公开(公告)号：US08716224B2

公开(公告)日：2014-05-06

申请号：US13010267

申请日：2011-01-20

Applicant: Kunwar Shailubhai ,  Gary S. Jacob

Inventor： Kunwar Shailubhai ,  Gary S. Jacob

IPC: A61K38/00

CPC classification number: C07K7/08 ,  A61K9/0031 ,  A61K9/02 ,  A61K9/08 ,  A61K31/192 ,  A61K31/519 ,  A61K38/10 ,  A61K38/12 ,  A61K45/06 ,  A61K47/02 ,  A61K47/60 ,  C07K7/64

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

Abstract translation: 本发明提供新的鸟苷酸环化酶-C激动剂肽及其在治疗包括胃肠道疾病，炎症或癌症（例如胃肠癌））的人类疾病中的用途。 肽可以单独施用或与cGMP依赖性磷酸二酯酶抑制剂组合施用。 胃肠道疾病可以分为肠易激综合征，便秘或过度酸度等。胃肠道疾病可分为炎症性肠病或其他GI病症，包括克罗恩病和溃疡性结肠炎，以及癌症。

公开(公告)号：US08637451B2

公开(公告)日：2014-01-28

申请号：US13339785

申请日：2011-12-29

Applicant: Kunwar Shailubhai ,  Gregory Nikiforovich ,  Gary S. Jacob

Inventor： Kunwar Shailubhai ,  Gregory Nikiforovich ,  Gary S. Jacob

IPC: A61K38/12

CPC classification number: C07K7/64 ,  A61K38/00 ,  A61K38/10 ,  A61K38/12 ,  A61K45/06 ,  A61K47/60 ,  C07K7/08 ,  C07K7/50 ,  C07K2299/00 ,  Y02A50/473

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis. Thus, the method may be used to treat, inter alia, inflammation, including gastrointestinal inflammatory disorders, general organ inflammation and asthma, and carcinogenesis of the lung, gastrointestinal tract, bladder, testis, prostate and pancreas, or polyps.

Abstract translation: 公开了一种在哺乳动物受试者中治疗发炎，癌前或癌性组织或息肉的方法。 该治疗包括施用至少一种鸟苷酸环化酶受体的肽激动剂和/或增强细胞内cGMP产生的其它小分子的组合物。 鸟苷酸环化酶受体的至少一种肽激动剂可以单独施用或与cGMP依赖性磷酸二酯酶抑制剂组合施用。 抑制剂可以是抑制cGMP降解的小分子，肽，蛋白质或其它化合物。 不需要特定的作用机制，这种治疗可以恢复受试者上皮细胞群体的增殖和细胞凋亡之间的健康平衡，并且还抑制致癌作用。 因此，该方法可以用于治疗炎症，包括胃肠道炎症性疾病，一般器官炎症和哮喘，以及肺，胃肠道，膀胱，睾丸，前列腺和胰腺或息肉的致癌作用。

公开(公告)号：US08367800B2

公开(公告)日：2013-02-05

申请号：US13226300

申请日：2011-09-06

Applicant: Kunwar Shailubhai

Inventor： Kunwar Shailubhai

IPC: A61K38/00 ,  A61K38/10

CPC classification number: C07K7/08 ,  A61K38/00 ,  A61K38/10 ,  A61K45/06 ,  C07K7/64

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

Abstract translation: 本发明提供新的鸟苷酸环化酶-C激动剂肽及其在治疗包括胃肠道疾病，炎症或癌症（例如胃肠癌））的人类疾病中的用途。 肽可以单独施用或与cGMP依赖性磷酸二酯酶抑制剂组合施用。 胃肠道疾病可以分为肠易激综合征，便秘或过度酸度等。胃肠道疾病可分为炎症性肠病或其他胃肠道疾病，包括克罗恩病和溃疡性结肠炎，以及癌症。

公开(公告)号：US20060154868A1

公开(公告)日：2006-07-13

申请号：US11347115

申请日：2006-02-02

Applicant: Kunwar Shailubhai ,  Gregory Nikiforovich ,  Gary Jacob

Inventor： Kunwar Shailubhai ,  Gregory Nikiforovich ,  Gary Jacob

IPC: A61K38/17 ,  A61K38/10 ,  C07K14/705 ,  C07K7/08

CPC classification number: C07K7/64 ,  A61K38/00 ,  A61K38/10 ,  A61K38/12 ,  A61K45/06 ,  A61K47/60 ,  C07K7/08 ,  C07K7/50 ,  C07K2299/00 ,  Y02A50/473

Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis. Thus, the method may be used to treat, inter alia, inflammation, including gastrointestinal inflammatory disorders, general organ inflammation and asthma, and carcinogenesis of the lung, gastrointestinal tract, bladder, testis, prostate and pancreas, or polyps.

公开(公告)号：US20140155575A1

公开(公告)日：2014-06-05

申请号：US14001638

申请日：2012-03-01

Applicant: Juncai Bai ,  Ruoping Zhang ,  Jun Jian ,  Junfeng Zhou ,  Qiao Zhao ,  Guoquing Zhang ,  Kunwar Shailubhai ,  Stephen Comiskey ,  Rong Feng

Inventor： Juncai Bai ,  Ruoping Zhang ,  Jun Jian ,  Junfeng Zhou ,  Qiao Zhao ,  Guoquing Zhang ,  Kunwar Shailubhai ,  Stephen Comiskey ,  Rong Feng

IPC: C07K7/64 ,  C07K7/08

CPC classification number: C07K7/64 ,  C07K7/08 ,  C07K14/195

Abstract: The invention provides processes of preparing a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-249 described herein.

Abstract translation: 本发明提供制备包含选自本文所述的SEQ ID NO：1-249的GCC激动剂序列的肽的方法。

公开(公告)号：US08357775B2

公开(公告)日：2013-01-22

申请号：US13467703

申请日：2012-05-09

Applicant: Kunwar Shailubhai ,  Gary S. Jacob

Inventor： Kunwar Shailubhai ,  Gary S. Jacob

IPC: A61K38/10 ,  A61K38/04

CPC classification number: C07K7/64 ,  A61K38/04 ,  A61K45/06 ,  C07K7/08 ,  A61K2300/00

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.

公开(公告)号：US07879802B2

公开(公告)日：2011-02-01

申请号：US12133344

申请日：2008-06-04

Applicant: Kunwar Shailubhai ,  Gary S. Jacob

Inventor： Kunwar Shailubhai ,  Gary S. Jacob

IPC: A61K38/00

CPC classification number: C07K7/08 ,  A61K9/0031 ,  A61K9/02 ,  A61K9/08 ,  A61K31/192 ,  A61K31/519 ,  A61K38/10 ,  A61K38/12 ,  A61K45/06 ,  A61K47/02 ,  A61K47/60 ,  C07K7/64

Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition, including Crohn's disease and ulcerative colitis, and cancer.

Abstract translation: 本发明提供新的鸟苷酸环化酶-C激动剂肽及其在治疗包括胃肠道疾病，炎症或癌症（例如胃肠癌））的人类疾病中的用途。 肽可以单独施用或与cGMP依赖性磷酸二酯酶抑制剂组合施用。 胃肠道疾病可以分为肠易激综合征，便秘或过度酸度等。胃肠道疾病可分为炎症性肠病或其他GI病症，包括克罗恩病和溃疡性结肠炎，以及癌症。

公开(公告)号：US20100152118A1

公开(公告)日：2010-06-17

申请号：US12630654

申请日：2009-12-03

Applicant: Kunwar Shailubhai

Inventor： Kunwar Shailubhai

IPC: A61K38/10 ,  A61P3/00 ,  A61P9/00 ,  A61P3/04 ,  A61P5/00

CPC classification number: A61K38/10 ,  A61K45/06 ,  A61K47/60 ,  A61P35/00 ,  C07K7/08

Abstract: This invention also provides a method to prevent, control, and treata lipid metabolism disorder, a billary disorder, cardiovascular disease, obesity or an endocrine disorder by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound typically used to treat the disorder and or with an inhibitor of cGMP-dependent phosphodieasterases.

Abstract translation: 本发明还提供一种通过单独给予至少一种鸟苷酸环化酶受体的激动剂或与通常用于治疗的化合物组合的方法，来预防，控制和调节脂质代谢紊乱，结肠疾病，心血管疾病，肥胖症或内分泌疾病 治疗疾病和/或与cGMP依赖性磷酸二酯酶的抑制剂。

公开(公告)号：US20070015780A1

公开(公告)日：2007-01-18

申请号：US10548794

申请日：2004-03-10

Applicant: Donald Picker ,  Geoffrey Henson ,  Simon Fricker ,  Kunwar Shailubhai ,  Gary Jacob

Inventor： Donald Picker ,  Geoffrey Henson ,  Simon Fricker ,  Kunwar Shailubhai ,  Gary Jacob

IPC: A61K31/4747 ,  A61K31/403

CPC classification number: A61K31/403 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4747 ,  A61K45/06 ,  A61K2300/00

Abstract: A method of treating cancer by administering a therapeutically effective amount of a compound represented by the following Formula (I), or salt, hydrate, or solvate thereof; wherein: n represents a number from 3 to 7; m represents a number from 1 to 2; R1 and R2 independently represent a hydrogen atom or are a substituted or unsubstituted, branched or unbranched or cyclic, alkyl provided that the total number of carbon atoms represented by R1 and R2 when taken together is no less than 5 and no greater than 10; or R1 and R2 together independently represent a cyclic alkyl group having no less than 3 or no more than 7 carbon atoms; R3 and R4 independently represent a hydrogen atom or a saturated or unsaturated, substituted or unsubstituted, branched or unbranched or cyclic, hydrocarbyl radical.

Abstract translation: 通过施用治疗有效量的由下式（I）表示的化合物或其盐，水合物或溶剂合物来治疗癌症的方法; 其中：n表示3〜7的数; m表示1〜2的数; R 1和R 2独立地表示氢原子，或者是取代或未取代的，支链或非支链或环状烷基，条件是由R 1表示的碳原子总数， 当共在一起时，SUB> 1和R 2 2不小于5且不大于10; 或R 1和R 2共同独立地表示具有不少于3个或不超过7个碳原子的环状烷基; R 3和R 4独立地表示氢原子或饱和或不饱和的取代或未取代的支链或非支链或环状烃基。

公开(公告)号：US20050250801A1

公开(公告)日：2005-11-10

申请号：US10796292

申请日：2004-03-10

Applicant: Kunwar Shailubhai ,  Gary Jacob ,  Donald Picker ,  Geoffrey Henson ,  Simon Fricker

Inventor： Kunwar Shailubhai ,  Gary Jacob ,  Donald Picker ,  Geoffrey Henson ,  Simon Fricker

IPC: A61K20060101 ,  A61K31/403 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4747 ,  A61K38/00 ,  A61K45/06

CPC classification number: A61K31/403 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4747 ,  A61K45/06 ,  A61K2300/00

Abstract: A method of treating cancer by administering a therapeutically effective amount of a compound represented by the following Formula (I), or salt, hydrate, or solvate thereof: wherein: n represents a number from 3 to 7; m represents a number from 1 to 2; R1 and R2 independently represent a hydrogen atom or are a substituted or unsubstituted, branched or unbranched or cyclic, alkyl provided that the total number of carbon atoms represented by R1 and R2 when taken together is no less than 5 and no greater than 10; or R1 and R2 together independently represent a cyclic alkyl group having no less than 3 or no more than 7 carbon atoms; R3 and R4 independently represent a hydrogen atom or a saturated or unsaturated, substituted or unsubstituted, branched or unbranched or cyclic, hydrocarbyl radical.

Abstract translation: 通过给予治疗有效量的由下式（I）表示的化合物或其盐，水合物或溶剂合物来治疗癌症的方法：其中：n表示3至7的数; m表示1〜2的数; R 1和R 2独立地表示氢原子，或者是取代或未取代的，支链或非支链或环状烷基，条件是由R 1表示的碳原子总数， 当共在一起时，SUB> 1和R 2 2不小于5且不大于10; 或R 1和R 2共同独立地表示具有不少于3个或不超过7个碳原子的环状烷基; R 3和R 4独立地表示氢原子或饱和或不饱和的取代或未取代的支链或非支链或环状烃基。