Ranbaxy Laboratories, Inc.

Council of Scientific and Industrial Research

Nitya Anand

Neelima Sinha

Sanjay Kumar Jain

Anita Mehta

Anil Kumar Saxena

Jang Bahadur Gupta

Arvind Kumar Srivastava

Ram Pratap

Anil Kumar Rastogi

Ramesh Chander

Ram Chandra Gupta

Deepak Raina

Omkar Prasad Asthana

Ashok Kumar Khanna

Narinder Kumar Kapoor

Madhur Ray

Satyavan Singh

Savita Srivastava

Swarn Nityanand

Ashim Ghatak

Sukh Dev

Mangal Prasad Dubey

Ram Mohan Saxena

Gyanendra Kumar Patnaik, Deceased

Anita Chugh

Suprabhat Ray

Bhola Nath Dhawan

Rikhab Chand Srimal

Mohammad Salman

Ved P Kamboj

Jang Bahadurgupta

Padam Chand Jain

Jitendra Nath Sharma

Laxminarayan G Hegde

Varanasi Aruna Murthi

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 &#x3b1;-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.

1,4-Disubstituted piperazine derivatives useful as uro-selective &#x3b1;1-adrenoceptor blockers

The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I) as shown herein belowWherein X&#x2550;OH or O or combination thereof and positioning of olefinic bonds are at 4(5); 5(6); 16(17); 17(20) or various combinations and said compounds containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals, said method comprising administering an effective amount of the said compounds to the recipient mammals.

Method of treating hyperlipidemic and hyperglycemic conditions in mammals using pregnadienols and pregnadienones

The present invention relates to certain novel piperazine derivatives having protracted uro-selective &agr; -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.

1-(4-Arylpiperazin-1-yl)-&ohgr;-&lsqb;N-(&agr;,&ohgr;-dicarboximidoL)&rsqb;-alkanes useful as uro-selective &agr;1-adrenoceptor blockers

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; 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.

1-(4-arylpiperazin-1-yl)-&ohgr;-&lsqb;N-(&agr;&ohgr;-dicarboximido)&rsqb;-alkanes useful as uro-selective &agr;1-adrenoceptor blockers

1-(4-arylpiperazin-1-yl)-&ohgr;-&lsqb;N-(&agr;,&ohgr;-dicarboximido)&rsqb;-alkanes useful as uro-selective &agr;1-adrenoceptor blockers

1-(4-arylpiperazin-1-y1)-&ohgr;-&lsqb;N-(&agr;,&ohgr;-dicarboximido)&rsqb;-alkanes useful as uro-selective &agr;1-adrenoceptor blockers

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.

1-[4-arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes and

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.

1-(4-arylpiperazin-1-yl)-.omega.-[n-(.alpha...

1-(4-arylpiperazin-1-yl)-.omega.-[n-(.alpha.,.omega.-dicarboximido)]-alka

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.

Methods for preparing

The laevo and dextro forms of dl-3,4-trans-2,2-disubstituted-3,4-diarylchromans and similar derivatives thereof have substantially double the post-coital anti-fertility activity of the known racemic compound. The resolution of such known compound into the l- and d-isomeric forms may be carried out using di-p-toluoyl-l-tartaric acid monohydrate or di-p-toluoyl-d-tartaric acid.

Preparation of l- and d-isomers of

Pharmacologically active 1-substituted 4-(.beta.-2-quinolylethyl)piperazines of the formula ##SPC1## And their 1,2,3,4-tetrahydroquinolylethyl analogues, wherein R represents a lower alkyl, a phenyl, benzyl or a phenethyl group; and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof.

1-Substituted 4-(.beta.-2-quinolylethyl)piperazines and

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Nitya Anand