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1. 发明授权

US08129386B2 Fused azole-pyrimidine derivatives 有权
标题翻译：熔融唑 - 嘧啶衍生物
公开(公告)号：US08129386B2
公开(公告)日：2012-03-06
申请号：US12414257
申请日：2009-03-30
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Jishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Jishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及新型稠合吡唑嘧啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合唑类嘧啶衍生物对磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是PI3K-γ抑制作用，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

2. 发明申请

US20090270388A1 FUSED AZOLE-PYRIMIDINE DERIVATIVES 有权
标题翻译：熔融的偶氮吡啶衍生物
公开(公告)号：US20090270388A1
公开(公告)日：2009-10-29
申请号：US12414257
申请日：2009-03-30
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A61K31/519 , C07D487/04 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P3/10 , A61P35/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity.More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及新的稠合唑吡喃衍生物，其制备方法和含有它们的药物制剂。本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

3. 发明授权

US07511041B2 Fused azole-pyrimidine derivatives 有权
标题翻译：熔融唑 - 嘧啶衍生物
公开(公告)号：US07511041B2
公开(公告)日：2009-03-31
申请号：US10527376
申请日：2003-09-18
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , Florian Gantner , Kevin Bacon
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D237/26 , C07D237/36 , C07D241/36 , C07D239/00 , C07D471/00 , C07D471/04 , C07D401/04 , C07D401/22 , C07D487/00 , C07D487/04 , C07D491/00 , C07D495/00 , C07D497/00
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.
摘要翻译：本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合吡唑嘧啶衍生物对于磷脂酰肌醇-3-激酶（PI3K）抑制的效力显着增强，特别是对于PI3K-γ抑制，可用于预防和治疗与PI3K相关的疾病，特别是PI3K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的PI3K活性学科。

4. 发明申请

US20060128732A1 Fused azole-pyrimidine derivatives 有权
公开(公告)号：US20060128732A1
公开(公告)日：2006-06-15
申请号：US10527376
申请日：2003-09-18
申请人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , florian Gantner , Kevin Bacon
发明人： Mitsuyuki Shimada , Toshiki Murata , Kinji Fuchikami , Hideki Tsujishita , Naoki Omori , Issei Kato , Mami Miura , Klaus Urbahns , florian Gantner , Kevin Bacon
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

5. 发明授权

US08349857B2 Quinazoline derivatives having tyrosine kinase inhibitory activity 有权
标题翻译：具有酪氨酸激酶抑制活性的喹唑啉衍生物
公开(公告)号：US08349857B2
公开(公告)日：2013-01-08
申请号：US13359326
申请日：2012-01-26
申请人： Masaharu Kume , Kenji Matsuo , Naoki Omori , Masami Takayama , Aiko Omori , Takeshi Endo
发明人： Masaharu Kume , Kenji Matsuo , Naoki Omori , Masami Takayama , Aiko Omori , Takeshi Endo
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D407/12 , C07D417/12
摘要： A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译：提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。由通式（I）表示的化合物：其中RX是由下式表示的基团：其中R1是氢原子，任选取代的烷基等; Z是-O - ， - N（R 10） - 等; R10是氢原子，烷基等; R2是氢原子，任选取代的烷基等; R18是氢原子，任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子，任选取代的烷基等; R3和R4独立地是氢原子，任选取代的烷基等; X是-O-，-S-或-N（R 12） - 等; R12是氢原子，烷基等; 和A是任选具有取代基的苯基等，其药学上可接受的盐或其溶剂合物。

6. 发明授权

US08202879B2 Quinazoline derivatives having tyrosine kinase inhibitory activity 有权
标题翻译：具有酪氨酸激酶抑制活性的喹唑啉衍生物
公开(公告)号：US08202879B2
公开(公告)日：2012-06-19
申请号：US11884819
申请日：2006-02-22
申请人： Masaharu Kume , Kenji Matsuo , Naoki Omori , Masami Takayama
发明人： Masaharu Kume , Kenji Matsuo , Naoki Omori , Masami Takayama
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D407/12 , C07D417/12
摘要： A compound which inhibits both of EGF receptor tyrosine kinase and HER2 tyrosine kinase is provided.A compound represented by the general formula (I): wherein RX is a group represented by the formula: wherein R1 is a hydrogen atom, optionally substituted alkyl, etc.; Z is —O—, —N(R10)—, etc.; R10 is a hydrogen atom, alkyl, etc.; R2 is a hydrogen atom, optionally substituted alkyl, etc.; R18 is a hydrogen atom, optionally substituted alkyl, etc.; R19 is optionally substituted alkyl, etc.; W1 is an optionally substituted non-aromatic nitrogen-containing group; R17 is a hydrogen atom, optionally substituted alkyl, etc.; R3 and R4 are independently a hydrogen atom, optionally substituted alkyl, etc.; X is —O—, —S—, or —N(R12)—, etc.; R12 is a hydrogen atom, alkyl, etc.; and A is phenyl optionally having a substituent, etc., its pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译：提供抑制EGF受体酪氨酸激酶和HER2酪氨酸激酶两者的化合物。由通式（I）表示的化合物：其中RX是由下式表示的基团：其中R1是氢原子，任选取代的烷基等; Z是-O - ， - N（R 10） - 等; R10是氢原子，烷基等; R2是氢原子，任选取代的烷基等; R18是氢原子，任意取代的烷基等; R19是任选取代的烷基等; W1是任选取代的非芳族含氮基团; R 17是氢原子，任选取代的烷基等; R3和R4独立地是氢原子，任选取代的烷基等; X是-O-，-S-或-N（R 12） - 等; R12是氢原子，烷基等; 和A是任选具有取代基的苯基等，其药学上可接受的盐或其溶剂合物。

7. 发明申请

US20140051862A1 5-MEMBERED RING HETEROAROMATIC DERIVATIVES HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY 有权
标题翻译：具有NPY Y5受体拮抗活性的5结构环异构体衍生物
公开(公告)号：US20140051862A1
公开(公告)日：2014-02-20
申请号：US14114113
申请日：2012-04-25
申请人： Kyohei Hayashi , Yuusuke Tamura , Naoki Omori
发明人： Kyohei Hayashi , Yuusuke Tamura , Naoki Omori
IPC分类号： C07D271/113 , C07D263/48 , C07D277/42 , C07D285/08 , C07D271/07 , C07D413/04
CPC分类号： C07D271/113 , A61K31/4245 , A61K31/4439 , A61K45/06 , C07D263/48 , C07D271/06 , C07D271/07 , C07D271/08 , C07D271/10 , C07D277/20 , C07D277/42 , C07D285/08 , C07D413/04
摘要： This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
摘要翻译：本发明提供具有NPY Y5拮抗活性的新化合物。本发明人发现式（I）的化合物：其中R 1是取代或未取代的烷基等; p，q和r各自独立地为0或1; 环A是恶二唑; 并且R 2为取代或未取代的烷基等，具有NPY Y5拮抗活性。

8. 发明申请

US20060125149A1 Method for forming duct made of elastomer 审中-公开
标题翻译：形成弹性体导管的方法
公开(公告)号：US20060125149A1
公开(公告)日：2006-06-15
申请号：US11350793
申请日：2006-02-10
申请人： Seiichiro Takada , Naoki Omori
发明人： Seiichiro Takada , Naoki Omori
IPC分类号： B29C45/00 , B29C45/43
CPC分类号： F02M35/10347 , B29C45/435 , B29K2021/00 , B29L2016/00 , F02M35/10137 , F02M35/10321
摘要： [Objects] In a method for forming a duct used as, e.g., an air duct for an automobile engine, and provided with a corrugated section as an undercut part in a part of the longitudinal direction of the duct, an elastomeric duct is formed with ensuring easy removal of a duct molded by injection from a core die even when the duct is made of a resin poor in elasticity. [Means to Solve the Problems] A method for forming an elastomeric duct having a corrugated section in a longitudinal direction thereof as a part of the duct by injection molding, which comprises injecting an elastomer material into a cavity formed with a cavity die for forming an external surface of the duct, and a core die for forming an internal surface of the duct, wherein the core die is a splittable core die which is axially splittable into two parts, one is a core die A for forming a duct area at least containing the corrugated section, and the other is a core die B for forming a duct area free from the corrugated section, and removing the duct area containing the corrugated section from the core die A with expanding at least the corrugated section in the radius direction by air injection after opening the cavity die.
摘要翻译：在用于形成例如用于汽车发动机的空气管道并且在管道的纵向方向的一部分中设置有作为底切部分的波纹部分的管道的方法中，形成弹性体管道，其具有即使当管道由弹性差的树脂制成时，也能够容易地从芯模上去除注射成形的管道。 [解决问题的手段]一种用于通过注射成型形成具有其纵向方向的波纹状部分作为管道的一部分的弹性体管道的方法，其包括将弹性体材料注射到形成有用于形成管芯的外表面和用于形成管道内表面的芯模，其中芯模是可分离的芯模，其可轴向分为两部分，一个是芯模A，用于形成至少包含波纹部分，另一个是用于形成没有波纹部分的管道区域的芯模B，并且从芯模A中除去包含波纹部分的管道区域，至少沿着半径方向扩张波纹部分打开模腔后注射。

9. 发明授权

US08916594B2 5-membered ring heteroaromatic derivatives having NPY Y5 receptor antagonistic activity 有权
标题翻译：具有NPY Y5受体拮抗活性的5元环杂芳族衍生物
公开(公告)号：US08916594B2
公开(公告)日：2014-12-23
申请号：US14114113
申请日：2012-04-25
申请人： Kyohei Hayashi , Yuusuke Tamura , Naoki Omori
发明人： Kyohei Hayashi , Yuusuke Tamura , Naoki Omori
IPC分类号： A61K31/4439 , A61K31/4245 , C07D413/04 , C07D271/07 , C07D277/42 , C07D271/10 , C07D263/48 , C07D277/20 , C07D271/06 , A61K45/06 , C07D285/08 , C07D271/113
CPC分类号： C07D271/113 , A61K31/4245 , A61K31/4439 , A61K45/06 , C07D263/48 , C07D271/06 , C07D271/07 , C07D271/08 , C07D271/10 , C07D277/20 , C07D277/42 , C07D285/08 , C07D413/04
摘要： This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
摘要翻译：本发明提供具有NPY Y5拮抗活性的新化合物。本发明人发现式（I）的化合物：其中R 1是取代或未取代的烷基等; p，q和r各自独立地为0或1; 环A是恶二唑; 并且R 2为取代或未取代的烷基等，具有NPY Y5拮抗活性。

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