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1. 发明申请

US20110124553A1 INSULIN-OLIGOMER CONJUGATES, FORMULATIONS AND USES THEREOF 审中-公开
标题翻译：胰岛素寡聚体结合体，其制剂及其用途
公开(公告)号：US20110124553A1
公开(公告)日：2011-05-26
申请号：US13008094
申请日：2011-01-18
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28 , C07K14/62 , A61P3/10
CPC分类号： C07K14/62 , A61K9/0095 , A61K9/2013 , A61K9/2018 , A61K33/30 , A61K38/00 , A61K38/28 , A61K45/06 , A61K47/60 , A61K47/69 , A61K2300/00
摘要： An insulin compound coupled to a modifying moiety having a formula: —X—R1—Y—PAG-Z—R2 (Formula VI) where, X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond, either R1 or R2 is a lower alkyl, optionally including a carbonyl group, and when R1 is a lower alkyl, R2 is a capping group, and PAG is a linear or branched carbon chain incorporating one or more alkalene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —S—, —O—, —N—, and —C(O)—.
摘要翻译：与具有下式的-X-R1-Y-PAG-Z-R2（式VI）的修饰部分偶联的胰岛素化合物，其中X，Y和Z独立选择连接基团，并且各自任选存在，X，当存在的通过共价键与胰岛素化合物偶联，R 1或R 2是任选地包括羰基的低级烷基，当R 1是低级烷基时，R 2是封端基，PAG是直链或支链碳含有一个或多个碱金属二醇部分，以及任选地引入一个或多个选自-S-，-O-，-N-和-C（O） - 的其它部分的链。

2. 发明申请

US20090221485A1 ORAL PEPTIDES CONJUGATES FOR METABOLIC DISEASES 有权
标题翻译：口服胶囊与代谢性疾病相关
公开(公告)号：US20090221485A1
公开(公告)日：2009-09-03
申请号：US12090306
申请日：2006-10-18
申请人： Kenneth D. James
发明人： Kenneth D. James
IPC分类号： A61K38/12 , C07K14/00
CPC分类号： C07K14/605 , A61K38/00
摘要： The present invention relates to the field of metabolic compound conjugates, methods of forming said conjugates and uses of these conjugates in the treatment of diabetes and conditions related to this condition. The metabolic compound conjugates of this invention include a metabolic peptide having a glucagon-like peptide (GLP-1) receptor binding motif for action on a GLP-1 receptor and at least one oligomer conjugation site for binding with at least one oligomer, wherein the oligomer includes a polyethylene glycol moiety (PEG), and/or alkyl moiety.
摘要翻译：本发明涉及代谢化合物缀合物的领域，形成所述缀合物的方法和这些缀合物在治疗糖尿病中的用途以及与该病症相关的病症。本发明的代谢化合物缀合物包括具有用于对GLP-1受体作用的胰高血糖素样肽（GLP-1）受体结合基序和至少一个与至少一种低聚物结合的低聚物缀合位点的代谢肽，其中低聚物包括聚乙二醇部分（PEG）和/或烷基部分。

3. 发明授权

US06812362B2 Methods of synthesizing acylanilides including bicalutamide and derivatives thereof 有权
标题翻译：合成酰基辅酶包括比卡鲁胺及其衍生物的方法
公开(公告)号：US06812362B2
公开(公告)日：2004-11-02
申请号：US10268155
申请日：2002-10-10
申请人： Nnochiri N. Ekwuribe , Kenneth D. James, Jr.
发明人： Nnochiri N. Ekwuribe , Kenneth D. James, Jr.
IPC分类号： C07C25550
CPC分类号： C07C253/30 , C07C315/04 , C07C317/46 , C07C255/60
摘要： Methods of synthesizing an acylanilide include contacting a compound having the structure of Formula I: with a compound having the structure of Formula II: under conditions sufficient to provide a compound having the structure of Formula III: and treating the compound of Formula III under conditions sufficient to provide an acylanilide. The compound of Formula III may be addition reacted with a compound having the structure of Formula IV: R5—X1—R6—R7 Formula IV under conditions sufficient to provide an acylanilide having the structure of Formula V:
摘要翻译：合成酰基酰苯胺的方法包括使具有式I结构的化合物与具有式II结构的化合物接触：在足以提供具有式III结构的化合物的条件下：在足够的条件下处理式III化合物以提供酰基苯胺。式III的化合物可以与具有式IV结构的化合物反应：在足以提供具有式V结构的酰基酰苯胺的条件下：

4. 发明授权

US06593492B1 Resolution of intermediates in the synthesis of substantially pure bicalutamide 有权
标题翻译：中间体在合成基本纯粹的比卡鲁胺中的分辨率
公开(公告)号：US06593492B1
公开(公告)日：2003-07-15
申请号：US09695884
申请日：2000-10-25
申请人： Nnochiri Nkem Ekwuribe , Kenneth D. James
发明人： Nnochiri Nkem Ekwuribe , Kenneth D. James
IPC分类号： C07C6702
CPC分类号： C07C315/06 , C07B2200/07 , C07C315/04 , C07C319/28 , C07C323/52 , C07C317/46
摘要： A methods of preparing a substantially pure enantiomer of an acylanilide such as Casodex® (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula I: wherein R1 is alkyl or haloalkyl having up to 4 carbons; R2 is alkyl having up to 6 carbon atoms; R3 is a direct link or alkyl having up to 6 carbon atoms; R4 is alkyl, alkenyl, hydroxyalkyl or cycloalkyl each of up to 6 carbons; or R4 is phenyl which bears one, two or three substituents independently selected from hydrogen, halogen, nitro, carboxy, carbamoyl and cyano, and alkyl, alkoxy, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, perfluoroalkyl, perfluoroalkylthio, perfluoroalkylsulphinyl, perfluoroalkylsulphonyl, alkoxycarbonyl and N-alkylcarbamoyl each of up to 4 carbon atoms, and phenyl, phenylthio, phenylsulphinyl and phenylsulphonyl; or R4 is naphthyl; or R4 is a 5- or 6-membered saturated or unsaturated heterocyclic which contains one, two or three heteroatoms selected from oxygen, nitrogen and sulfur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two halogen, cyano or amino, or alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl each of up to 4 carbon atoms, or oxy or hydroxy substituents, or which if sufficiently saturated may bear one or two oxo substituents; and X1 is oxygen, sulfur, sulphinyl (—SO—), sulphonyl (—SO2—), imino (—NH—) or alkylimino (—NR5—) where R5 is alkyl having up to 6 carbon atoms. The resolved intermediate compound of Formula I is then treated under conditions sufficient to provide a substantially pure enantiomer of an acylanilide such as Casodex® (bicalutamide) and/or its derivatives.
摘要翻译：制备酰基酰苯胺（比卡鲁前列酰胺）和/或其衍生物的基本上纯的对映异构体的方法包括拆分具有式I结构的中间体化合物：其中R1是具有至多4个碳的烷基或卤代烷基; R2是具有至多6个碳原子的烷基; R 3是具有至多6个碳原子的直链或烷基; R 4是至多6个碳原子的烷基，烯基，羟基烷基或环烷基; 或R4是苯基，其具有独立地选自氢，卤素，硝基，羧基，氨基甲酰基和氰基的一个，两个或三个取代基，和烷基，烷氧基，烷酰基，烷硫基，烷基亚磺酰基，烷基磺酰基，全氟烷基，全氟烷基硫代，全氟烷基亚磺酰基，全氟烷基磺酰基，烷氧基羰基和最多4个碳原子的N-烷基氨基甲酰基，苯基，苯硫基，苯基亚磺酰基和苯基磺酰基; 或R 4为萘基; 或R 4是含有一个，两个或三个选自氧，氮和硫的杂原子的5-或6-元饱和或不饱和杂环，该杂环可以是单环或可以与苯并环稠合，以及哪些杂环或至少4个碳原子的烷基，烷氧基，烷硫基，烷基亚磺酰基或烷基磺酰基，或羟基或羟基取代基，或者如果足够饱和可以带有一个或两个氧代取代基; 和X 1是氧，硫，亚磺酰基（-SO-），磺酰基（-SO 2 - ），亚氨基（-NH-）或烷基亚氨基（-NR 5 - ），其中R 5是具有至多6个碳原子的烷基。然后在足以提供酰基酰苯胺（比卡鲁胺）和/或其衍生物的基本上纯的对映异构体的条件下处理。

5. 发明申请

US20100216714A1 NATRIURETIC COMPOUNDS, CONJUGATES, AND USES THEREOF 审中-公开
标题翻译： NATRIURETIC化合物，结合物及其用途
公开(公告)号：US20100216714A1
公开(公告)日：2010-08-26
申请号：US12689342
申请日：2010-01-19
申请人： Kenneth D. James , Balasingham Radhakrishnan , Navdeep B. Malkar , Mark A. Miller , Nnochiri N. Ekwuribe
发明人： Kenneth D. James , Balasingham Radhakrishnan , Navdeep B. Malkar , Mark A. Miller , Nnochiri N. Ekwuribe
IPC分类号： A61K38/17 , C07K14/47 , C07K14/58 , A61P9/00 , A61P9/04
CPC分类号： C07K14/58 , A61K38/00 , A61K47/60 , C07K14/72 , C07K16/26
摘要： Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, enteral, subcutaneous, pulmonary, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
摘要翻译：本发明公开了改良的利尿钠化合物及其缀合物。特别地，提供了缀合形式的hBNP，其包括与其连接的至少一个修饰部分。修饰的利尿钠化合物缀合物保留刺激cGMP产生，与NPR-A受体结合的活性，并且在一些实施方案中，与未修饰的对应利钠化合物相比，循环中的半衰期改善。口服，胃肠外，肠内，皮下，肺和静脉内形式的化合物和缀合物可以制备为用于心脏状况的治疗和/或治疗，特别是充血性心力衰竭。还公开了包含具有各种长度和构型的寡聚结构的修饰部分。还公开了利尿钠化合物的类似物，其具有不同于天然序列的氨基酸序列。

6. 发明申请

US20100105605A1 FATTY ACID FORMULATIONS AND ORAL DELIVERY OF PROTEINS AND PEPTIDES, AND USES THEREOF 有权
标题翻译：脂肪酸制剂和口服递送蛋白质和肽，及其用途
公开(公告)号：US20100105605A1
公开(公告)日：2010-04-29
申请号：US12581953
申请日：2009-10-20
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28 , A61P3/10
CPC分类号： C07K14/62 , A61K9/0095 , A61K9/2013 , A61K9/2018 , A61K33/30 , A61K38/00 , A61K38/28 , A61K45/06 , A61K47/60 , A61K47/69 , A61K2300/00
摘要： Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.
摘要翻译：用于施用药剂例如蛋白质和肽，蛋白质和肽缀合物和/或阳离子 - 多肽缀合物复合物的脂肪酸组合物。特别地，本发明提供了一种配制成通过摄取口服给药的固体药物组合物，其具有约0.1至约75％w / w脂肪酸组分，其中脂肪酸组分包含饱和或不饱和C4，C5，C6，C7，C8 ，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐; 和治疗剂。此外，本发明提供配制成通过摄取口服给药的液体药物组合物，其包含：约0.1至约10％w / v脂肪酸组分，其中脂肪酸组分包含饱和或不饱和C4，C5，C6，C7，C8 ，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐; 和治疗剂。

7. 发明授权

US07662773B2 Natriuretic compounds, conjugates, and uses thereof 失效
标题翻译：利尿钠化合物，缀合物及其用途
公开(公告)号：US07662773B2
公开(公告)日：2010-02-16
申请号：US10723933
申请日：2003-11-26
申请人： Kenneth D. James , Balasingam Radhakrishnan , Navdeep B. Malkar , Mark A. Miller , Nnochiri N. Ekwuribe
发明人： Kenneth D. James , Balasingam Radhakrishnan , Navdeep B. Malkar , Mark A. Miller , Nnochiri N. Ekwuribe
IPC分类号： A61K38/03 , A61K8/64
CPC分类号： C08G65/329 , A61K47/60 , C07K14/58 , C07K14/72 , C08L2203/02
摘要： Modified natriuretic compounds and conjugates thereof are disclosed in the present invention. In particular, conjugated forms of hBNP are provided that include at least one modifying moiety attached thereto. The modified natriuretic compound conjugates retain activity for stimulating cGMP production, binding to NPR-A receptor, and in some embodiments an improved half-life in circulation as compared to unmodified counterpart natriuretic compounds. Oral, parenteral, subcutaneous, and intravenous forms of the compounds and conjugates may be prepared as treatments and/or therapies for heart conditions particularly congestive heart failure. Modifying moieties comprising oligomeric structures having a variety of lengths and configurations are also disclosed. Analogs of the natriuretic compound are also disclosed, having an amino acid sequence that is other than the native sequence.
摘要翻译：本发明公开了改良的利尿钠化合物及其缀合物。特别地，提供了缀合形式的hBNP，其包括与其连接的至少一个修饰部分。修饰的利钠化合物缀合物保留用于刺激cGMP产生，与NPR-A受体结合的活性，并且在一些实施方案中，与未修饰的对应利钠化合物相比，循环中的半衰期改善。可以将口服，胃肠外，皮下和静脉内形式的化合物和缀合物制备为用于心脏状况的治疗和/或治疗，特别是充血性心力衰竭。还公开了包含具有各种长度和构型的寡聚结构的修饰部分。还公开了利尿钠化合物的类似物，其具有不同于天然序列的氨基酸序列。

8. 发明授权

US08563685B2 Fatty acid formulations and oral delivery of proteins and peptides, and uses thereof 有权
标题翻译：脂肪酸制剂和蛋白质和肽的口服递送及其用途
公开(公告)号：US08563685B2
公开(公告)日：2013-10-22
申请号：US12581953
申请日：2009-10-20
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri N. Ekwuribe
IPC分类号： C07K14/62
CPC分类号： C07K14/62 , A61K9/0095 , A61K9/2013 , A61K9/2018 , A61K33/30 , A61K38/00 , A61K38/28 , A61K45/06 , A61K47/60 , A61K47/69 , A61K2300/00
摘要： Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.
摘要翻译：用于施用药剂例如蛋白质和肽，蛋白质和肽缀合物和/或阳离子 - 多肽缀合物复合物的脂肪酸组合物。特别地，本发明提供了一种配制成通过摄取口服给药的固体药物组合物，其具有约0.1至约75％w / w脂肪酸组分，其中脂肪酸组分包含饱和或不饱和C4，C5，C6，C7，C8 ，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐; 和治疗剂。此外，本发明提供配制成通过摄取口服给药的液体药物组合物，其包含：约0.1至约10％w / v脂肪酸组分，其中脂肪酸组分包含饱和或不饱和C4，C5，C6，C7，C8 ，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐; 和治疗剂。

9. 发明授权

US09101596B2 Cation complexes of insulin compound conjugates, formulations and uses thereof 有权
标题翻译：胰岛素化合物缀合物的阳离子配合物，其制剂及其用途
公开(公告)号：US09101596B2
公开(公告)日：2015-08-11
申请号：US13012146
申请日：2011-01-24
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28 , A61K9/00 , A61K9/20 , A61K33/30 , A61K45/06 , A61K47/48 , C07K14/62 , A61K38/00
CPC分类号： C07K14/62 , A61K9/0095 , A61K9/2013 , A61K9/2018 , A61K33/30 , A61K38/00 , A61K38/28 , A61K45/06 , A61K47/60 , A61K47/69 , A61K2300/00
摘要： An insulin compound coupled to a modifying moiety having a formula: —X—R1—Y-PAG-Z—R2 (Formula VI) where, X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond, either R1 or R2 is a lower alkyl, optionally including a carbonyl group, and when R1 is a lower alkyl, R2 is a capping group, and PAG is a linear or branched carbon chain incorporating one or more alkalene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —S—, —O—, —N—, and —C(O)—.
摘要翻译：与具有下式的-X-R1-Y-PAG-Z-R2（式VI）的修饰部分偶联的胰岛素化合物，其中X，Y和Z独立选择连接基团，并且各自任选存在，X，当存在的通过共价键与胰岛素化合物偶联，R 1或R 2是任选地包括羰基的低级烷基，当R 1是低级烷基时，R 2是封端基，PAG是直链或支链碳含有一个或多个碱金属二醇部分，以及任选地引入一个或多个选自-S-，-O-，-N-和-C（O） - 的其它部分的链。

10. 发明授权

US07875700B2 Cation complexes of insulin compound conjugates, formulation and uses thereof 有权
标题翻译：胰岛素化合物缀合物的阳离子配合物，其制剂及其用途
公开(公告)号：US07875700B2
公开(公告)日：2011-01-25
申请号：US11184668
申请日：2005-07-19
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth D. James , Navdeep B. Malkar , Mark A. Miller , Monica Puskas , Nnochiri N. Ekwuribe
IPC分类号： A61K38/28
CPC分类号： C07K14/62 , A61K9/0095 , A61K9/2013 , A61K9/2018 , A61K33/30 , A61K38/00 , A61K38/28 , A61K45/06 , A61K47/60 , A61K47/69 , A61K2300/00
摘要： The invention provides a complex including a cation and an insulin compound conjugate. The insulin compound conjugate includes insulin compound, such as human insulin or an analog thereof, conjugated to a modifying moiety, such as a polyethylene glycol moiety. The invention also includes solids and pharmaceutical compositions including such complexes, methods of making such complexes, and methods of using such complexes in the treatment of insulin compound deficiencies and other ailments. Further, the invention includes novel insulin compound conjugates and modifying moieties for use in making novel insulin compound conjugates. The invention also includes fatty acid compositions for administration of pharmaceutical agents, such as the novel insulin compound conjugates, and/or the cation-insulin compound conjugate complexes of the invention.
摘要翻译：本发明提供了包含阳离子和胰岛素化合物缀合物的复合物。胰岛素化合物缀合物包括与修饰部分如聚乙二醇部分缀合的胰岛素化合物，例如人胰岛素或其类似物。本发明还包括固体和包含这种复合物的药物组合物，制备这种复合物的方法，以及使用这些复合物治疗胰岛素化合物缺乏症和其它疾病的方法。此外，本发明包括用于制备新型胰岛素化合物缀合物的新型胰岛素化合物缀合物和修饰部分。本发明还包括用于给药药物的脂肪酸组合物，例如本发明的新型胰岛素化合物缀合物和/或阳离子 - 胰岛素复合物缀合复合物。

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