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1. 发明授权

US5861529A Farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：法呢基转移酶抑制剂，它们的制备和含有它们的药物组合物
公开(公告)号：US5861529A
公开(公告)日：1999-01-19
申请号：US750819
申请日：1997-06-18
申请人： Bernard Baudoin , Christopher Burns , Alain Commercon , Jean-Dominique Guitton
发明人： Bernard Baudoin , Christopher Burns , Alain Commercon , Jean-Dominique Guitton
IPC分类号： C07C323/25 , C07C323/59 , C07C323/60 , A01N37/12
CPC分类号： C07C323/25 , C07C323/59 , C07C323/60 , C07C2102/08
摘要： This invention relates to transferase inhibitors of the formula (I), their preparation, and pharmaceutical compositions containing them. ##STR1## In formula (I), R.sub.1 is Y--S--A.sub.1 --(Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl radical, an alkoxycarbonyl radical, or an R.sub.4 --S-- radical in which R.sub.4 is an alkyl radical containing 1 to 4 carbon atoms optionally substituted by a phenyl radical or a radical of the formula (II) ##STR2## in which A.sub.1 is an alkylene radical containing 1 to 4 carbon atoms optionally substituted at the position a in the grouping >C(X.sub.1)(Y.sub.1) with an amino, alkylamino, dialkylamino, alkanoylamino, or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or form, together with the carbon atom to which they are connected, a >C.dbd.O grouping; R'.sub.1 is hydrogen or methyl; R.sub.2 is an alkyl, alkenyl or an alkynyl radical containing 1 to 6 carbon atoms optionally substituted by a hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl, or alkylsulphonyl, wherein when R.sub.2 is an alkyl radical substituted by a hydroxyl radical, R.sub.2 can form a lactone with the carboxyl radical at the .alpha. position; R'.sub.2 is hydrogen or methyl; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical; and the radical ##STR3## is in position 5 or 6 of the naphthyl ring. These compounds have anti-cancer properties.
摘要翻译： PCT No.PCT / FR95 / 00739 Sec。 371日期：1997年6月18日 102（e）日期1997年6月18日PCT提交1995年6月7日PCT公布。第WO95 / 34535号公报日期1995年12月21日本发明涉及式（I）的转移酶抑制剂，其制备方法和含有它们的药物组合物。（I）式（I）中，R 1为YS-A1-（Y为氢原子，氨基酸残基，脂肪酸残基，烷基，烷氧基羰基或R4-S-基）其中R 4是任选被苯基或式（II）的基团取代的含有1至4个碳原子的烷基，其中A 1是含有1至4个碳原子的亚烷基，任选地被取代在在具有氨基，烷基氨基，二烷基氨基，烷酰基氨基或烷氧基羰基氨基的基团> C（X1）（Y1）中的位置a）; X1和Y1各自为氢原子或形式，与它们连接的碳原子一起为> C = O基团; R'1是氢或甲基; R2是任选被羟基，烷氧基，巯基，烷硫基，烷基亚磺酰基或烷基磺酰基取代的含有1至6个碳原子的烷基，烯基或炔基，其中当R2是被羟基取代的烷基时，R2可以形成内酯与羧基在α位置; R'2是氢或甲基; 并且R是氢原子或任选取代的烷基或任选取代的苯基; 并且基团在萘环的5或6位。这些化合物具有抗癌特性。

2. 发明授权

US5750567A Farnesyl transferase inhibitors, preparation thereof and pharmaceutical compositions containing same 失效
标题翻译：法呢基转移酶抑制剂，其制备方法和含有其的药物组合物
公开(公告)号：US5750567A
公开(公告)日：1998-05-12
申请号：US875005
申请日：1997-07-15
申请人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Le Brun
发明人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Le Brun
IPC分类号： A61K31/195 , A61K31/215 , A61P35/00 , A61P43/00 , C07C323/25 , C07C323/59 , A61K31/21
CPC分类号： C07C323/25 , C07C323/59
摘要： Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, or an alkyl or alkoxycarbonyl radical, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1,) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical wherein the alkyl or alkanoyl portion contains 1-6 carbon atoms; each of X.sub.1 and Y.sub.1 is a hydrogen atom or X.sub.1 and Y.sub.1, taken toether with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl.
摘要翻译： PCT No.PCT / FR96 / 00067 Sec。 371日期1997年7月15日 102（e）日期1997年7月15日PCT 1996年1月16日PCT PCT。公开号WO96 / 22278 日本1996年7月25日通式（I）的新型法呢基转移酶抑制剂（I）其制备方法和含有其的药物组合物。在通式（I）中，R 1为YS-A1-（其中Y为氢原子，氨基酸残基，脂肪酸残基或烷基或烷氧羰基，A1为C1-4亚烷基，在其中烷基或烷酰基部分含有1-6个碳原子的氨基，烷基氨基，烷酰基氨基或烷氧基羰基氨基的基团中被取代> C（X1）（Y1）中的每一个，X1和Y1各自为氢原子或X1和Y1，与其连接的碳原子一起形成C = O基团; R'1是氢或C1-6烷基; X是氧或硫原子; R2是C1-6烷基，烯基或任选被羟基，烷氧基，巯基，烷硫基，烷基亚磺酰基或烷基磺酰基取代的炔基。

3. 发明授权

US5889053A Farnesyl transferase inhibitors, preparation thereof and pharmaceuticals compositions containing said inhibitors 失效
标题翻译：法呢基转移酶抑制剂，其制备物和含有所述抑制剂的药物组合物
公开(公告)号：US5889053A
公开(公告)日：1999-03-30
申请号：US5154
申请日：1998-01-09
申请人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Lebrun
发明人： Bernard Baudoin , Christopher Burns , Alain Commercon , Alain Lebrun
IPC分类号： A61K31/195 , A61K31/215 , A61P35/00 , A61P43/00 , C07C323/59 , A61K31/235
CPC分类号： C07C323/59
摘要： Novel farnesyl transferase inhibitors of general formula (I), ##STR1## the preparation thereof and pharmaceutical compositions containing said inhibitors, are disclosed. In general formula (I), R.sub.1 is Y--S--A.sub.1 (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical or a radical R.sub.4 --S-- where R.sub.4 is a C.sub.1-4 alkyl radical optionally substituted by a phenyl radical or a radical of general formula (II) ##STR2## wherein A.sub.1, X, X.sub.1, Y.sub.1, R'.sub.1, R.sub.2, R'.sub.2 and R are defined as below, and A.sub.1 is a C.sub.1-4 alkylene radical optionally alpha-substituted in the >C(X.sub.1)(Y.sub.1) grouping by an amino or alkylamino, dialkylamino, alkanoylamino or alkoxycarbonylamino radical); X.sub.1 and Y.sub.1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that when R.sub.2 is an alkyl radical substituted by a hydroxy radical, R.sub.2 can form a lactone with the .alpha.-carboxy radical; and R'.sub.2 is hydrogen or a C.sub.1-6 alkyl radical; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted pheny radical, with the proviso that radical (a) ##STR3## is in the 3 or 4 position of the naphthyl ring. The novel products have anticancer properties.
摘要翻译：公开了通式（I）的新型法呢基转移酶抑制剂，其制备方法和含有所述抑制剂的药物组合物。在通式（I）中，R 1是YS-A1（其中Y是氢原子，氨基酸残基，脂肪酸残基，烷基或烷氧基羰基或基团R 4 -S-，其中R 4是C 1-4烷基任选被苯基或通式（II）的基团取代的基团其中A1，X，X1，Y1，R'1，R2，R'2和R定义如下，而A1是通过氨基或烷基氨基，二烷基氨基，烷酰基氨基或烷氧基羰基氨基，在> C（X1）（Y1）组中任意α-取代的C1-4亚烷基; X1和Y1各自为氢原子，或与它们所连接的碳原子一起形成> C = O基团; R 1是氢或C 1-6烷基; X是氧或硫原子; R2是任选被羟基，烷氧基，巯基，烷硫基，烷基亚磺酰基或烷基磺酰基取代的C 1-6烷基，烯基或炔基，条件是当R 2是被羟基取代的烷基时，R 2可以与 α-羧基; 和R'2是氢或C 1-6烷基; 并且R是氢原子或任选取代的烷基或任选取代的苯基，条件是基团（a）（a）在萘环的3或4位。新产品具有抗癌性能。

4. 发明授权

US08372864B2 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives, preparation and therapeutic use thereof 有权
标题翻译： 1-氧代 - 异吲哚啉-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺衍生物，其制备和治疗用途
公开(公告)号：US08372864B2
公开(公告)日：2013-02-12
申请号：US12693597
申请日：2010-01-26
申请人： Bernard Baudoin , Michel Evers , Arielle Genevois-Borella , Andreas Karlsson , Jean-Luc Malleron , Magali Mathieu
发明人： Bernard Baudoin , Michel Evers , Arielle Genevois-Borella , Andreas Karlsson , Jean-Luc Malleron , Magali Mathieu
IPC分类号： A61K31/4035 , A61K31/47 , C07D209/44 , C07D217/24
CPC分类号： C07D209/46 , C07D217/24 , C07D413/12
摘要： The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof.
摘要翻译：本发明涉及1-氧代 - 异吲哚啉-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺的衍生物及其制备方法及其治疗用途。

5. 发明申请

US20060199837A1 SUBSTITUTED TETRAHYDRO-1H-PYRAZOLO [3,4-C]PYRIDINES COMPOSITIONS COMPRISING THEM, AND USE 失效
标题翻译：取代的四氢-1H-吡唑并[3,4-C]吡啶类化合物及其用途
公开(公告)号：US20060199837A1
公开(公告)日：2006-09-07
申请号：US11419794
申请日：2006-05-23
申请人： Fabienne Thompson , Patrick Mailliet , Teresa Damiano , Marie-Pierre Cherrier , Francois Clerc , Frank Halley , Herve Bouchard , Laurence Gauzy-Lazo , Bernard Baudoin , Catherine Squaille , Fabrice Viviani , Michel Tabart
发明人： Fabienne Thompson , Patrick Mailliet , Teresa Damiano , Marie-Pierre Cherrier , Francois Clerc , Frank Halley , Herve Bouchard , Laurence Gauzy-Lazo , Bernard Baudoin , Catherine Squaille , Fabrice Viviani , Michel Tabart
IPC分类号： C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology.
摘要翻译：取代的四氢-1H-吡唑并[3,4-c]吡啶，包含它们的组合物和用途。本发明特别涉及具有治疗活性的新型取代的四氢-1H-吡唑并[3,4-c]吡啶，其特别可用于肿瘤学。

6. 发明授权

US07309701B2 Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them 有权
标题翻译：哒嗪酮衍生物作为药物和含有它们的药物组合物
公开(公告)号：US07309701B2
公开(公告)日：2007-12-18
申请号：US10715358
申请日：2003-11-19
申请人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi
发明人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi
IPC分类号： C07D413/12 , C07D403/12 , C07D237/04 , A61K31/501 , A61K31/50
CPC分类号： C07D401/04 , C07D237/14 , C07D237/24 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
摘要翻译：本发明涉及通式（I）的新的哒嗪酮衍生物，其中A为A 1或A 2; R是未取代的或至少单取代的C 1 -C 10 - 烷基，芳基，芳基 - （C 1 -C 10 - 烷基） - ，杂芳基，杂芳基 - （C 1 -C 10 - 烷基） - ，杂环基，杂环基 - （C 1 -C 12 - C 1 -C 10 - 烷基） - ，C 3 -C 10 - 环烷基，多环烷基，C 2 - C 10 - 链烯基或C 2 -C 10 - 炔基，Ar是未取代的或至少单取代的芳基或杂芳基。

7. 发明授权

US07259154B2 Pyrrolopyrimidines 失效
标题翻译：吡咯并嘧啶
公开(公告)号：US07259154B2
公开(公告)日：2007-08-21
申请号：US10744478
申请日：2003-12-23
申请人： Paul Joseph Cox , Tahir Nadeem Majid , Stephanie Daniele Deprets , Shelley Amendola , Iain McFarlane McLay , Christopher Edlin , David John Aldous , Brian Pedgrift , Frank Halley , Michael Edwards , Bernard Baudoin
发明人： Paul Joseph Cox , Tahir Nadeem Majid , Stephanie Daniele Deprets , Shelley Amendola , Iain McFarlane McLay , Christopher Edlin , David John Aldous , Brian Pedgrift , Frank Halley , Michael Edwards , Bernard Baudoin
IPC分类号： C07D413/04 , C07D487/04 , A61P11/06 , A61K31/5355 , A61K31/519 , A61K31/66 , C07F9/38
CPC分类号： C07D487/04
摘要： Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.
摘要翻译：这些化合物的式和N-氧化物，前体药物，酸性生物电子等排物，这些化合物的药学上可接受的盐或溶剂化物，或这些盐或溶剂化物的N-氧化物，前体药物或酸性生物电子等离子体对包含这些化合物的组合物，以及包括向有需要的患者施用此类化合物和组合物。

8. 发明授权

US07462613B2 Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them 失效
标题翻译：哒嗪酮衍生物作为药物和含有它们的药物组合物
公开(公告)号：US07462613B2
公开(公告)日：2008-12-09
申请号：US10715556
申请日：2003-11-19
申请人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cécile Combeau , Ingrid Sassoon , Anke Steinmetz
发明人： Swen Hölder , Thorsten Naumann , Karl Schönafinger , David William Will , Hans Matter , Günther Müller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cécile Combeau , Ingrid Sassoon , Anke Steinmetz
IPC分类号： C07D403/02 , A61K31/501
CPC分类号： C07D401/04 , C07D237/14
摘要： The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
摘要翻译：本发明涉及通式（I）的新的哒嗪酮衍生物，其中A为A 1或A 2; R是未取代的或至少单取代的C 1 -C 10 - 烷基，芳基，芳基 - （C 1 -C 10 - 烷基） - ，杂芳基，杂芳基 - （C 1 -C 10 - 烷基） - ，杂环基，杂环基 - （C 1 -C 10 - 烷基） C 3 -C 10 - 环烷基，多环烷基，C 2 -C 10 - 烯基或C 2 -C 10 - 炔基，Ar是未取代的或至少单取代的芳基或杂芳基。

9. 发明申请

US20050026918A1 Novel pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them 失效
标题翻译：新的哒嗪酮衍生物作为药物和含有它们的药物组合物
公开(公告)号：US20050026918A1
公开(公告)日：2005-02-03
申请号：US10715556
申请日：2003-11-19
申请人： Swen Holder , Thorsten Naumann , Karl Schonafinger , David Will , Hans Matter , Gunther Muller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cecile Combeau , Ingrid Sassoon , Anke Steinmetz
发明人： Swen Holder , Thorsten Naumann , Karl Schonafinger , David Will , Hans Matter , Gunther Muller , Dominique Le Suisse , Bernard Baudoin , Thomas Rooney , Franck Halley , Gilles Tiraboschi , Cecile Combeau , Ingrid Sassoon , Anke Steinmetz
IPC分类号： C07D237/14 , C07D401/04 , A61K31/501 , A61K31/50 , C07
CPC分类号： C07D401/04 , C07D237/14
摘要： The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.
摘要翻译：本发明涉及通式（I）的新的哒嗪酮衍生物，其中A为A 1或A 2; R是未取代的或至少单取代的C 1 -C 10 - 烷基，芳基，芳基 - （C 1 -C 10 - 烷基） - ，杂芳基，杂芳基 - （C 1 -C 10 - 烷基） - ，杂环基，杂环基 - （C 1 -C 10 - 烷基） C 3 -C 10 - 环烷基，多环烷基，C 2 -C 10 - 烯基或C 2 -C 10 - 炔基，Ar是未取代的或至少单取代的芳基或杂芳基。

10. 发明授权

US07435820B2 Substituted tetrahydro-1H-pyrazolo [3,4-c]pyridines compositions comprising them, and use 失效
标题翻译：包含它们的取代的四氢-1H-吡唑并[3,4-c]吡啶组合物，并使用
公开(公告)号：US07435820B2
公开(公告)日：2008-10-14
申请号：US11419794
申请日：2006-05-23
申请人： Fabienne Thompson , Catherine Souaille , Fabrice Viviani , Michel Tabart , Patrick Mailliet , Teresa Damiano , Marie-Pierre Cherrier , Francois Clerc , Frank Halley , Herve Bouchard , Laurence Gauzy-Lazo , Bernard Baudoin
发明人： Fabienne Thompson , Catherine Souaille , Fabrice Viviani , Michel Tabart , Patrick Mailliet , Teresa Damiano , Marie-Pierre Cherrier , Francois Clerc , Frank Halley , Herve Bouchard , Laurence Gauzy-Lazo , Bernard Baudoin
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04
摘要： Substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines, compositions comprising them and use. The present invention relates in particular to novel substituted tetrahydro-1H-pyrazolo[3,4-c]pyridines having therapeutic activity, which can be used in particular in oncology.
摘要翻译：取代的四氢-1H-吡唑并[3,4-c]吡啶，包含它们的组合物和用途。本发明特别涉及具有治疗活性的新型取代的四氢-1H-吡唑并[3,4-c]吡啶，其特别可用于肿瘤学。

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