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N-(PHENYLSULFONYL)BENZAMIDES AND RELATED COMPOUNDS AS BCL-2 INHIBITORS
专利权人:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人:
WANG, Shaomeng (US),ВАН, Шаомэн (US),CHEN, Jianyong (US),ЧЭНЬ, Цзяньюн (US)
申请号:
RU2019105721
公开号:
RU0002722560C1
申请日:
2017.08.04
申请国别(地区):
RU
年份:
2020
代理人:
摘要:
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to compounds of formula IA, having properties of BCL-2 inhibitors, pharmaceutical compositions based thereon, use, a method of treating and a kit for treating diseases, disorders or conditions susceptible to BCL-2 protein inhibition, including hyperproliferative protein, such as cancer. In general formula IA: A is selected from a group consisting of:E is a carbon atom and is a double bond; or E is -C(H)- and is a single bond; or E is a nitrogen atom and is a single bond; X1, X2, and X3 are each independently selected from a group consisting of -CR8 =; R1a and R1b, taken together with the carbon atom to which they are bonded, form 4-member cycloalkyl; or R1a and R1b, taken together with the carbon atom to which they are bonded, form 4-member heterocycle with 1 oxygen atom; R2 is selected from a group consisting of -NO2; R2a is selected from a group consisting of hydrogen and halogen; R3 is selected from a group consisting of hydrogen and -N(R4a)(R4b); R4a is selected from a group consisting of C1-6 alkyl and 6-member (heterocycloalkyl) C1-6 alkyl with 1 to 2 oxygen atoms; R4b is selected from a group consisting of hydrogen and C1-4 alkyl; R5 is selected from a group consisting of 6-member (heterocycloalkyl) C1-6 alkyl with 1 oxygen atom; R6a , R6c, R6e, R6f, and R6g are each independently selected from a group consisting of hydrogen, C1-6 alkyl, 6-member heterocycloalkyl with 1 oxygen atom, C1-6 heteroalkyl with 1–2 oxygen atoms, and 6-member (heterocycloalkyl) C1-6 alkyl with 1 oxygen atom; R6b and R6d are each independently selected from a group consisting of hydrogen; and R8 is selected from a group consisting of hydrogen and halogen.I-A.EFFECT: treating diseases, disorders or conditions susceptible to BCL-2 protein inhibition, including hyperproliferative protein, such as cancer.49 cl, 7 tbl, 20 ex, 4 dwgИзобретение относится к соединениям Формулы I-A, обладающим свойствами ингибиторов BCL-2, фармац
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