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1. 发明授权

US06277845B1 Hydrazono-benzazulene derivatives, pharmaceutical compositions and intermediates 失效
标题翻译：肼基 - 苯并薁衍生物，药物组合物和中间体
公开(公告)号：US06277845B1
公开(公告)日：2001-08-21
申请号：US09509263
申请日：2000-07-07
申请人： Denis Carniato , Thomas R. Gadek , Francois Goubet , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Karl-Heinz Scheunemann
发明人： Denis Carniato , Thomas R. Gadek , Francois Goubet , Jean-Francois Gourvest , Jochen Knolle , Robert S. McDowell , Karl-Heinz Scheunemann
IPC分类号： C07D23350
CPC分类号： C07C333/04 , C07C49/747 , C07C323/22 , C07D233/52
摘要： Compounds of the formula wherein the substituents are as defined in the application and their pharmaceutically acceptable acid and base salts thereof which are useful for preventing loss of bone matrix.
摘要翻译：取代基中的取代基的化合物如本申请中所定义，并且其药学上可接受的酸和碱盐可用于防止骨基质的损失。

2. 发明授权

US5556983A Phenylimidazolidines 失效
标题翻译：苯基咪唑烷
公开(公告)号：US5556983A
公开(公告)日：1996-09-17
申请号：US388131
申请日：1995-02-13
申请人： Andr e Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andr e Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D233/72 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , C07D233/74 , C07D233/76 , C07D233/82 , C07D233/86 , C07D233/88 , C07D235/02 , C07D233/42 , C07D233/40
CPC分类号： C07D233/76 , C07D233/86 , C07D233/88 , C07D235/02
摘要： Novel phenyimidazolidines having the following formula ##STR1## wherein the substituents are as recited in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-androgenic activity.
摘要翻译：具有下列结构式的新型苯基咪唑烷：其中取代基如说明书中所述及其无毒的，药学上可接受的具有抗雄激素活性的酸加成盐。

3. 发明授权

US6087509A 1-Imidazolidinyl-phenyls 失效
标题翻译： 1-咪唑烷基 - 苯基
公开(公告)号：US6087509A
公开(公告)日：2000-07-11
申请号：US77223
申请日：1998-05-20
申请人： Andre Claussner , Francois Goubet , Jean-George Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-George Teutsch
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4164 , A61K31/4166 , A61K31/4184 , A61P13/00 , A61P13/08 , A61P17/00 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07D233/72 , C07D233/76 , C07D233/78 , C07D235/02 , C07D405/12 , A61N5/28 , A61N17/10
CPC分类号： C07D235/02 , A61K31/4166 , C07D233/76
摘要： A particular subject of the invention is the products of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 represent in particular cyano and trifluoromethyl,R.sub.3 represents in particular alkyl, alkenyl or alkynyl, optionally substituted by one or more halogen, cyano or hydroxyl radicals,R.sub.4 and R.sub.5 either represent in particular methyl optionally substituted by fluorine,or form in particular a cyclohexyl radical,X and Y represent in particular oxygen,as well as their salts and isomers.
摘要翻译： PCT No.PCT / FR96 / 01846 Sec。 371日期1998年6月23日第 102（e）日期1998年6月23日PCT 1996年11月21日PCT PCT。 WO97 / 19064 PCT公开号日期：1997年5月29日本发明的具体主题是式（I）的产物：其中：R1和R2特别表示氰基和三氟甲基，R3表示特别是烷基，烯基或炔基，任选地被一个或多个卤素，氰基或羟基，R4和R5特别表示任选被氟取代的甲基，或特别形成环己基，X和Y特别表示氧，以及它们的盐和异构体。

4. 发明授权

US5646172A Method of inducing antiandrogenic activity using imidazolidines substituted with a heterocycle 失效
标题翻译：用杂环取代咪唑烷诱导抗雄激素活性的方法
公开(公告)号：US5646172A
公开(公告)日：1997-07-08
申请号：US524508
申请日：1995-09-07
申请人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D487/10 , A61K31/415 , A61K31/4178 , A61K31/445 , A61P5/28 , A61P43/00 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/113 , C07D495/10 , C07D401/04 , C07D403/04
CPC分类号： C07D471/10 , C07D491/10 , C07D495/10
摘要： Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
摘要翻译：式I的新型咪唑，其中取代基如本公开内容所定义，它们与具有抗雄激素活性的酸和碱的无毒的药学上可接受的加成盐。

5. 发明授权

US5627201A Phenylimidazolidines having antiandrogenic activity 失效
标题翻译：具有抗雄激素活性的苯基咪唑烷
公开(公告)号：US5627201A
公开(公告)日：1997-05-06
申请号：US372648
申请日：1995-01-13
申请人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
发明人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
IPC分类号： C07D233/72 , C07D233/74 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88 , A61K31/415
CPC分类号： C07D233/74 , C07D233/72 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88
摘要： A compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --NO.sub.2 and halogen, R.sub.2 is --CF.sub.3 or halogen, --A--B-- is selected from the group consisting of ##STR2## X is --O-- or --S--, R.sub.3 is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted with at least one member of the group consisting of --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted with a member of the group consisting of halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl and alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted with at least one member of the group consisting of oxygen, nitrogen and sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A--B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
摘要翻译：式Ⅰ化合物，其中R 1选自-CN，-NO 2和卤素，R 2为-CF 3或卤素，-AB-选自下组：X为-O - 或-S-，R 3选自氢，烷基，烯基和至多12个碳原子的炔基，最多12个碳原子的芳基和芳烷基，全部任选被至少一个成员组成的基团的至多7个碳原子的-OH，卤素，-SH，-CN，酰基和酰氧基，至多12个碳原子的芳基，-O-芳基，-O-芳烷基-S-芳基，芳基和芳烷基任选地被卤素，-CF 3，烷基，烷氧基，烯基，烯氧基，炔基和炔氧基取代，硫任选被氧化成砜或亚砜，游离，酯化，酰胺化或成盐的羧基，-NH 2，单和 3至6个环成员的二烷基氨基和杂环基并含有至少一个选自氧，硫的杂原子 ur和氮，烷基，烯基和炔基任选地被至少一个由氧，氮和硫组成的组中任意地被氧化成亚砜或砜，具有1-6个碳原子的烷基的三烷基甲硅烷基和酰基和酰氧基 1至7个碳原子的有机羧酸，Y是-O - ， - S-或-NH-，但其中-AB-是X的化合物是氧，R 3是氢，Y是氧或-NH - ，R 2是-CF 3或卤素，R 1是-NO 2或卤素及其无毒的药学上可接受的酸加成盐。

6. 发明授权

US5705654A Imidazolidines substituted with a heterocycle 失效
标题翻译：被杂环取代的咪唑啉
公开(公告)号：US5705654A
公开(公告)日：1998-01-06
申请号：US695690
申请日：1996-08-12
申请人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D487/10 , A61K31/415 , A61K31/4178 , A61K31/445 , A61P5/28 , A61P43/00 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/113 , C07D495/10 , C07D235/00
CPC分类号： C07D471/10 , C07D491/10 , C07D495/10
摘要： Described herein are novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
摘要翻译：本文描述的是式I的新型咪唑，其中取代基如本公开内容所定义，它们与具有抗雄激素活性的酸和碱的无毒的药学上可接受的加成盐。

7. 发明授权

US5434176A Phenylimidazolidines 失效
标题翻译：苯基咪唑烷
公开(公告)号：US5434176A
公开(公告)日：1995-07-18
申请号：US68736
申请日：1993-05-28
申请人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D233/72 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , C07D233/74 , C07D233/76 , C07D233/82 , C07D233/86 , C07D233/88 , C07D235/02
CPC分类号： C07D233/76 , C07D233/86 , C07D233/88 , C07D235/02
摘要： A compound selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of --CN, --NO.sub.2, halogen, --CF.sub.3, free carboxy, salified carboxy, and carboxy esterified with lower alkyl; -A-B- is selected from the group consisting of ##STR2## and X, R.sub.3, R.sub.4 and R.sub.5 are defined as in the specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-androgenic activity.
摘要翻译：选自下列化合物的化合物：其中R 1和R 2分别选自-CN，-NO 2，卤素，-CF 3，游离羧基，盐化羧基和羧基酯化的化合物烷基; -A-B-选自和X，R3，R4和R5如说明书中所定义，它们的无毒的药学上可接受的具有抗雄激素活性的酸加成盐。

8. 发明授权

US5411981A Phenylimidazolidines having antiandrogenic activity 失效
标题翻译：具有抗雄激素活性的苯基咪唑烷
公开(公告)号：US5411981A
公开(公告)日：1995-05-02
申请号：US64257
申请日：1993-05-18
申请人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
发明人： Martine Gaillard-Kelly , Francois Goubet , Daniel Philibert , Jean-Georges Teutsch
IPC分类号： C07D233/72 , C07D233/74 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88 , A61K31/415
CPC分类号： C07D233/74 , C07D233/72 , C07D233/76 , C07D233/84 , C07D233/86 , C07D233/88
摘要： A compound of the formula ##STR1## wherein R.sub.1 is --CN, --NO.sub.2 or halogen, R.sub.2 is --CF.sub.3 or halogen, --A-B-- is of ##STR2## X is --O-- or --S--, R.sub.3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen or sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
摘要翻译：其中R 1是-CN，-NO 2或卤素，R 2是-CF 3或卤素，-AB-的化合物，其中X是-O-或-S-，R 3是氢，烷基至多12个碳原子的烯基或炔基，最多12个碳原子的芳基和芳烷基，全部任选被-OH，卤素，-SH，-CN，最多7个碳原子的酰基和酰氧基取代， - 芳基， - 任选被卤素，-CF 3，烷基，烷氧基，烯基，链烯氧基，炔基或炔氧基取代的芳基和芳烷基，其中硫任选被氧化成砜的O-芳基，至多12个碳原子的-O-芳烷基-S-芳基或亚砜，游离，酯化，酰胺化或盐化的羧基，-NH 2，单和二烷基氨基和3至6个环成员的杂环，并含有至少一个选自氧，硫和氮的杂原子，烷基，烯基和炔基任选地被至少一个氧，氮或硫任选地中断，所述氧，氮或硫任选地被氧化成亚砜或砜，具有烷基的三烷基甲硅烷基 1至6个碳原子，1至7个碳原子的有机羧酸的酰基和酰氧基，Y为-O - ， - S-或-NH-，但其中-AB-为X的化合物为氧， R3是氢，Y是氧或-NH-，R2是-CF3或卤素，R1是-NO2或卤素及其无毒的药学上可接受的酸加成盐。

9. 发明授权

US06242611B1 Phenylimidazolidines containing nitrooxy or carbonyloxy groups 失效
标题翻译：含有硝基氧基或羰基氧基的苯基咪唑烷
公开(公告)号：US06242611B1
公开(公告)日：2001-06-05
申请号：US09101027
申请日：1998-09-28
申请人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D23372
CPC分类号： C07D233/78
摘要： A subject of the invention is the products of formula (I): in which: R1 and R2 represent in particular cyano and trifluoromethyl, R3 represents in particular alkyl, alkenyl or alkynyl, substituted in particular by nitrooxy or carbonyloxy, R4 and R5 represent in particular methyl optionally substituted by fluorine, X and Y represent in particular oxygen, as well as their salts and isomers.
摘要翻译：本发明的主题是式（I）的产物：其中：R 1和R 2特别表示氰基和三氟甲基，R 3特别表示烷基，烯基或炔基，特别被硝基氧基或羰氧基取代，R 4和R 5表示任选被氟取代的特定甲基，X和Y特别表示氧，以及它们的盐和异构体。

10. 发明授权

US5958936A Imidazolidines substituted with a heterocycle 失效
标题翻译：被杂环取代的咪唑啉
公开(公告)号：US5958936A
公开(公告)日：1999-09-28
申请号：US935708
申请日：1997-09-23
申请人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
发明人： Andre Claussner , Francois Goubet , Jean-Georges Teutsch
IPC分类号： C07D487/10 , A61K31/415 , A61K31/4178 , A61K31/445 , A61P5/28 , A61P43/00 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/113 , C07D495/10
CPC分类号： C07D471/10 , C07D491/10 , C07D495/10
摘要： Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
摘要翻译：新的具有下式的咪唑，其中取代基如本公开内容所定义，它们与具有抗雄激素活性的酸和碱的无毒的药学上可接受的加成盐。

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