公开(公告)号：US06914064B2

公开(公告)日：2005-07-05

申请号：US09998115

申请日：2001-11-30

Applicant: Nitya Anand ,  Sanjay Jain ,  Neelima Sinha ,  Anita Chugh ,  Laxminarayan G. Hegde ,  Jang Bahadur Gupta

Inventor： Nitya Anand ,  Sanjay Jain ,  Neelima Sinha ,  Anita Chugh ,  Laxminarayan G. Hegde ,  Jang Bahadur Gupta

IPC: A61K31/497 ,  A61P13/08 ,  A61P43/00 ,  C07D209/48 ,  A61K31/496 ,  C07D403/06

CPC classification number: C07D209/48

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06579862B1

公开(公告)日：2003-06-17

申请号：US09280448

申请日：1999-03-30

Applicant: Ram Pratap ,  Ram Chandra Gupta ,  Ramesh Chander ,  Ashok Kumar Khanna ,  Arvind Kumar Srivastava ,  Deepak Raina ,  Satyavan Singh ,  Savita Srivastava ,  Anil Kumar Rastogi ,  Omkar Prasad Asthana ,  Swarn Nityanand ,  Nitya Anand ,  Ashim Ghatak ,  Narinder Kumar Kapoor ,  Sukh Dev

Inventor： Ram Pratap ,  Ram Chandra Gupta ,  Ramesh Chander ,  Ashok Kumar Khanna ,  Arvind Kumar Srivastava ,  Deepak Raina ,  Satyavan Singh ,  Savita Srivastava ,  Anil Kumar Rastogi ,  Omkar Prasad Asthana ,  Swarn Nityanand ,  Nitya Anand ,  Ashim Ghatak ,  Narinder Kumar Kapoor ,  Sukh Dev

IPC: A61K3158

CPC classification number: A61K31/573 ,  C07J13/005 ,  C07J13/007

Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I): containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals wherein X═OH or O and the olefinic bonds are at 4(5); 5(6); 16(17); or 17(20) or various combinations, and wherein the compounds contain at lest one olefinic bond in or on their D-ring. The method comprises administering an effective amount of said compounds to recipient mammals.

Abstract translation: 本发明提供了一种使用由结构式（I）表示的孕ad酮和孕二烯醇的方法：在D环中或其D环上含有至少一个烯键，用于治疗哺乳动物中的高脂血症和高血糖病症，其中X = OH或O， 烯键为4（5）; 5（6）; 16（17）; 或17（20）或各种组合，并且其中所述化合物在其D环中或其上含有至少一个烯键。 该方法包括向受体哺乳动物施用有效量的所述化合物。

公开(公告)号：US06420559B1

公开(公告)日：2002-07-16

申请号：US09577789

申请日：2000-05-24

Applicant: Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Anil Kumar Saxena

Inventor： Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Anil Kumar Saxena

IPC: C07D40106

CPC classification number: C07D207/404 ,  A61K31/496 ,  C07D207/408 ,  C07D211/88 ,  C07D401/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US6150367A

公开(公告)日：2000-11-21

申请号：US954516

申请日：1997-10-20

Applicant: Neelima Sinha ,  Sanjay Jain ,  Anil Kumar Saxena ,  Nitya Anand ,  Ram Mohan Saxena ,  Mangal Prasad Dubey ,  Madhur Ray ,  Gyanendra K. Patnaik, deceased

Inventor： Neelima Sinha ,  Sanjay Jain ,  Anil Kumar Saxena ,  Nitya Anand ,  Ram Mohan Saxena ,  Mangal Prasad Dubey ,  Madhur Ray ,  Gyanendra K. Patnaik, deceased

IPC: C07D207/26 ,  C07D207/27 ,  C07D211/76 ,  A61K31/496 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

CPC classification number: C07D207/27 ,  C07D211/76

Abstract: A chemical compound and composition of Formula 1: ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; said compounds and compositions as being useful therapeutic agents for hypertension, ischemic, cardiovascular and other adrenergic receptor related disorders.

Abstract translation: 式1的化合物和组合物：其中Ar表示被诸如卤素，烷氧基，烷基或杂芳基的基团取代的苯环，n = 1或n = 2; 所述化合物和组合物作为高血压，缺血性，心血管和其它肾上腺素能受体相关疾病的有用治疗剂。

公开(公告)号：US6090809A

公开(公告)日：2000-07-18

申请号：US203855

申请日：1998-12-02

Applicant: Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Anil Kumar Saxena

Inventor： Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Anil Kumar Saxena

IPC: A61K31/496 ,  C07D207/40 ,  C07D207/404 ,  C07D207/408 ,  C07D211/88 ,  C07D401/06 ,  C07D403/06

CPC classification number: C07D207/404 ,  A61K31/496 ,  C07D207/408 ,  C07D211/88 ,  C07D401/06

Abstract: 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 .alpha..sub.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.

Abstract translation: 已经发现通过芳族体系在一个氮上取代的新颖的哌嗪衍生物，在另一个氮上被（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α 1A肾上腺素能活动。 该化合物可用于治疗疾病状况，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。

公开(公告)号：US6084097A

公开(公告)日：2000-07-04

申请号：US960335

申请日：1997-10-29

Applicant: Neelima Sinha ,  Sanjay Jain ,  Anil Kumar Saxena ,  Nitya Anand ,  Ram Mohan Saxena ,  Mangal Prasad Dubey ,  Madhur Ray ,  Gyanendra Kumar Patnaik, deceased

Inventor： Neelima Sinha ,  Sanjay Jain ,  Anil Kumar Saxena ,  Nitya Anand ,  Ram Mohan Saxena ,  Mangal Prasad Dubey ,  Madhur Ray ,  Gyanendra Kumar Patnaik, deceased

IPC: C07D207/26 ,  C07D207/27 ,  C07D211/76 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

CPC classification number: C07D211/76 ,  C07D207/27

Abstract: The invention relates to a process for the synthesis of 1-[4-Arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes used as potential therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders, having general formula 1 ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; a process of preparing said compounds and a method of treating hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders.

Abstract translation: 本发明涉及用作高血压，缺血，心血管和其他肾上腺素能潜在治疗剂的1- [4-芳基哌嗪-1-基] -3- [2-氧代吡咯烷/哌啶-1-基]丙烷的合成方法 受体相关疾病，具有通式1，其中Ar表示被诸如卤素，烷氧基，烷基或杂芳基的基团取代的苯环，n = 1或n = 2; 制备所述化合物的方法和治疗高血压，缺血，心血管和其它肾上腺素能受体相关疾病的方法。

公开(公告)号：US6083950A

公开(公告)日：2000-07-04

申请号：US120265

申请日：1998-07-21

Applicant: Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Jang Bahadurgupta

Inventor： Nitya Anand ,  Neelima Sinha ,  Sanjay Jain ,  Anita Mehta ,  Jang Bahadurgupta

IPC: A61K31/496 ,  C07D207/40 ,  C07D207/404 ,  C07D207/408 ,  C07D211/88 ,  C07D401/06 ,  A61K31/495

CPC classification number: C07D207/404 ,  A61K31/496 ,  C07D207/408 ,  C07D211/88 ,  C07D401/06

Abstract: 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 .alpha..sub.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.

Abstract translation: 已经发现通过芳族体系在一个氮上取代的新颖的哌嗪衍生物，在另一个氮上被（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α 1A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。

公开(公告)号：US3532710A

公开(公告)日：1970-10-06

申请号：US3532710D

申请日：1967-11-09

Applicant: HARMANDER PAL SINGH CHAWLA ,  PYARA KRISHEN GROVER ,  NITYA ANAND ,  VED PRAKASH KAMBOJ ,  AMIYA BHUSON KAR

Inventor： CHAWLA HARMANDER PAL SINGH ,  GROVER PYARA KRISHEN ,  ANAND NITYA ,  KAMBOJ VED PRAKASH ,  KAR AMIYA BHUSON

IPC: C07D307/93 ,  C07D311/92 ,  C07D27/04 ,  C07D5/32

CPC classification number: C07D311/92 ,  C07D307/93