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1. 发明授权

US11179455B2 Use of a growth hormone secretagogue peptide as a vaccine adjuvant 有权
公开(公告)号：US11179455B2
公开(公告)日：2021-11-23
申请号：US16346034
申请日：2017-10-30
申请人： CENTRO DE INGENIERIA GENÉTICA BIOTECNOLOGIA
发明人： Rebeca Martínez Rodríguez , Liz Hernandez Perez , Lázaro Gil González , Yamila Carpio González , Mario Pablo Estrada García
IPC分类号： A61K39/12 , A61P31/12 , A61K38/25 , A61K39/00
摘要： The present invention is related to the use of the GHRP-6 and one structural analogue as molecular adjuvants for vaccines. Among other applications, these vaccines may be employed for preventing diseases caused by infectious agents, like viruses, bacteria and ectoparasites, that affect mammals, birds and aquatic organisms. The GHRP-6 and its analogue A233 are effectives as adjuvants when they are combine with a given antigen, since they enhance the specific immune response against it.

2. 发明申请

US20210177943A1 GHRH OR ANALOGUES THEREOF FOR USE IN TREATMENT OF HEPATIC DISEASE 有权
公开(公告)号：US20210177943A1
公开(公告)日：2021-06-17
申请号：US17170579
申请日：2021-02-08
申请人： The General Hospital Corporation
发明人： Steven K. GRINSPOON
IPC分类号： A61K38/25 , A61P1/16
摘要： The present application relates to novel methods for preventing, slowing the progression of, or treating nonalcoholic fatty liver (NAFL), nonalcoholic steatohepatitis (NASH), and/or liver fibrosis, and/or reducing the risks of liver cancer in subjects, such as HIV-infected subjects, using a GHRH molecule, e.g., trans-3-hexenoyl-GHRH(1-44)-NH2, or a pharmaceutically acceptable salt thereof. The subjects may have particular pathological features such as liver fibrosis, a hepatic fat fraction (HFF) of at least about 10%, serum alanine aminotransferase (ALT) levels of at least about 30 U/L, and/or a NAFLD Activity Score (NAS) of at least 4 or 5.

3. 发明授权

US10111929B1 Growth hormone releasing factor analogs and uses 有权
公开(公告)号：US10111929B1
公开(公告)日：2018-10-30
申请号：US15482592
申请日：2017-04-07
申请人： EZ IP, LLC
发明人： Chanda Zaveri , Joey D. Edge
IPC分类号： A61K38/25 , A61K38/08 , C07K7/06 , C07K7/00 , C07K14/60 , C07K14/00 , A61K47/48
摘要： Growth hormone releasing factor (GHRF) analogs that can be used to induce endogenous growth hormone secretion are disclosed, as well as pharmaceutical compositions comprising the GHRF analogs and methods of using the GHRF analogs.

4. 发明授权

US09988428B2 Pegylated bioactive peptides and uses thereof 有权
公开(公告)号：US09988428B2
公开(公告)日：2018-06-05
申请号：US15490618
申请日：2017-04-18
申请人： GRIFFON PHARMACEUTICALS INC.
发明人： Krishna G. Peri
IPC分类号： A61K38/25 , C07K14/60 , A61K47/48
CPC分类号： C07K14/60 , A61K38/25 , A61K47/48215 , A61K47/60
摘要： Described herein are bioactive peptides that are modified at one or more positions with a PEG moiety. An example of such a PEGylated bioactive peptide is a GHRH analog that is modified at one or more positions with a PEG moiety. Also described are pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising such analogs or salts thereof, as well as methods, kits and uses thereof, for example for inducing or stimulating growth hormone secretion in a subject and for diagnosing, preventing or treating GH-deficient conditions in a subject.

5. 发明授权

US09987333B2 Method for suppressing malignant tumor metastasis 有权
公开(公告)号：US09987333B2
公开(公告)日：2018-06-05
申请号：US15270669
申请日：2016-09-20
申请人： Shionogi & Co., Ltd. , National Cerebral and Cardiovascular Center
发明人： Kenji Kangawa , Hiroshi Hosoda , Takashi Nojiri
IPC分类号： A61K38/25 , A61K31/41 , A61K38/22 , A61K45/06 , A61K31/4184 , A61K31/47 , A61K33/24 , A61K31/4178 , A61K31/4245 , A61K31/555 , A61K31/473
CPC分类号： A61K38/25 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/4245 , A61K31/47 , A61K31/473 , A61K31/555 , A61K33/24 , A61K38/22 , A61K45/06 , A61K2300/00
摘要： A medicinal composition for suppressing or preventing the metastasis of a malignant tumor, the composition comprising, as an active ingredient, at least one kind of vasoprotective agent selected from the following (i) to (iv): (i) angiotensin II receptor antagonist, (ii) HMG-CoA reductase inhibitor, (iii) ghrelin or its derivative, and (iv) adrenomedullin or its derivative; or a pharmacologically acceptable salt thereof.

6. 发明授权

US09381159B2 Microspheres for controlled- or sustained-release delivery of therapeutics 有权
标题翻译：控制或持续释放治疗剂的微球
公开(公告)号：US09381159B2
公开(公告)日：2016-07-05
申请号：US14362575
申请日：2012-12-05
申请人： Tuo Jin , Zhenhua Hu , Weien Yuan
发明人： Tuo Jin , Zhenhua Hu , Weien Yuan
IPC分类号： A61K38/16 , A61K9/50 , A61P3/10 , A61K9/16 , A61K38/22 , A61K38/23 , A61K38/25 , A61K38/26 , A61K38/31
CPC分类号： A61K9/1647 , A61K9/1611 , A61K9/1694 , A61K38/22 , A61K38/23 , A61K38/25 , A61K38/26 , A61K38/31
摘要： A new microsphere formulation (composition) for controlled- or sustained-release delivery of therapeutic ingredient(s), mainly peptides and proteins not over 10K in molecular weight, comprises at least a therapeutic ingredient, a helping agent (such as PH sensitive agent whose solubility is a function of pH) and a biodegradable polymer. The therapeutic ingredient(s) and the helping agent are in the form of fine particles, less than 1O um in diameter, encapsulated in the polymer which forms the microsphere matrix. A method for preparing the composition comprises a step of in-situ precipitating the therapeutic ingredient(s) and the helping agent to the fine particles and successive steps for forming the microspheres. Such a microsphere formulation offers a well-controlled release profile for prolonged period and encapsulation efficiency over 95%.
摘要翻译：治疗成分（主要是分子量不超过10K的肽和蛋白质）的受控或持续释放递送的新微球制剂（组合物）至少包含治疗成分，助剂（例如PH敏感剂溶解度是pH的函数）和可生物降解的聚合物。治疗成分和助剂为直径小于10μm的细颗粒形式，包封在形成微球基质的聚合物中。制备组合物的方法包括将治疗成分和辅助剂原位沉淀到细颗粒和用于形成微球的连续步骤的步骤。这种微球制剂提供了良好控制的释放曲线，其延长的时间和包封效率超过95％。

7. 发明申请

US20160166652A1 NOVEL N- AND C-TERMINAL SUBSTITUTED ANTAGONISTIC ANALOGS OF GH-RH 审中-公开
标题翻译：新型N-和C-末端取代的GH-RH的拮抗剂模拟物
公开(公告)号：US20160166652A1
公开(公告)日：2016-06-16
申请号：US14971445
申请日：2015-12-16
申请人： UNIVERSITY OF MIAMI , U.S.A., REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS
发明人： Andrew V. SCHALLY , Marta ZARANDI , Jozsef L. VARGA , Ren Zhi CAI
IPC分类号： A61K38/25
CPC分类号： A61K38/25 , A61K38/00 , C07K14/60 , C07K14/645
摘要： There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and β-Ala, Amc, Apa, Ada, AE2A, AE4P, ε-Lys(α-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
摘要翻译：提供了一系列hGH-RH（1-29）NH2（SEQ ID NO：1）和hGH-RH（1-30）NH2的合成类似物。特别感兴趣的是携带PhAc，N-Me-Aib，Dca，Ac-Ada，Fer，Ac-Amc，Me-NH-Sub，PhAc-Ada，Ac-Ada-D-Phe，Ac-Ada-Phe， Dca-Ada，Dca-Amc，Nac-Ada，Ada-Ada或CH 3 - （CH 2）10-CO-Ada，在N-Terminus和-Ab，-Ala，Amc，Apa，Ada，AE2A，AE4P， ; -Lys（α-NH2），Agm，Lys（Oct）或Ahx。这些类似物通过对癌和非恶性细胞的直接作用，抑制哺乳动物垂体中生长激素的释放以及抑制人类癌症的增殖，并抑制各种器官的增生和良性增生性疾病。与之前描述的相比，新类似物的更强的抑制效力是由于各种氨基酸的替换而产生的。

8. 发明授权

US09339545B2 Stable formulations for parenteral injection of peptide drugs 有权
公开(公告)号：US09339545B2
公开(公告)日：2016-05-17
申请号：US14192697
申请日：2014-02-27
申请人： Xeris Pharmaceuticals, Inc.
发明人： Steven Prestrelski , John Kinzell
IPC分类号： A61K47/22 , A61K47/20 , A61K38/26 , A61K47/26 , A61K9/00 , A61K9/19 , A61K38/22 , A61K38/28 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K38/09 , A61K38/16 , A61K38/17 , A61K38/18 , A61K38/25 , A61K38/29 , A61K38/30 , A61K38/48
CPC分类号： A61K38/28 , A61K9/0019 , A61K9/19 , A61K38/02 , A61K38/09 , A61K38/16 , A61K38/17 , A61K38/1709 , A61K38/1816 , A61K38/22 , A61K38/2207 , A61K38/25 , A61K38/26 , A61K38/29 , A61K38/30 , A61K38/4893 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/36
摘要： Stable formulations for parenteral injection of peptide drugs and methods of using such stable formulations are provided. In particular, the present invention provides stable formulations for parenteral injection of glucagon and methods of using such glucagon formulations to treat hypoglycemia, especially severe hypoglycemia in emergency situations.

9. 发明授权

US09315546B2 Growth hormone secretatogue receptor antagonists and uses thereof 有权
标题翻译：生长激素分泌受体拮抗剂及其用途
公开(公告)号：US09315546B2
公开(公告)日：2016-04-19
申请号：US13704052
申请日：2011-06-16
申请人： Cyril Y. Bowers , David H. Coy , Simon J. Hocart , Gloria S. Tannenbaum
发明人： Cyril Y. Bowers , David H. Coy , Simon J. Hocart , Gloria S. Tannenbaum
IPC分类号： A61K38/08 , A61K38/10 , A61K38/16 , A61K38/22 , C07K14/575 , A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/04 , C07K7/08 , A61K38/03 , C07K14/475 , A61K38/25 , C07K5/062 , C07K14/60 , C07K5/08 , C07K7/06 , C07K14/00 , C07K14/72
CPC分类号： C07K7/08 , A61K38/00 , A61K38/03 , A61K38/04 , A61K38/08 , A61K38/10 , A61K38/16 , A61K38/25 , C07K5/06026 , C07K5/08 , C07K7/06 , C07K14/00 , C07K14/475 , C07K14/60 , C07K14/723
摘要： The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperpro-liferative disorders.
摘要翻译：本发明提供可以调节生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的新型肽。这些肽可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为用于治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和超高血压疾病。

10. 发明授权

US09302010B2 Stable formulations for parenteral injection of peptide drugs 有权
公开(公告)号：US09302010B2
公开(公告)日：2016-04-05
申请号：US14188464
申请日：2014-02-24
申请人： Xeris Pharmaceuticals, Inc.
发明人： Steven Prestrelski , John Kinzell
IPC分类号： A61K38/29 , A61K38/22 , A61K38/26 , A61K38/28 , A61K47/26 , A61K9/00 , A61K9/19 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/20 , A61K47/22 , A61K38/09 , A61K38/16 , A61K38/17 , A61K38/18 , A61K38/25 , A61K38/30 , A61K38/48
CPC分类号： A61K38/28 , A61K9/0019 , A61K9/19 , A61K38/02 , A61K38/09 , A61K38/16 , A61K38/17 , A61K38/1709 , A61K38/1816 , A61K38/22 , A61K38/2207 , A61K38/25 , A61K38/26 , A61K38/29 , A61K38/30 , A61K38/4893 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/183 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/36
摘要： Stable formulations for parenteral injection of peptide drugs and methods of using such stable formulations are provided. In particular, the present invention provides stable formulations for parenteral injection of glucagon and methods of using such glucagon formulations to treat hypoglycemia, especially severe hypoglycemia in emergency situations.

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