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1. 发明申请

US20150210643A1 DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTOR 审中-公开
标题翻译： 4-（2-氨基-1-羟基乙基）苯酚的衍生物作为BETA2 ADRENERGIC受体的激动剂
公开(公告)号：US20150210643A1
公开(公告)日：2015-07-30
申请号：US13538117
申请日：2012-06-29
申请人： JORDI BACH TAÑA , MARIA ISABEL CRESPO CRESPO , CARLOS PUIG DURAN , SILVIA GUAL ROIG , ALBERTO ORTEGA MUÑOZ
发明人： JORDI BACH TAÑA , MARIA ISABEL CRESPO CRESPO , CARLOS PUIG DURAN , SILVIA GUAL ROIG , ALBERTO ORTEGA MUÑOZ
IPC分类号： C07D215/227 , A61K45/06 , A61K31/573 , A61K31/137 , C07C233/43 , A61K31/167 , A61K31/4704 , C07C217/60
CPC分类号： C07D215/227 , A61K31/137 , A61K31/167 , A61K31/4704 , A61K31/573 , A61K45/06 , C07C217/60 , C07C233/43
摘要： The present relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂化物或立体异构体。本公开还涉及包含式（I）化合物的药物组合物及其在治疗中的使用方法。

2. 发明授权

US08946296B2 Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use 有权
标题翻译：取代的杂芳基 - 和芳基 - 环丙胺乙酰胺及其用途
公开(公告)号：US08946296B2
公开(公告)日：2015-02-03
申请号：US13500687
申请日：2010-04-19
申请人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
发明人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
IPC分类号： A61K31/165 , C07C237/20 , C07C237/06 , C07C255/54 , C07D213/36
CPC分类号： C07C237/06 , C07C255/54 , C07C2601/02 , C07D213/36
摘要： The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; 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—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
摘要翻译：本发明涉及式（I）化合物：（A'）x-（A） - （B） - （Z） - （L）-C（= O）NH 2或其药学上可接受的盐或溶剂合物，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，芳基，芳基烷氧基，烷基，烷氧基，氰基，磺酰基，亚磺酰基和羧酰胺的取代基; 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-; 和（L）是 - （CH 2）m CR 1，R 2 - ，其中m是0,1,2,3,4,5或6，并且其中R 1和R 2各自独立地是氢或C 1 -C 6烷基; 条件是，如果（L）是-CH 2 - 或-CH（CH 3） - ，则X不为0.本发明的化合物可用于治疗疾病如癌症和神经变性疾病。

3. 发明授权

US09616058B2 Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use 有权
公开(公告)号：US09616058B2
公开(公告)日：2017-04-11
申请号：US13580553
申请日：2011-02-24
申请人： Julio Cesar Castro Palomino Laria , Alberto Ortega Muñoz , Nathalie Guibourt , Jonathan Alleman Baker
发明人： Julio Cesar Castro Palomino Laria , Alberto Ortega Muñoz , Nathalie Guibourt , Jonathan Alleman Baker
IPC分类号： A61K31/135 , A61K31/131 , A61K31/137 , A61K31/15 , A61K31/495 , A61K31/13 , A61K31/16 , A61K31/40 , A61K31/505 , A61K45/06 , A61K31/165
CPC分类号： A61K31/495 , A61K31/13 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/505 , A61K45/06 , Y02A50/467 , A61K2300/00
摘要： The present invention relates to the use of potent selective LSD inhibitors and LSD/MAO-B inhibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defined herein, for treating or preventing viral infection and treating or preventing reactivation of a virus after latency.

4. 发明授权

US09006449B2 Cyclopropylamine derivatives useful as LSD1 inhibitors 有权
标题翻译：可用作LSD1抑制剂的环丙胺衍生物
公开(公告)号：US09006449B2
公开(公告)日：2015-04-14
申请号：US13812386
申请日：2011-07-27
申请人： Matthew Colin Thor Fyfe , Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Marc Martinell Pedemonte , Maria de los Ángeles Estiarte-Martinez , Nuria Valls Vidal
发明人： Matthew Colin Thor Fyfe , Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Marc Martinell Pedemonte , Maria de los Ángeles Estiarte-Martinez , Nuria Valls Vidal
IPC分类号： C07D401/00 , C07D277/28 , A61K31/44 , C07C211/40 , C07C215/64 , C07C217/74 , C07C255/53 , C07C255/54 , C07C311/08 , C07C311/09 , C07C311/21 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D239/26 , C07D333/20 , C07D401/04 , C07D405/04 , C07D409/04 , C07C255/59 , C07D213/64 , C07D401/10 , C07D405/10 , C07D409/10
CPC分类号： C07C211/40 , C07B2200/07 , C07C215/64 , C07C217/74 , C07C255/53 , C07C255/54 , C07C255/59 , C07C311/08 , C07C311/09 , C07C311/21 , C07C2601/02 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D213/64 , C07D239/26 , C07D277/28 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
摘要翻译：本发明涉及环丙胺化合物，特别是式（I）的化合物及其在治疗中的应用，包括例如。治疗或预防癌症，神经系统疾病或病症或病毒感染。

5. 发明授权

US08859555B2 Lysine Specific Demethylase-1 inhibitors and their use 有权
公开(公告)号：US08859555B2
公开(公告)日：2014-10-14
申请号：US13497994
申请日：2010-04-19
申请人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
发明人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
IPC分类号： A61K31/495 , C07D295/13 , A61K31/075 , C07C211/40 , C07D211/14 , C07D241/04 , A61K45/06 , C07C323/25 , C07C217/74 , C07D207/14 , A61K31/40 , C07C217/08 , A61K31/095
CPC分类号： C07D241/04 , A61K31/075 , A61K31/095 , A61K31/40 , A61K31/495 , A61K45/06 , C07C211/40 , C07C217/08 , C07C217/74 , C07C323/25 , C07C2601/02 , C07D207/14 , C07D211/14 , A61K2300/00
摘要： The invention relates to a compound of Formula (I): (A′)x-(A)-(B)-(Z)-(L)-(D), 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, 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 —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is chosen from —N(—R1)-R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; and R3 is chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.

6. 发明申请

US20130289076A1 CYCLOPROPYLAMINE INHIBITORS OF OXIDASES 有权
标题翻译：氧化锌的环丙基胺抑制剂
公开(公告)号：US20130289076A1
公开(公告)日：2013-10-31
申请号：US13877919
申请日：2011-10-07
申请人： Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe , Marc Murtinell Pedemonte , Alberto Ortega Muñoz , Núrla Valls Vidal
发明人： Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe , Marc Murtinell Pedemonte , Alberto Ortega Muñoz , Núrla Valls Vidal
IPC分类号： C07D401/12 , C07C237/30 , C07C217/92 , C07C255/58 , C07D213/74 , C07C211/52
CPC分类号： A61K31/4439 , A61K31/136 , A61K31/166 , A61K31/277 , A61K31/4418 , C07C211/52 , C07C211/53 , C07C211/55 , C07C211/56 , C07C217/92 , C07C237/30 , C07C255/58 , C07D213/74 , C07D401/12
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
摘要翻译：本发明涉及环丙胺化合物，特别是本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症。

7. 发明申请

US20130197013A1 CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS 有权
标题翻译：环丙基胺衍生物作为LSD1抑制剂有用
公开(公告)号：US20130197013A1
公开(公告)日：2013-08-01
申请号：US13812386
申请日：2011-07-27
申请人： Mathew Colin Thor Fyfe , Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Marc Martinell Pedemonte , Maria de los Ángeles Estiarte-Martínez , Nuria Valls Vidal
发明人： Mathew Colin Thor Fyfe , Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Marc Martinell Pedemonte , Maria de los Ángeles Estiarte-Martínez , Nuria Valls Vidal
IPC分类号： C07C211/40 , C07D213/38 , C07D213/57 , C07D213/56 , C07D409/04 , C07D277/28 , C07D409/10 , C07D213/42 , C07C255/59 , C07D405/10 , C07D213/64 , C07D333/20 , C07C215/64 , C07D401/10
CPC分类号： C07C211/40 , C07B2200/07 , C07C215/64 , C07C217/74 , C07C255/53 , C07C255/54 , C07C255/59 , C07C311/08 , C07C311/09 , C07C311/21 , C07C2601/02 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/56 , C07D213/57 , C07D213/64 , C07D239/26 , C07D277/28 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/04 , C07D405/10 , C07D409/04 , C07D409/10
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
摘要翻译：本发明涉及环丙胺化合物，特别是式（I）的化合物及其在治疗中的应用，包括例如。治疗或预防癌症，神经系统疾病或病症或病毒感染。

8. 发明申请

US20120283266A1 LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE 有权
公开(公告)号：US20120283266A1
公开(公告)日：2012-11-08
申请号：US13497994
申请日：2010-04-19
申请人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
发明人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
IPC分类号： A61K31/135 , A61K31/495 , C07C211/36 , A61P35/00 , A61K31/40 , C07D211/26 , A61K31/445 , C07C323/29 , C07D241/04 , C07D207/14
CPC分类号： C07D241/04 , A61K31/075 , A61K31/095 , A61K31/40 , A61K31/495 , A61K45/06 , C07C211/40 , C07C217/08 , C07C217/74 , C07C323/25 , C07C2601/02 , C07D207/14 , C07D211/14 , A61K2300/00
摘要： The invention relates to a compound of Formula (I): (A′)x-(A)-(B)-(Z)-(L)-(D), 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, 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 —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; and R3 is chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.

9. 发明授权

US09181198B2 Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use 有权
标题翻译： LSD1的芳基环丙基胺脱甲基酶抑制剂及其用途
公开(公告)号：US09181198B2
公开(公告)日：2015-11-10
申请号：US13812366
申请日：2011-07-27
申请人： Alberto Ortega Muñoz , Matthew Colin Thor Fyfe , Marc Martinell Pedemonte , Iñigo Tirapu Fernandez de la Cuesta , Maria de los Ángeles Estiarte-Martínez
发明人： Alberto Ortega Muñoz , Matthew Colin Thor Fyfe , Marc Martinell Pedemonte , Iñigo Tirapu Fernandez de la Cuesta , Maria de los Ángeles Estiarte-Martínez
IPC分类号： C07D285/12 , C07D271/12 , C07D263/02 , C07D275/02 , C07D261/02 , C07D239/42 , A61K31/433 , A61K31/4245 , A61K31/422 , C07D213/73 , C07D237/20 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D401/12 , C07D413/12 , C07D417/12 , C07D285/135
CPC分类号： C07D417/12 , A61K31/422 , A61K31/4245 , A61K31/433 , C07D213/73 , C07D237/20 , C07D239/42 , C07D241/20 , C07D253/07 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/113 , C07D277/40 , C07D285/08 , C07D285/12 , C07D285/135 , C07D401/12 , C07D413/12
摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
摘要翻译：本发明涉及（异）芳基环丙胺化合物，特别包括本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症，神经疾病或病症，或病毒感染。因此，在一个具体方面，本发明涉及式（II），（III），（IV），（V），（VI），（VII），（VIII），（IX）。

10. 发明授权

US09061966B2 Cyclopropylamine inhibitors of oxidases 有权
标题翻译：氧化酶环丙胺抑制剂
公开(公告)号：US09061966B2
公开(公告)日：2015-06-23
申请号：US13877919
申请日：2011-10-07
申请人： Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe , Marc Martinell Pedemonte , Alberto Ortega Muñoz , Núrla Valls Vidal
发明人： Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe , Marc Martinell Pedemonte , Alberto Ortega Muñoz , Núrla Valls Vidal
IPC分类号： C07D401/12 , C07D213/74 , A61K31/136 , C07C211/52 , C07C211/53 , C07C211/55 , C07C211/56 , C07C217/92 , C07C237/30 , C07C255/58
CPC分类号： A61K31/4439 , A61K31/136 , A61K31/166 , A61K31/277 , A61K31/4418 , C07C211/52 , C07C211/53 , C07C211/55 , C07C211/56 , C07C217/92 , C07C237/30 , C07C255/58 , C07D213/74 , C07D401/12
摘要： The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
摘要翻译：本发明涉及环丙胺化合物，特别是本文所述和定义的式（I）化合物及其在治疗中的用途，包括例如治疗或预防癌症。

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