专利号:US-2001044142-A1 优先权日:2000-04-28 标题:Microbial reductase useful for the stereoselective reduction of a racemic tetralone 发明人:BROWN MARIA S; FEDECHKO RONALD W; WONG JOHN W 摘要:The present invention relates to novel compositions of matter comprising an enzyme activity capable of carrying out the following stereoselective reduction of a racemic tetralone: n n n The chiral tetralone can be used in the synthesis of sertraline, well known to be useful, for example, as an antidepressant and anorectic agent, and in the treatment of chemical dependencies, anxiety-related disorders, premature ejaculation, cancer and post-myocardial infarction.
专利号:US-6589777-B1 优先权日:1998-10-29 标题:Stereoselective microbial reduction of a racemic tetralone 发明人:MORSE BROOK K; TRUESDELL SUSAN J; WONG JOHN W 权利人:PFIZER 摘要:The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: n which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or “chiral tetralone.â€? The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).
专利号:US-9884844-B2 优先权日:2012-12-31 标 题:Heterocyclic compounds and methods of use thereof 发明人:FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
专利号:US-3850911-A 优先权日:1960-09-22 标题:Steroid synthesis 发明人:HUGHES G; SMITH H 权利人:HUGHES G; SMITH H 摘要:1. A CHEMICAL COMPOUND HAVING A CYCLOPENTANOPHENANTHRENE CARBON-CARBON SKELETON CONTAINING AT LEAST 19 AND UP TO A MAXIMUM OF 40 CARBON ATOMS AND IN WHICH AT LEAST B AND THE C RING ARE AT LEAST PARTIALLY HYDROGENATED, INCLUDING A NUCLEUS SELECTED FROM THE GROUP CONSISTING OF SATURATED AND UNSATURATED GONANE AND 8ISOGONANE NUCLEI HAVING UP TO A MAXIMUM OF FIVE (5) DOUBLE BONDS AND HAVING A PART THEREOF IN THE 13-POSITION F MONOVALENT POLYCARBON ALKYL RADICAL HAVING 2 TO ABOUT 16 CARBON ATOMS, SAID RINGS AND THE 13 AND OTHER POSITIONS OF THE NUCLEUS BEING IDENTIFIED ACCORDING TO STEROID NOMENCLATURE.
专利号:CN-101337186-A 优先权日:2008-08-27 标题 :Preparation method of meso-porous alumina and catalytic synthesis of alpha-tetralone