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公开(公告)号：US20060172933A1
公开(公告)日：2006-08-03
申请号：US10999761
申请日：2004-11-30
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，结合NPR-A受体的活性，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。
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公开(公告)号：US20060074009A1
公开(公告)日：2006-04-06
申请号：US11138194
申请日：2005-05-26
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.
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3.发明申请Cation complexes of insulin compound conjugates, formulations and uses thereof 有权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：US20060019873A1
公开(公告)日：2006-01-26
申请号：US11184594
申请日：2005-07-19
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Monica Puskas , Nnochiri Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Monica Puskas , Nnochiri Ekwuribe
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-R (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 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)—, and where the modifying moiety has a maximum number of 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, or 25 heavy atoms.
摘要翻译： 与具有下式的修饰部分偶联的胰岛素化合物：<？in-line-formula description =“In-line formula”end =“lead”→XR 1 -Y-PAG-ZR （式VI）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中，X，Y和Z是独立选择的连接基团，并且每个可选地存在，X如果存在， 通过共价键与胰岛素化合物偶联，R 1或R 2是低级烷基，任选地包括羰基，当R 1 低级烷基是R 2是封端基团，PAG是含有一个或多个二烷基二醇部分的直链或支链碳链，并且任选地加入一个或多个选自以下的另外的部分： 由-S-，-O-，-N-和-C（O） - 组成的组，其中改性部分具有最大数目为3,4,5,6,7,8,9,10， 11，12，13，14，15，16，17，18，19，20，21，22，23，24或25个重原子。
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4.发明申请Cation complexes of insulin compund conjugates, formulation and uses thereof 有权胰岛素共轭物的阳离子配合物，其制剂和用途公开(公告)号：US20060019874A1
公开(公告)日：2006-01-26
申请号：US11184668
申请日：2005-07-19
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Monica Puskas , Nnochiri Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Monica Puskas , Nnochiri Ekwuribe
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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公开(公告)号：US20060018874A1
公开(公告)日：2006-01-26
申请号：US11184528
申请日：2005-07-19
申请人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri Ekwuribe
发明人： Balasingam Radhakrishnan , Diti Aggarwal , Michelle Ferro , Kenneth James , Navdeep Malkar , Mark Miller , Leo Pavliv , Karen Polowy , Monica Puskas , Nnochiri Ekwuribe
IPC分类号： A61K38/28 , A61K38/21 , A61K39/395 , A61K38/22 , A61K38/18
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.
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公开(公告)号：US20080033153A1
公开(公告)日：2008-02-07
申请号：US11631582
申请日：2005-07-07
IPC分类号： C07C245/08
CPC分类号： C07C245/08
摘要： Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.
摘要翻译： 公开了制备式I化合物的方法：其中R 1，R 3和R 4独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C C 1至C 4烷基，或其中R 6，R 7和R 8是 独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。 该方法可以包括将适当官能化的苯胺化合物转化为重氮盐（可以首先通过还原硝基苯形成苯胺化合物）并将重氮盐与适当官能化的苯化合物偶联。 适当官能化的苯胺化合物包括伯醇或醛基，然后将其氧化成羧酸基团，或包括被水解成羧酸基团的腈或酰胺基团。 所述方法还可以涉及适当官能化的硝基苯的直接偶联（通过还原硝基以形成偶氮键）。 化合物及其代谢物可用于治疗或预防各种疾病，特别是胃肠道的炎性病症。
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7.发明申请公开(公告)号：US20110319267A1
公开(公告)日：2011-12-29
申请号：US13063445
申请日：2009-09-10
申请人： Nnochiri Ekwuribe
发明人： Nnochiri Ekwuribe
IPC分类号： A01N47/30 , C07C309/24 , C07C245/06 , C07D311/68 , A61K31/655 , A61K31/196 , A61K31/185 , A61K31/353 , A01N41/06 , A01N41/04 , A01N43/16 , A61P1/00 , A61P31/12 , A61P31/04 , A61P31/10 , A61P29/00 , A61P1/04 , A61P35/00 , A61P1/14 , A01P7/04 , A01P13/00 , A01P3/00 , A61P31/00 , A61P37/02 , A61K31/56 , C07C245/08
CPC分类号： A61K31/655 , A01N41/04 , A01N41/06 , A01N41/08 , A61K45/06 , C07C245/06 , C07C245/08 , C07C309/15 , C07C309/24 , C07C311/46 , C07C311/49 , C07C311/54 , C07D311/54 , C07D311/68
摘要： Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.
摘要翻译： 公开了在结肠部位代谢为5-ASA或其类似物的前体化合物及其牛磺酸或其类似物。 还公开了包括该化合物的药物组合物和使用该化合物的治疗方法。 这些化合物可用于治疗或预防胃肠道疾病，包括结肠癌，溃疡性结肠炎和克罗恩氏病。
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8.发明申请IMMUNOREGULATORY COMPOUNDS AND DERIVATIVES AND METHODS OF TREATING DISEASES THEREWITH 有权免疫组化化合物及其衍生物及其治疗疾病的方法公开(公告)号：US20070004800A1
公开(公告)日：2007-01-04
申请号：US11470655
申请日：2006-09-07
IPC分类号： A61K31/24 , A61K31/195
CPC分类号： A61K31/195 , A61K31/196 , A61K31/215 , A61K31/24 , C07C229/42 , C07C245/08 , Y02A50/475 , Y02A50/481 , A61K2300/00
摘要： Compounds are disclosed having the structure of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. Such compounds may be utilized for the prophylaxis or treatment of various diseases, particularly inflammatory conditions of the GI tract. Methods of treating inflammatory conditions of the GI tract such as inflammatory bowel disease using compounds having the following formula are also disclosed: where R9, R10 and R11 are independently selected from the group consisting of hydrogen and C1 to C4 alkyl, and R12 is selected from the group consisting of hydrogen and —C(O)R13, where R13 is a C1 to C6 alkyl or an aryl group.
摘要翻译： 公开了具有式I结构的化合物：其中R 1，R 3和R 4独立地是氢或C 1 C 1至C 4烷基，R 2是：其中R 5选自氢和C C 1至C 4烷基，或其中R 6，R 7和R 8是 独立地是氢或C 1至C 4烷基; 或其酯或药理学上可接受的盐。 这些化合物可用于预防或治疗各种疾病，特别是GI道的炎性病症。 还公开了使用具有下式的化合物治疗胃肠道炎症性疾病如炎症性肠病的方法：其中R 9，R 10和R 11 独立地选自氢和C 1至C 4烷基，R 12选自基团 由氢和-C（O）R 13组成，其中R 13是C 1至C 6 - 烷基或芳基。
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9.发明申请Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties 有权具有聚乙二醇部分的聚合物的主要单分散混合物公开(公告)号：US20050059799A1
公开(公告)日：2005-03-17
申请号：US10977973
申请日：2004-10-29
CPC分类号： C08G65/334 , C08L71/02 , C08L71/00
摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)b—O−X+ (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMs (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1 (III). Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.
摘要翻译： 合成包含聚乙二醇部分的聚合物的基本上单分散的混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：R 1（OC 2 H 4）b O - X +（I） 1>是H或亲脂性部分; n为1至25; 并且X +是具有式II结构的化合物的基本上单分散的混合物：R 2（OC 2 H 4）m-OM（II）其中R 2是H或亲油部分; 并且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本单分散混合物的条件下：R 2（OC 2 H 4）m + n -OR 1（III）。 还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。
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公开(公告)号：US20050054735A1
公开(公告)日：2005-03-10
申请号：US10970571
申请日：2004-10-21
IPC分类号： A61P29/00 , A61K31/085 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/21 , A61K31/216 , A61K31/222 , A61K31/235 , A61K31/265 , C07C43/23 , A61K31/445 , A61K31/075 , A61K31/12
CPC分类号： A61K31/16 , A61K31/085 , A61K31/167 , A61K31/21 , A61K31/216 , A61K31/235 , A61K31/265
摘要： The present invention provides therapeutically effective amounts of 6MNA prodrugs. The pharmaceutical composition comprises wherein R is H or COR′, wherein R′ is selected from the group consisting of C1 to C6 alkyl, (CH2)m O(CH2)n, (CH2)m(OC2H4)p O(CH2)n, (CH2)m(OC2H4)p, (OCH2H4)p ONO2 and (OCH2H4)p O(CH2)n wherein m is an integer from 2 to 4, and n and p are integers from 1 to 4. Alternatively, R is a therapeutic moiety.
摘要翻译： 本发明提供治疗有效量的6MNA前药。 该药物组合物包含其中R是H或COR'，其中R'选自C1-C6烷基，（CH2）m O（CH2）n，（CH2）m（OC2H4）pO（CH2）n ，（CH 2）m（OC 2 H 4）p，（OCH 2 H 4）p ONO 2和（OCH 2 H 4）p O（CH 2）n，其中m是2至4的整数，n和p是1至4的整数。 治疗部分。
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