Piramal Life Sciences Limited

Aventis Pharma Deutschland, Gmbh

Piramal Enterprises Limited

Hikal Limited

Ashok Kumar Gangopadhyay

Ravindra Dattatraya Gupte

Asha Adrian Kulkarni-Almeida

Bansi Lal

Swati Bal-Tembe

Somesh Sharma

Sapna Parikh

Vijay Singh Chauhan

Ashish Suthar

Radha Bhaskar Panicker

Nilesh Dagia

Aditi Amol Tannu

Eleanor Pinto De Souza

Dhananjay Sapre

Sridevi Krishnan

Gopal Vishnu Gole

Shruta Sudheer Dadarkar

Mahesh Gundaji Jadhav

Vadlamudi V S V Rao

Rajiv Sharma

Hitesh Mistry

Ravindra Dnyandev Jadhav

Nabajyoti Deka

Rosalind Adaikalasamy Marita

Kishorkumar Shivajirao Kadam

Peter David Nightingale

Swapnil Surendra Mohile

Vitthal G Gund

Swapnil Gulabrao Yerande

Sarika Madhukarrao Lunge

Rameshkumar Maghabhai Patel

Shivaji Balbhim Gugale

Rajesh Mataprasad Thakur

Ramesh Ananda Mokal

Sapna Hasit Parikh

Jessy Anthony

Aditee Ghate

Kumar Venkata Subrahmanya Nemmani

Aditya Kelkar

Sujit Kaur Bhumra

The present invention provides an improved process for the preparation of a compound of formula (I), which comprises the steps of: formula (I), (a) reacting isovaleraldehyde of formula (II) and alkyl cyanoacetate of formula (III) optionally in presence of salts of weak acid and weak base or weak base in a suitable solvent to get 2-cyano-5-methyl-hex-2-enoic acid alkyl ester of formula (IV); (b) reacting 2-cyano-5-methyl-hex-2-enoic acid alkyl ester of formula (IV) with a suitable cyanide source in water or in an organic solvent or mixture thereof to get 2-isobutylsuccinonitrile of formula (V); (c) obtaining optionally 2-isobutylsuccinonitrile of formula (V) by reacting isovaleraldehyde of formula (II) and alkyl cyanoacetate of formula (III) in presence of suitable cyanide source in water or in an organic solvent or mixture thereof in single step; (d) converting 2-isobutylsuccinonitrile of formula (V) to racemic 3-cyano-5-methyl-hexanoic acid or salt thereof of formula (VI) with a genetically modified nitrilase enzyme (Nit 9N_56_2) in water or optionally with an organic co-solvent at appropriate pH and temperature; (e) converting racemic 3-cyano-5-methyl-hexanoic acid or salt thereof of formula (VI) to racemic alkyl 3-cyano-5-methyl-hexanoate of formula (VII) by treatment with alcohol (R3OH) and acidic catalyst or alkyl halide (R3X) in presence of a base in a suitable solvent or a mixture of solvents thereof; (f) obtaining (S)-alkyl 3-cyano-5-methyl-hexanoate of formula (VIII) and (R)-3-cyano-5-methyl-hexanoic acid or salt thereof of formula (X) by enzymatic enantioselective hydrolysis in water or organic solvent or a mixture thereof from racemic alkyl 3-cyano-5-methyl-hexanoate of formula (VII); (g) obtaining optionally the compound of formula (VII) by racemizing unwanted (R)-3-cyano-5-methyl-hexanoic acid or salt thereof of formula (X) or substantially enriched (R)-3-cyano-5-methyl-hexanoic acid salt thereof of formula (X) in presence of a base in organic solvent or a mixture thereof; (h) converting (S)-alkyl 3-cyano-5-methyl-hexanoate of formula (VIII) to pregabalin of formula (I) by hydrolyzing ester group with suitable alkali or alkaline earth metal base followed by hydrogenation optionally in one pot in a solvent selected from water or other organic solvents or a mixture thereof in presence of a suitable hydrogenation catalyst. 

Process for the preparation of pregabalin

The present invention relates to isoxazole, thiazole and oxidiazole derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, in particular to the use of these compounds in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1.

Diacylglycerol acyltransferase inhibitors

This invention relates to a novel herbal composition comprising an extract of flowering and fruiting heads of the plant,. The said extract ofcontains a compound, 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (7-Hydroxy-4,11(13)-eudesmadien-12,6-olide) (compound 1), as a bioactive marker. The invention also relates to a composition comprising 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (compound 1) as an active ingredient. The invention also relates to methods of manufacture of the said compositions. The invention also relates to methods of administration of the said compositions to a subject in need of treatment for an inflammatory disorder. The invention also relates to tumor necrosis factor-(TNF-&#x3b1;) and interleukin (IL-1, IL-6, IL-8) inhibitory activity of the said compositions. The invention relates to inhibition of the expression of intercellular adhesion molecule 1 (ICAM-1), vascular-cell adhesion molecule 1 (VCAM-1), and E-Selectin by the said compositions. The said compositions may optionally contain at least one anti-inflammatory agent or can be used in combination with at least one anti-inflammatory agent.

Herbal composition for inflammatory disorders

This invention relates to novel fused bicyclic compounds of the general formula (I): wherein

Fibrinogen receptor antagonists and their use

This invention relates to novel fused bicyclic compounds of the general formula (I): whereinthe symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.

A cyclohexapeptide compound of general formula (I), wherein Ris C&#x2013;Calkyl; C&#x2013;Calkenyl; C&#x2013;Calkoxyphenyl; an aryl group selected from: phenyl, biphenyl, terphenyl and naphthyl; C&#x2013;Calkylphenyl, C&#x2013;Calkenylphenyl, C&#x2013;Calkoxyphenyl; linoleoyl; palmitoyl; 12-methylmyristoyl; 10,12-dimethylmyristoyl; or &#x2014;COCH(p)OCH, Rand Rare independently &#x2014;OH; &#x2014;CN; &#x2014;CHNH; &#x2014;N; aryl; substituted aryl; heterocyclyl and substituted heterocyclic with 1&#x2013;3 of the same or different heteroatoms; aminoalkylamino; mono or di-substituted linear or cyclic aminoalkylamino; &#x2014;OR, wherein, R is C&#x2013;Calkyl; substituted alkyl of the type &#x2014;(CH)&#x2014;X, where n is 1&#x2013;5 and X is Cl, Br, I, COOY, CN, NHor a heterocyclic and where Y is C&#x2013;Clinear or branched alkyl; C&#x2013;C-alkenyl; aryl; fused aryl; substituted aryl; a heterocyclic containing 1&#x2013;3 heteroatoms; mono or di-substituted aminoalkyl; or a hydroxy protecting group; and Rmay additionally be imidazolyl; Rand Rare independently &#x2014;H or &#x2014;OH; Ris &#x2014;H or &#x2014;CH, Ris &#x2014;H, &#x2014;CHor &#x2014;CHCONH. Ris &#x2014;H, &#x2014;CHor &#x2014;OH. Rand Rare independently &#x2014;H or &#x2014;CH-Sec.amine in which the sec.amine is attached to &#x2014;CHthrough its N linkage; and its pharmaceutically acceptable salts. The compounds are useful as antifungal agents.

Cyclohexapeptide compounds, processes for their production and their use as a pharmaceutical

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Mumbai, India

Ashok Kumar Gangopadhyay