公开(公告)号：US5138063A

公开(公告)日：1992-08-11

申请号：US701332

申请日：1991-05-09

申请人： Gary H. Rasmusson ,  Glenn F. Reynolds

发明人： Gary H. Rasmusson ,  Glenn F. Reynolds

IPC分类号： C07C62/38 ,  C07J73/00

CPC分类号： C07J73/005 ,  C07C62/38 ,  C07C2103/16 ,  Y10S514/859

摘要： 17.beta.-Acyl-4-aza-5.alpha.-androst-1-in-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl R.sup.2 is methoxy, a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulations of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, and benign prostatic hypertrophy.

摘要翻译： 17β-丙基-4-氮杂-5α-雄甾-1-酮-3-酮其中R选自氢，甲基和乙基，R2是甲氧基，一价基团选自直链和 1-12个碳原子的支链烷基或任选含有1个或多个1-2个碳原子和/或1个或更多个卤代（Cl或Br）取代基的低级烷基取代基的单环芳基，选自苄基和苯乙基和杂环的芳烷基 选自2-或4-吡啶基，2-吡咯基，2-呋喃基或噻吩基; 和R'，R“和R”'各自选自氢和甲基，并且上述化合物的药物制剂作为睾酮5α-还原酶抑制剂是有活性的，因此可用于治疗痤疮，皮脂溢，女性多毛症和 良性前列腺肥大。

公开(公告)号：US5116983A

公开(公告)日：1992-05-26

申请号：US520991

申请日：1990-05-08

申请人： Apurba Bhattacharya ,  Alan W. Douglas ,  Edward J. Grabowski ,  Ulf H. Dolling

发明人： Apurba Bhattacharya ,  Alan W. Douglas ,  Edward J. Grabowski ,  Ulf H. Dolling

IPC分类号： C07J51/00 ,  C07J73/00

CPC分类号： C07J73/003 ,  C07J51/00 ,  C07J73/005

摘要： A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a .DELTA..sup.1 double bond.

摘要翻译： （III）的化合物的脱氢方法，其包括使化合物与甲硅烷基化剂在醌存在下反应以引入DELTA 1双键。

公开(公告)号：US5061803A

公开(公告)日：1991-10-29

申请号：US587299

申请日：1990-09-24

申请人： John M. Williams

发明人： John M. Williams

IPC分类号： A61K31/56 ,  A61P13/02 ,  A61P15/00 ,  C07J73/00 ,  C07J75/00

CPC分类号： C07J73/005 ,  Y10S514/859

摘要： Disclosed is a new process for making 17-beta branched alkanoyl-3-oxo-4-aza-5-.alpha.-androst-1-enes, agents for treating benign prostatic hypertrophy (BPH), by reacting methyl 3-oxo-4-aza-5-.alpha.-androst-1-ene-17-beta carboxylate with isobutylmagnesium bromide in the novel presence of the hexamethyldisilazane (HMDS). Use of the HMDS results in higher yield and less by-products as opposed to the standard Grignard reaction in the absence of HMDS.

公开(公告)号：US5032586A

公开(公告)日：1991-07-16

申请号：US398192

申请日：1989-08-24

申请人： Brian W. Metcalf ,  Dennis A. Holt ,  Mark A. Levy

发明人： Brian W. Metcalf ,  Dennis A. Holt ,  Mark A. Levy

IPC分类号： A61K31/56 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P43/00 ,  C07J3/00 ,  C07J7/00 ,  C07J9/00 ,  C07J13/00 ,  C07J31/00 ,  C07J41/00 ,  C07J73/00

CPC分类号： C07J7/004 ,  C07J13/005 ,  C07J13/007 ,  C07J3/005 ,  C07J31/006 ,  C07J41/0005 ,  C07J41/0066 ,  C07J73/005 ,  C07J9/00 ,  C07J9/005

摘要： Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.

公开(公告)号：US4914106A

公开(公告)日：1990-04-03

申请号：US228316

申请日：1988-08-04

申请人： Kenyu Shibata ,  Nobuaki Yamakoshi ,  Naoyuki Koizumi ,  Shigehiro Takegawa ,  Eiichiro Shimazawa ,  Mamoru Mieda

发明人： Kenyu Shibata ,  Nobuaki Yamakoshi ,  Naoyuki Koizumi ,  Shigehiro Takegawa ,  Eiichiro Shimazawa ,  Mamoru Mieda

IPC分类号： C07J73/00

CPC分类号： C07J73/005 ,  C07J73/003 ,  C07C2103/16

摘要： A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing abortion or for contraception.

公开(公告)号：US4888336A

公开(公告)日：1989-12-19

申请号：US7539

申请日：1987-07-28

申请人： Dennis A. Holt ,  Mark A. Levy ,  Brian W. Metcalf

发明人： Dennis A. Holt ,  Mark A. Levy ,  Brian W. Metcalf

IPC分类号： A61K31/58 ,  C07J3/00 ,  C07J31/00 ,  C07J73/00

CPC分类号： C07J31/003 ,  C07J3/005 ,  C07J73/005 ,  C07C2103/16 ,  Y10S514/859

摘要： Invented are 4-aza-5-alpha-8(14)-17 substituted-androsten-3-ones having an 8(14), 7(8), or 16(17) double bond, optionally also having a 1(2) double bond, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase.

公开(公告)号：US4053476A

公开(公告)日：1977-10-11

申请号：US712449

申请日：1976-08-09

申请人： Robert J. Chorvat ,  Raphael Pappo

发明人： Robert J. Chorvat ,  Raphael Pappo

IPC分类号： C07D217/24 ,  C07D217/26 ,  C07J73/00

CPC分类号： C07J73/005 ,  C07D217/24 ,  C07D217/26

摘要： The preparation of 7-aza-6-alkoxy-1-tetralones which originates with dihydroresorcinol is disclosed herein. The subject compounds are useful intermediates in the synthesis of various compounds which possess valuable pharmacological properties.

公开(公告)号：US3887567A

公开(公告)日：1975-06-03

申请号：US38738973

申请日：1973-08-10

申请人： SEARLE & CO

发明人： CHORVAT ROBERT J ,  PAPPO RAPHAEL

IPC分类号： C07J71/00 ,  C07J73/00 ,  C07D101/00

CPC分类号： C07J71/001 ,  C07J73/003 ,  C07J73/005 ,  Y10S514/908

摘要： Derivatives of the 3-keto-2-oxaandrostane family are appropriately reacted to yield 3-alkoxy-2-azaestratrienes and intermediates thereto, which compounds display valuable pharmacological e.g. anti-viral, anti-leukemic and lipidmobilizing, properties.

摘要翻译： 3-酮-2-氧杂雄甾烷系的衍生物适当地反应，得到3-烷氧基-2-氮杂三烯及其中间体，该化合物显示有价值的药理学例如。 抗病毒，抗白血病和脂质动员等。

公开(公告)号：US3790574A

公开(公告)日：1974-02-05

申请号：US3790574D

申请日：1971-06-14

申请人： RICHTER GEDEON VEGYESZET

发明人： TUBA Z ,  BOR M

IPC分类号： C07J73/00 ,  C07D51/70

CPC分类号： C07J73/005

摘要： THIS INVENTION RELATES TO 21-SUBSTITUED 17-AZA-STEROIDS AND SALTS THEREOF HAVING THE FORMULA 1

1-(X-CH2-CO-),5A-F,6-E,7-C,7-D,8-B,9-A,9A-G-PERHYDRO-1H-

NAPHTH(1,2-E)INDOLE

WHEREIN A AND B EACH REPRESENT HYDROGEN, C IS HYDROXY GROUP, ESTER OR ETHER, D, E AND F EACH REPRESENT HYDROGEN ATOM, G IS A METHYL GROUP IF THE COMPOUNDS ARE OF ANDROSTANE TYPE,OR A AND B, D AND E AND F AND G EACH REPRESENT TERMINI OF DOUBLE BOND, OR C AND D REPRESENT TOGETHER AN OXO-GROUP, ESPECIALLY A KETAL GROUP, AND X REPRESENTS CHLORINE, BROMINE, HYDROXY OR ACYLOXY A SUBSTITUTED, SECONDARY OR TERTIARY AMINO.

公开(公告)号：US3733329A

公开(公告)日：1973-05-15

申请号：US3733329D

申请日：1971-06-14

申请人： RICHTER GEDEON VEGYESZET

发明人： TUBA Z ,  BOR M

IPC分类号： C07J9/00 ,  C07D221/18 ,  C07J73/00 ,  C07D39/00

CPC分类号： C07D221/18 ,  C07C2603/16 ,  C07J73/005

摘要： THE INVENTION RELATES TO A PROCESS FOR THE PREPARATION OF CHOLESTANE DERIVATIVES WITH A NITROGEN ATOM IN 2 TO 3 POSITION, HAVING THE ENERAL FORMULA

CHOLESTANE WHERE C2 IS A AND C3 IS B

WHEREIN A AND B STAND FOR A CARBONYL, METHYLENE OR IMINO OR N-METHYLIMINO GROUP, WITH THE RESTRICTION, THAT WITHIN ONE COMPOUND A AND B ARE DIFFERENT, BUT EITHER A OR B STANDS FOR AN IMINO OR N-METHYLIMINO GROUP IN EACH CASE.