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1. 发明申请

WO2007137874A3 IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH 审中-公开
公开(公告)号：WO2007137874A3
公开(公告)日：2007-12-06
申请号：PCT/EP2007/005145
申请日：2007-05-31
申请人： GALAPAGOS SAS , NIQUE, François , ROBIN-JAGERSCHMIDT, Catherine , CLEMENT-LACROIX, Philippe
发明人： NIQUE, François , ROBIN-JAGERSCHMIDT, Catherine , CLEMENT-LACROIX, Philippe
IPC分类号： A61K31/4166 , C07D231/20 , A61P5/26
摘要： Compounds of formula (I): wherein X is O or S, R 1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R 2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R 3 and R 4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R 3 and R 4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R 5 is H, halogen, trifluoromethyl, -CN, or -NO2; not all of R 3 , R 4 , and R 5 being H, R 6 and R 9 are H, halogen, OH; alkyl. hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R 7 and R 8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R 7 and R 8 not being H or halogen; or one of R 7 and R 8 is a pharmaceutically acceptable ester or thioester grouping, or R 6 is C 1-3 -alkyl or, together with either R 1 or R 2 , represents C 1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.

2. 发明申请

WO2007137874A8 IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH 审中-公开
标题翻译：咪唑啉衍生物，其用途及其制备方法和包含此类化合物的组合物
公开(公告)号：WO2007137874A8
公开(公告)日：2008-02-07
申请号：PCT/EP2007005145
申请日：2007-05-31
申请人： PROSKELIA SAS , NIQUE FRANCOIS , ROBIN-JAGERSCHMIDT CATHERINE , CLEMENT-LACROIX PHILIPPE
发明人： NIQUE FRANCOIS , ROBIN-JAGERSCHMIDT CATHERINE , CLEMENT-LACROIX PHILIPPE
CPC分类号： A61K31/4166 , C07D233/78 , C07D405/06 , C07D405/12 , C07D409/06 , C07D487/04 , C07D493/04
摘要： Compounds of formula (I): wherein X is O or S, R 1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R 2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R 3 and R 4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R 3 and R 4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R 5 is H, halogen, trifluoromethyl, -CN, or -NO2; not all of R 3 , R 4 , and R 5 being H, R 6 and R 9 are H, halogen, OH; alkyl. hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R 7 and R 8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R 7 and R 8 not being H or halogen; or one of R 7 and R 8 is a pharmaceutically acceptable ester or thioester grouping, or R 6 is C 1-3 -alkyl or, together with either R 1 or R 2 , represents C 1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
摘要翻译：式（I）化合物：其中X为O或S，R 1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R 2为H 烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 羰基; R 3和R 4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN ，或-NO 2; 不是全部R 3，R 4和R 5都是H，R 6和R 3， 9是H，卤素，OH; 烷基。羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R 7和R 8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R 7和R 8之一不是H或卤素; 或R 7和R 8中的一个是药学上可接受的酯或硫酯基团，或R 6是C 1-3烷基，或者与R 1或R 2 2一起代表C 1-3亚烷基或亚烯基连接基团，任选取代的甲基，三氟甲基，OH或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

3. 发明申请

WO2007137874A2 INIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH 审中-公开
标题翻译：氮杂吲哚衍生物，其用途，其制备方法和包含此类化合物的组合物
公开(公告)号：WO2007137874A2
公开(公告)日：2007-12-06
申请号：PCT/EP2007005145
申请日：2007-05-31
申请人： PROSKELIA SAS , NIQUE FRANCOISE , ROBIN-JAGERSCHMIDT CATHERINE , CLEMENT-LACROIX PHILIPPE
发明人： NIQUE FRANCOISE , ROBIN-JAGERSCHMIDT CATHERINE , CLEMENT-LACROIX PHILIPPE
CPC分类号： A61K31/4166 , C07D233/78 , C07D405/06 , C07D405/12 , C07D409/06 , C07D487/04 , C07D493/04
摘要： Compounds of formula (I): wherein X is O or S, R 1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R 2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R 3 and R 4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R 3 and R 4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R 5 is H, halogen, trifluoromethyl, -CN, or -NO2; not all of R 3 , R 4 , and R 5 being H, R 6 and R 9 are H, halogen, OH; alkyl. hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R 7 and R 8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R 7 and R 8 not being H or halogen; or one of R 7 and R 8 is a pharmaceutically acceptable ester or thioester grouping, or R 6 is C 1-3 -alkyl or, together with either R 1 or R 2 , represents C 1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
摘要翻译：式（I）化合物：其中X为O或S，R 1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R 2为H 烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 羰基; R 3和R 4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN ，或-NO 2; 不是全部R 3，R 4和R 5都是H，R 6和R 3， 9是H，卤素，OH; 烷基。羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R 7和R 8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R 7和R 8之一不是H或卤素; 或R 7和R 8中的一个是药学上可接受的酯或硫酯基团，或R 6是C 1-3烷基，或者与R 1或R 2 2一起代表C 1-3亚烷基或亚烯基连接基团，任选取代的甲基，三氟甲基，OH或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

4. 发明申请

WO2005027883A1 GSK-3 BETA INHIBITORS IN THE TREATMENT OF BONE-RELATED DISEASES 审中-公开
标题翻译：葛根素-3抑制剂治疗骨相关疾病
公开(公告)号：WO2005027883A1
公开(公告)日：2005-03-31
申请号：PCT/IB2004/003297
申请日：2004-09-20
申请人： PROSKELIA PHARMACEUTICALS , RAWADI, Georges , ROMAN, Sergio , CLEMENT-LACROIX, Philippe
发明人： RAWADI, Georges , ROMAN, Sergio , CLEMENT-LACROIX, Philippe
IPC分类号： A61K31/00
CPC分类号： A61K31/00 , A61K33/00 , A61K33/24 , A61K33/30
摘要： The present invention relates to methods for preventing and/or treating bone-related diseases in mammals, especially humans, using GSK-3ß inhibitors. The invention also concerns methods for selecting in vitro and/or in vivo compounds useful for preventing and/or treating bone-related diseases in mammals, including humans.
摘要翻译：本发明涉及使用GSK-3β抑制剂预防和/或治疗哺乳动物，特别是人类的骨相关疾病的方法。本发明还涉及用于选择体外和/或体内用于预防和/或治疗哺乳动物（包括人）中骨相关疾病的化合物的方法。

5. 发明申请

WO2006061430A3 BONE METASTASIS MARKERS AS A TARGET REGULATING BONE METASTASIS AND BONE DEVELOPMENT 审中-公开
标题翻译：骨转移标记物作为靶标调节骨转移和骨发育
公开(公告)号：WO2006061430A3
公开(公告)日：2006-08-03
申请号：PCT/EP2005056636
申请日：2005-12-09
申请人： PROSKELIA , EDICALE INSERM INST NAT DE LA , CLEMENT-LACROIX PHILIPPE , CLEZARDIN PHILIPPE , JACKSON AMANDA , PUJUGUET PHILIPPE
发明人： CLEMENT-LACROIX PHILIPPE , CLEZARDIN PHILIPPE , JACKSON AMANDA , PUJUGUET PHILIPPE
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/136 , C12Q2600/158
摘要： The present invention concerns a method of, and products for, diagnosing bone disorders using bone metastasis specifie gene markers, including ITGBL1.
摘要翻译：本发明涉及使用骨转移特异性基因标记（包括ITGBL1）诊断骨骼疾病的方法和产品。

6. 发明申请

WO2006061430A2 ITGBL-1 AS A TARGET REGULATING BONE METASTASIS AND BONE DEVELOPMENT 审中-公开
标题翻译： ITGBL-1作为目标调节骨转移和骨发育
公开(公告)号：WO2006061430A2
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056636
申请日：2005-12-09
申请人： PROSKELIA , INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM) , CLEMENT-LACROIX, Philippe , CLEZARDIN, Philippe , JACKSON, Amanda , PUJUGUET, Philippe
发明人： CLEMENT-LACROIX, Philippe , CLEZARDIN, Philippe , JACKSON, Amanda , PUJUGUET, Philippe
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6886 , C12Q2600/136 , C12Q2600/158
摘要： The present invention concerns a method of, and products for, diagnosing bone disorders using bone metastasis specifie gene markers, including ITGBL1.
摘要翻译：本发明涉及使用骨转移特异性基因标记（包括ITGBL1）诊断骨骼疾病的方法和产品。

7. 发明申请

WO2006005633A1 COMBINATIONS OF PURE ANTI-ESTROGEN WITH AROMATASE INHIBITORS 审中-公开
标题翻译：纯抗雌激素与芳香酶抑制剂的组合
公开(公告)号：WO2006005633A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/008205
申请日：2005-07-06
申请人： PROSKELIA S.A.S. , NIQUE, François , CLEMENT-LACROIX, Philippe
发明人： NIQUE, François , CLEMENT-LACROIX, Philippe
IPC分类号： A61K31/58
CPC分类号： A61K31/58 , A61K31/56 , A61K2300/00
摘要： Combinations of pure anti-estrogens, with aromatase inhibitors. The pure anti-estrogen can be a 19-nor steroid having a thiocarbonated chain in position 11β. The activity of the aromatase inhibitor is potentiated by the pure anti-estrogen.
摘要翻译：纯抗雌激素与芳香酶抑制剂的组合。纯抗雌激素可以是在11β位置具有硫代碳链的19-类固醇。芳香酶抑制剂的活性由纯抗雌激素增强。

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