Publication number: 20140336173
Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(?O)—NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR2R10, —C(?O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
Type:
Application
Filed:
December 10, 2012
Publication date:
November 13, 2014
Inventors:
Dirk Brohm, Melanie Heroult, Marie-Pierre Collin, Walter Hübsch, Mario Lobell, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer
Publication number: 20100137361
Abstract: This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
Type:
Application
Filed:
February 4, 2010
Publication date:
June 3, 2010
Applicant:
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Inventors:
Axel BOUCHON, Nicole Diedrichs, Achim Hermann, Klemens Lustig, Heinrich Meier, Josef Pernerstorfer, Elke Reissmüller, Muneto Mogi, Hiroshi Fujishima, Masaomi Tajimi, Noriyuki Yamamoto