公开(公告)号：US20090098130A1

公开(公告)日：2009-04-16

申请号：US11969850

申请日：2008-01-04

Applicant: Curt W. BRADSHAW ,  Sukumar Sakamuri ,  Yanwen Fu ,  Bryan Oates ,  Joel Desharnais ,  David Tumelty

Inventor： Curt W. BRADSHAW ,  Sukumar Sakamuri ,  Yanwen Fu ,  Bryan Oates ,  Joel Desharnais ,  David Tumelty

IPC: A61K39/44 ,  A61P3/10 ,  C07K19/00

CPC classification number: C07K14/605 ,  A61K47/6811 ,  A61K47/6843

Abstract: The present invention provides GA targeting compounds which comprise GA targeting agent-linker conjugates linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.

Abstract translation: 本发明提供了GA靶向化合物，其包含与抗体的结合位点连接的GA靶向剂 - 接头缀合物。 提供了化合物的各种用途，包括预防或治疗糖尿病或糖尿病相关病症的方法。

公开(公告)号：US20050239713A1

公开(公告)日：2005-10-27

申请号：US10520793

申请日：2003-07-09

Applicant: Alexander Domling ,  Bernd Henkel ,  Barbara Beck ,  Katrin Illgen ,  Sukumar Sakamuri ,  Sanjay Menon

Inventor： Alexander Domling ,  Bernd Henkel ,  Barbara Beck ,  Katrin Illgen ,  Sukumar Sakamuri ,  Sanjay Menon

IPC: A61K38/00 ,  A61P35/00 ,  C07D417/12 ,  C07K5/02 ,  A61K38/04 ,  C07D213/46 ,  C07K5/04

CPC classification number: C07D417/12 ,  A61K38/00 ,  C07K5/021

Abstract: The invention relates to tubulysin derivatives of general formula (II), said derivatives having a cytostatic effect.

Abstract translation: 本发明涉及通式（II）的微管蛋白衍生物，所述衍生物具有细胞抑制作用。

公开(公告)号：US08466145B2

公开(公告)日：2013-06-18

申请号：US13140997

申请日：2010-01-07

Applicant: Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

Inventor： Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

IPC: A61K31/541 ,  A61K31/4196 ,  A61K31/4025 ,  A61K31/46 ,  A61K31/4245 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/40 ,  A61K31/454 ,  C07D413/12 ,  C07D405/12

CPC classification number: C07D417/12 ,  C07D207/10 ,  C07D207/12 ,  C07D211/46 ,  C07D213/12 ,  C07D401/12 ,  C07D403/12

Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.

Abstract translation: 描述了式（I）的新化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物有效降低血糖，血清胰岛素，游离脂肪酸，胆固醇，甘油三酯水平; 治疗肥胖，炎症，自身免疫性疾病如多发性硬化，类风湿性关节炎; 治疗和/或预防II型糖尿病。 这些化合物更特别是二肽基肽酶（DPP IV）抑制剂。

公开(公告)号：US20050228017A1

公开(公告)日：2005-10-13

申请号：US10497449

申请日：2002-10-31

Applicant: Sanjay Menon ,  Yingchun Lu ,  Sukumar Sakamuri ,  Quin-Zene Chen ,  Vladimir Khazak

Inventor： Sanjay Menon ,  Yingchun Lu ,  Sukumar Sakamuri ,  Quin-Zene Chen ,  Vladimir Khazak

IPC: A61K31/445 ,  A61K31/455 ,  A61P35/00 ,  C07C233/22 ,  C07C233/36 ,  C07C233/40 ,  C07C233/73 ,  C07C233/78 ,  C07C235/50 ,  C07C275/14 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C279/18 ,  C07C311/05 ,  C07C311/13 ,  C07C311/18 ,  C07C311/29 ,  C07D211/26 ,  C07D213/38 ,  C07D213/40 ,  C07D213/42 ,  C07D213/46 ,  C07D213/81 ,  C07D277/46 ,  C07D295/13 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D213/40 ,  C07C233/22 ,  C07C233/36 ,  C07C233/40 ,  C07C233/73 ,  C07C233/78 ,  C07C235/50 ,  C07C275/14 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C279/18 ,  C07C311/05 ,  C07C311/13 ,  C07C311/18 ,  C07C311/29 ,  C07D211/26 ,  C07D213/38 ,  C07D213/42 ,  C07D213/81 ,  C07D277/46 ,  C07D295/13 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention relates to compounds of formula (I): (I) their pharmacologically acceptable salts, or solvates and hydrates, and their prodrugs, respectively, and to pharmaceutical compositions containing the same as active ingredient. These novel compounds are especially useful in the treatment of cancer.

Abstract translation: 本发明涉及式（I）的化合物：（I）其药理学上可接受的盐，或溶剂化物和水合物及其前药，以及含有与活性成分相同的药物组合物。 这些新型化合物特别可用于治疗癌症。

公开(公告)号：US20190202855A1

公开(公告)日：2019-07-04

申请号：US16326542

申请日：2017-08-17

Applicant: Sukumar SAKAMURI ,  Curt W. BRADSHAW ,  Laxman ELTEPU ,  Bryan R. MEADE ,  Son LAM ,  Solstice Biologics, Ltd.

Inventor： Sukumar SAKAMURI ,  Curt W. BRADSHAW ,  Laxman ELTEPU ,  Bryan R. MEADE ,  Son LAM

IPC: C07H21/00 ,  C07F9/24 ,  C12N15/85 ,  C12N15/113

CPC classification number: C07H21/00 ,  C07F9/2408 ,  C07F9/65586 ,  C07F9/65616 ,  C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C12N15/85 ,  C12N2310/14

Abstract: Disclosed are polynucleotide constructs having a strand linked to a moiety carrying one or more auxiliary moieties. Also disclosed are polynucleotide constructs interrupted with a sugar analogue, and polynucleotide constructs with stereochemical{circumflex over ( )}enriched phosphorothioates. The polynucleotide constructs may be provided as hybridized polynucleotide constructs. Also featured are methods of delivery a polynucleotide construct to a cell and methods of reducing the expression of a protein in a cell by contacting the cell with the disclosed polynucleotide construct or hybridized polynucleotide construct.

公开(公告)号：US20190194655A1

公开(公告)日：2019-06-27

申请号：US16060171

申请日：2016-12-08

Applicant: Curt W. Bradshaw ,  Sukumar Sakamuri ,  Bryan R. Meade ,  Laxman Eltepu ,  Giuseppe Dello Iacono ,  Son Lam ,  Joseph Stock ,  Dingguo Liu ,  Bin Liu ,  Solstice Biologics, Ltd.

Inventor： Curt W. BRADSHAW ,  Sukumar SAKAMURI ,  Bryan R. MEADE ,  Laxman ELTEPU ,  Giuseppe Dello IACONO ,  Son LAM ,  Joseph STOCK ,  Dingguo LIU ,  Bin LIU

IPC: C12N15/113

CPC classification number: C12N15/113 ,  A61K31/7088 ,  A61K47/549 ,  C07F9/65515 ,  C07F9/65586 ,  C07F9/65616 ,  C12N2310/311 ,  C12N2310/312 ,  C12N2310/315 ,  C12N2310/351

Abstract: The invention features a hybridized polynucleotide construct including a passenger strand, a guide strand loadable into a RISC complex, and one or more auxiliary moieties. At least one of the auxiliary moieties is non-bioreversibly linked to an internucleoside phosphate or phosphorothioate in the passenger strand. The invention further features methods of delivery a polynucleotide construct to a cell and methods of reducing the expression of a protein in a cell. The methods typically involve contacting the cell with the hybridized polynucleotide construct.

公开(公告)号：US20170114341A1

公开(公告)日：2017-04-27

申请号：US15315608

申请日：2015-06-08

Applicant: Curt W. BRADSHAW ,  Sukumar SAKAMURI ,  Laxman ELTEPU ,  Son LAM ,  Dingguo LIU ,  Bryan MEADE ,  Giuseppe Dello IACONO ,  Joseph STOCK ,  Bin LIU ,  Solstice Biologics, Ltd.

Inventor： Curt W. BRADSHAW ,  Sukumar SAKAMURI ,  Laxman ELTEPU ,  Son LAM ,  Dingguo LIU ,  Bryan MEADE ,  Giuseppe Dello IACONO ,  Joseph STOCK ,  Bin LIU

IPC: C12N15/113 ,  C07H19/20 ,  C07H21/02 ,  C07H19/10 ,  C12N15/85 ,  C07H21/04

CPC classification number: C12N15/113 ,  C07H19/10 ,  C07H19/20 ,  C07H21/02 ,  C07H21/04 ,  C12N15/85 ,  C12N2310/14 ,  C12N2310/31 ,  C12N2310/32 ,  C12N2310/346 ,  C12N2310/3513 ,  C12N2310/3515 ,  C12N2330/30

Abstract: The invention features a hybridized polynucleotide construct containing a passenger strand, a guide strand loadable into a RISC complex, and (i) a 3′-terminal or an internucleotide non-bioreversible group in the guide strand; or (ii) a 5′-terminal, a 3′-terminal, or an internucleotide non-bioreversible group in the passenger strand, and a 5′-terminal, a 3′-terminal, or an internucleotide disulfide bioreversible group in the guide strand or the passenger strand. The invention also features methods of delivering a polynucleotide to a cell using the hybridized polynucleotide construct. The invention further features methods of reducing the expression of a polypeptide in a cell using the hybridized polynucleotide construct.

公开(公告)号：US20160257961A1

公开(公告)日：2016-09-08

申请号：US15034973

申请日：2014-11-06

Applicant: Curt W. BRADSHAW ,  Laxman ELTEPU ,  Ayman KABAKIBI ,  Son LAM ,  Bin LIE ,  Dingguo LIE ,  Bryan R. MEADE ,  Sukumar SAKAMURI ,  SOLSTICE BIOLOGICS, LTD.

Inventor： Curt W. BRADSHAW ,  Laxman ELTEPU ,  Ayman KABAKIBI ,  Son LAM ,  Bin LIU ,  Dingguo LIU ,  Bryan R. MEADE ,  Sukumar SAKAMURI

IPC: C12N15/113

CPC classification number: C12N15/1137 ,  C07F9/65586 ,  C07F9/65616 ,  C07H21/00 ,  C12N2310/14 ,  C12N2310/311 ,  C12N2310/321 ,  C12N2310/351

Abstract: The invention features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components is attached to an internucleotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains one or more bulky groups proximal to the disulfide group. The invention also features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components (i) is attached to an internucleotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains at least 4 atoms in a chain between the disulfide linkage and the phosphorus atom of the internucleotide bridging group or the terminal group; and where the chain does not contain a phosphate, an amide, an ester, or an alkenylene. The invention also features methods of delivering a polynucleotide to a cell using the polynucleotide constructs of the invention.

Abstract translation: 本发明的特征在于含有一种或多种组分（i）的多核苷酸构建体，其中所述组分（i）含有二硫键，其中所述一种或多种组分中的每一种与多核苷酸构建物的核苷酸间桥基团或末端基团连接，并且所述一种或多种组分 （i）含有一个或多个邻近二硫基的体积大的基团。 本发明还具有含有一种或多种组分（i）的多核苷酸构建体，其含有二硫键，其中所述一种或多种组分（i）中的每一个连接到多核苷酸构建体的核苷酸间桥基团或末端基团， 一个或多个组分（i）在二核苷酸桥连基团或末端基团的二硫键和磷原子之间的链中含有至少4个原子; 并且其中链不含有磷酸酯，酰胺，酯或亚烯基。 本发明还涉及使用本发明的多核苷酸构建体将多核苷酸递送至细胞的方法。

公开(公告)号：US20110257164A1

公开(公告)日：2011-10-20

申请号：US13140997

申请日：2010-01-07

Applicant: Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

Inventor： Gopalan Balasubramanian ,  Sukumar Sakamuri ,  Gajendra Singh ,  Sivanesan Dharmalingam ,  Franklin Pooppady Xavier ,  Shridhar Narayanan ,  Jeyamurugan Mookkan ,  Jeganatha Sivakumar Balasubramanian ,  Agneeswari Rajalingam ,  Jayanarayan Kulathingal

IPC: A61K31/541 ,  A61K31/4196 ,  C07D405/12 ,  A61K31/4025 ,  A61K31/46 ,  C07D413/12 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/497 ,  A61K31/4439 ,  C07D207/00 ,  A61K31/40 ,  C07D401/12 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/41 ,  C07D417/12 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/00 ,  A61P1/00 ,  A61P25/00 ,  A61P25/28 ,  C07D403/12

CPC classification number: C07D417/12 ,  C07D207/10 ,  C07D207/12 ,  C07D211/46 ,  C07D213/12 ,  C07D401/12 ,  C07D403/12

Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.

Abstract translation: 描述了式（I）的新化合物，其衍生物，类似物，互变异构体，区域异构体，立体异构体，多晶型物，溶剂合物，中间体，药学上可接受的盐，药物组合物，代谢物和前药。 这些化合物有效降低血糖，血清胰岛素，游离脂肪酸，胆固醇，甘油三酯水平; 治疗肥胖，炎症，自身免疫性疾病如多发性硬化，类风湿性关节炎; 治疗和/或预防II型糖尿病。 这些化合物更特别是二肽基肽酶（DPP IV）抑制剂。

公开(公告)号：US07816377B2

公开(公告)日：2010-10-19

申请号：US10520793

申请日：2003-07-09

Applicant: Alexander Dömling ,  Bernd Henkel ,  Barbara Beck ,  Katrin Illgen ,  Sukumar Sakamuri ,  Sanjay Menon

Inventor： Alexander Dömling ,  Bernd Henkel ,  Barbara Beck ,  Katrin Illgen ,  Sukumar Sakamuri ,  Sanjay Menon

IPC: A61K31/445 ,  C07D417/12

CPC classification number: C07D417/12 ,  A61K38/00 ,  C07K5/021

Abstract: The invention relates to tubulysin derivatives of general formula (II), said derivatives having a cytostatic effect.

Abstract translation: 本发明涉及通式（II）的微管蛋白衍生物，所述衍生物具有细胞抑制作用。