公开(公告)号：US10233209B2

公开(公告)日：2019-03-19

申请号：US15371032

申请日：2016-12-06

Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services ,  The Penn State Research Foundation

Inventor： Frank J. Gonzalez ,  Changtao Jiang ,  Cen Xie ,  Andrew D. Patterson ,  Fei Li ,  James B. Mitchell ,  Shantu Amin ,  Dhimant Desai

IPC: C07J9/00 ,  C07J41/00 ,  C07J31/00

Abstract: Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R1, R2, R4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non-alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal.

公开(公告)号：US20160159851A1

公开(公告)日：2016-06-09

申请号：US14909263

申请日：2014-08-01

Applicant: THE UNITED STATES OF AMEMRICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERV ,  THE PENN STATE RESEARCH FOUNDATION

Inventor： Frank J. Gonzalez ,  Changtao Jiang ,  Cen Xie ,  Andrew D. Patterson ,  Fei Li ,  James B. Mitchell ,  Shantu Amin ,  Dhimant Desai

IPC: C07J41/00

CPC classification number: C07J41/0061 ,  C07J9/005 ,  C07J31/006 ,  C07J41/0055 ,  C07J41/0066

Abstract: Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R1, R2, R4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least Cone compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal.

Abstract translation: 公开了法呢酯X受体的抑制剂，例如式（I），其中R 1，R 2，R 4，X，Y，Z，m和n如本文所定义，其可用于治疗或预防肥胖，2型 糖尿病/胰岛素抵抗和非酒精性脂肪肝疾病。 还公开了包含药学上合适的载体和至少本发明的锥形化合物，哺乳动物中抑制法尼素X受体的方法的方法，以及治疗或预防哺乳动物肥胖的方法的组合物。

公开(公告)号：US20170152283A1

公开(公告)日：2017-06-01

申请号：US15371032

申请日：2016-12-06

Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human Services ,  The Penn State Research Foundation

Inventor： Frank J. Gonzalez ,  Changtao Jiang ,  Cen Xie ,  Andrew D. Patterson ,  Fei Li ,  James B. Mitchell ,  Shantu Amin ,  Dhimant Desai

IPC: C07J41/00 ,  C07J31/00

CPC classification number: C07J41/0061 ,  C07J9/005 ,  C07J31/006 ,  C07J41/0055 ,  C07J41/0066

Abstract: Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R1, R2, R4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non-alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal.

公开(公告)号：US08772274B1

公开(公告)日：2014-07-08

申请号：US13659501

申请日：2012-10-24

Applicant: The Penn State Research Foundation

Inventor： Gavin P. Robertson ,  Subbarao V. Madhunapantula ,  Shantu Amin ,  Dhimant Desai

IPC: A01N43/00 ,  A61K31/33 ,  A01N31/00 ,  A61K31/095 ,  C07C391/00 ,  C07C395/00 ,  A61K31/155 ,  A61K8/23

CPC classification number: C07C391/00 ,  A61K8/23 ,  A61K31/095 ,  A61K31/155 ,  A61K31/33

Abstract: Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: R2-R—R1, where R is phenyl, where R1 is (CH2)n—Se—C(═NH)—NH2, where R2 is (CH2)n—Se—C(═NH)—NH2 or R2 is H, and where each n is independently 2, 3, 4, 5, 6, 7, or 8. Methods of treating a subject are provided according to embodiments of the present invention which include administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject having a condition characterized by Akt dysregulation. Administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject detectably increases apoptosis and/or decreases proliferation of cancer cells, particularly cancer cells characterized by Akt dysregulation. Compositions of the present invention inhibit Akt enzymes, iNOS, and increase MAP kinase activity such that cancer cells contacted with the compositions are inhibited.

Abstract translation: 描述了抗癌组合物和方法，其包括一种或多种具有结构式I的化合物：其中R是苯基，其中R1是（CH2）n-Se-C（= NHN）-NH2，其中R2 是（CH2）n-Se-C（= NH）-NH2或R2是H，并且其中每个n独立地是2,3,4,5,6,7或8.治疗受试者的方法根据 本发明的实施方案包括将具有结构式I的治疗有效量的包含一种或多种具有结构式I的化合物的组合物施用于具有由Akt调节异常表征的病症的受试者。 向受试者施用治疗有效量的包含一种或多种具有结构式I的化合物的组合物可检测地增加癌细胞，特别是Akt失调特征的癌细胞的凋亡和/或降低增殖。 本发明的组合物抑制Akt酶，iNOS，并且增加MAP激酶活性，使得与组合物接触的癌细胞被抑制。