公开(公告)号：US11827633B2

公开(公告)日：2023-11-28

申请号：US17409513

申请日：2021-08-23

申请人： Sanofi

发明人： Dirk Gretzke ,  Olaf Ritzeler ,  Uwe Heinelt ,  Volkmar Wehner ,  Friedemann Schmidt

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P19/02

CPC分类号： C07D471/04 ,  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, R1 to R6 and R10 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.

公开(公告)号：US20240182469A1

公开(公告)日：2024-06-06

申请号：US18488871

申请日：2023-10-17

申请人： Sanofi

发明人： Dirk Gretzke ,  Olaf Ritzeler ,  Uwe Heinelt ,  Volkmar Wehner ,  Friedemann Schmidt

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P19/02

CPC分类号： C07D471/04 ,  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, R1 to R6 and R10 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.

公开(公告)号：US20140349986A1

公开(公告)日：2014-11-27

申请号：US14339957

申请日：2014-07-24

申请人： SANOFI

发明人： Nils Rackelmann ,  Laurent Bialy ,  Heinrich Englert ,  Klaus Wirth ,  Petra Arndt ,  John Weston ,  Uwe Heinelt ,  Markus Follmann

IPC分类号： C07D487/10 ,  C07D487/04 ,  C07D401/12 ,  C07D211/56 ,  C07D411/12 ,  C07D413/12 ,  C07D405/12 ,  C07D403/04 ,  C07D205/04 ,  C07D243/08 ,  C07D487/08 ,  C07D417/12

CPC分类号： C07D487/10 ,  C07D205/04 ,  C07D207/08 ,  C07D211/56 ,  C07D243/08 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D487/08

摘要： The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

摘要翻译： 本发明涉及式I的取代氨基茚满及其类似物及其药学用途。 包含这种类型化合物的药物适用于预防或治疗多种疾病，例如呼吸系统疾病，囊性纤维化疾病，急性或慢性肾脏疾病或排便障碍。

公开(公告)号：US08871798B2

公开(公告)日：2014-10-28

申请号：US13652898

申请日：2012-10-16

申请人： Sanofi

发明人： Karl Schoenafinger ,  Henning Steinhagen ,  Bodo Scheiper ,  Uwe Heinelt ,  Volkmar Herrmann ,  Matthias Herrmann

IPC分类号： C07D471/14 ,  C07D487/14 ,  C07D498/14 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5383 ,  A61P7/02

CPC分类号： C07D471/14 ,  C07D487/14 ,  C07D498/14

摘要： This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.

摘要翻译： 本公开涉及式I化合物：其中R 1，R 2，R 3，R 4，X和Y具有本公开中表示的含义。 式I的化合物具有抗血栓活性，特别是抑制蛋白酶活化的受体1（PAR1）。 本公开还涉及制备式I化合物的方法及其作为药物产品的用途。

公开(公告)号：US08791133B2

公开(公告)日：2014-07-29

申请号：US13652893

申请日：2012-10-16

申请人： Sanofi

发明人： Karl Schoenafinager ,  Henning Steinhagen ,  Bodo Scheiper ,  Uwe Heinelt ,  Volkmar Wehner ,  Matthias Herrmann ,  Jacques Mauger ,  Pavel Safar

IPC分类号： A61K31/4745

CPC分类号： C07D471/04

摘要： The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.

摘要翻译： 本公开涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5和X基团如本公开所定义，具有抗血栓活性，其特别是抑制蛋白酶活化的受体1（PAR1）。 本公开进一步涉及其制备方法及其作为药物产品的用途。

公开(公告)号：US09550788B2

公开(公告)日：2017-01-24

申请号：US14339957

申请日：2014-07-24

申请人： SANOFI

发明人： Nils Rackelmann ,  Laurent Bialy ,  Heinrich Englert ,  Klaus Wirth ,  Petra Arndt ,  John Weston ,  Uwe Heinelt ,  Markus Follmann

IPC分类号： C07D487/10 ,  C07D487/04 ,  C07D401/12 ,  C07D211/56 ,  C07D411/12 ,  C07D413/12 ,  C07D405/12 ,  C07D403/04 ,  C07D205/04 ,  C07D243/08 ,  C07D487/08 ,  C07D417/12 ,  C07D207/08 ,  C07D403/12

CPC分类号： C07D487/10 ,  C07D205/04 ,  C07D207/08 ,  C07D211/56 ,  C07D243/08 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D487/08

摘要： The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

摘要翻译： 本发明涉及式I的取代氨基茚子及其类似物及其药学用途。 包含这种类型化合物的药物适用于预防或治疗多种疾病，例如呼吸系统疾病，囊性纤维化疾病，急性或慢性肾脏疾病或排便障碍。

公开(公告)号：US11130755B2

公开(公告)日：2021-09-28

申请号：US16347386

申请日：2017-11-02

申请人： SANOFI

发明人： Dirk Gretzke ,  Olaf Ritzeler ,  Uwe Heinelt ,  Volkmar Wehner ,  Friedemann Schmidt

IPC分类号： A61K31/437 ,  C07D471/04 ,  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, R1 to R6 and R10 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.