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。

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。

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。

公开(公告)号：US20070232626A1

公开(公告)日：2007-10-04

申请号：US11574779

申请日：2005-09-02

申请人： Kenneth Jacobson ,  Bhalchandra Joshi ,  Susanna Tchilibon

发明人： Kenneth Jacobson ,  Bhalchandra Joshi ,  Susanna Tchilibon

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。

公开(公告)号：US06413736B1

公开(公告)日：2002-07-02

申请号：US09372991

申请日：1999-08-12

申请人： Gunnard Kenneth Jacobson ,  Setsuko Omata Jolly ,  Joseph James Sedmak ,  Thomas Joseph Skatrud ,  John Marion Wasileski

发明人： Gunnard Kenneth Jacobson ,  Setsuko Omata Jolly ,  Joseph James Sedmak ,  Thomas Joseph Skatrud ,  John Marion Wasileski

IPC分类号： C12P2300

CPC分类号： C12R1/645 ,  A23K20/179 ,  A23L5/44 ,  C12N13/00 ,  C12P23/00

摘要： Phaffia rhodozyma strains are described which produce greater than 3,000 ppm astaxanthin based on dry yeast solids when cultivated in a volume of nutrient medium of at least about 1,500 liters and containing in excess of 4 percent, preferably in excess of 6 percent, dry yeast solids. These and other strains are cultivated by an improved fermentation method comprising extending the maturation phase of the fermentation by one or more various techniques including exposing the yeast cells to a low-intensity light, slow feeding the cells with a rapidly metabolized energy source, e.g. glucose, and replacing the rapidly metabolized energy source with a slowly metabolized energy source, e.g. gylcerol. The cells of these strains are incorporated into animal feeds, particularly feeds for salmonid fishes, to impart or enhance the red pigmentation of these animals and products made from these animals.

摘要翻译： 描述了红酵母酵母菌株，当在至少约1,500升的营养培养基的体积中培养并含有超过4％，优选超过6％的干燥酵母固体时，其基于干酵母固体产生大于3,000ppm的虾青素。 这些和其它菌株通过改进的发酵方法培养，包括通过一种或多种各种技术延长发酵的成熟期，包括将酵母细胞暴露于低强度光，用快速代谢的能量来缓慢喂养细胞，例如， 葡萄糖，并用缓慢代谢的能量源代替快速代谢的能量源，例如， gylcerol。 这些菌株的细胞被并入动物饲料，特别是鲑鱼的饲料中，以赋予或增强这些动物的红色色素沉着和由这些动物制成的产品。

公开(公告)号：US5922560A

公开(公告)日：1999-07-13

申请号：US557714

申请日：1995-11-13

申请人： Gunnard Kenneth Jacobson ,  Setsuko Omata Jolly ,  Joseph James Sedmak ,  Thomas Joseph Skatrud ,  John Marion Wasileski

发明人： Gunnard Kenneth Jacobson ,  Setsuko Omata Jolly ,  Joseph James Sedmak ,  Thomas Joseph Skatrud ,  John Marion Wasileski

IPC分类号： A23K1/16 ,  A23L1/275 ,  C07C49/743 ,  C12N1/16 ,  C12N13/00 ,  C12P23/00 ,  C12R1/645

CPC分类号： C12R1/645 ,  A23K20/179 ,  A23L5/44 ,  C12N13/00 ,  C12P23/00

摘要： Phaffia rhodozyma strains are described which produce greater than 3,000 ppm astaxanthin based on dry yeast solids when cultivated in a volume of nutrient medium of at least about 1,500 liters and containing in excess of 4 percent, preferably in excess of 6 percent, dry yeast solids. These and other strains are cultivated by an improved fermentation method comprising extending the maturation phase of the fermentation by one or more various techniques including exposing the yeast cells to a low-intensity light, slow feeding the cells with a rapidly metabolized energy source e.g. glucose, and replacing the rapidly metabolized energy source with a slowly metabolized energy source, e.g. gylcerol. The cells of these strains are incorporated into animal feeds, particularly feeds for salmonid fishes, to impart or enhance the red pigmentation of these animals and products made from these animals.

摘要翻译： 描述了红酵母酵母菌株，当在至少约1,500升的营养培养基的体积中培养并含有超过4％，优选超过6％的干燥酵母固体时，其基于干酵母固体产生大于3,000ppm的虾青素。 这些和其它菌株通过改进的发酵方法培养，包括通过一种或多种各种技术延长发酵的成熟期，包括将酵母细胞暴露于低强度光，用快速代谢的能量源缓慢喂养细胞，例如， 葡萄糖，并用缓慢代谢的能量源代替快速代谢的能量源，例如， gylcerol。 这些菌株的细胞被并入动物饲料，特别是鲑鱼的饲料中，以赋予或增强这些动物的红色色素沉着和由这些动物制成的产品。

公开(公告)号：US07893094B2

公开(公告)日：2011-02-22

申请号：US10560590

申请日：2004-06-28

申请人： Harvey B. Pollard ,  Kenneth Jacobson

发明人： Harvey B. Pollard ,  Kenneth Jacobson

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。

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。

公开(公告)号：US20070059844A1

公开(公告)日：2007-03-15

申请号：US11162485

申请日：2005-09-12

申请人： James HARPER ,  David TURNER ,  Kenneth JACOBSON ,  Brian WEST

发明人： James HARPER ,  David TURNER ,  Kenneth JACOBSON ,  Brian WEST

IPC分类号： C40B40/04 ,  C40B30/02 ,  G06Q99/00

CPC分类号： G01J3/52 ,  G01J3/463 ,  G01J3/465

摘要： A pigment library and a method for preparing it are provided, which includes identifying a plurality of thermoplastic polymers and then selecting pigments useful in the plurality of thermoplastic polymers. The pigments are heat stable at the melt temperature of each of the plurality of thermoplastic polymers and are not chemically interactive or reactive with each of the polymers of the plurality of thermoplastic polymer. Further, each of the pigments in combination with each of the polymers of the plurality of thermoplastic polymers possesses the property of being lightfast, injection moldable, and fiber spinnable and also not crocking. A colorant database is then prepared using the pigment library. The colorant database is used with color matching software that predict formulations using the colorant database. The result is the development of formulations that minimize or eliminate metameric color effect under various lighting conditions across multiple polymers and end product types.

摘要翻译： 提供了颜料库及其制备方法，其包括鉴定多种热塑性聚合物，然后选择可用于多种热塑性聚合物的颜料。 颜料在多种热塑性聚合物的熔融温度下是热稳定的，并且与多种热塑性聚合物中的每一种聚合物不化学相互作用或具有反应性。 此外，与多种热塑性聚合物的每种聚合物组合的每种颜料都具有耐光性，可注射模塑性和可纺纤维性，并且也不会变质的性质。 然后使用颜料库制备着色剂数据库。 着色剂数据库与使用着色剂数据库预测配方的颜色匹配软件一起使用。 结果是开发了在多个聚合物和最终产品类型下在各种照明条件下最小化或消除同色异色效应的配方。

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。