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1. 发明申请

WO2018083157A1 SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS 审中-公开
标题翻译：用于治疗软骨病的替代吡啶[3,4-B]吲哚
公开(公告)号：WO2018083157A1
公开(公告)日：2018-05-11
申请号：PCT/EP2017/078026
申请日：2017-11-02
申请人： SANOFI
发明人： GRETZKE, Dirk , RITZELER, Olaf , HEINELT, Uwe , WEHNER, Volkmar , SCHMIDT, Friedemann
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P19/02
摘要： The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R 1 to R 6 and R 10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的8-芳基取代的和8-杂芳基取代的9H-吡啶并[3,4-b]吲哚，其中A，E，G， R 1至R 6和R 10如权利要求中所定义，其刺激软骨形成和软骨基质合成并可用于治疗需要软骨病症和需要再生受损软骨的病症，例如关节病如骨关节炎。本发明还涉及合成式（I）化合物的方法，其作为药物的用途以及包含它们的药物组合物。

2. 发明申请

WO2013041502A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：WO2013041502A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/068291
申请日：2012-09-18
申请人： SANOFI
发明人： NAZARE, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I），（R2）n的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和 n具有权利要求中所示的含义。式（I）的化合物是调节蛋白激酶活性的有价值的药理学活性化合物，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性，并且适用于治疗SGK活性不合适的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及制备式（I）化合物，其作为药物的用途以及包含它们的药物组合物的方法。

3. 发明申请

WO2014140065A1 N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N-（4-（AZAINDAZOL-6-YL） - 苯基） - 磺酰胺及其作为药物的用途
公开(公告)号：WO2014140065A1
公开(公告)日：2014-09-18
申请号：PCT/EP2014/054770
申请日：2014-03-12
申请人： SANOFI
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , KLEEMANN, Heinz-Werner , WEISS, Tilo , SAAS, Joachim , STRUEBING, Carsten
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61P9/00 , A61P19/02
CPC分类号： C07D487/04 , A61K31/4162 , C07D471/04
摘要： N-(4-(Azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译： N-（4-（苯并恶唑-6-基） - 苯基） - 磺酰胺及其作为药物的用途本发明涉及式I的N-（4-（氮杂唑-6-基） - 苯基） - 磺酰胺，其中 Ar，n，X，Z，R 1，R 2和R 3具有权利要求中所示的含义。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适合于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

4. 发明申请

WO2013041119A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：WO2013041119A1
公开(公告)日：2013-03-28
申请号：PCT/EP2011/066220
申请日：2011-09-19
申请人： SANOFI , NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]- sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基]磺酰胺，其中Ar，R 1，R 2和n具有如索赔。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适用于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

5. 发明授权

EP3535263B1 SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS 有权转让
公开(公告)号：EP3535263B1
公开(公告)日：2020-09-30
申请号：EP17794307.3
申请日：2017-11-02
申请人： Sanofi
发明人： GRETZKE, Dirk , RITZELER, Olaf , HEINELT, Uwe , WEHNER, Volkmar , SCHMIDT, Friedemann
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P19/02

6. 发明公开

EP2970259A1 N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N- [4-（AZAINDAZOL-6-YL） - 苯基] - 磺基苯甲酸酯在VERWENDUNG ALS ARZNEIMITTEL
公开(公告)号：EP2970259A1
公开(公告)日：2016-01-20
申请号：EP14711467.2
申请日：2014-03-12
申请人： SANOFI
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , KLEEMANN, Heinz-Werner , WEISS, Tilo , SAAS, Joachim , STRUEBING, Carsten
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61P9/00 , A61P19/02
CPC分类号： C07D487/04 , A61K31/4162 , C07D471/04
摘要： N-(4-(Azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的N-（4-（氮杂吲唑-6-基） - 苯基） - 磺酰胺，其中Ar，n，X，Z，R 1，R 2和R 3具有权利要求中所示的含义。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶异构体1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适用于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及制备式I化合物，其作为药物的用途以及包含它们的药物组合物的方法。

7. 发明授权

EP2758399B1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：EP2758399B1
公开(公告)日：2017-11-15
申请号：EP12759725.0
申请日：2012-09-18
申请人： SANOFI
发明人： NAZARE, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin , CARRY, Jean-Christophe
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04

8. 发明公开

EP3535263A1 SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS 有权转让
公开(公告)号：EP3535263A1
公开(公告)日：2019-09-11
申请号：EP17794307.3
申请日：2017-11-02
申请人： Sanofi
发明人： GRETZKE, Dirk , RITZELER, Olaf , HEINELT, Uwe , WEHNER, Volkmar , SCHMIDT, Friedemann
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P19/02
摘要： Substituted pyrido[3,4-b]indoles and their use as pharmaceuticals The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula I, in which A, E, G, R 1 to R 6 and R 10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

9. 发明授权

EP2970259B1 N-(4-(AZAINDAZOL-6-YL)-PHENYL)-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N-（4-（AZAINDAZOL-6-YL） - 苯基） - 磺酰胺及其作为药物的用途
公开(公告)号：EP2970259B1
公开(公告)日：2016-12-21
申请号：EP14711467.2
申请日：2014-03-12
申请人： SANOFI
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , KLEEMANN, Heinz-Werner , WEISS, Tilo , SAAS, Joachim , STRUEBING, Carsten
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/52 , A61P9/00 , A61P19/02
CPC分类号： C07D487/04 , A61K31/4162 , C07D471/04

10. 发明公开

EP2758399A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 有权
标题翻译： N- [4-（1H-吡唑并[3,4-B]哒嗪-6-基） - 苯基] - 磺酰胺在DEREN VERWENDUNG ALS ARZNEIMITTEL
公开(公告)号：EP2758399A1
公开(公告)日：2014-07-30
申请号：EP12759725.0
申请日：2012-09-18
申请人： SANOFI
发明人： NAZARE, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin , CARRY, Jean-Christophe
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如索赔。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶异构体1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适用于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及制备式I化合物，其作为药物的用途以及包含它们的药物组合物的方法。

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