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1. 发明申请

US20110144156A1 A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS 审中-公开
标题翻译： A3腺苷受体免疫调节剂
公开(公告)号：US20110144156A1
公开(公告)日：2011-06-16
申请号：US13059836
申请日：2009-08-12
申请人： Adriaan P. Ijzerman , Aniko Goblyos , Johannes Brussee
发明人： Adriaan P. Ijzerman , Aniko Goblyos , Johannes Brussee
IPC分类号： A61K31/4709 , A61K31/47 , C07D215/38 , A61P35/00
CPC分类号： A61K31/4709 , C07D215/38 , C07D215/42 , C07D405/12
摘要： Provided are 2,4-disubstituted quinoline derivatives that are A3 adenosine receptor modulators (A3RM), for use in the treatment of a condition which is treatable by adenosine, an A3 adenosine receptor (A3AR) agonist, or an A3 adenosine receptor antagonist. The 2,4-disubstituted quinoline derivatives can be used in the treatment of a condition treatable by an adenosine or an A3AR agonist, by enhancing activity of a protein (by binding of said 2,4-disubstituted quinoline derivative to the A3AR). Some conditions treatable by the 2,4-disubstituted quinoline derivative when used for enhancing activity include, malignancy, an immuno-compromised affliction, high intraocular pressure, or a condition associated with high intraocular pressure. Further provided is a method for treatment of a subject having a condition treatable by adenosine, an A3AR agonist, or an A3AR antagonist making use of the defined 2,4-disubstituted quinoline derivative (s), and pharmaceutical composition and comprising said derivative and a kit comprising the derivative and instructions for use thereof. One specific 2,4-disubstituted quinoline derivative includes N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarboxamide. The 2,4-disubstituted quinoline derivatives can be formulated in a form suitable for oral administration.
摘要翻译：提供作为可用腺苷，A3腺苷受体（A3AR）激动剂或A3腺苷受体拮抗剂治疗的病症的A3腺苷受体调节剂（A3RM）的2,4-二取代喹啉衍生物。 2,4-二取代喹啉衍生物可用于通过增强蛋白质的活性（通过将所述2,4-二取代喹啉衍生物与A3AR结合）来治疗由腺苷或A3AR激动剂可治疗的病症。当用于增强活性时，2,4-二取代喹啉衍生物可治疗的一些病症包括恶性肿瘤，免疫受损的痛苦，高眼内压或与高眼内压相关的病症。还提供了一种用于治疗具有可由腺苷治疗的病症的受试者的方法，使用所定义的2,4-二取代喹啉衍生物的A3AR激动剂或A3AR拮抗剂，以及包含所述衍生物和包含衍生物的试剂盒和使用说明书。一种特定的2,4-二取代喹啉衍生物包括N- {2 - [（3,4-二氯苯基）氨基]喹啉-4-基}环己烷甲酰胺。 2,4-二取代喹啉衍生物可以配制成适于口服给药的形式。

2. 发明授权

US06284754B1 Pharmaceutical compositions containing 1-oleylazacycloheptan-2-one as enhancing agent of transport across biological membranes 失效
标题翻译：含有1-油基氮杂环庚烷-2-酮的药物组合物作为在生物膜上运输的增强剂
公开(公告)号：US06284754B1
公开(公告)日：2001-09-04
申请号：US08004603
申请日：1993-01-14
申请人： Henri Ernest Boddé , Johanna Aaltje Bouwstra , Maria Helène Ponec , Ferdinand Spies , Klaus Sandrock , Johannes Brussee
发明人： Henri Ernest Boddé , Johanna Aaltje Bouwstra , Maria Helène Ponec , Ferdinand Spies , Klaus Sandrock , Johannes Brussee
IPC分类号： A61K3155
CPC分类号： A61K47/22 , A61K9/0014 , C07D223/10
摘要： The invention relates to pharmaceutical compositions for topical application containing at least one physiologically active agent and an effective amount of 1-oleylazacycloheptan-2-one as the human or animal epithelial membrane permeability enhancer, to the application of such pharmaceutical compositions by means of locally contacting the skin or other membrane of the human or animal with the above composition and to the 1-oleylazacycloheptan-2-one compound per se.
摘要翻译：本发明涉及用于局部应用的药物组合物，其含有至少一种生理活性剂和有效量的1-油基氮杂环庚烷-2-酮作为人或动物上皮膜通透性增强剂，通过局部接触具有上述组成的人或动物的皮肤或其它膜，以及1-油基氮杂环庚烷-2-酮化合物本身。

3. 发明授权

US5329023A Method of preparing optically active alcohols which consist substantially or entirely of one enantiomer 失效
标题翻译：制备基本上或完全由一种对映异构体组成的光学活性醇的方法
公开(公告)号：US5329023A
公开(公告)日：1994-07-12
申请号：US899026
申请日：1992-06-15
申请人： Johannes Brussee , Arne Van Der Gen
发明人： Johannes Brussee , Arne Van Der Gen
IPC分类号： C07C45/00 , C07C45/67 , C07C49/245 , C07C49/255 , C07C215/30 , C07F7/18 , C07C209/48
CPC分类号： C07C255/00 , C07C45/004 , C07C45/673 , C07C49/245 , C07C49/255 , C07F7/1852 , Y02P20/55
摘要： The invention relates to a method of preparing optically active alcohols which consist substantially (at least 75% e.e.) or entirely of one enantiomer of formula 4 ##STR1## wherein R and A are as defined therein. The method comprises, which maintaining enantiomeric excess, converting an optically active cyanohydrin of formula 1 ##STR2## into optically active protected cyanohydrin of formula 2 ##STR3## converting the protected cyanohydrin of formula 2 into an optically active compound of formula 3 ##STR4## removing the protecting group B.
摘要翻译：本发明涉及一种制备光学活性醇的方法，其基本上（至少75％e.e。）或完全由式4（4）的对映异构体组成，其中R和A如其中所定义。该方法包括保持对映异构体过量，将式1的光学活性羟考酮（1）转化成式2的光学活性保护的氰醇（2）将式2的被保护的氰醇转化为（3）除去保护基团B.

4. 发明申请

US20090054476A1 A3 Adenosine receptor allosteric modulators 有权
标题翻译： A3腺苷受体变构调节剂
公开(公告)号：US20090054476A1
公开(公告)日：2009-02-26
申请号：US12219772
申请日：2008-07-28
申请人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
发明人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：本发明涉及A3腺苷受体（A3AR）的变构调节，并提供使用A3腺苷受体调节剂（A3RM），用于制备用于调节受试者中的A3AR的药物组合物，以及包含相同和治疗方法包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据本发明的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。本发明还提供了一些这样的新颖的1H-咪唑并〔4,5-c〕喹啉-4-胺衍生物。

5. 发明申请

US20070032510A1 Substituted pyrimidines as ligands of adenosine receptors 失效
标题翻译：取代的嘧啶作为腺苷受体的配体
公开(公告)号：US20070032510A1
公开(公告)日：2007-02-08
申请号：US10574436
申请日：2004-10-01
申请人： Lisa Chang , Adriaan Ijzerman , Johannes Brussee
发明人： Lisa Chang , Adriaan Ijzerman , Johannes Brussee
IPC分类号： A61K31/506 , A61K31/505 , C07D403/02
CPC分类号： C07D239/42
摘要： The invention provides a compound of formula (I) wherein R and R′ are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R″ and R′″ are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.
摘要翻译：本发明提供式（I）化合物，其中R和R'选自氢，烷基，烯基，炔基或芳基; R“和R”'选自氢，酰基，硫代酰基，硒酰基，烷基，烯基，炔基或芳基; 或其药学上可接受的盐在有益治疗和/或预防由所述受体产生的（dis）顺序的情况下与腺苷受体相互作用。本发明还提供包含所述化合物的药物组合物。本发明还涉及所述组合物用于治疗/或预防各种疾病的用途。

6. 发明授权

US07449470B2 Substituted pyrimidines as ligands of adenosine receptors 失效
标题翻译：取代的嘧啶作为腺苷受体的配体
公开(公告)号：US07449470B2
公开(公告)日：2008-11-11
申请号：US10574436
申请日：2004-10-01
申请人： Lisa Chung Wai Chang , Adriaan P. Ijzerman , Johannes Brussee
发明人： Lisa Chung Wai Chang , Adriaan P. Ijzerman , Johannes Brussee
IPC分类号： C07D239/42 , A61K31/505 , A61P9/00 , A61P11/00 , A61P25/00 , A61P35/00
CPC分类号： C07D239/42
摘要： The invention provides a compound of formula (I) wherein R and R′ are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R″ and R′″ are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.
摘要翻译：本发明提供式（I）化合物，其中R和R'选自氢，烷基，烯基，炔基或芳基; R“和R”'选自氢，酰基，硫代酰基，硒酰基，烷基，烯基，炔基或芳基; 或其药学上可接受的盐在有益治疗和/或预防由所述受体产生的（dis）顺序的情况下与腺苷受体相互作用。本发明还提供包含所述化合物的药物组合物。本发明还涉及所述组合物用于治疗/或预防各种疾病的用途。

7. 发明申请

US20080139608A1 2,6,8, Trisubstituted 1-deazapurines and their different uses 审中-公开
标题翻译： 2,6,8，三取代1-脱氮嘌呤及其不同用途
公开(公告)号：US20080139608A1
公开(公告)日：2008-06-12
申请号：US11634806
申请日：2006-12-06
申请人： Lisa Chung Wai Chang , Johannes Brussee , Adriaan Pieter IJzerman
发明人： Lisa Chung Wai Chang , Johannes Brussee , Adriaan Pieter IJzerman
IPC分类号： A61K31/4375 , C07D471/02
CPC分类号： C07D471/04
摘要： The invention provides a compound having the structure of general formula (I): or a salt thereof, wherein, R represents hydrogen (except when R′=H), halogen, (substituted) alkyl except —CH3, (substituted) alkenyl, (substituted) alkynyl, or (substituted) —(CH2)n-aryl; R′ represents hydrogen (except when R=H), halogen, (substituted) alkyl except —CH3, (substituted) alkenyl, (substituted) alkynyl, or (substituted) —CH2)n-aryl; R″ represents hydrogen, —(CH2)n-hydroxyl, halogen, acyl, thio-acyl, seleno-acyl, (substituted) alkyl, (substituted) alkenyl, (substituted) alkynyl, or (substituted) —(CH2)n-aryl; and n is a number in the range from 0 to 10. The invention further provides pharmaceutical compositions comprising said compound, and the use of said compound to treat and/or prevent a variety of diseases.
摘要翻译：本发明提供具有通式（I）结构的化合物或其盐，其中R表示氢（除R'= H时除外），卤素，除-CH 3之外的（取代的）烷基 >，（取代的）烯基，（取代的）炔基或（取代的） - （CH 2）n - R'表示氢（除了当R = H时除外），卤素，除取代的（取代的）烯基，（取代的）炔基或（取代的）-CH 2 N 2 - 芳基; R“表示氢， - （CH 2）n - 羟基，卤素，酰基，硫代酰基，硒酰基，（取代的）烷基，（取代的），（取代的）炔基或（取代的） - （CH 2）n - 芳基; 并且n是0至10范围内的数字。本发明还提供包含所述化合物的药物组合物和所述化合物用于治疗和/或预防各种疾病的用途。

8. 发明授权

US5189219A Method for the preparation of erythro vicinal amino-alcohols 失效
标题翻译：制备硫代氨基甲醇的方法
公开(公告)号：US5189219A
公开(公告)日：1993-02-23
申请号：US810139
申请日：1991-12-19
申请人： Johannes Brussee , Arne van der Gen , Cornelis G. Kruse
发明人： Johannes Brussee , Arne van der Gen , Cornelis G. Kruse
IPC分类号： C07F7/18 , C07B53/00 , C07C213/00 , C07C213/02 , C07C215/30 , C07C215/52 , C07C215/60
CPC分类号： C07C213/02 , C07C213/00 , C07C215/30 , Y02P20/55
摘要： The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.

9. 发明申请

US20130197025A1 A3 ADENOSINE RECEPTOR ALLOSTERIC MODULATORS 审中-公开
标题翻译： A3腺苷受体免疫调节剂
公开(公告)号：US20130197025A1
公开(公告)日：2013-08-01
申请号：US13800560
申请日：2013-03-13
申请人： Anikó GÖBLYÖS , Johannes BRUSSEE , Adriaan P. IJZERMAN , Zhan-Guo GAO , Kenneth JACOBSON
发明人： Anikó GÖBLYÖS , Johannes BRUSSEE , Adriaan P. IJZERMAN , Zhan-Guo GAO , Kenneth JACOBSON
IPC分类号： A61K31/4745
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：所要求保护的主题涉及A3腺苷受体（A3AR）的变构调节并提供使用A3腺苷受体调节剂（A3RM）用于制备用于调节受试者中的A3AR的药物组合物，以及药物组合物，包括相同和治疗方法，包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据要求保护的主题的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。还提供了1H-咪唑并[4,5-c]喹啉-4-胺衍生物。

10. 发明授权

US08420664B2 A3 adenosine receptor allosteric modulators 有权
标题翻译： A3腺苷受体变构调节剂
公开(公告)号：US08420664B2
公开(公告)日：2013-04-16
申请号：US12219772
申请日：2008-07-28
申请人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
发明人： Aniko Goblyos , Johannes Brussee , Adriaan P. Ijzerman , Zhan-Guo Gao , Kenneth Jacobson
IPC分类号： A61K31/4745 , C07D471/04
CPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
摘要： The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions comprising the same and therapeutic methods comprising administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to the invention are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. The invention also provides some of such novel 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
摘要翻译：本发明涉及A3腺苷受体（A3AR）的变构调节，并提供使用A3腺苷受体调节剂（A3RM），用于制备用于调节受试者中的A3AR的药物组合物，以及包含相同和治疗方法包括向受试者施用一定量的有效调节A3AR活性的量的A3RM。根据本发明的A3RM是1H-咪唑并[4,5-c]喹啉-4-胺衍生物。本发明还提供了一些这样的新颖的1H-咪唑并〔4,5-c〕喹啉-4-胺衍生物。

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