Publication number: 20160194321
Abstract: The present invention relates to compounds of formula wherein R1 halogen, lower alkyl, lower alkoxy, cyano, phenyl, C(O)NHCH3, C(O)NH2, lower alkyl substituted by halogen or is a five-membered heteroaryl group, optionally substituted by lower alkyl; Y1 is N or CH; Y2 is CH; and if Y1 is CH, Y1 and Y2 may form together with the C-atoms to which they are attached a ring, containing —CH?N—N(CH3)—, —CH?N—N(H)—; X is CH or N; R is (CH2)m-cycloalkyl, optionally substituted by hydroxy, lower alkoxy or lower alkyl, or is tetrahydropyran, optionally substituted by hydroxy, or is lower alkoxy, substituted by hydroxy, or is lower alkyl substituted by one or two hydroxy, or is (CH2)m-pyridinyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, or is L-phenyl, optionally substituted by hydroxy, lower alkyl or lower alkyl substituted by hydroxy, and L is a bond, —CH(CH2OH)— or —CH2CH(OH)—; n is 0, 1 or 2; m is 0 or 1; or to a pharmaceutically acceptable acid addition salt, to
Type:
Application
Filed:
March 11, 2016
Publication date:
July 7, 2016
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Theresa Maria BALLARD, Emmanuel PINARD, Herve SCHAFFHAUSER, Katrin GROEBKE ZBINDEN, Thomas RYCKMANS, Alexander FLOHR
Patent number: 6849624
Abstract: The invention is the compounds 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1?6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1?6-thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide. Compounds of the invention are useful in pharmaceutical compositions for the treatment of migraine, rheumatoid arthritis, asthma, bronchial hyperreactivity, inflammatory bowel disease or for the treatment of disorders including Parkinson's disease, anxiety, depression, pain, headache, Alzheimer's disease, multiple sclerosis, edema, allergic rhinitis, Crohn's disease, ocular injury, ocular inflammatory diseases, psychosis, motion sickness, induced vomiting, emesis, urinary incontinence, psychoimmunologic or psychosomatic disorders, cancer, withdrawal symptoms of addictive drugs from opiates or nicotine, traumatic brain injury or benign prostatic hyperplasia.
Type:
Grant
Filed:
July 17, 2002
Date of Patent:
February 1, 2005
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Theresa Maria Ballard, Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight