公开(公告)号：US12098117B2

公开(公告)日：2024-09-24

申请号：US17312858

申请日：2019-12-11

Applicant: DUKE UNIVERSITY

Inventor： Dennis J. Thiele ,  Bushu Dong ,  Alexander M. Jaeger ,  Philip F. Hughes ,  Timothy Haystead ,  Jiyong Hong

IPC: C07C275/30 ,  A61P35/00 ,  C07C211/40 ,  C07C255/60 ,  C07C275/28 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C279/18 ,  C07C279/28 ,  C07C281/06 ,  C07C311/46 ,  C07C317/36 ,  C07C317/42 ,  C07D213/40 ,  C07D213/75 ,  C07D223/04 ,  C07D229/02 ,  C07D231/56 ,  C07D233/64 ,  C07D241/24 ,  C07D249/14 ,  C07D271/12 ,  C07D285/10 ,  C07D317/66 ,  C07D333/20 ,  C07D333/36 ,  C07D333/72 ,  C07D405/04 ,  C07D405/12 ,  C07D417/12

CPC classification number: C07C275/30 ,  A61P35/00 ,  C07C211/40 ,  C07C255/60 ,  C07C275/28 ,  C07C275/34 ,  C07C275/40 ,  C07C275/42 ,  C07C279/18 ,  C07C279/28 ,  C07C281/06 ,  C07C311/46 ,  C07C317/36 ,  C07C317/42 ,  C07D213/40 ,  C07D213/75 ,  C07D223/04 ,  C07D229/02 ,  C07D231/56 ,  C07D233/64 ,  C07D241/24 ,  C07D249/14 ,  C07D271/12 ,  C07D285/10 ,  C07D317/66 ,  C07D333/20 ,  C07D333/36 ,  C07D333/72 ,  C07D405/04 ,  C07D405/12 ,  C07D417/12

Abstract: This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to Heat Shock Transcription Factor 1 (HSF1) activity and/or function. More particularly, this disclosure relates to methods of inhibiting HSF1 activity with these compounds and pharmaceutical compositions thereof, and methods of treating diseases associated with HSF1 activity and/or function, such as cancer.

公开(公告)号：US20240124388A1

公开(公告)日：2024-04-18

申请号：US18467190

申请日：2023-09-14

Applicant: ModernaTX, Inc.

Inventor： Kerry E. BENENATO ,  Mark CORNEBISE

IPC: C07C229/12 ,  A61K9/00 ,  A61K9/127 ,  A61K9/16 ,  A61K9/51 ,  A61K31/7105 ,  A61K38/17 ,  A61K38/18 ,  A61K47/54 ,  A61K47/69 ,  A61K48/00 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C233/72 ,  C07C235/10 ,  C07C255/24 ,  C07C263/20 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/09 ,  C07K14/505

CPC classification number: C07C229/12 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/127 ,  A61K9/1272 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/7105 ,  A61K38/1725 ,  A61K38/1816 ,  A61K47/543 ,  A61K47/6911 ,  A61K48/0033 ,  A61K48/005 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C233/72 ,  C07C235/10 ,  C07C255/24 ,  C07C263/20 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/091 ,  C07K14/505 ,  A61K9/1271 ,  A61K48/00 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US20230233551A1

公开(公告)日：2023-07-27

申请号：US17815256

申请日：2022-07-27

Applicant: Novartis Pharmaceuticals Corporation

Inventor： Thomas GADEK ,  John BURNIER

IPC: A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/17 ,  G01N33/50 ,  G01N33/68 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/00 ,  G01N33/566 ,  A61B3/10 ,  A61B3/14

CPC classification number: A61K31/4725 ,  C07D217/00 ,  C07D217/02 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P27/02 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06 ,  A61K31/405 ,  A61K31/495 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/6872 ,  A61K31/197 ,  A61K31/341 ,  A61K31/352 ,  A61K31/472 ,  C07D401/06 ,  G01N33/5047 ,  A61K31/275 ,  A61K31/40 ,  A61K31/517 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/26 ,  C07D307/52 ,  C07D413/14 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0053 ,  G01N33/566 ,  A61B3/101 ,  A61K9/0051 ,  A61B3/145 ,  G01N2333/70525 ,  G01N2500/02 ,  G01N2500/10 ,  G01N2333/705 ,  G01N2333/70546 ,  G01N2500/20 ,  G01N2500/04 ,  G01N2800/16

Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US20170210698A1

公开(公告)日：2017-07-27

申请号：US15476263

申请日：2017-03-31

Applicant: MODERNATX, Inc.

Inventor： Kerry E. Benenato ,  Ellalahewage Sathyajith Kumarasinghe ,  Mark Cornebise

IPC: C07C229/12 ,  A61K38/18 ,  A61K9/00 ,  A61K9/16

CPC classification number: C07C229/12 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0073 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1272 ,  A61K9/1617 ,  A61K9/1641 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/7105 ,  A61K38/1725 ,  A61K38/1816 ,  A61K47/543 ,  A61K47/6911 ,  A61K48/00 ,  A61K48/0033 ,  A61K48/005 ,  C07C227/16 ,  C07C227/18 ,  C07C229/16 ,  C07C233/36 ,  C07C235/10 ,  C07C255/24 ,  C07C271/20 ,  C07C275/14 ,  C07C279/12 ,  C07C279/24 ,  C07C279/28 ,  C07C279/32 ,  C07C311/05 ,  C07C335/08 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/27 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D277/38 ,  C07F9/091 ,  C07K14/505

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US09045457B2

公开(公告)日：2015-06-02

申请号：US14045131

申请日：2013-10-03

Applicant: SARCODE BIOSCIENCE INC.

Inventor： Thomas Gadek ,  John Burnier ,  Min Zhong ,  Wang Shen ,  Johan D. Oslob ,  Kenneth Barr

IPC: C07D217/00 ,  C07D405/06 ,  A61K31/198 ,  A61K31/404 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K31/381 ,  A61K45/06 ,  C07D333/38 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  A61K33/00 ,  A61K33/06 ,  C07D217/20 ,  C07D217/06

CPC classification number: A61K31/4725 ,  A61B3/101 ,  A61B3/145 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0051 ,  A61K9/0053 ,  A61K31/197 ,  A61K31/198 ,  A61K31/275 ,  A61K31/341 ,  A61K31/352 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K33/00 ,  A61K33/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  A61K45/06 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/00 ,  C07D217/02 ,  C07D217/06 ,  C07D217/20 ,  C07D217/26 ,  C07D307/52 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/5047 ,  G01N33/566 ,  G01N33/6872 ,  G01N2333/705 ,  G01N2333/70525 ,  G01N2333/70546 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20 ,  G01N2800/16 ,  Y10S514/912 ,  Y10S514/914

Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US20140378506A1

公开(公告)日：2014-12-25

申请号：US14275159

申请日：2014-05-12

Applicant: SARCODE BIOSCIENCE INC.

Inventor： Thomas Gadek ,  John Burnier ,  Min Zhong ,  Wang Shen ,  Johan D. Oslob ,  Kenneth Barr

IPC: C07D405/06

CPC classification number: A61K31/4725 ,  A61B3/101 ,  A61B3/145 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0048 ,  A61K9/0051 ,  A61K9/0053 ,  A61K31/197 ,  A61K31/198 ,  A61K31/275 ,  A61K31/341 ,  A61K31/352 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61K33/00 ,  A61K33/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/12 ,  A61K38/1703 ,  A61K45/06 ,  C07C279/28 ,  C07C317/50 ,  C07D207/06 ,  C07D217/00 ,  C07D217/02 ,  C07D217/06 ,  C07D217/20 ,  C07D217/26 ,  C07D307/52 ,  C07D333/38 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  G01N33/5011 ,  G01N33/5032 ,  G01N33/5047 ,  G01N33/566 ,  G01N33/6872 ,  G01N2333/705 ,  G01N2333/70525 ,  G01N2333/70546 ,  G01N2500/02 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20 ,  G01N2800/16 ,  Y10S514/912 ,  Y10S514/914

Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

公开(公告)号：US07884244B2

公开(公告)日：2011-02-08

申请号：US12058037

申请日：2008-03-28

Applicant: Ken Chow ,  Wenkui K. Fang ,  Evelyn G. Corpuz ,  Daniel W. Gil ,  Michael E. Garst

Inventor： Ken Chow ,  Wenkui K. Fang ,  Evelyn G. Corpuz ,  Daniel W. Gil ,  Michael E. Garst

IPC: C07C277/00

CPC classification number: C07D307/81 ,  C07C279/28 ,  C07C323/44 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/16

Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract translation: 本文公开的是具有本文所述的式的化合物。 还公开了与之相关的治疗方法，组合物和药物。

公开(公告)号：US20070142333A1

公开(公告)日：2007-06-21

申请号：US11670482

申请日：2007-02-02

Applicant: John Lloyd ,  Yoon Jeon ,  Heather Finlay ,  Lin Yan ,  Michael Gross ,  Serge Beaudoin

Inventor： John Lloyd ,  Yoon Jeon ,  Heather Finlay ,  Lin Yan ,  Michael Gross ,  Serge Beaudoin

IPC: A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/426 ,  A61K31/421 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07D213/40 ,  A61K45/06 ,  C07C233/58 ,  C07C233/59 ,  C07C233/60 ,  C07C233/65 ,  C07C235/06 ,  C07C235/34 ,  C07C235/46 ,  C07C235/60 ,  C07C279/16 ,  C07C279/24 ,  C07C279/28 ,  C07C307/02 ,  C07C307/04 ,  C07C307/08 ,  C07C307/10 ,  C07C311/16 ,  C07C311/29 ,  C07C311/55 ,  C07C311/59 ,  C07C311/64 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2603/66 ,  C07D213/69 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/48 ,  C07D233/56 ,  C07D233/64 ,  C07D233/76 ,  C07D235/14 ,  C07D239/42 ,  C07D239/94 ,  C07D239/95 ,  C07D241/06 ,  C07D249/04 ,  C07D249/08 ,  C07D251/44 ,  C07D251/46 ,  C07D261/08 ,  C07D261/14 ,  C07D271/06 ,  C07D295/13 ,  C07D295/185 ,  C07D295/215 ,  C07D295/26 ,  C07D307/68 ,  C07D309/04 ,  C07D309/08 ,  C07D333/20 ,  C07D333/28 ,  C07D333/38 ,  C07D333/58 ,  C07D333/62 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

Abstract translation: 可用作钾通道功能抑制剂的新型环烷基化合物（特别是电压门控K +通道抑制剂，尤其是抑制剂K + > 1.5，其与超快速活化延迟整流器K +电流I K连接），使用这些化合物在预防和治疗心律失常中的方法， 相关条件和含有这些化合物的药物组合物。

公开(公告)号：US07202269B2

公开(公告)日：2007-04-10

申请号：US10976067

申请日：2004-10-28

Applicant: Tristin K. Barclay ,  Alejandro Santillán, Jr. ,  Liu Y. Tang ,  Hariharan Venkatesan ,  Ronald L. Wolin

Inventor： Tristin K. Barclay ,  Alejandro Santillán, Jr. ,  Liu Y. Tang ,  Hariharan Venkatesan ,  Ronald L. Wolin

IPC: A61K31/40 ,  A61K31/17 ,  C07D207/06 ,  C07C335/18

CPC classification number: C07D295/13 ,  C07C275/28 ,  C07C275/36 ,  C07C279/28 ,  C07D213/56 ,  C07D277/30 ,  C07D333/20 ,  C07D333/24

Abstract: Certain α-, β-, and γ-amino acid derivatives are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain.

Abstract translation: 公开了某些α-，β-和γ-氨基酸衍生物作为选择性GlyT2抑制剂用于治疗中枢神经系统（CNS）病症如肌肉痉挛，耳鸣，癫痫和神经性疼痛。

公开(公告)号：US06927218B2

公开(公告)日：2005-08-09

申请号：US10386154

申请日：2003-03-11

Applicant: Soumitra S. Ghosh ,  Tomas R. Szabo

Inventor： Soumitra S. Ghosh ,  Tomas R. Szabo

IPC: C07D295/12 ,  A61K31/155 ,  A61K31/277 ,  A61K31/5375 ,  A61P3/10 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C279/28

CPC classification number: A61K31/5375 ,  A61K31/155 ,  C07C279/28

Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1-5 are as defined herein. The methods of this invention are directed to administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.