8-CARBAMOYL-2-(2,3-DISUBSTITUTED PYRID-6-YL)-1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES AS APOPTOSIS-INDUCING AGENTS FOR TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

• Main Authors: GEORGE DOHERTY, TAO ZHI-FU, SONG XIAOHONG, ANDREW SOUERS, AARON R KUNZER, LE WANG, XILU WANG, ANDREW JUDD, TODD M HANSEN, SULLIVAN GERARD M, ROBIN FREY, WENDT MICHAEL D, MILAN BRUNCKO
• Format: Patent
• Language: English; Japanese
• Published: 02.11.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide: compounds which selectively inhibit activity of one type or one subset of anti-apoptotic Bcl-2 proteins, e.g., anti-apoptotic Bcl-xL proteins, and are effective for treatment of various types of cancer including leukemia; and pharmaceutical compositions containing the compounds.SOLUTION: The invention provides compounds represented by formula (I), and pharmaceutical compositions containing the compounds. [X is 1,3-benzothiazole; Yis phenylene; Lis methylene, O, CO, OCH, NH, NHCOCONH, S, NHSO, SO, or 2-oxo-1,2-dihydropyridyl group; Yis tricyclo[3.3.1.1]dec-1-yl group; Zis carboxyl group; Ris cyano group or methyl group; p is 0 or 1; m is 0; and n is 0.]SELECTED DRAWING: None 【課題】１種類又は１下位集合の抗アポトーシスＢｃｌ−２蛋白質、例えば抗アポトーシスＢｃｌ−ｘＬタンパク質の活性を選択的に阻害し、白血病を含む各種ガンの治療に対して有効な化合物、及び該化合物を含む医薬組成物の提供。【解決手段】式（Ｉ）で示される化合物、及び該化合物を含有する医薬組成物。［Ｘは１、３−ベンゾチアゾール：Ｙ１はフェニレン、；Ｌ１はメチレン，Ｏ、ＣＯ、ＯＣＨ２，ＮＨ，ＮＨＣＯＣＯＮＨ，Ｓ，ＮＨＳＯ２，ＳＯ２，２−オキソ−１、２−ジヒドロピリジル基；Ｙ２はトリシクロ［３．３．１．１３，７］デク−１−イル基；Ｚ１はカルボキシル基：Ｒ３はシアノ基又はメチル基；ｐは０又は１；ｍは０；ｎは０］【選択図】なし