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公开(公告)号：US07893094B2
公开(公告)日：2011-02-22
申请号：US10560590
申请日：2004-06-28
IPC分类号： A61K31/4425 , C07D213/20 , C07D213/30
CPC分类号： C07D213/20 , C07D213/30 , C07D213/80 , C07D231/12 , C07D233/60 , C07D295/088 , C07D401/12 , C07D409/12
摘要： The present invention is directed to the amphiphilic pyridinium compounds, such as for suppressing IL-8 secretion and production. The present invention further provides methods of making and using such compounds for the treatment of the IL-8 related diseases, such as cystic fibrosis.
摘要翻译： 本发明涉及两性吡啶鎓化合物，例如用于抑制IL-8分泌和产生。 本发明还提供制备和使用这些化合物治疗IL-8相关疾病如囊性纤维化的方法。
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公开(公告)号：US4587046A
公开(公告)日：1986-05-06
申请号：US379463
申请日：1982-05-18
申请人： Murray Goodman , Neal Castagnoli , Kenneth Jacobson , Kenneth L. Melmon , Roberto P. Rosenkranz , Michael S. Verlander
发明人： Murray Goodman , Neal Castagnoli , Kenneth Jacobson , Kenneth L. Melmon , Roberto P. Rosenkranz , Michael S. Verlander
IPC分类号： A61K31/135 , A61K31/19 , A61K38/00 , A61K47/48 , A61P9/04 , A61P25/02 , C07K1/113 , C07K5/065 , C07K5/093 , C07K14/00 , C07K16/00 , C07K17/02 , C12Q1/04 , C07C101/72
CPC分类号： C07K5/0819 , A61K47/48238 , C07K5/06078 , Y10S930/28 , Y10S930/29
摘要： Biologically active drugs, e.g. catecholamine hormones, are coupled to carrier molecules, e.g. monodisperse peptides to produce conjugate molecules. The conjugate molecules retain biological activity, but the pharmacokinetic, pharmacodynamic and/or potency properties of the drug is modified. The drug is coupled to the carrier via a spacer moiety which not only serves to covalently link the drug to the carrier, but also insulates the biologically active portion of the drug, i.e., the pharmacophore, from degradation during the coupling process. The carrier preferably consists of a monodisperse peptide in which the sequence of amino acid residues is carefully preselected and controlled.
摘要翻译： 生物活性药物，例如 儿茶酚胺激素与载体分子偶联。 单分散肽产生共轭分子。 缀合物分子保留生物活性，但药物的药代动力学，药效学和/或效力性质被改变。 药物通过间隔物部分偶联到载体上，其不仅用于将药物共价连接到载体，而且使药物的生物活性部分（即药效基团）在结合过程中不发生降解。 载体优选由单分散肽组成，其中仔细预选和控制氨基酸残基的序列。
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公开(公告)号：US08420664B2
公开(公告)日：2013-04-16
申请号：US12219772
申请日：2008-07-28
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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公开(公告)号：US20070232626A1
公开(公告)日：2007-10-04
申请号：US11574779
申请日：2005-09-02
IPC分类号： A61K31/52 , C07D473/26
CPC分类号： C07D473/00
摘要： Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.
摘要翻译： 公开了具有下式的（N） - 甲烷卡巴腺嘌呤核苷：作为高效A 3 N 3腺苷受体激动剂，包含这种核苷的药物组合物，以及这些核苷的使用方法，其中R < SUB> 1 6 如说明书中所定义。 这些核苷被考虑用于治疗许多疾病，例如炎症，心脏缺血，中风，哮喘，糖尿病和心律失常。 本发明还提供了用于心脏保护的作为Aβ1 N和A 3 N 3腺苷受体的激动剂的化合物。
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公开(公告)号：US20090054476A1
公开(公告)日：2009-02-26
申请号：US12219772
申请日：2008-07-28
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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公开(公告)号：US20050256143A1
公开(公告)日：2005-11-17
申请号：US10530552
申请日：2003-10-24
申请人： Lak Jeong , Kenneth Jacobson , Hyung Moon , Hea Kim
发明人： Lak Jeong , Kenneth Jacobson , Hyung Moon , Hea Kim
IPC分类号： A61K31/52 , A61K31/7076 , A61P29/00 , A61P35/00 , C07D473/00 , C07D473/14 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167
CPC分类号： C07H5/10 , C07D473/00 , C07D473/32 , C07D473/34 , C07H19/16 , C07H19/167
摘要： Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3′ are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R3 and R3′ do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.
摘要翻译： 公开了对Aβ3 +腺苷受体有选择性的嘌呤核苷化合物，可用于治疗癌症和炎性疾病。 所述化合物由以下通式（I）表示，包括其异构体：其中X为硫或氧; R 1是氢，烷基，苄基，卤代苄基或苯基烷基; R 2是氢，卤素，烷氧基，烯基，炔基，烷硫基或硫代; R 3和R 3'是氢，羟基烷基，烷氧基羰基或烷基氨基羰基，而R 3和R 3' “同时没有相同的取代基; 并且R 4是氢或烷基。 还公开了包含式（I）化合物，异构体或其药理学上可接受的盐作为活性成分的药物组合物和预防或治疗各种疾病，状态或病症的方法，包括哮喘，炎症，脑缺血， 心脏病和癌症。
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公开(公告)号：US20050173954A1
公开(公告)日：2005-08-11
申请号：US10773094
申请日：2004-02-05
申请人： Patrick Weber , Kenneth Jacobson
发明人： Patrick Weber , Kenneth Jacobson
摘要： A musician's chair that enhances the musician's posture when performing vocal or wind instruments. The music posture chair includes a seat and back that are mounted on a frame with respect to a floor to not only enhance diaphragmatic breathing of the musician but also to enhance the comfort of the musician.
摘要翻译： 一位音乐家的椅子，可以在演奏声乐或乐器时增强音乐家的姿势。 音乐姿势椅子包括相对于地板安装在框架上的座椅和背部，不仅增强了音乐家的膈肌呼吸，而且还增强了音乐家的舒适度。
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公开(公告)号：US09326978B2
公开(公告)日：2016-05-03
申请号：US13800560
申请日：2013-03-13
IPC分类号： A61K31/4745 , A61K31/00 , C07D471/04
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。
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公开(公告)号：US20070105916A1
公开(公告)日：2007-05-10
申请号：US10560590
申请日：2004-06-28
申请人： Harvey Pollard , Kenneth Jacobson
发明人： Harvey Pollard , Kenneth Jacobson
IPC分类号： C07D213/55 , A61K31/44
CPC分类号： C07D213/20 , C07D213/30 , C07D213/80 , C07D231/12 , C07D233/60 , C07D295/088 , C07D401/12 , C07D409/12
摘要： The present invention is directed to the amphiphilic pyridinium compounds, such as for suppressing IL-8 secretion and production. The present invention further provides methods of making and using such compounds for the treatment of the IL-8 related diseases, such as cystic fibrosis.
摘要翻译： 本发明涉及两性吡啶鎓化合物，例如用于抑制IL-8分泌和产生。 本发明还提供制备和使用这些化合物治疗IL-8相关疾病如囊性纤维化的方法。
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公开(公告)号：US20060270629A1
公开(公告)日：2006-11-30
申请号：US11500860
申请日：2006-08-08
申请人： Kenneth Jacobson , Victor Marquez
发明人： Kenneth Jacobson , Victor Marquez
IPC分类号： A61K31/69 , A61K31/675 , C07F5/04 , A61K31/52 , A61K31/522 , C07F9/6512 , C07D473/10 , C07D473/02
CPC分类号： C07D473/34
摘要： The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil and M is a constrained cycloalkyl group. The adenine or uracil is bonded to the constrained cycloalkyl group. The compounds of the present invention are useful in the treatment or prevention of various diseases including airway diseases (through A2B, A3, P2Y2 receptors), cancer (through A3, P2 receptors), cardiac arrhythmias (through A1 receptors), cardiac ischemia (through A1, A3 receptors), epilepsy (through A1, P2X receptors), and Huntington's Disease (through A2A receptors).
摘要翻译： 本发明提供了新的核苷和核苷酸衍生物，其是P1和P2受体的有用的激动剂或拮抗剂。 例如，本发明提供式A-M的化合物，其中A是修饰的腺嘌呤或尿嘧啶，M是受限制的环烷基。 腺嘌呤或尿嘧啶与受限制的环烷基键合。 本发明的化合物可用于治疗或预防各种疾病，包括气道疾病（通过A 2B，A 3，P 2，N 2， 受体），癌症（通过Aβ3 P2受体），心律失常（通过A1受体），心脏缺血（通过A 3， >受体），癫痫（通过A1，P2X受体）和亨廷顿氏病（通过2A2受体）。
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