公开(公告)号：US4607054A

公开(公告)日：1986-08-19

申请号：US543315

申请日：1983-10-19

申请人： Marie-Madeleine Bouton ,  Jean Jacques ,  Andre Pierdet

发明人： Marie-Madeleine Bouton ,  Jean Jacques ,  Andre Pierdet

IPC分类号： C07C69/013 ,  A61K8/00 ,  A61K8/11 ,  A61K8/35 ,  A61K8/37 ,  A61K8/49 ,  A61K31/045 ,  A61K31/12 ,  A61K31/215 ,  A61K31/22 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/455 ,  A61P17/00 ,  A61P43/00 ,  A61Q5/00 ,  C07C45/00 ,  C07C45/61 ,  C07C45/67 ,  C07C49/513 ,  C07C49/517 ,  C07C49/737 ,  C07C49/753 ,  C07C67/00 ,  C07C69/03 ,  C07C69/08 ,  C07C313/00 ,  C07C323/13 ,  C07D213/79 ,  C07D213/80 ,  C07D317/70 ,  C07D317/72 ,  C07C69/14

CPC分类号： C07D213/80 ,  C07C49/513 ,  C07D317/70 ,  C07D317/72 ,  C07C2103/16

摘要： Novel antiandrogenic compositions comprising an antiandrogenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.- or .beta.-position and a non-toxic, pharmaceutical carrier or excipient and a method of treating hyperandrogenic conditions in warm-blooded animals.

摘要翻译： 包含抗雄激素有效量的至少一种下式化合物的新型抗雄激素组合物，其中R是1至4个碳原子的烷基，R 1是1至2个碳原子的烷基，R 2选自氢 任选地被2至8个碳原子的链烯基和炔基任选地中断为具有2至18个碳原子的有机羧酸的杂原子，甲酰基和酰基的1-8个碳原子的烷基，所述烷基任选地被2至8个碳原子的烯基和炔基中断， 由氢，1至4个碳原子的烷基和2至4个碳原子的烯基和炔基组成，R4选自氢和1至4个碳原子的烷基，虚线表示任选存在双键 在4（5）和5a（6）碳之间，波浪线表示R4可以是α或β-位，一种无毒的药物载体或赋形剂，以及一种在温暖血液中治疗雄激素过多症状的方法 有动物

公开(公告)号：US4466971A

公开(公告)日：1984-08-21

申请号：US350151

申请日：1982-02-19

申请人： Marie-Madeleine Bouton ,  Jean Jacques ,  Andre Pierdet

发明人： Marie-Madeleine Bouton ,  Jean Jacques ,  Andre Pierdet

IPC分类号： C07C69/013 ,  A61K8/00 ,  A61K8/11 ,  A61K8/35 ,  A61K8/37 ,  A61K8/49 ,  A61K31/045 ,  A61K31/12 ,  A61K31/215 ,  A61K31/22 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/455 ,  A61P17/00 ,  A61P43/00 ,  A61Q5/00 ,  C07C45/00 ,  C07C45/61 ,  C07C45/67 ,  C07C49/513 ,  C07C49/517 ,  C07C49/737 ,  C07C49/753 ,  C07C67/00 ,  C07C69/03 ,  C07C69/08 ,  C07C313/00 ,  C07C323/13 ,  C07D213/79 ,  C07D213/80 ,  C07D317/70 ,  C07D317/72 ,  C07D213/55 ,  C07C49/38 ,  C07C69/14

CPC分类号： C07D213/80 ,  C07C49/513 ,  C07D317/70 ,  C07D317/72 ,  C07C2103/16

摘要： Novel antiandrogenic compositions comprising an antiandrogenically effective amount of at least one compound of the formula ##STR1## wherein R is alkyl of 1 to 4 carbon atoms, R.sub.1 is alkyl of 1 to 2 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms optionally interrupted with a heteroatom, alkenyl and alkynyl of 2 to 8 carbon atoms optionally interrupted with a heteroatom, formyl and acyl of an organic carboxylic acid of 2 to 18 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the dotted lines indicate optional presence of a double bond between the 4(5) and 5a(6) carbons and the wavy line indicates that R.sub.4 may be in the .alpha.-or .beta.-position and a non-toxic, pharmaceutical carrier or excipient and a method of treating hyperandrogenic conditions in warm-blooded animals.

摘要翻译： 包含抗雄激素有效量的至少一种下式化合物的新型抗雄激素组合物，其中R是1至4个碳原子的烷基，R 1是1至2个碳原子的烷基，R 2选自氢 任选地被2至8个碳原子的链烯基和炔基任选地中断为具有2至18个碳原子的有机羧酸的杂原子，甲酰基和酰基的1-8个碳原子的烷基，所述烷基任选地被2至8个碳原子的烯基和炔基中断， 由氢，1至4个碳原子的烷基和2至4个碳原子的烯基和炔基组成，R4选自氢和1至4个碳原子的烷基，虚线表示任选存在双键 在4（5）和5a（6）之间的碳和波浪线表示R4可能是α或β-位和一种无毒的药物载体或赋形剂和一种治疗高血压雄激素病症的方法 给动物

公开(公告)号：US4189447A

公开(公告)日：1980-02-19

申请号：US914840

申请日：1978-06-12

申请人： David R. Parrish ,  Zoltan G. Hajos

发明人： David R. Parrish ,  Zoltan G. Hajos

IPC分类号： C07C69/716 ,  C07C20060101 ,  C07C45/00 ,  C07C45/73 ,  C07C49/385 ,  C07C49/395 ,  C07C49/493 ,  C07C49/623 ,  C07C51/00 ,  C07C59/205 ,  C07C67/00 ,  C07D263/52 ,  C07D317/46 ,  C07D317/54 ,  C07D325/00 ,  C07J1/00 ,  C07C49/56

CPC分类号： C07D263/52 ,  C07C45/56 ,  C07C45/66 ,  C07C45/67 ,  C07C45/69 ,  C07C45/73 ,  C07C49/513 ,  C07C2103/16

摘要： Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.

摘要翻译： 通过影响反应过程的光学活性剂由光学惰性反应物开始制备光学活性的有机化合物。 特别是具有“内消旋”型碳原子的光学活性化合物在光学活性剂的存在下进行分子内闭环，得到具有一个另外的环的光学活性产物。 本方法特别可用于制备在全合成类固醇中重要的中间体的光学双环二酮。

公开(公告)号：US4122093A

公开(公告)日：1978-10-24

申请号：US787593

申请日：1977-04-14

申请人： Elias J. Corey ,  Jasjit S. Bindra ,  Thomas K. Schaaf

发明人： Elias J. Corey ,  Jasjit S. Bindra ,  Thomas K. Schaaf

IPC分类号： C07C45/67 ,  C07C49/513 ,  C07C49/733 ,  C07C62/24 ,  C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D311/00 ,  C07D317/72 ,  C07D493/10 ,  C07D307/77

CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C45/673 ,  C07C49/513 ,  C07C49/733 ,  C07C62/24 ,  C07D307/93 ,  C07D311/00 ,  C07D317/72 ,  C07D493/10

摘要： A new synthesis of key prostaglandin precursors and intermediates employed in their preparation. The novel synthetic sequence of this invention is shorter and more efficient than those previously employed to prepare to key intermediate.

摘要翻译： 关键的前列腺素前体和中间体的新合成在其制备中使用。 本发明的新型合成序列比以前用于制备关键中间体的更短和更有效。

公开(公告)号：US3915641A

公开(公告)日：1975-10-28

申请号：US37561473

申请日：1973-07-02

申请人： WISCONSIN ALUMNI RES FOUND

发明人： GOERING HARLAN L ,  EIKENBERRY JOHN N ,  KOERMER GERALD S

IPC分类号： C07F5/00 ,  G01N24/08 ,  G01R33/28 ,  G01N27/78

CPC分类号： C07C49/92 ,  C07C45/455 ,  C07C45/88 ,  C07C49/477 ,  C07C49/513 ,  C07F5/003 ,  G01N24/08 ,  G01R33/281 ,  Y10T436/24

摘要： Optically active fluorinated compounds derived from d- or lcamphor and their corresponding europium and praseodymium chelates and their use as chiral NMR shift reagents.

摘要翻译： 衍生自d-或l-樟脑的光学活性氟化物及其相应的铕和镨螯合物及其作为手性NMR转移试剂的用途。

公开(公告)号：US3879466A

公开(公告)日：1975-04-22

申请号：US43684774

申请日：1974-01-28

申请人： INT FLAVORS & FRAGRANCES INC

发明人： LIGHT KENNETH K

IPC分类号： C07C43/162 ,  A23L27/20 ,  A24B15/34 ,  C07C27/00 ,  C07C35/22 ,  C07C35/52 ,  C07C41/00 ,  C07C43/15 ,  C07C43/166 ,  C07C43/205 ,  C07C45/00 ,  C07C49/385 ,  C07C49/587 ,  C07C67/00 ,  C11B9/00 ,  C11D3/50 ,  C11D9/00 ,  C07C49/54

CPC分类号： C07C45/69 ,  A23L27/203 ,  A24B15/345 ,  C07C43/15 ,  C07C43/166 ,  C07C45/62 ,  C07C45/63 ,  C07C49/477 ,  C07C49/513 ,  C07C49/693 ,  C07C49/733 ,  C11B9/00 ,  C11B9/0042 ,  C11D3/50 ,  C11D9/00 ,  Y10S426/805

摘要： Chemical compounds having the structure:

WHEREIN Z is a moiety selected from the group consisting of:

AND WHEREIN R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are the same or different and each is selected from the group consisting of methyl and hydrogen and wherein R11 is selected from the group consisting of methyl, ethyl and hydrogen; and wherein X is selected from the group consisting of bromo, chloro, hydroxyl, benzyloxyl and alkoxyl and a process for preparing such compounds involving intimately admixing a methyl substituted cyclohexadienone having the structure:

WITH ONE OF THE FOLLOWING ACETYLENIC COMPOUNDS HAVING THE STRUCTURES:

The compounds thus produced are valuable intermediates used in producing chemical compounds having valuable organoleptic properties; particularly in perfumery, in flavoring foodstuffs and in flavoring tobacco.

摘要翻译： 具有以下结构的化合物：

公开(公告)号：US3821307A

公开(公告)日：1974-06-28

申请号：US13925471

申请日：1971-04-30

申请人： HOOKER CHEMICAL CORP

发明人： HOCH P

IPC分类号： C07D307/93 ,  C07C49/27 ,  C07C49/80

CPC分类号： C07C49/477 ,  C07C49/513 ,  C07C49/517 ,  C07C49/693 ,  C07C49/697 ,  C07C49/753 ,  C07D307/93

摘要： Bicyclic ketones of the formula

WHEREIN R1, R2, R3, R4, X1, X2, X3, X4 and X5 are certain substituents selected from hydrogen, halogen, alkyl, alkenyl, halogenated alkyl, halogenated alkenyl, alkoxy, hydrocarbyl, halogen-substituted hydrocarbyl, carboxy, hydroxy-substituted alkyl, alkoxy-substituted alkyl, and hydroxy-substituted alkoxyalkyl, with at least two of X1, X2, X3 and X4 being halogen, and X6 is halogen. The bicyclic ketones are made by treating a corresponding tricyclic hemiketal with phosphorus halide and hydrolyzing. The bicyclic ketones are useful as chemical intermediates and as insecticides.

公开(公告)号：US2821557A

公开(公告)日：1958-01-28

申请号：US50831755

申请日：1955-05-13

申请人： GEN ANILINE & FILM CORP

发明人： ALBERT BLOOM ,  DEUTSCH DENNIS L

CPC分类号： C07C45/27 ,  C07C2603/50 ,  C07C49/513

公开(公告)号：US20180339956A1

公开(公告)日：2018-11-29

申请号：US15771436

申请日：2016-10-28

申请人： INDUSTRIALE CHIMICA S.R.L.

发明人： Roberto LENNA ,  Roberto DI BRISCO

IPC分类号： C07C45/00 ,  C07C49/513

CPC分类号： C07C45/004 ,  C07C45/292 ,  C07C45/64 ,  C07C45/74 ,  C07C49/513 ,  C07C2603/12 ,  C07D311/78 ,  C07J75/005 ,  C07C49/443 ,  C07C49/643 ,  C07C49/733

摘要： The present invention relates to a new process for the synthesis of 17β-hydroxy-des-A-androst-9,10-en-5-one, the compound of the following formula (1), which can be used as an intermediate in the synthesis of retroprogesterones.

公开(公告)号：US09562026B2

公开(公告)日：2017-02-07

申请号：US14203678

申请日：2014-03-11

申请人： Washington University

发明人： Douglas Covey

IPC分类号： C07C61/125 ,  C07C255/47 ,  C07D303/14 ,  C07C49/513

CPC分类号： C07D303/14 ,  C07C49/423 ,  C07C49/513 ,  C07C255/47 ,  C07C2603/40 ,  C07C2603/42

摘要： The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

摘要翻译： 本公开一般涉及本文所述的神经活性取代的环戊烯[a]蒽及其药学上可接受的盐，用作例如麻醉剂和/或用于治疗与GABA功能和活性相关的疾病。 本公开进一步涉及包含这些化合物的药物组合物。