53 ,  A61K31/7028 ,  A61K31/706 ,  A61K51/00 ,  A61P17/00 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/00 ,  C07D253/075 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07H15/26 ,  C07D253/07

CPC分类号： C07D253/075 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14

摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR5 or a direct bond; Y is O, S, NR5 or S(O)2; R1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is Het1, C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR5, then R2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het1carbonyl or Het1thiocarbonyl; R3 and R4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R3 and R4 form a C2-6alkanediyl; R5 is hydrogen or C1-4alkyl; R6 is a sulfonyl or sulfinyl derivative; R7 and R8 are independently hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl containing moiety, C3-7cycloalkyl, —Y—C1-4alkanediyl-C(═O)—O—R14, Het3, Het4 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, formyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, C1-4alkanediyl-C(═O)—O—R14, —C(═O)—O—R14, —Y—C1-4alkanediyl-C(═O)—O—R14, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R14 is hydrogen, C1-4alkyl, C3-7cycloalkyl, aminocarbonylmethylene or mono- or di(C1-4alkyl)aminocarbonylmethylene; aryl is optionally substituted phenyl; Het1, Het2, Het3 and Het4 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.

公开(公告)号：US06833375B2

公开(公告)日：2004-12-21

申请号：US10238686

申请日：2002-09-10

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： C07D41710

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R 2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R 3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

公开(公告)号：US06458800B1

公开(公告)日：2002-10-01

申请号：US09868992

申请日：2001-08-29

申请人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

发明人： Patrick René Angibaud ,  Marc Gaston Venet ,  Xavier Marc Bourdrez

IPC分类号： C07D47104

CPC分类号： C07D401/06 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein ═X1—X2—X3— is a trivalent radical,; >Y1—Y2— is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula —O—R10, —S—R10 or —NR11R12; R4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

摘要翻译： 本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中= X 1 -X 2 -X 3 - 是三价基团; Y1-Y2-是三价基; r和s各自独立地为0,1,2,3,4或5; t为0,1,2或3; 每个R 1和R 2独立地是羟基，卤素，氰基，C 1-6烷基，三卤甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基， 单或二（C 1-6烷基）氨基，单或二（C 1-6烷基）氨基C 1-6烷氧基，芳基，芳基C 1-6烷基，芳氧基或芳基C 1-6烷氧基，羟基羰基，C 1-6烷氧基羰基; 或相邻位置上的两个R1或R2一起形成二价基团; R 3是氢，卤素，C 1-6烷基，氰基，卤代C 1-6烷基，羟基C 1-6烷基，氰基C 1-6烷基，氨基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基-C 1-6烷基，氨基羰基C 1-6烷基，羟基羰基，羟基羰基C1- C 1-6烷氧基羰基C 1-6烷基，C 1-6烷基羰基C 1-6烷基，C 1-6烷氧基羰基，芳基，芳基C 1-6烷氧基C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷基，或式-O-R 10基团， S-R10或-NR11R12; R4是任选取代的咪唑基; 芳基是任选取代的苯基或萘基; 具有法呢基转移酶和香叶基香叶基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。