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APOPTOSIS INDUCING AGENTS FOR TREATING CANCER, IMMUNE AND AUTOIMMUNE DISEASES
专利权人:
EHBBVI INK.
发明人:
DIN Khun (US),ДИН Хун (US),EhLMOR Stiven (US),ЭЛМОР Стивен (US),KhEKSAMER Laura (US),ХЕКСАМЕР Лаура (US),KANZER Aaron R. (US),КАНЗЕР Аарон Р. (US),PARK Cheol-Min (SG),ПАРК Чеол-Мин (SG),SAUEhRS Ehndrj,DIN KHUN,ДИН Хун,EHLMOR STIVEN,ЭЛМОР Стивен,KHEKSAMER LAURA,ХЕКСАМЕР Лаура,KANZER AARON R.,КАНЗЕР Аарон Р.,PARK CHEOL-MIN,ПАРК Чеол-Мин,SAUEHRS EHNDRJU DZH.,САУЭРС Эндрю Дж.,SALLIVAN DZHERARD,САЛЛИВАН
申请号:
RU2012145298/04
公开号:
RU0002568611C2
申请日:
2011.03.10
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new compounds specified in a group shown below. The compounds contain at least 5 rings including a fragment with a bridge structure with a carbon side of the central group C(O)-NH-SO2, piperidinyl, or piperazinyl, or phenyl; phenyl attached to each carbon and sulphur atom of the group C(O)-NH-SO2, wherein phenyl from the sulphur atom side is substituted by a nitro group and NH-CH2(tetrahydro-2H-pyran-4-yl or cyclohexyl) group. The compounds possess the properties of Bcl-2 antiapoptotic protein activity inhibitor and can be used in treating the diseases expressing Bcl-2 protein. These diseases are malignant diseases specified in bladder cancer, cerebral cancer, breast cancer, bone marrow cancer, cervical cancer, chronic lymphocytic leukaemia etc. The compounds of the present invention are specified in a group consisting of 4-(4-{acetyl[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; 4-(4-{benzoyl[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)-N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)benzamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-3′-{[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}biphenyl-4-carboxamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-4-(4-{(phenylacetyl)[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-yl)benzamide; N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulphonyl)-4-(4-{2-[(1R,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-en-2-yl]benzylidene}piperidin-1-yl)benzamide; 4-[4-(2-{5-[8-azabicyclo[3.2.1]oct-8-ylmethyl]-2-thienyl}benzyl)piperazin-1-yl]-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulphonyl)benzamide; N-({4-[(cyclohexylmethyl)amino]-3-nitrophenyl}sulphonyl)-4-(4-{(3-phenylpropanoyl)[(1S,2S,3S,5R)-2,6,6-trimethylbicyclo[3.1.1]hept-3-yl]amino}piperidin-1-
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