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1. 发明授权

US09878981B2 Method for producing heterocyclic compound 有权
公开(公告)号：US09878981B2
公开(公告)日：2018-01-30
申请号：US15301525
申请日：2015-04-09
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人： Hironori Yamashita , Kazuhiro Miwa
IPC分类号： C07D211/60 , C07C231/02 , C07D401/06
CPC分类号： C07D211/60 , C07C231/02 , C07C231/08 , C07C2101/02 , C07C2101/08 , C07C2101/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D401/06 , C07C233/58
摘要： Provided is a production method of a synthetic intermediate for a heterocyclic compound having a renin inhibitory activity and useful as a prophylactic or therapeutic drug for diabetic nephropathy, hypertension and the like. A production method of a compound represented by the formula (III-1a), the formula (III-1b), the formula (III-1c) and/or the formula (III-1d); wherein each symbol is as described in DESCRIPTION, or a salt thereof, including reacting a compound represented by the formula (Ia) or (Ib): wherein each symbol is as described in DESCRIPTION, or a salt thereof with a compound represented by the formula (II): wherein each symbol is as described in DESCRIPTION, or a salt thereof, in the presence of an aluminum compound and a chiral amine compound.

2. 发明授权

US09624166B2 Tetracycline compounds 有权
公开(公告)号：US09624166B2
公开(公告)日：2017-04-18
申请号：US13391407
申请日：2010-08-27
申请人： Yonghong Deng , Louis Plamondon , Cuixiang Sun , Xiao-Yi Xiao , Jingye Zhou , Joyce A. Sutcliffe , Magnus P. Ronn
发明人： Yonghong Deng , Louis Plamondon , Cuixiang Sun , Xiao-Yi Xiao , Jingye Zhou , Joyce A. Sutcliffe , Magnus P. Ronn
IPC分类号： A61K31/65 , A61P31/04 , C07C237/26 , C07C311/08 , C07C307/10 , C07C311/09 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07D205/04 , C07D207/12 , C07D207/16 , C07D209/44 , C07D209/52 , C07D211/54 , C07D211/60 , C07D213/70 , C07D213/74 , C07D213/82 , C07D223/06 , C07D231/18 , C07D233/60 , C07D233/84 , C07D295/15 , C07D307/64
CPC分类号： C07C311/08 , C07C237/26 , C07C307/10 , C07C311/09 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/44 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/40 , C07C2103/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/40 , C07C2603/44 , C07C2603/46 , C07D205/04 , C07D207/12 , C07D207/16 , C07D209/44 , C07D209/52 , C07D211/54 , C07D211/60 , C07D213/70 , C07D213/74 , C07D213/82 , C07D223/06 , C07D231/18 , C07D233/60 , C07D233/84 , C07D295/15 , C07D307/64
摘要： The present invention is directed to a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

3. 发明申请

US20170073286A1 CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：环烷基羟基化合物及其组合物用于胆固醇管理及相关用途
公开(公告)号：US20170073286A1
公开(公告)日：2017-03-16
申请号：US15274436
申请日：2016-09-23
申请人： Esperion Therapeutics, Inc.
发明人： Jean-Louis H. Dasseux , Carmen D. Oniciu
IPC分类号： C07C31/27 , C07C69/757 , C07C47/34 , C07C309/25 , C07F9/11 , C07C59/11 , C07C59/29 , C07D495/04 , C07C255/00 , C07F9/24 , C07D257/04 , C07D261/12 , C07D309/12 , C07D305/12 , C07D307/33 , C07D309/30 , C07C61/12
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译：本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。

4. 发明授权

US09452964B2 Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses 有权
公开(公告)号：US09452964B2
公开(公告)日：2016-09-27
申请号：US14674025
申请日：2015-03-31
申请人： Esperion Therapeutics, Inc.
发明人： Jean-Louis H. Dasseux , Carmen D. Oniciu
IPC分类号： C07C31/27 , C07C61/12 , C07C47/34 , C07C309/25 , C07F9/24 , C07D261/12 , C07C59/105 , C07C33/26 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07F9/11 , C07C309/24 , C07F9/12 , C07D495/04 , C07C255/00 , C07D257/04 , C07D261/08 , C07D305/12 , C07D307/33 , C07C59/01 , C07D309/30 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/44
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

5. 发明申请

US20150344388A1 HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 有权
标题翻译：羟丙基化合物和组合物用于胆固醇管理和相关用途
公开(公告)号：US20150344388A1
公开(公告)日：2015-12-03
申请号：US14674028
申请日：2015-03-31
申请人： Esperion Therapeutics, Inc.
发明人： Jean-Louis H. Dasseux , Carmen D. Oniciu
IPC分类号： C07C31/20 , C07C59/105 , C07C59/245 , C07C33/26 , C07C59/48 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07F9/11 , C07C309/24 , C07F9/12 , C07D495/04 , C07C255/00 , C07F9/24 , C07D257/04 , C07D261/08 , C07D309/12 , C07D305/12 , C07D307/33 , C07C59/01 , C07D309/30 , C07C31/22
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译：本发明涉及新的羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病性视网膜病变，葡萄糖代谢异常，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质清除，肥胖，胆汁中的氧固醇消除，胰腺炎，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除胆汁，肾脏疾病，败血症，代谢综合症（如X综合症），血栓形成障碍。本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。

6. 发明授权

US09067905B2 Sulphone compounds and methods of making and using same 有权
标题翻译：砜类化合物及其使用方法
公开(公告)号：US09067905B2
公开(公告)日：2015-06-30
申请号：US13453219
申请日：2012-04-23
申请人： Hazel J. Dyke , Susan M. Cramp , Thomas D. Pallin , Janusz J. Kulagowski , John G. Montana , Robert Zahler
发明人： Hazel J. Dyke , Susan M. Cramp , Thomas D. Pallin , Janusz J. Kulagowski , John G. Montana , Robert Zahler
IPC分类号： C07D307/54 , A61K31/192 , C07C317/46 , C07C317/44 , C07D213/55 , C07D231/12 , C07D263/32 , C07D275/02 , C07D277/30 , C07D307/16 , C07D333/24 , C07D405/12 , C07D451/02 , C07D487/08
CPC分类号： A61K31/46 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/407 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/4418 , A61K31/443 , A61K31/4525 , C07C317/44 , C07C317/46 , C07C2101/02 , C07C2601/02 , C07D213/55 , C07D231/12 , C07D263/32 , C07D275/02 , C07D277/30 , C07D307/16 , C07D307/54 , C07D333/24 , C07D405/12 , C07D451/02 , C07D487/08
摘要： The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
摘要翻译：本发明提供了砜类化合物及其在治疗医学疾病如肥胖症中的用途。提供制备各种砜化合物的药物组合物和方法。化合物被认为具有抗甲硫氨酰氨基肽酶2的活性。

7. 发明申请

US20140315954A1 CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME 有权
标题翻译：细胞毒素和抗微生物化合物及其使用方法
公开(公告)号：US20140315954A1
公开(公告)日：2014-10-23
申请号：US14213504
申请日：2014-03-14
申请人： THE CENTRE FOR DRUG RESEARCH AND DEVELOPMENT
发明人： Geoffrey C. WINTERS , Alexander L. Mandel , BRADLEY J. HEDBERG
IPC分类号： C07C317/50 , C07C317/28 , C07D213/56 , C07C317/32 , C07D211/60 , C07D213/71
CPC分类号： C07C311/51 , A61K31/445 , A61K38/05 , A61K38/06 , A61K39/3955 , A61K47/48261 , A61K47/48415 , A61K47/6415 , C07C317/28 , C07C317/32 , C07C317/50 , C07C323/12 , C07C323/67 , C07C327/06 , C07C381/08 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D207/452 , C07D211/34 , C07D211/60 , C07D213/56 , C07D213/71 , C07D333/34 , C07K5/0205 , C07K5/06078 , Y02A50/385 , Y02A50/414 , Y02A50/423
摘要： Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
摘要翻译：公开了具有细胞毒性和/或抗有丝分裂活性的化合物。该化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中R 1，R 2，R 3，R 4和R 5如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。还公开了具有以下结构的组合物：（T） - （L） - （D），其中（T）是靶向部分，（L）是任选的连接体，（D）是具有结构（I）的化合物。

8. 发明申请

US20140187546A1 Cystine Diamide Analogs for the Prevention of Cystine Stone Formation in Cystinuria 有权
标题翻译：胱氨酸二酰胺类似物用于预防胱氨酸尿中胱氨酸石形成
公开(公告)号：US20140187546A1
公开(公告)日：2014-07-03
申请号：US14146103
申请日：2014-01-02
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Amrik Sahota
IPC分类号： C07C323/60 , C07D295/185 , C07C319/24
CPC分类号： C07D295/185 , C07C323/60 , C07C2101/02 , C07C2601/02 , C07D211/16
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
摘要翻译：提高L-胱氨酸在尿中用于治疗尿胱症的结构的胱氨酸类似物及其药学上可接受的盐，溶剂合物和前药，其中每个R和R'对独立地选自（i）或（ii） ; （i）R和R'独立地选自氢，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的醇，取代或未取代的芳基，取代或未取代的环烷基，取代或未取代的杂环，以及取代或未取代的杂芳基，或（ii）R和R'一起形成取代或未取代的杂环结构，或取代或未取代的杂芳基环结构; X是氢或烷基; Y是O或S.

9. 发明授权

US08497301B2 Hydroxyl compounds and compositions for cholesterol management and related uses 有权
公开(公告)号：US08497301B2
公开(公告)日：2013-07-30
申请号：US13470825
申请日：2012-05-14
申请人： Jean-Louis Henri Dasseux , Carmen Daniela Oniciu
发明人： Jean-Louis Henri Dasseux , Carmen Daniela Oniciu
IPC分类号： A61K31/20
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

10. 发明申请

US20130090386A1 LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE 有权
标题翻译： LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS及其使用
公开(公告)号：US20130090386A1
公开(公告)日：2013-04-11
申请号：US13641916
申请日：2011-04-19
申请人： Alberto Ortega Munoz , Juio Castro-Palomino Laria , Matthew Colin Thor Fyfe
发明人： Alberto Ortega Munoz , Juio Castro-Palomino Laria , Matthew Colin Thor Fyfe
IPC分类号： A61K31/135 , C07C211/42 , A61K45/06 , C07C237/24 , A61K31/165 , C07C217/74 , C07C211/40
CPC分类号： C07C217/74 , A61K31/135 , A61K31/165 , A61K45/06 , A61N5/10 , C07C211/35 , C07C211/40 , C07C211/42 , C07C217/52 , C07C237/24 , C07C2101/02 , C07C2101/14 , C07C2101/18 , C07C2102/08 , C07C2102/10 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2602/08 , C07C2602/10
摘要： The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.
摘要翻译：本发明涉及式1的化合物，其中：（A）是杂芳基或芳基; 每个（A'）如果存在，独立地选自芳基，芳基烷氧基，芳基烷基，杂环基，芳氧基，卤素，烷氧基，卤代烷基，环烷基，卤代烷氧基和氰基，其中每个（A'）被0,1,2 ，或3个独立地选自卤素，卤代烷基，卤代烷氧基，芳基，芳基烷氧基，烷基，烷氧基，酰氨基，-CH 2 C（= O）NH 2，杂芳基，氰基，磺酰基和亚磺酰基的取代基。 X为0,1,2或3; （B）是环丙基环，其中（A）和（Z）与（B）的不同碳原子共价结合; （Z）为-NH-; （L）选自单键-CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - 和-CH 2 CH 2 CH 2 CH 2 - ; - 和（D）是脂族碳环基或苯并环烷基，其中所述脂族碳环基或所述苯并环烷基具有0,1,2或3个独立地选自-NH 2，-NH（C 1 -C 6烷基）， - N（C1- C6烷基）（C1-C6烷基），烷基，卤素，酰胺基，氰基，烷氧基，卤代烷基和卤代烷氧基。（A'）X-（A） - （B） - （Z） - （L） - （D）式（I）本发明化合物显示出抑制LSD1的活性，使其可用于治疗或预防疾病如癌症。

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