| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS | PCT/US2004020753 | 2004-06-25 | WO2005004807A3 | 2005-04-07 | DANKULICH WILLIAM P; MEISSNER ROBERT S; MITCHELL HELEN J |
| Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents. | ||||||
| 142 | METHOD OF PRODUCING 17beta-(SUBSTITUTED)-3-OXO-DELTA1,2-4-AZASTEROIDS AND INTERMEDIATES | PCT/ES0200453 | 2002-09-26 | WO03029267A3 | 2003-06-19 | GORGOJO LOBATO JOSE MARIA; LORENTE BONDE-LARSEN ANTONIO; MARTIN JUAREZ JORGE |
| The invention relates to the production of 17beta-(substituted)-3-oxo-DELTA1,2-4-azasteroids (I), wherein R1 is a C1-C4 alkyl, OR2, wherein R2 is a C1-C4 alkyl, or NR3R4, wherein R3 and R4, which may be identical or different, denote hydrogen or a C1-C4 alkyl radical. According to the invention, the latter are obtained using a method consisting in: breaking the oxazolidinethione ring present in a 2-(substituted)-3-hydroxyoxazolidinethione having formula (IV), wherein R5 is Br or trichloromethylsulphonyl; and eliminating the substituent in position 2 in order to form a double bond in position 1,2. Some (I) compounds are inhibitors of testosterone-5alpha-reductase and can be used in the treatment of hyperandrogenic alterations. | ||||||
| 143 | NATURAL BRASSINOSTEROIDS FOR USE FOR TREATING HYPERPROLIFERATION, TREATING PROLIFERATIVE DISEASES AND REDUCING ADVERSE EFFECTS OF STEROID DYSFUNCTION IN MAMMALS, PHARMACEUTICAL COMPOSITION AND ITS USE | PCT/CZ2008000097 | 2008-08-20 | WO2009024103A3 | 2009-07-16 | OKLESTKOVA JANA; HOFFMANNOVA LUCIE; STEIGEROVA JANA; KOHOUT LADISLAV; KOLAR ZDENEK; STRNAD MIROSLAV |
| The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O-CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids. This invention also describes new use for treating consisting in a new therapeutic way for modifying cell viability of human breast and prostate cancer cells. | ||||||
| 144 | PROCESS FOR OBTAINING 17 beta -(N-TERC-BUTYLCARBAMOYL)-3-ONE-4-AZA-STEROIDS | PCT/ES0000239 | 2000-07-05 | WO0102422A9 | 2001-04-05 | SILVA GUISASOLA LUIS OCTAVIO; BLANCO FERNANDEZ CRISTINA; LORENTE BONDE-LARSEN ANTONIO; MARTIN JUAREZ JORGE |
| 17 beta -(N-terc-butylcarbamoyl)-3-one-4-aza-steroids (I) can be obtained by a process which comprises the reaction of 17 beta -(alcoxycarbonyl)-3-one-4-aza-steroid with terc-butylamide of lithium in an organic solvent. Some compounds of formula (I), for example finasteride, are useful as inhibitors of 5- alpha -reductase and can be used in the treatment of benign prostatic hyperplasia and alopecia. | ||||||
QQ群二维码
意见反馈
意见反馈