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CARBOXYLIC ACIDS COMPOUNDS
专利权人:
LTD.;SUMITOMO DAJNIPPON FARMA KO.
发明人:
KHORI Sejdzi (JP),ХОРИ Сейдзи (JP),KHASEGAVA Futosi (JP),ХАСЕГАВА Футоси (JP),URABE Dajsuke (JP),УРАБЕ Дайсукэ (JP),KUREBAYASI Khirotaka (JP),КУРЕБАЯСИ Хиротака (JP)
申请号:
RU2014151221
公开号:
RU0002636146C2
申请日:
2013.05.17
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: compounds may find use in the treatment of a disease mediated by TLR7. This disease can be a cancer selected from bladder cancer, head and neck cancers, prostate cancer, breast cancer, lung cancer, uterine cancer, pancreatic cancer, liver cancer, kidney cancer, ovarian cancer, colon cancer, stomach cancer, skin cancer, brain tumour, myeloma and lymphoproliferative tumours, such a disease or condition can also be represented by asthma, COPD (chronic obstructive pulmonary disease), allergic rhinitis, allergic conjunctivitis, allergic dermatitis, hepatitis B, hepatitis C, HIV, HPV (human papillomavirus), bacterial infection, or dermatosis. In the formula,n is equal to 0, 1 or 2; m is 1 or 2; p is 1, 2 or 3, provided that when X is oxygen, p is 2 or 3, and when X is a single bond, p is 1; X is oxygen or a single bond; R1 is chosen from C1-4 alkyl group, C1-3alkyl-(CH2)group, in which C1-3 alkyl functional group is substituted by 1, 2 or 3 fluorine atoms, and C1-4 an alkylcarbonyl group; R2 is hydrogen; or R1 and R2 together with the nitrogen and carbon atoms to which they are attached form a saturated or unsaturated 5-membered heterocyclic ring optionally containing an additional heteroatom selected from N; R3 is selected from hydrogen, hydroxymethyl and 2-hydroxyethyl. The invention also relates to a method for preparation of a compound of formula (I) and to an intermediate of formulawherein n, p, X, R1, R2 have the above values, Y is a hydroxy or substituted group selected from mesitylenesulfonyloxy, or tri(isopropyl)phenylsulfonyloxy; and PG1 is a carboxylic acid protecting group selected from C1-4 alkyl; or a salt thereof.EFFECT: compound application efficiency increase.37 cl, 13 dwg, 7 tbl, 30 exИзобретение относится к новым соединениям формулы (I) и их фармацевтически приемлемым солям, обладающим свойствами агониста TLR7. Соединения могут найти применение при лечении заболевания опосредуемого TLR7. Указанным заболеванием может быть р
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