Ranbaxy Laboratories, Inc.

Daiichi Sankyo Company, Limited

Sunanda Ghosh Dastidar

Venkata Poornapragnacharyulu Palle

Abhijit Ray

Punit Kumar Srivastava

Manoj Kumar Khera

Viswajanani Jitendra Sattigeri

Sarala Balachandran

Manoj Kumar Tiwari

Ajay Soni

Abdul Rehman Abdul Rauf

Ranadheer Reddy

Arpita Musib

Sony Joseph

Rie Miyauchi

Masatoshi Nagamochi

Shin Iimura

Ashwani Kumar Verma

Masayuki Ishizaki

Kumaragurubaran Nagaswamy

Nidhi Gupta

Lalima Sharma

Rijwan Jaffer Momin

Pradip Balu Wagh

Soma Ghosh

Sonali Nanasaheb Pansare

Balkrishna Ramchandra Kale

Pramod Raosaheb Markad

Yogesh Balasaheb Khairnar

Takeshi Murata

Aniruddha Mondal

Lalit Kumar Baregama

Mohammad Salman

Sonali Rudra

Vinayak Vasantrao Khairnar

Gagan Kukreja

Ritu Agarwal

Mandadapu Raghu Ramaiah

Atul Kondaskar

Manohar Salla

Lalitha Vijaykrishnan

Saswati Chakladar

Sarika Ramnani

Nagarajan Muthukamal

Punit Kumar Sricastava

Sreedhara Rao Voleti

Viswajanani J Sattigeri

The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R, Rand Rare as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.

Heterocyclic compounds as protein kinase inhibitors

The present invention relates to &#x3b2;-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure &#x3b2;-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.

Matrix metalloproteinase inhibitors

The present invention relates to Compounds having the structure of Formula I: wherein n is an integer from 1 to 5; Ris optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or alkynyloxy; Ris alkenyl, allcynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, NRR, &#x2014;NHC(&#x2550;Y)R, &#x2014;NHC(&#x2550;Y)NRR, &#x2014;NHC(&#x2550;O)OR, &#x2014;NHSOR, C(&#x2550;Y)NRR, C(&#x2550;O)OR[wherein Y is oxygen or sulphur], OR, &#x2014;O(C&#x2550;O)NRR, O-acyl, S(O)R, &#x2014;SON(R), cyano, amidino or guanidino [wherein Ris alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl and m is an integer 0-2; Ris hydrogen or R; Ris Ror &#x2014;SON(R)and Ris hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl]; Ris hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR, &#x2014;OC(&#x2550;O)NRR, O-acyl, NH, NRR, &#x2014;NHC(&#x2550;Y)R, &#x2014;NHC(&#x2550;Y)NRR, &#x2014;NHC(&#x2550;O)OR, &#x2014;NHSOR, and to processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by over-expression and over-activation of an matrix metalloproteinase, using the compounds. 

5-phenyl-pentanoic acid derivatives as matrix metalloproteinase inhibitors for the treatment of asthma and other diseases

The present invention relates to &#x3b2;-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure &#x3b2;-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, periodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.

The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4/PDE type 7 inhibitors are provided. 

Pyrazolo (3, 4-B) pyridine derivatives as phosphodiesterase inhibitors

The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

Inhibitors of phosphodiesterase type-IV

The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors. 

Substituted indazoles as inhibitors of phosphodiesterase type-IV

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New Delhi, India

Sunanda Ghosh Dastidar