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1. 发明申请

US20070155726A1 Diamine derivatives as inhibitors of leukotriene A4 hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US20070155726A1
公开(公告)日：2007-07-05
申请号：US11644244
申请日：2006-12-22
申请人： 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
发明人： 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分类号： A61K31/551 , A61K31/495 , A61K31/46 , A61K31/445 , A61K31/407
CPC分类号： 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
摘要： 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.
摘要翻译：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。

2. 发明授权

US07737145B2 Diamine derivatives as inhibitors of leukotriene A4 hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US07737145B2
公开(公告)日：2010-06-15
申请号：US11644244
申请日：2006-12-22
申请人： 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
发明人： 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分类号： A01N43/60 , A61K31/495 , C07D241/36 , C07D271/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D498/00 , C07D513/00
CPC分类号： 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
摘要： 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.
摘要翻译：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。

3. 发明申请

US20100210630A1 Diamine Derivatives as Inhibitors of Leukotriene A4 Hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US20100210630A1
公开(公告)日：2010-08-19
申请号：US12771659
申请日：2010-04-30
申请人： 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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

4. 发明申请

US20070155727A1 Amide inhibitors of leukotriene A4 hydrolase 审中-公开
标题翻译：白三烯A4水解酶的酰胺抑制剂
公开(公告)号：US20070155727A1
公开(公告)日：2007-07-05
申请号：US11644822
申请日：2006-12-22
申请人： 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
发明人： 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分类号： A61K31/551 , A61K31/407 , C07D487/02 , C07D243/08
CPC分类号： 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
摘要： 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.
摘要翻译：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。

5. 发明授权

US08569303B2 Diamine derivatives as inhibitors of leukotriene A4 hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US08569303B2
公开(公告)日：2013-10-29
申请号：US12771659
申请日：2010-04-30
申请人： 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
发明人： 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分类号： A61K31/495 , C07D241/36
CPC分类号： 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
摘要： 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.
摘要翻译：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。

6. 发明申请

US20100086943A1 METHOD FOR THE DETECTION OF POST-TRANSLATIONAL MODIFICATIONS 有权
标题翻译：检测翻译后修改的方法
公开(公告)号：US20100086943A1
公开(公告)日：2010-04-08
申请号：US12516333
申请日：2007-11-27
申请人： Eric Trinquet , Achim Brinker , Emmanuel Claret , Gérard Mathis
发明人： Eric Trinquet , Achim Brinker , Emmanuel Claret , Gérard Mathis
IPC分类号： G01N33/53 , C12N5/00 , C12N5/071
CPC分类号： G01N33/542 , C12Q1/37 , C12Q1/48 , C12Q1/485
摘要： Method for the detection in homogeneous medium of a post-translational modification of a protein substrate catalyzed by a cell enzyme, characterized in that the post-translational modification reaction takes place in intact living cells, in that these cells comprise a heterologous expression vector coding for a fusion protein comprising the protein substrate and a first coupling domain and in that it comprises the following stages: (v) Incubation of the cells in the presence or in the absence of a compound to be tested capable of modulating the activity of said enzyme, (vi) Addition to the reaction medium of a first fluorescent compound member of a first pair of FRET partners covalently bonded to a coupling agent capable of binding specifically to the first coupling domain present on the protein substrate, (vii) Addition to the reaction medium of a second fluorescent compound member of this first pair of FRET partners, and covalently bonded to a binding domain specific to the site of the protein substrate having undergone the post-translational modification and not binding to the non-modified protein substrate, (i) Measurement of the FRET signal emitted by the sample, this signal being representative of the quantity of protein substrate having undergone said post-translational modification; and cells for the implementation of said method.
摘要翻译：用于在均匀培养基中检测由细胞酶催化的蛋白质底物的翻译后修饰的方法，其特征在于翻译后修饰反应在完整的活细胞中进行，因为这些细胞包含编码包含蛋白质底物和第一偶联结构域的融合蛋白，并且其包含以下阶段：（v）在待测化合物存在或不存在下能够调节所述酶的活性的细胞的孵育，（vi）向第一对FRET配偶体的第一荧光化合物成员的反应介质中加入共价结合到能够特异性结合蛋白质底物上存在的第一偶联结构域的偶联剂，（vii）加入到反应介质中的第一对FRET配偶体的第二荧光化合物成员，并且共价键合到特异于t位点的结合结构域已经经历了翻译后修饰并且不结合未修饰的蛋白质底物的蛋白质底物，（i）测量由样品发射的FRET信号，该信号代表已经经历所述翻译后蛋白质底物的量修改; 以及用于执行所述方法的单元。

7. 发明申请

US20120009593A1 ANALYSIS METHOD FOR THE IN VITRO DIAGNOSIS OF BENIGN PROSTATIC HYPERPLASIA (BPH) IN DOGS BY ASSAYING CANINE PROSTATE SPECIFIC ESTERASE, AND BPH TREATMENT FOLLOW UP 审中-公开
标题翻译：通过测定犬类前景特异性蛋白酶和BPH治疗进行血液中胆固醇血症（BPH）的血液分析方法的分析方法
公开(公告)号：US20120009593A1
公开(公告)日：2012-01-12
申请号：US13202930
申请日：2010-02-23
申请人： Emmanuel Claret , Stephane Audhuy , Jerome Morlet , Gerard Papierok
发明人： Emmanuel Claret , Stephane Audhuy , Jerome Morlet , Gerard Papierok
IPC分类号： G01N33/573 , C12N9/96 , C07K16/40 , G01N33/577
CPC分类号： G01N33/573 , C12N9/6445 , G01N33/6893 , G01N2333/916 , G01N2800/342
摘要： The invention relates to an analysis method for the in vitro diagnosis of benign prostatic hyperplasia (BPH) in a dog, using the CPSE contained in biological fluid samples collected from the dog as well as biological molecules specifically binding CPSE. The invention is characterised in that it includes the following steps: a. collecting a biological fluid sample from a dog; b. measuring the canine prostate specific esterase (CPSE) of said sample; c. comparing said measured CPSE concentration with a reference value, said value being from around 34 ng/ml to around 102.4 ng/ml for serum or plasma, preferably around 61 ng/ml; d. using the CPSE concentration as a BPH marker; and e. diagnosing BPH in a dog when measured CPSE concentrations in said sample exceed said reference value.
摘要翻译：本发明涉及使用狗收集的生物流体样品中包含的CPSE以及特异性结合CPSE的生物分子来体内诊断狗良性前列腺增生（BPH）的分析方法。本发明的特征在于其包括以下步骤：a。从狗收集生物流体样品; b。测量所述样品的犬前列腺特异性酯酶（CPSE）; C。将所述测量的CPSE浓度与参考值进行比较，对于血清或血浆，所述值为约34ng / ml至约102.4ng / ml，优选为约61ng / ml; d。使用CPSE浓度作为BPH标记; 和e。当所述样品中测量的CPSE浓度超过所述参考值时，诊断狗中的BPH。

8. 发明授权

US08663928B2 Method for the detection of post-translational modifications 有权
标题翻译：检测翻译后修饰的方法
公开(公告)号：US08663928B2
公开(公告)日：2014-03-04
申请号：US12516333
申请日：2007-11-27
申请人： Eric Trinquet , Achim Brinker , Emmanuel Claret , Gérard Mathis
发明人： Eric Trinquet , Achim Brinker , Emmanuel Claret , Gérard Mathis
IPC分类号： G01N33/68 , G01N33/53 , G01N33/58
CPC分类号： G01N33/542 , C12Q1/37 , C12Q1/48 , C12Q1/485
摘要： Method for the detection in homogeneous medium of a post-translational modification of a proteinaceous substrate catalyzed by a cell enzyme, characterized in that the post-translational modification reaction takes place in intact living cells, in that these cells comprise a heterologous expression vector coding for a fusion protein comprising the proteinaceous substrate and a first coupling domain and in that it comprises the following stages: (i) Incubation of the cells in the presence or in the absence of a compound to be tested capable of modulating the activity of said enzyme, (ii) Addition to the reaction medium of a first fluorescent compound member of a first pair of FRET partners covalently bonded to a coupling agent capable of binding specifically to the first coupling domain present on the proteinaceous substrate, (iii) Addition to the reaction medium of a second fluorescent compound member of this first pair of FRET partners, and covalently bonded to a binding domain specific to the site of the proteinaceous substrate having undergone the post-translational modification and not binding to the non-modified proteinaceous substrate, (i) Measurement of the FRET signal emitted by the sample, this signal being representative of the quantity of proteinaceous substrate having undergone said post-translational modification; and cells for the implementation of said method.
摘要翻译：在均质培养基中检测由细胞酶催化的蛋白质底物的翻译后修饰的方法，其特征在于翻译后修饰反应在完整的活细胞中进行，因为这些细胞包含编码包含蛋白质底物和第一偶联结构域的融合蛋白，并且其包含以下阶段：（i）在待测化合物存在或不存在下能够调节所述酶的活性的细胞的孵育，（ii）向第一对FRET伴侣的第一荧光化合物成员的反应介质中加入共价键合到能够特异性结合存在于蛋白质底物上的第一偶联结构域的偶联剂，（iii）加入反应介质的第一对FRET配偶体的第二荧光化合物成员，并共价键合到结合域 c到经过翻译后修饰并且不结合未修饰的蛋白质底物的蛋白质底物的位点，（i）测量由样品发射的FRET信号，该信号代表具有经过翻译后修改; 以及用于执行所述方法的单元。

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