公开(公告)号：US20100048625A1

公开(公告)日：2010-02-25

申请号：US12522030

申请日：2008-01-04

Applicant: Matthew Colin Thor Fyfe ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Simon Andrew Swain

Inventor： Matthew Colin Thor Fyfe ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Simon Andrew Swain

IPC: A61K31/4545 ,  C07D413/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D413/14

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

公开(公告)号：US20090325924A1

公开(公告)日：2009-12-31

申请号：US11922765

申请日：2006-06-29

Applicant: Stuart Edward ,  Graham John Dawson ,  Matthew Colin Thor Fyfe Oxford ,  Lisa Sarah Bertram ,  William Gattrell ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Neela Sumit Mistry ,  Martin James Procter ,  Chrystelle Marie Rasamison ,  Philip John Rushworth ,  Colin Peter Sambrook-Smith ,  David French Stonehouse

Inventor： Stuart Edward ,  Graham John Dawson ,  Matthew Colin Thor Fyfe Oxford ,  Lisa Sarah Bertram ,  William Gattrell ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Neela Sumit Mistry ,  Martin James Procter ,  Chrystelle Marie Rasamison ,  Philip John Rushworth ,  Colin Peter Sambrook-Smith ,  David French Stonehouse

IPC: A61K31/4245 ,  C07D413/14 ,  C07D413/12 ,  C07D271/06 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/506 ,  A61P3/00

CPC classification number: C07D271/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

Abstract translation: 式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗肥胖症和糖尿病。

公开(公告)号：US20080261952A1

公开(公告)日：2008-10-23

申请号：US11660405

申请日：2005-08-16

Applicant: Jason Bloxham ,  Matthew Colin Thor Fyfe ,  James Horswill ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Martin James Procter ,  Karen Lesley Schofield ,  Salam Shaaban ,  Andrew Simon Swain ,  Phillppe Wong-Kai-In

Inventor： Jason Bloxham ,  Matthew Colin Thor Fyfe ,  James Horswill ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Martin James Procter ,  Karen Lesley Schofield ,  Salam Shaaban ,  Andrew Simon Swain ,  Phillppe Wong-Kai-In

IPC: A61K31/167 ,  A61P1/00

CPC classification number: A61K31/381 ,  A61K31/341 ,  A61K31/404 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/455

Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract translation: 通过向需要这种治疗的受试者施用有效量的芳基脲CB-1受体调节化合物来治疗与CB-1受体相关的病症，特别是肥胖症的方法。

公开(公告)号：US07115745B2

公开(公告)日：2006-10-03

申请号：US10775405

申请日：2004-02-10

Applicant: Daniel Y. Du ,  Martin James Procter ,  Matthew Colin Thor Fyfe ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams ,  Karen Lesley Schofield

Inventor： Daniel Y. Du ,  Martin James Procter ,  Matthew Colin Thor Fyfe ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams ,  Karen Lesley Schofield

IPC: C07D435/02 ,  A01N43/90

CPC classification number: C07D215/227 ,  C07D311/08 ,  C07D311/14 ,  C07D405/12

Abstract: The present invention is directed to a new class of 6-benzyl urea/thiourea-quinolin-2-one derivatives and 2-oxo-6-benzylurea/thiourea-chromene derivatives. These compound are androgen antagonists and are useful in the treatment of alopecia, acne and other conditions associated with inappropriate activation of the androgen receptor.

Abstract translation: 本发明涉及一类新的6-苄基脲/硫脲 - 喹啉-2-酮衍生物和2-氧代-6-苄基脲/硫脲 - 色烯衍生物。 这些化合物是雄激素拮抗剂，可用于治疗脱发，痤疮和与雄激素受体不适当激活相关的其他病症。

公开(公告)号：US07098340B2

公开(公告)日：2006-08-29

申请号：US10824456

申请日：2004-04-14

Applicant: Daniel Y. Du ,  Martin James Procter ,  Matthew Colin Thor Fyfe ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams ,  Karen Lesley Schofield

Inventor： Daniel Y. Du ,  Martin James Procter ,  Matthew Colin Thor Fyfe ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams ,  Karen Lesley Schofield

IPC: C07D215/16

CPC classification number: C07D405/12 ,  C07D215/227 ,  C07D311/18 ,  C07D401/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention is directed to a new class of 6-benzylsulfonamido-quinoline/chromene derivatives, to their use as androgen antagonists, and to formulations containing these androgen antagonists.

Abstract translation: 本发明涉及一类新的6-苄基磺酰氨基 - 喹啉/色烯衍生物，其用作雄激素拮抗剂，以及含有这些雄激素拮抗剂的制剂。

公开(公告)号：US07057048B2

公开(公告)日：2006-06-06

申请号：US10758581

申请日：2004-01-15

Applicant: Daniel Y. Du ,  Matthew Colin Thor Fyfe ,  Martin James Procter ,  Karen Lesley Schofield ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams

Inventor： Daniel Y. Du ,  Matthew Colin Thor Fyfe ,  Martin James Procter ,  Karen Lesley Schofield ,  Vilasben Kanji Shah ,  Geoffrey Martyn Williams

IPC: C07D215/16 ,  C07D311/02

CPC classification number: C07D215/227 ,  C07D311/54 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention is directed to a new class of 6-sulfonamido-quinolin-2-one and 6-sulfonamido-2-oxo-chromene derivatives to their use as androgen antagonists, and to relieve conditions associated with inappropriate activation of the androgen receptor.

公开(公告)号：US09186337B2

公开(公告)日：2015-11-17

申请号：US13580710

申请日：2011-02-24

Applicant: Jonathan Alleman Baker ,  Matthew Colin Thor Fyfe

Inventor： Jonathan Alleman Baker ,  Matthew Colin Thor Fyfe

IPC: A61K31/131 ,  A61K31/135 ,  A61K31/165 ,  A61K31/15 ,  A61K38/21 ,  A61K45/06 ,  A61K31/137

CPC classification number: A61K31/135 ,  A61K31/131 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.

Abstract translation: 本发明提供治疗或预防肝炎病毒科感染和由肝炎病毒科感染引起的疾病。 特别地，本发明提供影响Hepadnaviridae利用宿主细胞机制作为病毒生命周期的一部分的能力的组合物和方法。 本发明涉及干扰病毒利用宿主细胞机制与LSD1抑制剂的正常能力的发现降低HBV复制。 因此，根据本发明的肝炎病毒科感染和肝炎病毒科引起的疾病的治疗和预防包括向需要治疗的个体施用治疗有效量的LSD1抑制剂。 需要治疗的个体可以是人或例如另一种哺乳动物。

公开(公告)号：US09006449B2

公开(公告)日：2015-04-14

申请号：US13812386

申请日：2011-07-27

Applicant: Matthew Colin Thor Fyfe ,  Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Marc Martinell Pedemonte ,  Maria de los Ángeles Estiarte-Martinez ,  Nuria Valls Vidal

Inventor： Matthew Colin Thor Fyfe ,  Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Marc Martinell Pedemonte ,  Maria de los Ángeles Estiarte-Martinez ,  Nuria Valls Vidal

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08859555B2

公开(公告)日：2014-10-14

申请号：US13497994

申请日：2010-04-19

Applicant: Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

Inventor： Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

IPC: 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 classification number: 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

Abstract: 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.

公开(公告)号：US20130289076A1

公开(公告)日：2013-10-31

申请号：US13877919

申请日：2011-10-07

Applicant: Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe ,  Marc Murtinell Pedemonte ,  Alberto Ortega Muñoz ,  Núrla Valls Vidal

Inventor： Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe ,  Marc Murtinell Pedemonte ,  Alberto Ortega Muñoz ,  Núrla Valls Vidal

IPC: C07D401/12 ,  C07C237/30 ,  C07C217/92 ,  C07C255/58 ,  C07D213/74 ,  C07C211/52

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。