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1. 发明授权

US6100252A Heterocyclic compounds and their use as angiotensin antagonists 失效
标题翻译：杂环化合物及其作为血管紧张素拮抗剂的用途
公开(公告)号：US6100252A
公开(公告)日：2000-08-08
申请号：US207044
申请日：1998-12-08
申请人： Takehiko Naka , Yoshiyuki Inada
发明人： Takehiko Naka , Yoshiyuki Inada
IPC分类号： A61K31/415 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/4365 , A61K31/495 , A61K31/505 , A61K31/513 , A61K31/517 , A61K31/535 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/28 , A61P43/00 , B29D22/00 , B32B27/42 , C07D285/08 , C07D403/10 , C07D413/10 , C07D417/10 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00
CPC分类号： C07D403/10 , A61K31/42 , A61K31/435 , C07D411/10 , C07D411/12 , C07D413/10 , C07D417/10 , C07D417/12 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , Y02P20/55
摘要： ##STR1## Compounds shown by the above formula or salt thereof show a strong angiotensin II antagonistic activity and hypotensive action and CNS activity, and are useful as therapeutic agents of circulatory diseases such as hypertensive diseases and heart diseases (e.g. hypercardia, heart failure, cardiac infarction), strokes, cerebral apoplexy, nephritis, atherosclerosis, Alzheimer's disease, senile dementia, etc.
摘要翻译：上述式表示的化合物或其盐显示出强的血管紧张素II拮抗作用和降血压作用和CNS活性，并且可用作循环系统疾病如高血压疾病和心脏病（例如高血压，心力衰竭，心肌梗塞）的治疗剂，脑卒中，脑中风，肾炎，动脉粥样硬化，阿尔茨海默病，老年痴呆等。

2. 发明授权

US5354766A Compound and salts thereof which antagonize angiotensin II 失效
标题翻译：拮抗血管紧张素II的化合物及其盐
公开(公告)号：US5354766A
公开(公告)日：1994-10-11
申请号：US080259
申请日：1993-06-23
申请人： Takehiko Naka , Yoshiyuki Inada
发明人： Takehiko Naka , Yoshiyuki Inada
IPC分类号： A61K31/415 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/4365 , A61K31/495 , A61K31/505 , A61K31/513 , A61K31/517 , A61K31/535 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/28 , A61P43/00 , B29D22/00 , B32B27/42 , C07D285/08 , C07D403/10 , C07D413/10 , C07D417/10 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00 , C07D271/07
CPC分类号： C07D403/10 , A61K31/42 , A61K31/435 , C07D411/10 , C07D411/12 , C07D413/10 , C07D417/10 , C07D417/12 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , Y02P20/55
摘要： ##STR1## Compounds shown by the above formula or salt thereof show a strong angiotensin II antagonistic activity and hypotensive action and CNS activity, and are useful as therapeutic agents of circulatory diseases such as hypertensive diseases and heart diseases (e.g. hypercardia, heart failure, cardiac infarction), strokes, cerebral apoplexy, nephritis, atherosclerosis, Alzheimer's disease, senile dementia, etc.
摘要翻译：上述式表示的化合物或其盐显示出强的血管紧张素II拮抗作用和降血压作用和CNS活性，并且可用作循环系统疾病如高血压性疾病和心脏病（例如高血压，心力衰竭，心脏病梗塞），中风，脑中风，肾炎，动脉粥样硬化，阿尔茨海默病，老年痴呆等。

3. 发明授权

US06420405B2 Pharmaceutical composition for angiotensin II-mediated diseases 失效
标题翻译：用于血管紧张素II介导的疾病的药物组合物
公开(公告)号：US06420405B2
公开(公告)日：2002-07-16
申请号：US09783579
申请日：2001-02-15
申请人： Yoshiyuki Inada , Keiji Kubo
发明人： Yoshiyuki Inada , Keiji Kubo
IPC分类号： A61K3141
CPC分类号： A61K45/06 , A61K31/495 , A61K31/54 , A61K31/415 , A61K2300/00
摘要： This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula wherein R1 is H or an optionally substituted hydrocarbon residue; R2 is an optionally esterified carboxyl group; R3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R2; and Y is a bond, —O—, —S(O)m- (wherein m is 0, 1 or 2) or —N(R4)— (wherein R4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.
摘要翻译：本发明涉及一种用于血管紧张素II介导的疾病的药物组合物，其包含具有血管紧张素II拮抗活性的化合物，其中R 1为H或任选取代的烃残基; R2是任选酯化的羧基; R3是能够形成阴离子或可转换的基团的基团; X是相邻的亚苯基和苯基之间的线性部分的2个苯环或链长为1〜2个原子的间隔基之间的共价键; n为1或2; 环A是除了R2之外具有1或2个任选取代基的苯环; 并且Y是键，-O - ， - S（O）m - （其中m是0,1或2）或-N（R 4） - （其中R 4是H或任选取代的烷基）其可接受的盐与具有利尿活性的化合物或具有钙拮抗作用的化合物组合。

4. 发明授权

US06228874B1 Pharmaceutical composition for angiotensin II-mediated diseases 失效
标题翻译：用于血管紧张素II介导的疾病的药物组合物
公开(公告)号：US06228874B1
公开(公告)日：2001-05-08
申请号：US09563855
申请日：2000-05-04
申请人： Yoshiyuki Inada , Keiji Kubo
发明人： Yoshiyuki Inada , Keiji Kubo
IPC分类号： A61K3141
CPC分类号： A61K45/06 , A61K31/495 , A61K31/54 , A61K31/415 , A61K2300/00
摘要： This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula wherein R1 is H or an optionally substituted hydrocarbon residue; R2 is an optionally esterified carboxyl group; R3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R2; and Y is a bond, —O—, —S(O)m— (wherein m is 0, 1 or 2) or —N(R4)— (wherein R4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.
摘要翻译：本发明涉及一种用于血管紧张素II介导的疾病的药物组合物，其包含具有血管紧张素II拮抗活性的化合物，其中R 1为H或任选取代的烃残基; R2是任选酯化的羧基; R3是能够形成阴离子或可转换的基团的基团; X是相邻的亚苯基和苯基之间的线性部分的2个苯环或链长为1〜2个原子的间隔基之间的共价键; n为1或2; 环A是除了R2之外具有1或2个任选取代基的苯环; 并且Y是键，-O - ， - S（O）m - （其中m是0,1或2）或-N（R 4） - （其中R 4是H或任选取代的烷基）其可接受的盐与具有利尿活性的化合物或具有钙拮抗作用的化合物组合。

5. 发明授权

US5958961A Pharmaceutical composition for angiotensin II-mediated diseases 失效
标题翻译：用于血管紧张素II介导的疾病的药物组合物
公开(公告)号：US5958961A
公开(公告)日：1999-09-28
申请号：US883040
申请日：1997-06-26
申请人： Yoshiyuki Inada , Keiji Kubo
发明人： Yoshiyuki Inada , Keiji Kubo
IPC分类号： A61K31/495 , A61K31/54 , A61K45/06 , A61K31/415 , A61K31/41
CPC分类号： A61K45/06 , A61K31/495 , A61K31/54
摘要： This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon residue; R.sup.2 is an optionally esterified carboxyl group; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R.sup.2 ; and Y is a bond, --O--, --S(O)m- (wherein m is 0, 1 or 2) or --N(R.sup.4)-- (wherein R.sup.4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.
摘要翻译：本发明涉及一种用于血管紧张素II介导的疾病的药物组合物，其包含具有下式的血管紧张素II拮抗活性的化合物：其中R 1为H或任选取代的烃残基; R2是任选酯化的羧基; R3是能够形成阴离子或可转换的基团的基团; X是相邻的亚苯基和苯基之间的线性部分的2个苯环或链长为1〜2个原子的间隔基之间的共价键; n为1或2; 环A是除了R2之外具有1或2个任选取代基的苯环; 并且Y是键，-O - ， - S（O）m - （其中m是0,1或2）或-N（R 4） - （其中R 4是H或任选取代的烷基）其可接受的盐与具有利尿活性的化合物或具有钙拮抗作用的化合物组合。

6. 发明授权

US5721263A Pharmaceutical composition for angiotensin II-mediated diseases 失效
标题翻译：用于血管紧张素II介导的疾病的药物组合物
公开(公告)号：US5721263A
公开(公告)日：1998-02-24
申请号：US351011
申请日：1994-12-07
申请人： Yoshiyuki Inada , Keiji Kubo
发明人： Yoshiyuki Inada , Keiji Kubo
IPC分类号： A61K31/495 , A61K31/54 , A61K45/06 , A61K31/41 , A61K31/50
CPC分类号： A61K45/06 , A61K31/495 , A61K31/54
摘要： This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon residue; R.sup.2 is an optionally esterified carboxyl group; R.sup.3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R.sup.2 ; and Y is a bond, --O--, --S(O)m-- (wherein m is 0, 1 or 2) or --N(R.sup.4)-- (wherein R.sup.4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.
摘要翻译：本发明涉及一种用于血管紧张素II介导的疾病的药物组合物，其包含具有式IMAMA的血管紧张素II拮抗活性的化合物，其中R 1为H或任选取代的烃残基; R2是任选酯化的羧基; R3是能够形成阴离子或可转换的基团的基团; X是相邻的亚苯基和苯基之间的线性部分的2个苯环或链长为1〜2个原子的间隔基之间的共价键; n为1或2; 环A是除了R2之外具有1或2个任选取代基的苯环; 并且Y是键，-O - ， - S（O）m - （其中m是0,1或2）或-N（R 4） - （其中R 4是H或任选取代的烷基）其可接受的盐与具有利尿活性的化合物或具有钙拮抗作用的化合物组合。

7. 发明授权

US5583141A Heterocyclic compounds and their use as angiotensin antagonists 失效
公开(公告)号：US5583141A
公开(公告)日：1996-12-10
申请号：US291435
申请日：1994-08-16
申请人： Takehiko Naka , Yoshiyuki Inada
发明人： Takehiko Naka , Yoshiyuki Inada
IPC分类号： A61K31/415 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/4365 , A61K31/495 , A61K31/505 , A61K31/513 , A61K31/517 , A61K31/535 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/28 , A61P43/00 , B29D22/00 , B32B27/42 , C07D285/08 , C07D403/10 , C07D413/10 , C07D417/10 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D519/00
CPC分类号： C07D403/10 , A61K31/42 , A61K31/435 , C07D411/10 , C07D411/12 , C07D413/10 , C07D417/10 , C07D417/12 , C07D419/10 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , Y02P20/55
摘要： ##STR1## Compounds shown by the above formula or salt thereof show a strong angiotensin II antagonistic activity and hypotensive action and CNS activity, and are useful as therapeutic agents of circulatory diseases such as hypertensive diseases and heart diseases (e.g. hypercardia, heart failure, cardiac infarction), strokes, cerebral apoplexy, nephritis, atherosclerosis, Alzheimer's disease, senile dementia, etc.

8. 发明授权

US5500427A Cyclic compounds and their use 失效
标题翻译：环状化合物及其用途
公开(公告)号：US5500427A
公开(公告)日：1996-03-19
申请号：US120450
申请日：1993-09-14
申请人： Keiji Kubo , Yoshiyuki Inada , Takehiko Naka
发明人： Keiji Kubo , Yoshiyuki Inada , Takehiko Naka
IPC分类号： C07D413/12 , C07D417/12 , A61K31/41
CPC分类号： C07D417/12 , C07D413/12
摘要： The present invention relates to a compounds represented by the following formula or salts thereof. ##STR1## The above compounds have strong angiotensin II antagonistic action, antihypertensive action and action on central nervous system, which are useful for the treatment of circulatory diseases such as hypertension, heart diseases, cerebral apoplexy, nephritis, atherosclerosis or Alzheimer's disease and senile dementia, and for agents of improving cerebral function.
摘要翻译：本发明涉及由下式表示的化合物或其盐。可用于治疗诸如高血压，心脏病，脑中风，肾炎，动脉粥样硬化或阿尔茨海默氏病和老年痴呆的循环系统疾病的中枢神经系统的拮抗作用，抗高血压作用和作用，以及用于改善脑功能。

9. 发明授权

US07294344B2 Sustained-release preparation for AII antagonist, production and use thereof 失效
标题翻译： AII拮抗剂的缓释制剂，其制备和使用
公开(公告)号：US07294344B2
公开(公告)日：2007-11-13
申请号：US10443308
申请日：2003-05-22
申请人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
发明人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
IPC分类号： A61F2/00 , A61K9/14 , A61K9/50
CPC分类号： A61K31/00 , A61K9/1611 , A61K9/1647 , A61K31/4178 , A61K31/4184 , Y10S514/965
摘要： The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.
摘要翻译：本发明提供一种缓释制剂，其包含具有血管紧张素II拮抗作用的化合物，其前药或其盐，以及可生物降解的聚合物，如果需要，提供多价金属，并且其具有高度稳定和活性的显示血管紧张素II拮抗活性，同时保持血压的昼夜节律长时间。

10. 发明授权

US06589547B1 Sustained-release preparation for AII antagonist, production and use thereof 失效
标题翻译： AII拮抗剂的缓释制剂，其制备和使用
公开(公告)号：US06589547B1
公开(公告)日：2003-07-08
申请号：US09601986
申请日：2000-08-09
申请人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
发明人： Yasutaka Igari , Akira Saikawa , Yoshiyuki Inada , Shigeru Kamei
IPC分类号： A61K916
CPC分类号： A61K31/00 , A61K9/1611 , A61K9/1647 , A61K31/4178 , A61K31/4184 , Y10S514/965
摘要： The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.
摘要翻译：本发明提供一种缓释制剂，其包含具有血管紧张素II拮抗作用的化合物，其前药或其盐，以及可生物降解的聚合物，如果需要，提供多价金属，并且其具有高度稳定和活性的显示血管紧张素II拮抗活性，同时保持血压的昼夜节律长时间。

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