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1. 发明授权

US10238712B2 Compositions useful for the treatment of gastrointestinal disorders 有权
公开(公告)号：US10238712B2
公开(公告)日：2019-03-26
申请号：US15272873
申请日：2016-09-22
申请人： Synergy Pharmaceuticals, Inc.
发明人： Kunwar Shailubhai
IPC分类号： A61K38/00 , A61K38/10 , A61K45/06 , C07K7/08 , C07K14/00 , A61K38/04 , A61K31/196 , A61K31/4402 , A61K47/55 , A61K47/64
摘要： This invention provides novel peptides and methods to prevent, control, and treat an inflammation, cancer and other disorders, particularly of the gastrointestinal tract and the lung by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound selected from i) 5-aminosalicyclic acid (5-ASA) or a derivative or a pharmaceutically acceptable salt thereof; ii) mercaptopurine; or iii) an anti-TNF therapy.

2. 发明授权

US10011637B2 Ultra-pure agonists of guanylate cyclase C, method of making and using same 有权
公开(公告)号：US10011637B2
公开(公告)日：2018-07-03
申请号：US14896019
申请日：2014-06-05
申请人： Synergy Pharmaceuticals, Inc.
发明人： Kunwar Shailubhai , Stephen Comiskey , Rong Feng , Juncai Bai , Ruoping Zhang , Jun Jia , Junfeng Zhou , Qiao Zhao , Guoqing Zhang
IPC分类号： C07K1/14 , C07K7/08 , C12N9/88 , B01D15/42
摘要： The invention provides processes of purifying a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-251 described herein. The processes include a solvent exchange step before a freeze-drying (lyophilization) step.

3. 发明授权

US09914752B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
公开(公告)号：US09914752B2
公开(公告)日：2018-03-13
申请号：US15049740
申请日：2016-02-22
申请人： SYNERGY PHARMACEUTICALS, INC.
发明人： Kunwar Shailubhai , Gary S. Jacob
IPC分类号： A61K38/00 , C07K7/08 , A61K47/60 , A61K47/48 , C07K7/64 , A61K31/192 , A61K31/519 , A61K38/10 , A61K9/00 , A61K9/02 , A61K9/08 , A61K47/02 , A61K45/06
CPC分类号： C07K7/08 , A61K9/0031 , A61K9/02 , A61K9/08 , A61K31/192 , A61K31/519 , A61K38/10 , A61K38/12 , A61K45/06 , A61K47/02 , A61K47/60 , C07K7/64
摘要： 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.

4. 发明授权

US09505805B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
公开(公告)号：US09505805B2
公开(公告)日：2016-11-29
申请号：US14632314
申请日：2015-02-26
申请人： SYNERGY PHARMACEUTICALS, INC.
发明人： Kunwar Shailubhai
IPC分类号： A61K38/00 , C07K16/00 , C07K7/08 , C07K7/64 , A61K38/10 , A61K45/06
CPC分类号： C07K7/08 , A61K38/00 , A61K38/10 , A61K45/06 , C07K7/64
摘要： 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.

5. 发明授权

US09486494B2 Compositions useful for the treatment of gastrointestinal disorders 有权
标题翻译：可用于治疗胃肠道疾病的组合物
公开(公告)号：US09486494B2
公开(公告)日：2016-11-08
申请号：US14207749
申请日：2014-03-13
申请人： Synergy Pharmaceuticals Inc.
发明人： Kunwar Shailubhai
IPC分类号： A61K38/00 , C07K9/00 , A61K38/10 , A61K45/06 , A61K47/48 , C07K7/08 , C07K14/00 , A61K38/04
CPC分类号： A61K38/10 , A61K31/196 , A61K31/4402 , A61K38/04 , A61K45/06 , A61K47/55 , A61K47/64 , C07K7/08 , C07K14/00
摘要： This invention provides novel peptides and methods to prevent, control, and treat an inflammation, cancer and other disorders, particularly of the gastrointestinal tract and the lung by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound selected from i) 5-aminosalicyclic acid (5-ASA) or a derivative or a pharmaceutically acceptable salt thereof; ii) mercaptopurine; or iii) an anti-TNF therapy.
摘要翻译：本发明提供新颖的肽和方法，通过单独给予至少一种鸟苷酸环化酶受体的激动剂或与选自以下的化合物组合来预防，控制和治疗炎症，癌症和其它疾病，特别是胃肠道和肺部疾病。 i）5-氨基水杨酸（5-ASA）或其衍生物或药学上可接受的盐; ii）巯基嘌呤; 或iii）抗TNF治疗。

6. 发明授权

US09266926B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
公开(公告)号：US09266926B2
公开(公告)日：2016-02-23
申请号：US14528257
申请日：2014-10-30
申请人： SYNERGY PHARMACEUTICALS, INC.
发明人： Kunwar Shailubhai , Gary S. Jacob
IPC分类号： C07K14/00 , C07K7/64 , A61K47/48 , C07K7/08 , A61K31/192 , A61K31/519 , A61K38/10
CPC分类号： C07K7/08 , A61K9/0031 , A61K9/02 , A61K9/08 , A61K31/192 , A61K31/519 , A61K38/10 , A61K38/12 , A61K45/06 , A61K47/02 , A61K47/60 , C07K7/64
摘要： 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.

7. 发明授权

US09238677B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
标题翻译：鸟苷酸环化酶的激动剂可用于治疗胃肠道疾病，炎症，癌症和其他疾病
公开(公告)号：US09238677B2
公开(公告)日：2016-01-19
申请号：US14228843
申请日：2014-03-28
申请人： Synergy Pharmaceuticals Inc.
发明人： Kunwar Shailubhai , Gary S. Jacob
IPC分类号： C07K14/00 , C07K7/64 , A61K47/48 , C07K7/08 , A61K31/192 , A61K31/519 , A61K38/10
CPC分类号： C07K7/08 , A61K9/0031 , A61K9/02 , A61K9/08 , A61K31/192 , A61K31/519 , A61K38/10 , A61K38/12 , A61K45/06 , A61K47/02 , A61K47/60 , C07K7/64
摘要： 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.
摘要翻译：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。

8. 发明授权

US08716224B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
标题翻译：鸟苷酸环化酶的激动剂可用于治疗胃肠道疾病，炎症，癌症和其他疾病
公开(公告)号：US08716224B2
公开(公告)日：2014-05-06
申请号：US13010267
申请日：2011-01-20
申请人： Kunwar Shailubhai , Gary S. Jacob
发明人： Kunwar Shailubhai , Gary S. Jacob
IPC分类号： A61K38/00
CPC分类号： C07K7/08 , A61K9/0031 , A61K9/02 , A61K9/08 , A61K31/192 , A61K31/519 , A61K38/10 , A61K38/12 , A61K45/06 , A61K47/02 , A61K47/60 , C07K7/64
摘要： 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.
摘要翻译：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。

9. 发明授权

US08637451B2 Guanylate cyclase receptor agonists for the treatment of tissue inflammation and carcinogenesis 有权
标题翻译：鸟苷酸环化酶受体激动剂用于治疗组织炎症和致癌作用
公开(公告)号：US08637451B2
公开(公告)日：2014-01-28
申请号：US13339785
申请日：2011-12-29
申请人： Kunwar Shailubhai , Gregory Nikiforovich , Gary S. Jacob
发明人： Kunwar Shailubhai , Gregory Nikiforovich , Gary S. Jacob
IPC分类号： A61K38/12
CPC分类号： C07K7/64 , A61K38/00 , A61K38/10 , A61K38/12 , A61K45/06 , A61K47/60 , C07K7/08 , C07K7/50 , C07K2299/00 , Y02A50/473
摘要： 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.
摘要翻译：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。

10. 发明授权

US08497348B2 Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders 有权
公开(公告)号：US08497348B2
公开(公告)日：2013-07-30
申请号：US13716874
申请日：2012-12-17
申请人： Synergy Pharmaceuticals Inc.
发明人： Kunwar Shailubhai , Gary S. Jacob
IPC分类号： A61K38/00 , A61K38/10
CPC分类号： C07K7/64 , A61K38/04 , A61K45/06 , C07K7/08 , A61K2300/00
摘要： 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.

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