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1. 发明申请

US20050107370A1 Pyrrole derivatives as antimycobacterial compounds 失效
标题翻译：吡咯衍生物作为抗分枝杆菌化合物
公开(公告)号：US20050107370A1
公开(公告)日：2005-05-19
申请号：US10497615
申请日：2002-09-20
申请人： Sudershan Arora , Neelima Sinha , Sanjay Jain , Ram Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Sinha
发明人： Sudershan Arora , Neelima Sinha , Sanjay Jain , Ram Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Sinha
IPC分类号： A61P31/06 , C07D207/32 , C07D207/335 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06 , C07D417/02 , A61K31/4025 , A61K31/426 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D413/02 , C07D43/02
CPC分类号： C07D207/335 , C07D207/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06
摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
摘要翻译：式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

2. 发明申请

US20080242676A1 PYRROLE DERIVATIVES AS ANTIMYCOBACTERIAL COMPOUNDS 失效
标题翻译：吡咯衍生物作为抗微生物化合物
公开(公告)号：US20080242676A1
公开(公告)日：2008-10-02
申请号：US12137170
申请日：2008-06-11
申请人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
发明人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
IPC分类号： A61K31/496 , C07D403/02 , C12N1/00 , C12N1/20 , A61P31/04
CPC分类号： C07D207/335 , C07D207/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06
摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
摘要翻译：式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

3. 发明授权

US07763602B2 Pyrrole derivatives as antimycobacterial compounds 失效
标题翻译：吡咯衍生物作为抗分枝杆菌化合物
公开(公告)号：US07763602B2
公开(公告)日：2010-07-27
申请号：US12137170
申请日：2008-06-11
申请人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
发明人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
IPC分类号： A01N43/00 , A01N43/36 , A01N43/50 , A01N43/62 , A01N43/76 , A61K31/00 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/445 , A61K31/497 , A61K31/535 , A61K31/54 , A61K31/55
CPC分类号： C07D207/335 , C07D207/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06
摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).
摘要翻译：式（I）的新型吡咯衍生物及其药学上可接受的酸加成盐对临床敏感性以及抗结核分枝杆菌菌株具有优异的抗分枝杆菌活性，并且与已知化合物相比具有较小的毒性。使用式（I）的新化合物用于治疗潜在结核病，包括多药耐药性结核病（MDR TB）。制备新化合物的方法，含有新化合物的药物组合物和通过施用式（I）化合物治疗MDR TB的方法。

4. 发明授权

US07691837B2 Pyrrole derivatives as antimycobacterial compounds 失效
公开(公告)号：US07691837B2
公开(公告)日：2010-04-06
申请号：US10497615
申请日：2002-09-20
申请人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
发明人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Gourhari Jana , Shankar Ajay , Rakesh Kumar Sinha
IPC分类号： A01N43/00 , A01N43/40 , A61K31/33 , A61K31/55 , A61K31/497 , A61K31/435 , C07D223/00 , C07D243/00 , C07D241/04 , C07D295/00 , C07D213/00
CPC分类号： C07D207/335 , C07D207/32 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/06
摘要： Novel pyrrole derivatives of formula (I) and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

5. 发明申请

US20090118509A1 PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES 审中-公开
公开(公告)号：US20090118509A1
公开(公告)日：2009-05-07
申请号：US11911272
申请日：2006-04-05
申请人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Om Dutt Tyagi , Vasanth Nalam , Yogendra Kumar Chauhan
发明人： Sudershan Kumar Arora , Neelima Sinha , Sanjay Jain , Ram Shankar Upadhayaya , Om Dutt Tyagi , Vasanth Nalam , Yogendra Kumar Chauhan
IPC分类号： C07D401/14
CPC分类号： C07D207/50 , C07D207/335 , C07D401/04 , C07D401/12
摘要： A process for the preparation of compounds of Formula I and their pharmaceutically acceptable acid addition salt wherein, R1 is phenyl or substituted phenyl R2 is selected from a group consisting of phenyl which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F, or pyridine, or naphthalene, or NHCOR4 wherein R4 is aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl. R3 is selected from a group of formula wherein R5 is phenyl which is unsubstituted or substituted with 1 or 2 substituents each independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, nitro, amino, haloalkyl, haloalkoxy etc.; unsubstituted or substituted benzyl; unsubstituted or substituted heteroaryl; unsubstituted or substituted heteroaroyl; unsubstituted or substituted diphenylmethyl, n=0-2 and X═—NCH3, CH2, S, SO, or SO2 Such that when R2 is phenyl, which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F; R5 is not C1-C4 alkyl, or X is not —NCH3, CH2, S, SO, or SO2, when n=1, or X is not —CH2 when n=0; comprising the steps of (a) reacting compound of Formula II with a chlorinating agent in the presence or absence of catalytic amount of N,N-dimethylformamide to yield the compound of Formula III, (b) reacting the compound of Formula III with a compound of Formula R1H (R1 is as defined above), in presence of a Lewis acid to obtain the compound of Formula IV, (c) reacting the compound of Formula IV with a compound of Formula R2NH2 (R2 is as defined above) in presence of catalytic amounts of an aryl or alkyl sulphonic acid in an organic solvent to obtain the compound of Formula V, (d) reacting the compound of Formula V with various secondary amines of the Formula R3H (R3 is as defined above) in the presence of formaldehyde and acetic acid in acetonitrile followed by crystallization yield the compound of Formula I, (e) purifying the compound of Formula I by crystallization, (f) converting the purified compound of Formula I to a pharmaceutically acceptable acid addition salt.

6. 发明授权

US06420366B1 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻断剂的1-（4-芳基哌嗪-1-基）-ω-[N-（α-甲基 - 二羧酰亚氨基）] - 烷烃
公开(公告)号：US06420366B1
公开(公告)日：2002-07-16
申请号：US09577788
申请日：2000-05-24
申请人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Jang Bahadur Gupta
发明人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Jang Bahadur Gupta
IPC分类号： A61K31495
CPC分类号： C07D207/404 , A61K31/496 , C07D207/408 , C07D211/88 , C07D401/06
摘要： Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
摘要翻译：已经发现，通过芳族系统在一个氮上取代的新颖的哌嗪衍生物，另一个氮被（2,5-二氧代吡咯烷-1-基）烷烃或（2,6-二氧代哌啶-1-基）烷烃取代，表现出选择性的α1A 肾上腺素能活动该化合物可用于治疗疾病状况，例如外周血管疾病，充血性心力衰竭，高血压，特别是良性前列腺肥大。

7. 发明授权

US06812344B1 1-(4-Arylpiperazin-1-yl)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximidoL)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻断剂的1-（4-芳基哌嗪-1-基）-ω-[N-（α，ω-二羧酰基L）] - 烷烃
公开(公告)号：US06812344B1
公开(公告)日：2004-11-02
申请号：US09578239
申请日：2000-05-24
申请人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
发明人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
IPC分类号： C07D40106
CPC分类号： C07D207/404 , A61K31/496 , C07D207/408 , C07D211/88 , C07D401/06
摘要： The present invention relates to certain novel piperazine derivatives having protracted uro-selective &agr;1-adrenoceptor antagonistic activity exceeding those of previously described compounds. The compounds of the present invention hold promise for treating benign prostratic hyperplasia (BPH). This invention also relates to methods for making the novel compounds, pharmaceutical compositions containing the compounds, and methods of treating benign prostatic hyperplasia using the compounds.
摘要翻译：本发明涉及某些具有延长的尿选择性α1-肾上腺素能受体拮抗活性的新型哌嗪衍生物，超过前述化合物。本发明化合物具有治疗良性前列腺增生（BPH）的希望。本发明还涉及制备新化合物的方法，含有该化合物的药物组合物，以及使用该化合物治疗良性前列腺增生的方法。

8. 发明授权

US06410735B1 1-(4-arylpiperazin-1-y1)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻断剂的1-（4-芳基哌嗪-1-基） - 大豆 - [N-（α，ω-二羧酰亚氨基）] -
公开(公告)号：US06410735B1
公开(公告)日：2002-06-25
申请号：US09578088
申请日：2000-05-24
申请人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
发明人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
IPC分类号： C07D40114
CPC分类号： C07D207/404 , A61K31/496 , C07D207/408 , C07D211/88 , C07D401/06
摘要： Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
摘要翻译：已经发现，通过芳族系统在一个氮上取代的新颖的哌嗪衍生物，另一个氮被（2,5-二氧代吡咯烷-1-基）烷烃或（2,6-二氧代哌啶-1-基）烷烃取代，表现出选择性的α1A 肾上腺素能活动该化合物可用于治疗疾病状况，例如外周血管疾病，充血性心力衰竭，高血压，特别是良性前列腺肥大。

9. 发明授权

US06914064B2 1,4-Disubstituted piperazine derivatives useful as uro-selective α1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻断剂的1,4-二取代哌嗪衍生物
公开(公告)号：US06914064B2
公开(公告)日：2005-07-05
申请号：US09998115
申请日：2001-11-30
申请人： Nitya Anand , Sanjay Jain , Neelima Sinha , Anita Chugh , Laxminarayan G. Hegde , Jang Bahadur Gupta
发明人： Nitya Anand , Sanjay Jain , Neelima Sinha , Anita Chugh , Laxminarayan G. Hegde , Jang Bahadur Gupta
IPC分类号： A61K31/497 , A61P13/08 , A61P43/00 , C07D209/48 , A61K31/496 , C07D403/06
CPC分类号： C07D209/48
摘要： The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I, and their pharmaceutically acceptable acid addition salts having excellent uro-selective α1-adrenoceptor antagonistic activity exceeding those of previously described compounds. The compounds of the present invention hold promise for treating the symptoms of benign prostatic hyperplasia (BPH). The invention also relates to methods for making the novel compounds, pharmaceutical compositions containing the compounds, and method of treating the symptoms of benign prostatic hyperplasia using the compounds.
摘要翻译：本发明涉及式I的新型1,4-二取代哌嗪衍生物及其药学上可接受的酸加成盐，其具有超过前述化合物的优异的尿选择性α1 - 肾上腺素受体拮抗活性。本发明的化合物有望治疗良性前列腺增生（BPH）的症状。本发明还涉及制备新化合物的方法，含有该化合物的药物组合物，以及使用该化合物治疗良性前列腺增生症状的方法。

10. 发明授权

US06420559B1 1-(4-arylpiperazin-1-yl)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻滞剂的1-（4-芳基哌嗪-1-基）-ω-[N-（α，ω-二羧酰亚氨基）] - 烷烃
公开(公告)号：US06420559B1
公开(公告)日：2002-07-16
申请号：US09577789
申请日：2000-05-24
申请人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
发明人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
IPC分类号： C07D40106
CPC分类号： C07D207/404 , A61K31/496 , C07D207/408 , C07D211/88 , C07D401/06
摘要： Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
摘要翻译：已经发现，通过芳族系统在一个氮上取代的新颖的哌嗪衍生物，另一个氮被（2,5-二氧代吡咯烷-1-基）烷烃或（2,6-二氧代哌啶-1-基）烷烃取代，表现出选择性的α1A 肾上腺素能活动该化合物可用于治疗疾病状况，例如外周血管疾病，充血性心力衰竭，高血压，特别是良性前列腺肥大。

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