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公开(公告)号：US08632992B2
公开(公告)日：2014-01-21
申请号：US13228791
申请日：2011-09-09
Applicant: Thomas Kirkland , Andrew L. Niles , Carolyn Woodroofe Hitko
Inventor： Thomas Kirkland , Andrew L. Niles , Carolyn Woodroofe Hitko
CPC classification number: C12Q1/34 , C07D417/04 , C07K5/0806 , C07K5/1019 , C07K7/06 , C12Q1/48
Abstract: The present invention provides compounds and methods for assaying activities of enzymes such as histone deacetylases and histone acetyltransferases. In some embodiments, the methods may be performed in one step. The compounds described herein features peptide-based compounds having at least one blocked lysine or arginine residue which are coupled to reporter moieties. The methods described herein involve reacting a compound described herein with an enzyme, such as a histone deacetylase enzyme or a histone acetyltransferase enzyme, and an endopeptidase that recognizes basic amino acids to release the reporter moiety which may be subsequently detected.
Abstract translation: 本发明提供了用于测定酶如组蛋白脱乙酰酶和组蛋白乙酰转移酶的活性的化合物和方法。 在一些实施例中，可以在一个步骤中执行该方法。 本文所述的化合物特征在于具有至少一个被封闭的赖氨酸或精氨酸残基的基于肽的化合物，其与报道部分偶联。 本文描述的方法包括使本文所述的化合物与酶，例如组蛋白脱乙酰酶或组蛋白乙酰转移酶，以及识别碱性氨基酸释放可能随后检测到的报道分子的内肽酶。
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公开(公告)号：US07737145B2
公开(公告)日：2010-06-15
申请号：US11644244
申请日：2006-12-22
Applicant: Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
Inventor： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC: A01N43/60 , A61K31/495 , C07D241/36 , C07D271/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D498/00 , C07D513/00
CPC classification number: C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract translation: 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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公开(公告)号：US20070155727A1
公开(公告)日：2007-07-05
申请号：US11644822
申请日：2006-12-22
Applicant: Ming Chen , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye , Hong Ye
Inventor： Ming Chen , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye , Hong Ye
IPC: A61K31/551 , A61K31/407 , C07D487/02 , C07D243/08
CPC classification number: C07D207/04 , C07C237/04 , C07C237/06 , C07C237/30 , C07C255/58 , C07C275/40 , C07C275/42 , C07C275/62 , C07C311/05 , C07C311/08 , C07C311/09 , C07C311/37 , C07C2601/08 , C07C2601/14 , C07D211/06 , C07D243/08 , C07D295/04 , C07D295/16 , C07D487/02 , C07D487/08
Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4a, R4b, R4c, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, R9 and R10 are described herein, or pharmaceutically acceptable salts, solvates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and which are therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of using and preparing the compounds of the invention are also disclosed.
Abstract translation: 本发明涉及式（I）化合物：其中r，q，R，R 2，R 3，R 4a，R 4， R 4b，R 4c，R 5a，R 5b，R 5c，R 5，R 5， R 6b，R 6b，R 6，R 7，R 8，R 8，R 8， 本文描述了本发明的其它药学上可接受的盐，溶剂合物，多晶型物，铵离子，N-氧化物或前体药物; 其是白三烯A 4水解酶抑制剂，因此其可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和使用和制备本发明化合物的方法。
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公开(公告)号：US20070155726A1
公开(公告)日：2007-07-05
申请号：US11644244
申请日：2006-12-22
Applicant: Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye
Inventor： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye
IPC: A61K31/551 , A61K31/495 , A61K31/46 , A61K31/445 , A61K31/407
CPC classification number: C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract translation: 本发明涉及式（I）化合物：其中r，q，R，R 2，R 3，R 4，R R 5，R 5b，R 5c，R 6a，R 6b，R 6b，R 6b，R 6b，R 6b， 本文描述了作为单一立体异构体或作为其中R 1，R 2，R 8和R 9的混合物 立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药; 其是白三烯A 4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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Patent Agency Ranking
公开(公告)号：US08569303B2
公开(公告)日：2013-10-29
申请号：US12771659
申请日：2010-04-30
Applicant: Damian O Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
Inventor： Damian O Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC: A61K31/495 , C07D241/36
CPC classification number: C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract translation: 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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公开(公告)号：US20120064554A1
公开(公告)日：2012-03-15
申请号：US13228791
申请日：2011-09-09
Applicant: Thomas Kirkland , Andrew L. Niles , Martha O'Brien , Carolyn Woodroofe Hitko
Inventor： Thomas Kirkland , Andrew L. Niles , Martha O'Brien , Carolyn Woodroofe Hitko
CPC classification number: C12Q1/34 , C07D417/04 , C07K5/0806 , C07K5/1019 , C07K7/06 , C12Q1/48
Abstract: The present invention provides compounds and methods for assaying activities of enzymes such as histone deacetylases and histone acetyltransferases. In some embodiments, the methods may be performed in one step. The compounds described herein features peptide-based compounds having at least one blocked lysine or arginine residue which are coupled to reporter moieties. The methods described herein involve reacting a compound described herein with an enzyme, such as a histone deacetylase enzyme or a histone acetyltransferase enzyme, and an endopeptidase that recognizes basic amino acids to release the reporter moiety which may be subsequently detected.
Abstract translation: 本发明提供了用于测定酶如组蛋白脱乙酰酶和组蛋白乙酰转移酶的活性的化合物和方法。 在一些实施例中，可以在一个步骤中执行该方法。 本文所述的化合物特征在于具有至少一个被封闭的赖氨酸或精氨酸残基的基于肽的化合物，其与报道部分偶联。 本文描述的方法包括使本文所述的化合物与酶，例如组蛋白脱乙酰酶或组蛋白乙酰转移酶，以及识别碱性氨基酸释放可能随后检测到的报道分子的内肽酶。
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公开(公告)号：US20050121137A1
公开(公告)日：2005-06-09
申请号：US11003872
申请日：2004-12-03
Applicant: Thomas Kirkland
Inventor： Thomas Kirkland
IPC: B29C20060101 , B29C65/00 , B29C65/16 , B32B31/00 , B32B31/24
CPC classification number: B29C66/51 , B29C65/1606 , B29C65/1612 , B29C65/1616 , B29C65/1635 , B29C65/1658 , B29C65/1667 , B29C65/1674 , B29C65/1687 , B29C66/12463 , B29C66/1248 , B29C66/1312 , B29C66/322 , B29C66/5346 , B29C66/54 , B29C66/542 , B29C66/73921 , B29C66/83221 , B29K2101/12 , B29K2995/0022 , B29K2995/0039 , B29K2995/004
Abstract: A welding system includes a pair of thermoplastic components forming a weld interface extending at an acute angle to the direction of application of a clamping force. A clamping mechanism applies a clamping force to the two components to urge the components together at said weld interface, and laser light is directed onto the weld interface to weld the two components together.
Abstract translation: 焊接系统包括一对热塑性部件，该热塑性部件形成以与夹紧力的施加方向成锐角延伸的焊接界面。 夹紧机构对两个部件施加夹紧力，以在所述焊接界面处将部件推动到一起，并将激光引导到焊接界面上以将两个部件焊接在一起。
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公开(公告)号：US20090099147A1
公开(公告)日：2009-04-16
申请号：US12170035
申请日：2008-07-09
Applicant: Wolfgnag SCHWEDE , Carsten Moeller , Anja Schmidt , Ulrike Fuhrmann , Andrea Rotgeri , Thomas Kirkland
Inventor： Wolfgnag SCHWEDE , Carsten Moeller , Anja Schmidt , Ulrike Fuhrmann , Andrea Rotgeri , Thomas Kirkland
IPC: A61K31/565 , C07C233/15 , A61K31/167 , C07D333/54 , A61P15/00 , A61K31/381 , C07D241/04
CPC classification number: C07D333/54 , C07C235/38 , C07C255/60 , C07D211/34 , C07D213/54 , C07D215/42 , C07D233/64
Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions which comprise these compounds.The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.
Abstract translation: 本发明涉及使用孕酮受体调节剂制备药物的通式I的非甾体孕激素受体调节剂和包含这些化合物的药物组合物。 根据本发明的化合物适用于治疗和预防妇科疾病如子宫内膜异位症，子宫平滑肌瘤，功能障碍性出血和痛经，以及用于治疗和预防激素依赖性肿瘤和用于女性生育控制和 激素替代疗法。
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公开(公告)号：US20100210630A1
公开(公告)日：2010-08-19
申请号：US12771659
申请日：2010-04-30
Applicant: Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
Inventor： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC: A61K31/551 , C07D487/08 , A61K31/504 , C07D243/08 , C07D263/32 , A61K31/421 , C07D211/58 , A61K31/4468 , C07D207/09 , A61K31/40 , C07D413/00 , A61K31/5377 , A61P29/00
CPC classification number: C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract translation: 本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体 或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。 还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。
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