公开(公告)号：US11718641B2

公开(公告)日：2023-08-08

申请号：US17186447

申请日：2021-02-26

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Guoqiang Wang ,  Yat Sun Or ,  Ruichao Shen ,  Jiang Long ,  Peng Dai ,  Xuechao Xing ,  Jing He

IPC: C07J41/00 ,  C07J43/00 ,  C07J9/00 ,  C07J51/00

CPC classification number: C07J41/0066 ,  C07J41/0055 ,  C07J41/0088 ,  C07J43/003 ,  C07J43/006 ,  C07J9/005 ,  C07J41/0094 ,  C07J51/00

Abstract: The present invention provides compounds of Formula I,




pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

公开(公告)号：US08716479B2

公开(公告)日：2014-05-06

申请号：US12810600

申请日：2008-12-24

Applicant: Brian C. Austad ,  Andre Lescarbeau ,  Lin-Chen Yu

Inventor： Brian C. Austad ,  Andre Lescarbeau ,  Lin-Chen Yu

IPC: C07D471/02 ,  C07D311/96

CPC classification number: C07J7/009 ,  C07B2200/09 ,  C07D471/10 ,  C07D491/22 ,  C07J1/0011 ,  C07J5/0053 ,  C07J9/00 ,  C07J21/00 ,  C07J43/006 ,  C07J63/00 ,  C07J65/00 ,  C07J69/00 ,  C07J71/0005

Abstract: The invention is directed to a method to reduce a C—C double bond of an enone of a steroidal compound to produce a mixture of β ketone product and α ketone product, comprising treating a solution or suspension of the steroidal compound in a solvent with hydrogen gas in the presence of a catalyst and a substituted pyridine.

Abstract translation: 本发明涉及一种降低甾族化合物的烯酮的C-C双键以产生“bgr”的混合物的方法。 酮产物和α-酮产物，包括在催化剂和取代的吡啶的存在下，用氢气处理溶剂中的甾族化合物的溶液或悬浮液。

公开(公告)号：US5872114A

公开(公告)日：1999-02-16

申请号：US481668

申请日：1995-06-07

Applicant: Fernand Labrie

Inventor： Fernand Labrie

IPC: A61K8/63 ,  A61K9/00 ,  A61K9/70 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P5/00 ,  A61P15/00 ,  A61P15/02 ,  A61P17/00 ,  A61P25/00 ,  A61Q19/00 ,  C07J1/00 ,  C07J17/00 ,  C07J43/00 ,  A61K31/56

CPC classification number: C07J43/006 ,  A61K31/565 ,  A61K31/566 ,  A61K31/5685 ,  A61K31/57 ,  A61K31/58 ,  C07J1/0011 ,  C07J43/003

Abstract: Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these precursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.

公开(公告)号：US5776923A

公开(公告)日：1998-07-07

申请号：US180361

申请日：1994-01-18

Applicant: Fernand Labrie

Inventor： Fernand Labrie

IPC: A61K8/63 ,  A61K31/565 ,  A61K31/566 ,  A61K31/57 ,  A61K31/58 ,  A61P5/00 ,  A61P15/02 ,  A61P17/00 ,  A61P25/00 ,  A61Q19/00 ,  C07J1/00 ,  C07J43/00

CPC classification number: C07J43/006 ,  A61K31/565 ,  A61K31/566 ,  A61K31/5685 ,  A61K31/57 ,  A61K31/58 ,  A61K8/63 ,  A61Q19/00 ,  C07J1/0011 ,  C07J43/003

Abstract: Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to ether of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hyprogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these precursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.

Abstract translation: 性类固醇前体如脱氢表雄酮和脱氢表雄酮硫酸盐，以及体内转化为上述醚的化合物，用于治疗和/或预防阴道萎缩，hyprogonadism，性欲降低，骨质疏松症，尿失禁，卵巢癌，子宫癌， 皮肤萎缩，避孕，以及与雌激素和/或孕激素组合用于治疗绝经。 可以配制前体用于经皮或经粘膜给药。 提供用于施用这些前体的凝胶，溶液，洗剂，霜剂，软膏和透皮贴剂，以及某些药物组合物和试剂盒，其可用于预防和治疗与性类固醇的分泌降低相关的各种各样的病症 前体由肾上腺。

公开(公告)号：US4719312A

公开(公告)日：1988-01-12

申请号：US902136

申请日：1986-09-02

Applicant: Raymond A. Firestone

Inventor： Raymond A. Firestone

IPC: A61K31/13 ,  A61K31/15 ,  A61K31/155 ,  A61K31/27 ,  A61K31/275 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61K31/575 ,  A61K31/675 ,  A61K38/00 ,  A61K47/48 ,  C07D521/00 ,  C07J43/00 ,  C07K5/06 ,  C07K5/072 ,  C07C87/22

CPC classification number: C07D231/12 ,  A61K31/13 ,  A61K31/15 ,  A61K31/155 ,  A61K31/27 ,  A61K31/275 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61K31/575 ,  A61K31/675 ,  A61K47/48023 ,  A61K47/48061 ,  A61K47/48246 ,  C07D233/56 ,  C07D249/08 ,  C07J43/003 ,  C07J43/006 ,  C07K5/06026 ,  C07K5/06095 ,  A61K38/00

Abstract: The present invention is concerned with the preparation of lysosomotropic detergent agents and pharmaceutical composition useful in the treatment of cancer. These compounds are amine derivatives having a pK of 3.5 of the general structure ##STR1## in which R.sub.1 is C.sub.8-30 alkyl, C.sub.8-30 -alkenyl, substituted C.sub.4-30 alkyl or substituted C.sub.4-30 -alkenyl; R.sub.2 is hydrogen or C.sub.1-4 alkyl and Y is an electron withdrawing group, to control the pK, selected from trifluoroethyl, and difluoroethyl.

Abstract translation: 本发明涉及用于治疗癌症的溶酶体洗涤剂和药物组合物的制备。 这些化合物是具有通式结构“IMAGE”的3.5的pK的胺衍生物，其中R1是C8-30烷基，C8-30-烯基，取代的C4-30烷基或取代的C4-30-烯基; R2是氢或C1-4烷基，Y是吸电子基团，以控制选自三氟乙基和二氟乙基的pK。

公开(公告)号：US3459739A

公开(公告)日：1969-08-05

申请号：US3459739D

申请日：1964-11-27

Applicant: NOVO TERAPEUTISK LABOR AS

Inventor： BORREVANG POUL

IPC: C07J41/00 ,  C07J43/00 ,  C07C173/10 ,  A61K27/00 ,  C07C169/20

CPC classification number: C07J43/006 ,  C07J41/0005 ,  C07J43/00

公开(公告)号：US3445461A

公开(公告)日：1969-05-20

申请号：US3445461D

申请日：1965-08-05

Applicant: NOVO TERAPEUTISK LABOR AS

Inventor： BORREVANG POUL ,  FAARUP PETER

IPC: C07J41/00 ,  C07J43/00 ,  C07C173/10 ,  C07C167/00

CPC classification number: C07J43/006 ,  C07J41/0005 ,  C07J43/00

公开(公告)号：US3338892A

公开(公告)日：1967-08-29

申请号：US41364264

申请日：1964-11-24

Applicant: LILLY CO ELI

Inventor： EUGENE FARKAS

IPC: C07J41/00 ,  C07J43/00

CPC classification number: C07J41/0044 ,  C07J41/0038 ,  C07J41/0072 ,  C07J43/006

公开(公告)号：US3094522A

公开(公告)日：1963-06-18

申请号：US12650961

申请日：1961-07-25

Applicant: MERCK & CO INC

Inventor： PATCHETT ARTHUR A ,  ARTH GLEN E ,  HARVEY SCHWAM

IPC: C07J1/00 ,  C07J41/00 ,  C07J43/00

CPC classification number: C07J41/005 ,  C07J1/0011 ,  C07J41/0005 ,  C07J41/0016 ,  C07J43/006

公开(公告)号：US1686930A

公开(公告)日：1928-10-09

申请号：US1686930D

CPC classification number: C07J43/006 ,  C07J9/005 ,  C07J75/00