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1. 发明申请

US20100130454A1 9,10-SECOPREGNANE DERIVATIVES AND MEDICINE 审中-公开
标题翻译： 9,10-SECOPREGNANE衍生物和药物
公开(公告)号：US20100130454A1
公开(公告)日：2010-05-27
申请号：US11720789
申请日：2005-12-05
申请人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku
发明人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku
IPC分类号： A61K31/59 , C07C401/00 , A61P17/12 , A61P17/06
CPC分类号： C07C401/00
摘要： A novel useful vitamin D3 derivative which is reduced in influence on systemic calcium metabolism while retaining excellent vitamin D3 activity. The derivative is a 9,10-secopregnane derivative represented by the following general formula [1]. Also provided is a medicinal composition containing the derivative as an active ingredient. In the general formula [1], Y represents (1) a single bond, (2) alkylene (3) alkenylene, or (4) phenylene; R1 and R2 are the same or different and each represents (1) hydrogen, (2) alkyl, or (3) cycloalkyl, or R1 and R2 in combination represent cycloalkyl in cooperation with the adjacent carbon atom; R3 represents hydrogen or methyl; and Z represents (1) hydrogen, (2) hydroxy, or (3) —NR11R12.
摘要翻译：一种新颖有用的维生素D3衍生物，其对全身钙代谢的影响减小，同时保持优异的维生素D3活性。该衍生物是由以下通式[1]表示的9,10-仲孕烷衍生物。还提供含有该衍生物作为活性成分的药物组合物。在通式[1]中，Y表示（1）单键，（2）亚烷基（3）亚烯基或（4）亚苯基; R1和R2相同或不同，各自表示（1）氢，（2）烷基或（3）环烷基，或者R1和R2组合表示与相邻碳原子配合的环烷基; R3表示氢或甲基; Z表示（1）氢，（2）羟基或（3）-NR11R12。

2. 发明授权

US08796246B2 9, 10-secopregnane derivative and pharmaceutical 有权
标题翻译： 9,10-孕代衍生物和药物
公开(公告)号：US08796246B2
公开(公告)日：2014-08-05
申请号：US12302975
申请日：2007-06-01
申请人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku , Masaaki Shirai
发明人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku , Masaaki Shirai
IPC分类号： A61K31/593 , C07C401/00
CPC分类号： C07C401/00
摘要： A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.
摘要翻译：本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物，与常规维生素D3衍生物相比，对全身钙代谢的影响相对较小。本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。在通式[1]中，16位和17位之间的以下部分结构是指单键或双键：Y为单键，亚烷基，亚烯基或亚苯基; R1和R2相同或不同，各自表示氢，烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢，羟基或-NR 11 R 12。

3. 发明申请

US20100016263A1 9, 10-SECOPREGNANE DERIVATIVE AND PHARMACEUTICAL 有权
标题翻译： 9，10-SECOPREGNANE DERIVATIVE AND PHARMACEUTICAL
公开(公告)号：US20100016263A1
公开(公告)日：2010-01-21
申请号：US12302975
申请日：2007-06-01
申请人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku , Masaaki Shirai
发明人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku , Masaaki Shirai
IPC分类号： A61K31/593 , C07C401/00 , A61P17/00
CPC分类号： C07C401/00
摘要： A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.
摘要翻译：本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物，与常规维生素D3衍生物相比，对全身钙代谢的影响相对较小。本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。在通式[1]中，16位和17位之间的以下部分结构是指单键或双键：Y为单键，亚烷基，亚烯基或亚苯基; R1和R2相同或不同，各自表示氢，烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢，羟基或-NR 11 R 12。

4. 发明授权

US09216968B2 Heterocyclic derivative and pharmaceutical drug 有权
标题翻译：杂环衍生物和药物
公开(公告)号：US09216968B2
公开(公告)日：2015-12-22
申请号：US14238749
申请日：2012-08-17
申请人： Hironori Otsu
发明人： Hironori Otsu
IPC分类号： C07D235/30 , C07D235/08 , C07D235/12 , C07D405/04 , C07D263/56 , C07D403/12 , A61K31/343 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/56 , C07D235/06 , C07D235/10 , C07D235/14 , C07D401/12 , C07D235/26 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D307/79
CPC分类号： C07D405/04 , A61K31/343 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/26 , C07D235/30 , C07D263/56 , C07D307/79 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
摘要翻译：本发明提供了一种新的杂环衍生物或其药学上可接受的盐。例如，本发明提供通式[1]的杂环衍生物或其互变异构体或其药学上可接受的盐：其中R1和R2是相同或不同的芳环等，环A是杂环。本发明的化合物或其药学上可接受的盐具有有效的mPGES-1抑制活性，可用作治疗或预防疾病的药物，例如类风湿性关节炎，骨关节炎，颞下颌关节疾病，腰痛，子宫内膜异位症，痛经，膀胱过度活动，恶性肿瘤或神经变性疾病。

5. 发明授权

US09732066B2 Heterocyclic derivative and pharmaceutical drug 有权
公开(公告)号：US09732066B2
公开(公告)日：2017-08-15
申请号：US14923502
申请日：2015-10-27
申请人： Hironori Otsu
发明人： Hironori Otsu
IPC分类号： C07D235/06 , C07D405/04 , C07D235/30 , C07D263/56 , C07D403/12 , A61K31/343 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/56 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D401/12 , C07D235/26 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D307/79
CPC分类号： C07D405/04 , A61K31/343 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/26 , C07D235/30 , C07D263/56 , C07D307/79 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.

6. 发明申请

US20140221339A1 Heterocyclic Derivative and Pharmaceutical Drug 有权
标题翻译：杂环衍生物和药物药物
公开(公告)号：US20140221339A1
公开(公告)日：2014-08-07
申请号：US14238749
申请日：2012-08-17
申请人： Hironori Otsu
发明人： Hironori Otsu
IPC分类号： C07D405/04 , C07D263/56 , C07D307/79 , C07D403/04 , C07D231/56 , C07D401/12 , C07D235/08
CPC分类号： C07D405/04 , A61K31/343 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/26 , C07D235/30 , C07D263/56 , C07D307/79 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
摘要翻译：本发明提供了一种新的杂环衍生物或其药学上可接受的盐。例如，本发明提供通式[1]的杂环衍生物或其互变异构体或其药学上可接受的盐：其中R1和R2是相同或不同的芳环等，环A是杂环。本发明的化合物或其药学上可接受的盐具有有效的mPGES-1抑制活性，可用作治疗或预防疾病的药物，例如类风湿性关节炎，骨关节炎，颞下颌关节疾病，腰痛，子宫内膜异位症，痛经，膀胱过度活动，恶性肿瘤或神经变性疾病。

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