公开(公告)号：US10508106B2

公开(公告)日：2019-12-17

申请号：US15779353

申请日：2016-11-23

申请人： ConverGene LLC ,  The United States of America, as represented by the Secretary, Department of Health and Human Services

发明人： Jeffrey William Strovel ,  Makoto Yoshioka ,  David J. Maloney ,  Shyh Ming Yang ,  Ajit Jadhav ,  Daniel Jason Urban

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D401/04 ,  C07D239/84 ,  C07D471/04 ,  C07D471/10 ,  A61P39/00 ,  C07D239/95 ,  C07D401/14 ,  C07D403/04 ,  C07D417/14

摘要： The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

公开(公告)号：US11795177B2

公开(公告)日：2023-10-24

申请号：US17682654

申请日：2022-02-28

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

发明人： Shyh Ming Yang ,  David J. Maloney ,  Natalia Martinez ,  Adam Yasgar ,  Anton Simeonov

IPC分类号： C07D491/113 ,  C07D215/54 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07D491/107 ,  C07D495/04 ,  C07D495/10 ,  C07D519/00

CPC分类号： C07D491/113 ,  C07D215/54 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07D491/107 ,  C07D495/04 ,  C07D495/10 ,  C07D519/00

摘要： The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I.

公开(公告)号：US11505559B2

公开(公告)日：2022-11-22

申请号：US16760345

申请日：2018-10-30

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  YALE UNIVERSITY

发明人： Shyh Ming Yang ,  David J. Maloney ,  Natalia Martinez ,  Adam Yasgar ,  Anton Simeonov ,  Vasilis Vasiliou

IPC分类号： C07D491/113 ,  C07D401/14 ,  C07D401/12 ,  C07D215/54 ,  C07D491/107 ,  C07D413/04 ,  C07D519/00 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D495/10 ,  C07D401/06 ,  C07D409/14

摘要： The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumors breast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I.

公开(公告)号：US11897845B2

公开(公告)日：2024-02-13

申请号：US17572359

申请日：2022-01-10

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  VANDERBILT UNIVERSITY ,  The UAB Research Foundation ,  The Trustees of the University of Pennsylvania

发明人： David J. Maloney ,  Alex Gregory Waterson ,  Ganesh Rai Bantukallu ,  Kyle Ryan Brimacombe ,  Plamen Christov ,  Chi V. Dang ,  Victor Darley-Usmar ,  Xin Hu ,  Ajit Jadhav ,  Somnath Jana ,  Kwangho Kim ,  Jennifer L. Kouznetsova ,  William J. Moore ,  Bryan T. Mott ,  Leonard M. Neckers ,  Anton Simeonov ,  Gary Allen Sulikowski ,  Daniel Jason Urban ,  Shyh Ming Yang

IPC分类号： C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K45/06 ,  A61K31/4178

CPC分类号： C07D231/20 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K45/06 ,  C07D231/38 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

摘要： Provided is a compound of formula (I)




in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

公开(公告)号：US11247971B2

公开(公告)日：2022-02-15

申请号：US17160868

申请日：2021-01-28

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  VANDERBILT UNIVERSITY ,  The UAB Research Foundation ,  The Trustees of the University of Pennsylvania

发明人： David J. Maloney ,  Alex Gregory Waterson ,  Ganesh Rai Bantukallu ,  Kyle Ryan Brimacombe ,  Plamen Christov ,  Chi V. Dang ,  Victor Darley-Usmar ,  Xin Hu ,  Ajit Jadhav ,  Somnath Jana ,  Kwangho Kim ,  Jennifer L. Kouznetsova ,  William J. Moore ,  Bryan T. Mott ,  Leonard M. Neckers ,  Anton Simeonov ,  Gary Allen Sulikowski ,  Daniel Jason Urban ,  Shyh Ming Yang

IPC分类号： C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/4439 ,  A61K45/06

摘要： Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

公开(公告)号：US20180305344A1

公开(公告)日：2018-10-25

申请号：US15779353

申请日：2016-11-23

申请人： Jeffrey William STROVEL ,  Makoto YOSHIOKA ,  David J. MALONEY ,  Shyh Ming YANG ,  Ajit JADHAV ,  Daniel Jason URBAN ,  ConverGene LLC

发明人： Jeffrey William Strovel ,  Makoto Yoshioka ,  David J. Maloney ,  Shyh Ming Yang ,  Ajit Jadhav ,  Daniel Jason Urban

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D239/95 ,  C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  A61P39/00

CPC分类号： C07D413/04 ,  A61P39/00 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.

公开(公告)号：US20200223836A1

公开(公告)日：2020-07-16

申请号：US16685128

申请日：2019-11-15

申请人： ConverGene LLC ,  The United States of America, as represented by the Secretary,Department of Health and Human Service

发明人： Jeffrey William Strovel ,  Makoto Yoshioka ,  David J. Maloney ,  Shyh Ming Yang ,  Ajit Jadhav ,  Daniel Jason Urban, JR.

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10 ,  C07D239/84 ,  A61P39/00 ,  C07D239/95 ,  C07D401/14 ,  C07D403/04 ,  C07D417/14

摘要： The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.