Showing papers by "Kunzer Aaron R published in 2017"

Apoptosis-inducing means for treatment of malignant tumour and immune and autoimmune diseases

Abstract: FIELD: pharmacology.SUBSTANCE: invention relates to application of a combination of a formula (III)compound with one or more additional drugs for the manufacture of a drug for use in therapy that inhibits the activity of anti-apoptotic Bcl-2 proteins. The radical values are set forth in claim p.1.EFFECT: increased efficiency of compounds.16 cl, 6 tbl, 19 ex

8-carbamoyl-2-(2,3-di-substituted pyrid-6-yl)-1,2,3,4-tetrahydroisoquinoline derivatives as apoptosis-inducing agents for cancer treatment

Abstract: FIELD: pharmacology.SUBSTANCE: invention relates to organic chemistry, namely a heterocyclic compound of formula(I) or to a therapeutically acceptable salt thereof, where X is benzo[d]thiazolyl, thiazolo[5,4-b]pyridinyl, thiazolo[4,5-c]pyridinyl, imidazo[1,2-a]pyridinyl, thiazolo[5,4-c]pyridinyl, thiazolo[4,5-b]pyridinyl, imidazo[1,2-a]pyrazinyl or imidazo[ 1,2-b]pyridazinyl; Ymeans pyrrolyl, pyrazolyl, triazolyl or pyridinyl; where Y1 is optionally substituted with 1 or 2 substituents independently selected from R, CN and Cl; Lis selected from (CRR), (CRR)-O-(CRR), (CRR)-S-(CRR), (CRR)-S(O)-(CRR)and (CRR)-NR-(CRR); Ymeans mono- or tricyclic C-C-cycloalkyl, spiro[2.5]octyl, spiro[3.5]nonyl, oxatricyclo[3.3.1.1]decyl or azabicyclo[3.2.1]octyl; where Yis optionally substituted with 1, 2 or 3 substituents independently selected from R, OR, SOR, CO(O)R, OH and Br; Zis selected from, Rand Rare absent; Ris deuterium or C-C-alkyl; Ris C-C-alkyl; Ris selected from hydrogen and C-C-alkyl; each Rand Rare hydrogen; Ris selected from the group consisting of C-C-alkyl, morpholinyl and dioxydothiomorpholinyl; where R, meaning C-C-alkyl, is optionally substituted with a substituent selected from R, OR, SORand NHR; Ris selected from C-C-alkyl, morpholinyl, cyclopropyl and C-haloalkyl; RIs selected from C-C-alkyl, phenyl, morpholinyl and tetrahydropyranyl; where R, meaning C-C-alkyl, is optionally substituted with 1 substituent selected from OCH, OCHCHOCHand OCHCHNHCH; q is 1 or 2; s, m and p is 0; r is 0 or 1; N is 0, 1, or 2. The invention also relates to specific compounds, pharmaceutical compositions based on these compounds and a method for treatment of these diseases.EFFECT: new heterocyclic compounds are obtained, that are useful for treatment of some cancers.16 cl, 3 tbl, 86 ex

APOPTOSIS INDUCING AGENTS SELECTIVE FOR Bcl-2 FOR CANCER AND IMMUNE DISEASES TREATMENT

Abstract: FIELD: pharmacy.SUBSTANCE: invention relates to specific heterocyclic compounds containing the sulphonyl amino carbonyl group. The invention also relates to a pharmaceutical composition based on this compound.EFFECT: new heterocyclic compounds with inhibitory activity in terms of anti-apoptotic Bcl-2 proteins are obtained.2 cl, 3 tbl, 481 ex

Apoptosis inducing agent for treatment of cancer, immunological diseases and autoimmune diseases

Abstract: PROBLEM TO BE SOLVED: To provide a compound selectively inhibiting activity of one kind or one lower subset anti-apoptosis Bcl-2 protein for example anti-apoptosis Bcl-xL protein effective for treatments of various cancer including leukemia and autoimmune diseases, and a pharmaceutical composition containing the compoundSOLUTION: There are provided a compound represented by the Formula (I) and a pharmaceutical composition containing the compound In the Formula (I), X is heteroaryl, Yis phenylene, heteroarylene or the like, Lis methylene or the like, Y2 is branched alkyl, cycloalkyl, cycloalkenyl, phenyl or a Cheterocycle, Zis a carboxyl group or the like, Ris halogen, alkyl or the like, p is an integer of 0 to 2, m is an integer of 0 to 3 and n is an integer of 0 to 6SELECTED DRAWING: None