子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 作为毒蕈碱性受体拮抗剂的碳酰胺衍生物 | CN200680034818.9 | 2006-09-01 | CN101268046B | 2012-07-25 | P·A·格洛索普; S·J·曼特尔; R·S·斯特朗; C·A·L·沃森; A·伍德 |
| 本发明涉及式(I)的化合物、其制备方法和中间体、其作为蕈毒碱拮抗剂的应用、以及含有其的药物组合物。 | ||||||
| 2 | 作为毒蕈碱性受体拮抗剂的碳酰胺衍生物 | CN200680034818.9 | 2006-09-01 | CN101268046A | 2008-09-17 | P·A·格洛索普; S·J·曼特尔; R·S·斯特朗; C·A·L·沃森; A·伍德 |
| 本发明涉及式(I)的化合物、其制备方法和中间体、其作为蕈毒碱拮抗剂的应用、以及含有其的药物组合物。 | ||||||
| 3 | Carboxamide derivatives as muscarinic receptor antagonist | JP2008531819 | 2006-09-01 | JP4221447B1 | 2009-02-12 | ウッド アンソニ−; アン ルイス ワトソン クリスティン; ジョン マンテル サイモン; アラン グロソップ ポール; シンクレア ストラング ロス |
| 本発明は、式（Ｉ）の化合物、それらを調製するための方法および中間体、ムスカリン様アンタゴニストとしてのそれらの使用ならびにそれらを含有する医薬組成物に関する。
【化１】 |
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| 4 | Carboxamide derivatives as muscarinic receptor antagonist | JP2008531819 | 2006-09-01 | JP2009508933A | 2009-03-05 | ウッド アンソニ−; アン ルイス ワトソン クリスティン; ジョン マンテル サイモン; アラン グロソップ ポール; シンクレア ストラング ロス |
| 本発明は、式（Ｉ）の化合物、それらを調製するための方法および中間体、ムスカリン様アンタゴニストとしてのそれらの使用ならびにそれらを含有する医薬組成物に関する。
【化１】 |
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| 5 | SUBSTITUTED 1H-IMIDAZO[4,5-b]PYRIDIN-2(3H)-ONES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS | US15725500 | 2017-10-05 | US20180125826A1 | 2018-05-10 | Christa C. Chrovian; Michael A. Letavic; Jason C. Rech; Dale A. Rudolph; Akinola Soyode-Johnson; Brice M. Stenne; Jessica L. Wall |
| Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity. | ||||||
| 6 | Carboxamide derivatives as muscarinic receptor antagonists | US12828732 | 2010-07-01 | US08486992B2 | 2013-07-16 | Paul Alan Glossop; Simon John Mantell; Anthony Wood; Christine Anne Louise Watson |
| The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them. | ||||||
| 7 | Carboxamide derivatives as muscarinic receptor antagonists | US12556285 | 2009-09-09 | US08268881B2 | 2012-09-18 | Paul Alan Glossop; Simon John Mantell; Anthony Wood; Christine Anne Louise Watson |
| The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them. | ||||||
| 8 | Ligands for monoamine receptors and transporters, and methods of use thereof | US12403311 | 2009-03-12 | US07816375B2 | 2010-10-19 | Brian M. Aquila; Thomas D. Bannister; Gregory D. Cuny; James R. Hauske; Joanne M. Holland; Paul E. Persons; Heike Radeke; Fengjiang Wang; Liming Shao |
| One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters. | ||||||
| 9 | Method of treating addiction or dependence using a ligand for a monamine receptor or transporter | US10771519 | 2004-02-04 | US07294637B2 | 2007-11-13 | Brian M. Aquila; Thomas D. Bannister; Gregory D. Cuny; James R. Hauske; Joanne M. Holland; Paul E. Persons; Heike S. Radeke; Fengjiang Wang; Liming Shao |
| One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction. | ||||||
| 10 | Carboxamide derivatives as muscarinic receptor antagonists | US11522840 | 2006-09-18 | US07772223B2 | 2010-08-10 | Paul Alan Glossop; Simon John Mantell; Anthony Wood; Christine Anne Louise Watson |
| The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them. | ||||||
| 11 | Carboxamide Derivatives As Muscarinic Receptor Antagonists | US12556285 | 2009-09-09 | US20100029720A1 | 2010-02-04 | Paul Alan Glossop; Simon John Mantell; Anthony Wood; Christine Anne Louise Watson |
| The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them. | ||||||
| 12 | LIGANDS FOR MONOAMINE RECEPTORS AND TRANSPORTERS, AND METHODS OF USE THEREOF | US12403311 | 2009-03-12 | US20090258901A1 | 2009-10-15 | Brian M. Aquila; Thomas D. Bannister; Gregory D. Cuny; James R. Hauske; Joanne M. Holland; Paul E. Persons; Heike Radeke; Fengjiang Wang; Liming Ahao |
| One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters. | ||||||
| 13 | Ligands for monoamine receptors and transporters, and methods of use thereof | US09951130 | 2001-09-12 | US07517892B2 | 2009-04-14 | Brian M. Aquila; Thomas D. Bannister; Gregory D. Cuny; James R. Hauske; Joanne M. Holland; Paul E. Persons; Heike Radeke; Fengjiang Wang; Liming Shao |
| One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters. | ||||||
| 14 | Carboxamide derivatives as muscarinic receptor antagonists | US11522840 | 2006-09-18 | US20070105831A1 | 2007-05-10 | Paul Glossop; Simon Mantell; Anthony Wood; Christine Watson |
| The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them. | ||||||
| 15 | Ligands for monoamine receptors and transporters, and methods of use thereof | US10607457 | 2003-06-26 | US07132551B2 | 2006-11-07 | Brian M. Aquila; Thomas D. Bannister; Gregory D. Cuny; James R. Hauske; Joanne M. Holland; Paul E. Persons; Heike S. Radeke; Fengjiang Wang; Liming Shao |
| One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters. | ||||||
| 16 | Process for the production of aziridines | US134863 | 1987-12-18 | US5120860A | 1992-06-09 | Kurt D. Olson; Steven W. Kaiser |
| .beta.-Hydroxyamines can be converted to the corresponding aziridines by contacting the amines with a molecular sieve, which has incorporated therein at least one alkali metal or alkaline metal, the preferred metal being cesium. Molecular sieves useful in the reaction include aluminosilicates, aluminophosphates and silicoaluminophosphates. The process is especially useful for the conversion of monoethanolamine to ethylenimine. | ||||||
| 17 | アダマンタンアミド製造方法 | JP2016536713 | 2014-12-04 | JP6434980B2 | 2018-12-05 | ハリチアン,ビジヤン; ロサ,ホセ・ギジエルモ |
| 18 | アダマンタンアミド製造方法 | JP2016536713 | 2014-12-04 | JP2016540774A | 2016-12-28 | ハリチアン，ビジヤン; ロサ，ホセ・ギジエルモ |
| アダマンタンアミドの有効な製造方法であって、該方法は迅速であり、有機溶媒も、有機溶媒又は副生成物の除去による多大な労力を要する生成物の単離若しくは精製も使用せず、改善された収率及び純度を有する。 | ||||||
| 19 | Ligand, as well as how to use the monoamine receptors and transporters | JP2002526825 | 2001-09-12 | JP2004509103A | 2004-03-25 | アクワイラ，ブライアン エム; カニー，グレゴリー ディー; シャオ，リミン; パーソンズ，ポール イー; バニスター，トーマス ディー; ホースク，ジェイムズ アール; ホーランド，ジョアンヌ エム; ラディク，ハイク; ワン，フェンジャン |
| 本発明の一態様はヘテロ環式化合物に関するものである。 本発明の第２の態様は、ドーパミン、セロトニン、またはノルエピネフリンなどの哺乳動物の異なる細胞輸送体のリガンドとしてのヘテロ環式化合物の使用に関するものである。 本発明の化合物は、哺乳動物における嗜癖、不安、うつ病、性的機能不全、高血圧、偏頭痛、アルツハイマー病、肥満、嘔吐、心因性精神病、無痛症、精神分裂病、パーキンソン病、不穏下肢症候群、睡眠障害、注意欠陥多動性障害、過敏性腸症候群、早漏、月経不機嫌症候群、尿失禁、炎症性疼痛、神経痛、レッシュ−ナイハン病、ウィルソン病、及びトゥレット症候群などの多くの疾患、病態、疾病の治療に用途を見出すものである。 本発明の更なる態様はヘテロ環式化合物のコンビナトリアルライブラリーの合成、及び、ドーパミン輸送体に基づいたアッセイなどの生物学的活性についてこれらのライブラリーをスクリーニングする方法に関するものである。 | ||||||
| 20 | FXR (NR1H4) MODULATING COMPOUNDS | EP17175336.1 | 2017-06-09 | EP3257847A1 | 2017-12-20 | BLOMGREN, Peter A; CURRIE, Kevin S; GEGE, Christian; KROPF, Jeffrey E; XU, Jianjun |
The present disclosure relates generally to compounds (I) which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
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