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1. 发明申请

WO2018048762A1 INDAZOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2018048762A1
公开(公告)日：2018-03-15
申请号：PCT/US2017/050003
申请日：2017-09-05
申请人： JANSSEN PHARMACEUTICA NV , GAUL, Micheal
发明人： GAUL, Micheal , XU, Guozhang , YANG, Shyh-Ming , LU, Tianbao , ZHANG, Rui , SONG, Fengbin
IPC分类号： C07D405/14 , C07D231/56 , C07D401/04 , C07D401/06 , C07D409/04 , A61K31/416 , A61P3/10
摘要： The present invention is directed to indazole derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.

2. 发明申请

WO2011075565A1 SUBSTITUTED AMINOTHIAZOLONE INDAZOLES AS ESTROGEN RELATED RECEPTOR-Aα MODULATORS 审中-公开
标题翻译：作为雌激素相关受体-Aa调节剂的替代氨苄西泮
公开(公告)号：WO2011075565A1
公开(公告)日：2011-06-23
申请号：PCT/US2010/060720
申请日：2010-12-16
申请人： JANSSEN PHARMACEUTICA NV , BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-Ping
发明人： BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-Ping
IPC分类号： C07D417/06 , C07D417/14 , C07D417/10 , C07D487/08 , C07D491/04 , A61K31/496 , A61P35/00
CPC分类号： C07D417/14 , C07D417/06 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/04 , C07D498/08
摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone- related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
摘要翻译：本发明涉及式（I）化合物，这些化合物的制备方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期关节炎，银屑病关节炎，反应性关节炎），骨相关疾病（包括与骨形成有关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失，软骨变性和与软骨形成相关的软骨变性），软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性呕吐，脂质障碍，代谢综合征骨髓瘤，肥胖，骨关节炎，成骨不全，骨溶解骨骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿综合征，赖特综合征，重复性应激损伤，高血糖，升高的血糖水平和胰岛素抵抗。

3. 发明申请

WO2018048763A1 INDAZOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚衍生物可用作胰高血糖素受体拮抗剂
公开(公告)号：WO2018048763A1
公开(公告)日：2018-03-15
申请号：PCT/US2017/050004
申请日：2017-09-05
申请人： JANSSEN PHARMACEUTICA NV , GAUL, Micheal
发明人： GAUL, Micheal , XU, Guozhang , YANG, Shyh-ming , LU, Tianbao , ZHANG, Rui , SONG, Fengbin
IPC分类号： C07D405/14 , C07D231/56 , C07D401/06 , C07D403/04 , C07D409/04 , A61K31/416 , A61P3/10
摘要： The present invention is directed to indazole derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
摘要翻译：本发明涉及式（I）的吲唑衍生物，含有它们的药物组合物以及它们在治疗和/或预防通过拮抗一种或多种胰高血糖素受体而改善的病症和病症中的用途，包括例如代谢性疾病，如II型糖尿病和肥胖症。

4. 发明申请

WO2018048761A1 INDOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚衍生物可用作胰高血糖素受体拮抗剂
公开(公告)号：WO2018048761A1
公开(公告)日：2018-03-15
申请号：PCT/US2017/050002
申请日：2017-09-05
申请人： JANSSEN PHARMACEUTICA NV , GAUL, Micheal
发明人： GAUL, Micheal , XU, Guozhang , ZHAO, Bao-ping
IPC分类号： C07D401/06 , C07D409/04 , C07D209/08 , A61K31/404 , A61P3/10
摘要： The present invention is directed to indole derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment and / or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
摘要翻译：本发明涉及式（I）的吲哚衍生物，含有它们的药物组合物以及它们在治疗和/或预防通过拮抗一种或多种胰高血糖素受体而改善的病症和病症中的用途，包括例如代谢性疾病，如II型糖尿病和肥胖症。

5. 发明申请

WO2014164286A1 DUAL SGLT1/SGLT2 INHIBITORS 审中-公开
标题翻译： DUAL SGLT1 / SGLT2抑制剂
公开(公告)号：WO2014164286A1
公开(公告)日：2014-10-09
申请号：PCT/US2014/021724
申请日：2014-03-07
申请人： JANSSEN PHARMACEUTICA NV , GAUL, Micheal , KUO, Gee-Hong , XU, Guozhang , ZHAO, Bao-Ping
发明人： GAUL, Micheal , KUO, Gee-Hong , XU, Guozhang , ZHAO, Bao-Ping
IPC分类号： A61K31/351 , C07D405/10 , C07D409/10 , C07D409/14 , C07D417/10 , A61P3/10
CPC分类号： C07D417/10 , C07D407/10 , C07D409/10 , C07D409/14
摘要： The present invention relates to compounds of Formula (I), as dual SGLT1/SGLT2 inhibitors for use in the treatment of diabetes, wherein A is selected from the group consisting of (AA) and (BB).
摘要翻译：本发明涉及作为用于治疗糖尿病的双重SGLT1 / SGLT2抑制剂的式（I）化合物，其中A选自（AA）和（BB）。

6. 发明申请

WO2011103134A1 AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS 审中-公开
标题翻译：作为雌激素相关受体 - 阿尔法调节剂的氨基丁糖
公开(公告)号：WO2011103134A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025004
申请日：2011-02-16
申请人： JANSSEN PHARMACEUTICA NV , BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-Ping
发明人： BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-Ping
IPC分类号： C07D417/06 , C07D417/14 , A61K31/4439 , A61K31/427 , A61P19/00
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone- related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
摘要翻译：本发明涉及式（I）化合物，制备这些化合物的方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（例如类风湿性关节炎，感染性关节炎，儿童期关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失，软骨变性和与软骨形成相关的软骨变性），软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性呕吐，脂质障碍，代谢综合征骨髓瘤，肥胖，骨关节炎，成骨不全，骨溶解骨转移，骨软化，骨质疏松症，佩吉特氏病，牙周病，风湿综合征，赖特综合征，重复性应激损伤，高血糖，升高的血糖水平和胰岛素抵抗。

7. 发明申请

WO2018089449A1 BENZOCYCLOBUTANE DERIVATIVES USEFUL AS DUAL SGLT1/SGLT2 MODULATORS 审中-公开
标题翻译：用作双SGLT1 / SGLT2调节剂的苯并环丁烷衍生物
公开(公告)号：WO2018089449A1
公开(公告)日：2018-05-17
申请号：PCT/US2017/060576
申请日：2017-11-08
申请人： JANSSEN PHARMACEUTICA NV , GAUL, Micheal
发明人： GAUL, Micheal , KUO, Gee-Hong , XU, Guozhang , LIANG, Yin
IPC分类号： C07D309/10 , C07H7/04 , A61P3/10 , A61K31/351
摘要： The present invention is directed to benzocyclobutane derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity. More particularly, the compounds of the present invention are useful in the treatment of for example, Type II diabetes mellitus, Syndrome X, and complications and symptoms associated with said disorders.
摘要翻译：本发明涉及苯并环丁烷衍生物，含有它们的药物组合物以及它们在治疗由SGLT活性调节的病症和病症中的用途，更具体地说是双重SGLT1 / 2活性。更具体地说，本发明化合物可用于治疗例如II型糖尿病，X综合征，以及与所述疾病相关的并发症和症状。

8. 发明申请

WO2011149841A1 SUBSTITUTED THIAZOLIDINEDIONE INDAZOLES, INDOLES AND BENZOTRIAZOLES AS ESTROGEN-RELATED RECEPTOR-α MODULATORS 审中-公开
标题翻译：作为雌激素相关受体 - 调节剂的替扎唑啉衍生物，吲哚酚和苯并噻唑
公开(公告)号：WO2011149841A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/037571
申请日：2011-05-23
申请人： JANSSEN PHARMACEUTICA NV , BIGNAN, Gilles , CHEUNG, Wing , GAUL, Micheal , HUANG, Hui , LI, Xun , PATCH, Raymond , PATEL, Sharmila , PLAYER, Mark , XU, Guozhang , ZHAO, Bao-ping , LIU, Jian
发明人： BIGNAN, Gilles , CHEUNG, Wing , GAUL, Micheal , HUANG, Hui , LI, Xun , PATCH, Raymond , PATEL, Sharmila , PLAYER, Mark , XU, Guozhang , ZHAO, Bao-ping , LIU, Jian
IPC分类号： C07D417/06 , A61K31/427 , A61P7/00 , A61P11/00 , A61P19/00 , A61P35/00
CPC分类号： C07D417/06
摘要： The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
摘要翻译：本发明涉及式（I）化合物，这些化合物的制备方法，组合物，中间体及其衍生物，用于治疗包括但不限于强直性脊柱炎，动脉粥样硬化，关节炎（如类风湿性关节炎，感染性关节炎，儿童期关节炎，牛皮癣关节炎，反应性关节炎），骨相关疾病（包括与骨形成相关的疾病），乳腺癌（包括对抗雌激素治疗无反应的那些），心血管疾病，软骨相关疾病（如软骨损伤/损失，软骨变性和与软骨形成相关的软骨变性），软骨发育不全，软骨肉瘤，慢性背部损伤，慢性支气管炎，慢性炎症性气道疾病，慢性阻塞性肺病，糖尿病，能量稳态障碍，痛风，假性呕吐，脂质障碍，代谢综合征骨髓瘤，肥胖症，骨关节炎，成骨不全，骨质溶解骨骨质疏松症，骨质疏松症，佩吉特氏病，牙周病，风湿性多肌痛，莱特综合征，重复性应激损伤，高血糖症，升高的血糖水平和胰岛素抵抗。

9. 发明申请

WO2011103130A8 AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS 审中-公开
公开(公告)号：WO2011103130A8
公开(公告)日：2011-08-25
申请号：PCT/US2011/024999
申请日：2011-02-16
申请人： JANSSEN PHARMACEUTICA NV , BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-ping
发明人： BIGNAN, Gilles , GAUL, Micheal , XU, Guozhang , ZHAO, Bao-ping
IPC分类号： C07D417/06 , C07D417/14 , A61K31/427 , A61P5/30
摘要： The present invention relates to compounds of Formula (I): methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone- related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

10. 发明申请

WO2021018951A1 PHTHALAZIN-1-ONE DERIVATIVES USEFUL AS GRK2 INHIBITORS 审中-公开
公开(公告)号：WO2021018951A1
公开(公告)日：2021-02-04
申请号：PCT/EP2020/071376
申请日：2020-07-29
申请人： JANSSEN PHARMACEUTICA NV
发明人： XU, Guozhang , GAUL, Micheal D.
IPC分类号： C07D403/04 , C07D405/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/12 , A61K31/502
摘要： The present invention is directed to phthalazin-1-one derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GRK2, including the treatment of for example, cardiac failure, cardiac hypertrophy, hypertension, Type II diabetes Mellitus, NASH, NAFLD, End-stage kidney disease, kidney failure, etc.

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