-
公开(公告)号：US20120028888A1
公开(公告)日：2012-02-02
申请号：US13127428
申请日：2009-11-04
申请人： Jay Janz , Athan Kuliopulos , Thomas J. McMurry
发明人： Jay Janz , Athan Kuliopulos , Thomas J. McMurry
IPC分类号： A61K38/16 , C07K7/06 , C07K7/08 , C07K14/00 , C07K5/10 , A61K38/03 , A61K38/04 , A61K38/08 , A61K38/10 , A61P9/12 , A61P9/10 , A61P35/00 , A61P35/04 , A61P3/10 , A61P3/04 , A61P37/00 , A61P31/18 , C07K5/08
CPC分类号： C07K14/7158 , A61K38/00 , A61K47/542 , A61K47/554
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.
摘要翻译： 本发明一般涉及G蛋白偶联受体apelin（也称为APJ受体）的变构调节剂（例如，负变构和正变构调节剂，变构激动剂和前变体调节剂）的化合物。 APJ受体化合物衍生自APJ受体的细胞内环和结构域。 本发明还涉及这些APJ受体化合物和包含APJ受体化合物的药物组合物在治疗与APJ受体调节有关的疾病和病症如心脏病（例如高血压和张力和心力衰竭，例如充血性 心力衰竭），癌症，糖尿病，干细胞运输，流体体内平衡，细胞增殖，免疫功能，肥胖，转移性疾病和HIV感染。
-
公开(公告)号：US09096646B2
公开(公告)日：2015-08-04
申请号：US13127443
申请日：2009-11-04
IPC分类号： C07K7/08 , C07K14/715 , C07K7/06 , A61K38/00
CPC分类号： C07K7/08 , A61K38/00 , C07K7/06 , C07K14/7158
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CXCR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow transplantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.
摘要翻译： 本发明一般涉及用于间质衍生因子1（SDF-1）（也称为CXCR4受体）的G蛋白偶联受体的变构调节剂（例如，正和负变构调节剂和变构兴奋剂）的化合物。 CXCR4受体化合物衍生自CXCR4受体的细胞内环和结构域。 本发明还涉及这些CXCR4受体化合物和包含CXCR4受体化合物的药物组合物在治疗与CXCR4调节相关的疾病和病症如骨髓移植，化学敏化，癌症，转移性疾病，炎性疾病，HIV感染和 干细胞再生医学。
-
公开(公告)号：US20110300167A1
公开(公告)日：2011-12-08
申请号：US13127666
申请日：2009-11-04
IPC分类号： A61P37/00 , C07K7/08 , C07K7/06 , A61P35/02 , A61P35/04 , A61K38/17 , A61P37/02 , A61P19/04 , A61P31/18 , A61P29/00 , A61K38/10 , A61K38/08 , C07K14/435 , A61P25/00
CPC分类号： C07K14/7158 , A61K38/00
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor CXCR5. The CXCR5 receptor compounds are derived from the intracellular loops and domains of the CXCR5 receptor. The invention also relates to the use of these CXCR5 receptor compounds and pharmaceutical compositions comprising the CXCR5 receptor compounds in the treatment of diseases and conditions associated with CXCR5 receptor modulation such as autoimmune diseases including lupus, HIV and rheumatoid arthritis, Primary Sjogren's Syndrome, chronic lymphocytic leukemia, Burkitt Lymphoma, colon and breast cancer tumor metastasis, Multiple Sclerosis and compromised immune function.
摘要翻译： 本发明一般涉及G蛋白偶联受体CXCR5的变构调节剂（例如，负变构和正变构调节剂，变构兴奋剂和前变体调节剂）的化合物。 CXCR5受体化合物衍生自CXCR5受体的细胞内环和结构域。 本发明还涉及这些CXCR5受体化合物和包含CXCR5受体化合物的药物组合物在治疗与CXCR5受体调节相关的疾病和病症的应用，例如包括狼疮，HIV和类风湿性关节炎的自身免疫性疾病，原发性干燥综合征，慢性淋巴细胞 白血病，伯基特淋巴瘤，结肠癌和乳腺癌肿瘤转移，多发性硬化和免疫功能受损。
-
公开(公告)号：US20130210709A1
公开(公告)日：2013-08-15
申请号：US13127443
申请日：2009-11-04
IPC分类号： C07K7/08 , C07K14/715 , C07K7/06
CPC分类号： C07K7/08 , A61K38/00 , C07K7/06 , C07K14/7158
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CX-CR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow trans-plantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.
摘要翻译： 本发明一般涉及用于间质衍生因子1（SDF-1）（也称为CX-CR4受体）的G蛋白偶联受体的变构调节剂（例如，正和负变构调节剂和变构兴奋剂）的化合物。 CXCR4受体化合物衍生自CXCR4受体的细胞内环和结构域。 本发明还涉及这些CXCR4受体化合物和包含CXCR4受体化合物的药物组合物在治疗与CXCR4调节相关的疾病和病症如骨髓转移，化学敏化，癌症，转移性疾病，炎性疾病，HIV 感染和干细胞再生医学。
-
公开(公告)号：US20110301087A1
公开(公告)日：2011-12-08
申请号：US13127602
申请日：2009-11-04
IPC分类号： A61K38/17 , C07K7/06 , C07K7/08 , C07K14/435 , A61P1/00 , A61K38/06 , A61P25/22 , A61P25/30 , A61P25/28 , A61P15/06 , A61K38/10 , A61K38/08 , C07K5/08 , A61P25/00
CPC分类号： C07K14/57509 , A61K38/00 , A61K47/542 , A61K47/543
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor for corticotrophin releasing hormone (or factor) receptor 1, also known as the CRF1, CRHR1, CRFR1, CRHR, CRF-R. The CRF1 receptor compounds are derived from the intracellular loops and domains of CRF1 receptor. The invention also relates to the use of these CRF1 receptor compounds and pharmaceutical compositions comprising the CRF1 receptor compounds in the treatment of diseases and conditions associated with CRF1 receptor modulation, such as inflammatory bowel disease (peripherally acting), irritable bowel syndrome (IBS), stress response (colonic motor activity), anxiety, sleep disorder, addictive behavior, acute and chronic neurodegeneration, preterm labor and pain.
摘要翻译： 本发明一般涉及用于促肾上腺皮质激素释放激素（或因子）受体1（也称为CRF1）的G蛋白偶联受体的变构调节剂（例如，负变构和正变构调节剂，变构激动剂和前变体调节剂） ，CRHR1，CRFR1，CRHR，CRF-R。 CRF1受体化合物衍生自CRF1受体的细胞内环和结构域。 本发明还涉及这些CRF1受体化合物和包含CRF1受体化合物的药物组合物在治疗与CRF1受体调节有关的疾病和病症（例如炎性肠病（外周作用）），肠易激综合征（IBS）， 压力反应（结肠运动活动），焦虑症，睡眠障碍，成瘾行为，急性和慢性神经变性，早产和疼痛。
-
公开(公告)号：US20110294738A1
公开(公告)日：2011-12-01
申请号：US13127694
申请日：2009-11-04
申请人： Yong Ren , Athan Kuliopulos , Thomas J. McMurry
发明人： Yong Ren , Athan Kuliopulos , Thomas J. McMurry
IPC分类号： A61K38/10 , C07K7/06 , C07K14/00 , A61K38/08 , A61P35/04 , A61P25/00 , A61P17/00 , A61P25/18 , A61P35/00 , C07K7/08 , A61P19/10
CPC分类号： C07K14/72 , A61K38/00 , A61K47/542
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor PTHR1, also known as parathyroid hormone/parathyroid hormone related protein receptor. The PTHR1 compounds are derived from the intracellular loops and domains of the PTHR1 receptor. The invention also relates to the use of these PTHR1 receptor compounds and pharmaceutical compositions comprising the PTHR1 receptor compounds in the treatment of diseases and conditions associated with PTHR1 receptor modulation, such as osteoporosis; humoral hypercalcemia of malignancy; osteolytic and osteoblastic metastasis to bone; primary and secondary hyperparathyroidism associated increase in bone absorption; vascular calcification; psychiatric disorders and cognitive disorders associated with hyperparathyroidism; dermatological disorders; and excess hair growth.
摘要翻译： 本发明一般涉及G蛋白偶联受体PTHR1（也称为甲状旁腺激素/甲状旁腺激素相关蛋白受体）的变构调节剂（例如，负变构和正变构调节剂，变构兴奋剂和前变体调节剂）的化合物。 PTHR1化合物衍生自PTHR1受体的细胞内环和结构域。 本发明还涉及这些PTHR1受体化合物和包含PTHR1受体化合物的药物组合物在治疗与PTHR1受体调节相关的疾病和病症如骨质疏松症中的用途; 体液性高钙血症恶性肿瘤; 骨质疏松和成骨细胞转移; 原发性和继发性甲状旁腺功能亢进相关的骨吸收增加; 血管钙化; 与甲状旁腺功能亢进相关的精神疾病和认知障碍; 皮肤病; 和头发生长过多。
-
7.发明申请G PROTEIN COUPLED RECEPTOR ANTAGONISTS AND METHODS OF ACTIVATING AND INHIBITING G PROTEIN COUPLED RECEPTORS USING THE SAME 有权G蛋白偶联受体拮抗剂和使用该蛋白激活和抑制G蛋白偶联受体的方法公开(公告)号：US20090270322A1
公开(公告)日：2009-10-29
申请号：US12394715
申请日：2009-02-27
申请人： Athan Kuliopulos , Lidija Covic
发明人： Athan Kuliopulos , Lidija Covic
CPC分类号： G01N33/567 , A61K38/00 , C07K14/705 , C07K14/723
摘要： The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.
摘要翻译： 本发明一般涉及G蛋白偶联受体，特别涉及G蛋白受体的激动剂和拮抗剂及其使用方法。
-
公开(公告)号：US20060166274A1
公开(公告)日：2006-07-27
申请号：US11075645
申请日：2005-03-07
申请人： Athan Kuliopulos , Lidija Covic
发明人： Athan Kuliopulos , Lidija Covic
IPC分类号： G01N33/53 , C07H21/04 , C12P21/06 , C07K14/705
CPC分类号： C07K14/723 , A61K38/00 , C07K14/705
摘要： The invention relates generally to G protein coupled receptors and in particular to agonists and antagonists of G protein receptors and methods of using the same.
-
公开(公告)号：US5648244A
公开(公告)日：1997-07-15
申请号：US127692
申请日：1993-09-27
CPC分类号： C12N9/644 , C07K14/39 , C12N15/62 , C12N9/90 , C12Y304/21022 , C07K2319/00 , C07K2319/23 , C07K2319/75
摘要： A method for producing a fusion peptide. A vector is provided with nucleic acid encoding a carrier peptide and at the 3' end of the nucleic acid, a unidirectional restriction endonuclease cleavage site recognized by a restriction endonuclease with the ability to create a non-palindromic 3-base overhang. The vector is cleaved with the restriction endonuclease to produce a cleaved vector. One or more nucleic acids encoding a desired peptide and having at least a 3-base overhang at each end configured and arranged for ligation with the cleaved vector is then ligated to the cleavage site.
摘要翻译： 一种融合肽的制备方法。 向载体提供编码载体肽的核酸，并且在核酸的3'末端，由限制性内切核酸酶识别的单向限制性内切核酸酶切割位点具有产生非回文性3-碱基突出端的能力。 用限制性内切核酸酶切割载体以产生切割的载体。 编码所需肽并且在每个末端具有至少3个碱基突出端的一个或多个核酸被配置并排列用于与切割的载体连接，然后连接到切割位点。
-
公开(公告)号：US10913781B2
公开(公告)日：2021-02-09
申请号：US14009479
申请日：2012-04-09
申请人： Athan Kuliopulos , Lidija Covic
发明人： Athan Kuliopulos , Lidija Covic
IPC分类号： C07K14/705 , A61K38/00
摘要： Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.
-
-
-
-
-
-
-
-
-
搜索结果
22 条记录 (耗时 0.027 秒)
