Aurigene Discovery Technologies Limited

Merck Patent Gmbh

Merck Serono S. a.

Um Pharmauji Sdn. Bhd.

Siva Sanjeeva Rao Thunuguntla

Subramanya Hosahalli

Satish Reddy Kunnam

Matthias Schwarz

Sunil Kumar Panigrahi

Hosahalli Subramanya

Michael Arlt

Chakrapani Bingi

Raviraj Kusanur

Michael Arit

Sekhar Reddy Sanivaru Vijay

The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which Rto Rand 'm' have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient. 

1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitors

The present invention provides methods for treating a cancer in a subject and for inhibiting tumor growth, metastasis or a dihydrorotate oxygenase enzyme activity of a tumor or cancer cell. At least one trisubstituted benzotriazole derivative with the formula (I) is administered to the subject or is contacted with the cancer cell. Compounds of formula (I) have substituents R, Rand Rwhich have the meanings given in the specification, and pharmaceutically acceptable salts thereof.

Trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors

The present invention provides trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors. wherein, R, Rand Rhave the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing trisubstituted benzotriazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

The invention relates to compounds of formula (I) wherein R, R, X, X, Y, R, R, Q have the meanings given in claim. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders. 

Dihydroorotate dehydrogenase inhibitors

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Hyderabad Telangana, India

Siva Sanjeeva Rao Thunuguntla