专利号:WO-0063168-A1 优先权日:1999-04-16 标题 :Synthesis of azetidine derivatives 发明人:CHEN ZHENGMING; KOLB HATMUTH C; RICHARDSON PAUL; HUANG ZHI-MIN 权利人:COELACANTH CHEMICAL CORP; CHEN ZHENGMING; KOLB HATMUTH C; RICHARDSON PAUL; HUANG ZHI MIN 摘要:The present invention provides compound having formula (I), useful as building blocks for combinatorial libraries and methods of making such compounds. Also provided is a novel process for synthesizing such compounds. In addition, the present invention includes products made by these processes.
专利号:US-9868746-B2 优先权日:2012-02-23 标题:Substituted 5-aminothieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; TARR JAMES C; SALOVICH JAMES M; POSLUSNEY MICHAEL S 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:US-4943641-A 优先权日:1984-02-27 标 题:3-aminoazetidine, its salts, process for their preparation and intermediates of synthesis 发明人:NISATO DINO; FRIGERIO MARCO 权利人:SANOFI SA 摘要:The 3-aminoazetidine, its salts, new intermediates of formula wherein X' represents hydrogen or a protecting group and both X'' represent hydrogen or, together with the nitrogen atom, a phthalimido group, X' not and both X'' being hydrogen at the same time; a process for the preparation of the 3-aminoazetidine, starting from a 1-protected 3-sulfonyloxyazetidine by reaction with the potassium phthalimide and transformation of the above mentioned intermediates.
专利号:US-5994575-A 优先权日:1996-04-16 标 题 :Phenylenediamines and process for preparing the same 发明人:YAZAKI AKIRA; YOSHIDA JIRO; NIINO YOSHIKO 权利人:WAKUNAGA PHARMA CO LTD 摘要:Phenylenediamines represented by general formula (1): ##STR1## wherein R represents an alkyl group or an optionally substituted aralkyl group, X 1 represents a hydrogen atom or a halogen atom, and X 2 represents a halogen atom; salts thereof, and a process for preparing the same. The compounds are useful as intermediates for synthesis of pyridonecarboxylic acid derivatives useful as antibacterial agents.
专利号:US-6080760-A 优先权日:1997-06-18 标题:Alpha 1A adrenergic receptor antagonists 发明人:PATANE MICHAEL A; BOCK MARK G 权利人:MERCK & CO INC 摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
专利号:WO-9857639-A1 优先权日:1997-06-18 标题 :ALPHA 1aADRENERGIC RECEPTOR ANTAGONISTS 发明人:PATANE MICHAEL A; BOCK MARK G 权利人:MERCK & CO INC; PATANE MICHAEL A; BOCK MARK G 摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha la adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
参考文献:10.1038/s41929-024-01206-4 摘要:Rodríguez RI, Corti V, Rizzo L, Visentini S, Bortolus M, Amati A, Natali M, Pelosi G, Costa P, Dell’Amico L. Radical strain-release photocatalysis for the synthesis of azetidines. Nat Catal. 2024 Aug 14;7(11):1223–31. doi: 10.1038/s41929-024-01206-4.