Piramal Life Sciences Limited

Usha Ghosh

Bansi Lal

Swati Bal-Tembe

Tulsidas More

Sapna Parikh

Somesh Sharma

Asha Adrian Kulkarni-Almeida

Ravindra Dattatraya Gupte

Muralidhara Padigaru

Radha Bhaskar Panicker

Arun Kumar Jain

Anagha Damre

Pravin Gagare

Sunil Jadhav

Shashikant Patil

Anil Ghate

Jacqueline Trivedi

Anandharajan Rathina Sabapathy

Sapna Hasit Parikh

Arvind Thakkar

Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRR, O, NRor S(O); V is CRRor NR; W is S(O); wherein Ris H, alkyl, cycloalkyl, alkenyl or aralkyl; Ris H, alkyl, OH, ORor OCOR, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.

Tricyclic guanidine derivatives as sodium-proton exchange inhibitors

Compounds of formula 1: are disclosed, wherein V is CH; W is S(O); m is the integer 0, 1 or 2; U is O, C(O), CRRor NR; where Ris H, alkyl; Ris H, OH, ORor OCOR; Ris H, alkyl, cycloalkyl, alkenyl, C(O)R, C(O)ORor alkylaminocarbonyl; R, R, R, R, R, R, Rand Rare as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-&#x3b1;) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-&#x3b1; activity, in particular inflammations.

Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha

Fused tricyclic compounds as inhibitors of tumor necrosis factor-&#x3b1;

Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRR, O, NRor S(O); V is CRRor NR; W is S(O); wherein Ris H, alkyl, cycloalkyl, alkenyl or aralkyl; Ris H, alkyl, OH, ORor OCOR, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.

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Mumbai, India

Usha Ghosh