公开(公告)号：US20180246110A1

公开(公告)日：2018-08-30

申请号：US15967406

申请日：2018-04-30

申请人： Xiujuan Hao ,  Isaac Angres

发明人： Xiujuan Hao ,  Isaac Angres

IPC分类号： G01N33/574 ,  C07D519/00 ,  C07D493/04 ,  C07D473/02 ,  C07H19/16 ,  C07K16/44

CPC分类号： G01N33/57484 ,  C07D473/02 ,  C07D493/04 ,  C07D519/00 ,  C07H19/16 ,  C07K16/44 ,  C07K2317/20 ,  C07K2317/33 ,  G01N2800/7033

摘要： The invention provides a method of detecting the presence or absence of a disease in a patient wherein said disease is accompanied by deficient levels of S-adenosylmethionine comprising: identifying a patient that is suspected of having said disease or is at risk of having said disease; obtaining a biological sample from said patient; determining the level of S-adenosylmethionine in said biological sample using an antibody derived from a hapten analog of S-adenosylmethionine; and correlating the level of S-adenosylmethionine in said biological sample with the presence, absence, or severity of said disease. The invention also provides methods for measuring SAH which is used to determine the methylation index (ratio of SAM/SAH) in biological fluids which is indicative of the health status of an individual. Additionally, the invention includes test strips which are useful for determining S-adenosylmethionine and S-adenosylhomocysteine.

公开(公告)号：US09958447B2

公开(公告)日：2018-05-01

申请号：US14457099

申请日：2014-08-11

申请人： Xiujuan Hao ,  Isaac A Angres

发明人： Xiujuan Hao ,  Isaac A Angres

IPC分类号： C07K16/44 ,  G01N33/574 ,  C07H19/16 ,  C07D473/02 ,  C07D493/04 ,  C07D519/00 ,  G01N33/53

CPC分类号： G01N33/57484 ,  C07D473/02 ,  C07D493/04 ,  C07D519/00 ,  C07H19/16 ,  C07K16/44 ,  C07K2317/20 ,  C07K2317/33 ,  G01N2800/7033

摘要： The invention provides a method of detecting the presence or absence of a disease in a patient wherein said disease is accompanied by deficient levels of S-adenosylmethionine comprising: identifying a patient that is suspected of having said disease or is at risk of having said disease; obtaining a biological sample from said patient; determining the level of S-adenosylmethionine in said biological sample using an antibody derived from a hapten analog of S-adenosylmethionine; and correlating the level of S-adenosylmethionine in said biological sample with the presence, absence, or severity of said disease. The invention also provides methods for measuring SAH which is used to determine the methylation index (ratio of SAM/SAH) in biological fluids which is indicative of the health status of an individual. Additionally, the invention includes test strips which are useful for determining S-adenosylmethionine and S-adenosylhomocysteine.

公开(公告)号：US09850214B2

公开(公告)日：2017-12-26

申请号：US14326051

申请日：2014-07-08

申请人： Millennium Pharmaceuticals, Inc.

发明人： Ashley Sue McCarron ,  Todd B. Sells ,  Matthew Stirling ,  Stephen G. Stroud

IPC分类号： A61K31/505 ,  C07D239/02 ,  C07D239/47 ,  C07D239/46 ,  C07D473/02

CPC分类号： C07D239/47 ,  C07D239/46 ,  C07D473/02

摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.

公开(公告)号：US09527869B2

公开(公告)日：2016-12-27

申请号：US14741965

申请日：2015-06-17

申请人： CHIESI FARMACEUTICI S.P.A.

发明人： Matteo Biagetti ,  Alessandro Accetta ,  Anna Maria Capelli ,  Matilde Guala ,  Michele Retini

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D473/02 ,  C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/53 ,  A61K31/52 ,  A61K31/506 ,  A61K31/497 ,  A61P19/02 ,  A61P11/00 ,  A61P11/02

CPC分类号： C07D519/00 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D471/04 ,  C07D473/02 ,  C07D487/04 ,  Y02A50/409

摘要： Compounds of formula (I), defined herein, inhibit phosphoinositide 3-kinases (PI3K) and are useful for the treatment of disorders associated with PI3K enzymes.

摘要翻译： 本文定义的式（I）化合物抑制磷酸肌醇3-激酶（PI3K），可用于治疗与PI3K酶相关的疾病。

公开(公告)号：US08865896B2

公开(公告)日：2014-10-21

申请号：US12863291

申请日：2009-01-16

申请人： Kazuki Hashimoto ,  Wataru Katoda ,  Kazuhiko Takahashi ,  Ayumu Kurimoto

发明人： Kazuki Hashimoto ,  Wataru Katoda ,  Kazuhiko Takahashi ,  Ayumu Kurimoto

IPC分类号： C07D473/02 ,  C07D413/14 ,  C07D473/18

CPC分类号： C07D473/18

摘要： A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.

摘要翻译： 一种腺嘌呤化合物（1）的制造方法，其中m和n分别为2〜5的整数，R1为C1-6烷基，R2和R3相同或不同，氢原子或C1-6烷基 ，或R2和R3与相邻的氮原子结合形成吡咯烷，吗啉，哌啶，哌嗪等，R4为C1-3烷基，其包括使化合物（2）与化合物（3）反应的步骤： ：在含硼还原剂的存在下。

公开(公告)号：US20090149475A1

公开(公告)日：2009-06-11

申请号：US12295306

申请日：2007-04-12

申请人： Anna-Karin Tiden ,  Jenny Viklund

发明人： Anna-Karin Tiden ,  Jenny Viklund

IPC分类号： A61K31/52 ,  C07D473/02 ,  A61P11/00 ,  A61P9/10 ,  A61P25/00

CPC分类号： C07D473/20 ,  C07D473/22

摘要： There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.

摘要翻译： 公开了式（I）的新化合物，其中L，R 1，X和Y如说明书中所定义，及其药学上可接受的盐; 以及其制备方法，含有它们的组合物及其在治疗中的用途。 这些化合物是MPO酶的抑制剂，因此特别可用于治疗或预防神经炎症性疾病，心脑血管动脉粥样硬化性疾病和外周动脉疾病和呼吸系统疾病。

公开(公告)号：US20090082332A1

公开(公告)日：2009-03-26

申请号：US12067536

申请日：2006-09-20

申请人： Philip Abbot ,  Roger Victor Bonnert ,  Stephen Brough ,  Kamaldeep Chohan ,  Thomas McInally ,  Stephen Thom ,  Yoshiaki Isobe ,  Kei Nakamura ,  Shingo Tojo

发明人： Philip Abbot ,  Roger Victor Bonnert ,  Stephen Brough ,  Kamaldeep Chohan ,  Thomas McInally ,  Stephen Thom ,  Yoshiaki Isobe ,  Kei Nakamura ,  Shingo Tojo

IPC分类号： A61K31/397 ,  C07D473/02 ,  A61P31/12 ,  A61P35/00 ,  A61P37/08 ,  A61K31/522

CPC分类号： C07D473/34

摘要： The present invention provides compounds of formula (I) wherein R1, Y1, X1, Z1, X2, Y2, A, Y3, n, R and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

摘要翻译： 本发明提供式（I）化合物，其中R1，Y1，X1，Z1，X2，Y2，A，Y3，n，R和R2如说明书中所定义，其制备方法，含有它们的药物组合物及其制备方法 用于治疗。

公开(公告)号：US20080293705A1

公开(公告)日：2008-11-27

申请号：US12186857

申请日：2008-08-06

申请人： Constance Neely Wilson ,  John J. Partridge

发明人： Constance Neely Wilson ,  John J. Partridge

IPC分类号： A61K31/541 ,  C07D473/02 ,  A61K31/5377 ,  A61K31/522

CPC分类号： C07D473/04

摘要： Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

摘要翻译： 描述通式（I）的化合物：其中A是5-或6-元芳族或杂芳族环。 还描述了包含这些化合物的组合物及其使用方法。

公开(公告)号：US20080058354A1

公开(公告)日：2008-03-06

申请号：US11852638

申请日：2007-09-10

申请人： Samuel Chackalamannil ,  Yuguang Wang ,  Craig Boyle ,  Andrew Stamford

发明人： Samuel Chackalamannil ,  Yuguang Wang ,  Craig Boyle ,  Andrew Stamford

IPC分类号： C07D473/02 ,  A61K31/522 ,  A61P11/00 ,  A61P15/00 ,  A61P35/00 ,  A61P9/00

CPC分类号： C07D473/04 ,  C07D473/06 ,  C07D473/08

摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:

摘要翻译： 具有式（I）的黄嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其特别用于治疗男性（勃起）和女性性功能障碍等生理障碍：例如，本发明的代表性化合物是：

公开(公告)号：US20070197564A1

公开(公告)日：2007-08-23

申请号：US11653511

申请日：2007-01-16

申请人： Brian Lavey ,  Joseph Kozlowski ,  Guowei Zhou ,  Ling Tong ,  Wensheng Yu ,  Michael Wong ,  Bandarpalle Shankar ,  Neng-Yang Shih ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Razia Rizvi ,  Lei Chen ,  De-Yi Yang ,  Robert Feltz ,  Seong-Heon Kim

发明人： Brian Lavey ,  Joseph Kozlowski ,  Guowei Zhou ,  Ling Tong ,  Wensheng Yu ,  Michael Wong ,  Bandarpalle Shankar ,  Neng-Yang Shih ,  M. Siddiqui ,  Kristin Rosner ,  Chaoyang Dai ,  Janeta Popovici-Muller ,  Vinay Girijavallabhan ,  Dansu Li ,  Razia Rizvi ,  Lei Chen ,  De-Yi Yang ,  Robert Feltz ,  Seong-Heon Kim

IPC分类号： A61K31/52 ,  C07D471/02 ,  A61K31/4745 ,  A61K31/513 ,  A61K31/519 ,  C07D473/02 ,  C07D487/02

CPC分类号： C07D403/14 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00

摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，聚集蛋白聚糖蛋白酶，TNF-α或其组合介导的疾病或病症 。