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公开(公告)号：US12071424B2
公开(公告)日：2024-08-27
申请号：US18176362
申请日：2023-02-28
申请人： Cornell University
IPC分类号： C07D401/04 , A61K31/517 , A61P35/00 , C07D217/22 , C07D239/74 , C07D239/84 , C07D239/94 , C07D401/10 , C07D403/04 , C07D403/10 , C07D413/04 , C07D417/04
CPC分类号： C07D401/10 , A61P35/00 , C07D217/22 , C07D239/84 , C07D401/04 , C07D403/04 , C07D403/10 , C07D413/04 , C07D417/04
摘要： Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
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公开(公告)号：US11945781B2
公开(公告)日：2024-04-02
申请号：US18183281
申请日：2023-03-14
申请人： Southern Research Institute , UAB Research Foundation , The United States Government as Represented by the Department of Veterans Affairs
发明人： Mark J. Suto , Bini Mathew , Anupam Agarwal , Amie M. Traylor
IPC分类号： C07D215/36 , C07C321/28 , C07D213/70 , C07D215/40 , C07D215/48 , C07D217/22
CPC分类号： C07D215/36 , C07C321/28 , C07D213/70 , C07D215/40 , C07D215/48 , C07D217/22
摘要： The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US11912719B2
公开(公告)日：2024-02-27
申请号：US17565231
申请日：2021-12-29
IPC分类号： A61K31/4725 , C07D217/22 , C07D498/08 , C07D401/12 , C07D405/14 , C07D471/04 , C07D403/12
CPC分类号： C07D498/08 , C07D401/12 , C07D403/12 , C07D405/14 , C07D471/04
摘要： The present invention relates to indoline-based compounds that inhibit Rho-associated protein kinase (ROCK) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
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公开(公告)号：US20230303586A1
公开(公告)日：2023-09-28
申请号：US18178452
申请日：2023-03-03
申请人： Araxes Pharma LLC
发明人： Liansheng LI , Jun FENG , Tao WU , Pingda REN , Yi LIU , Yuan Liu , Yun Oliver Long
IPC分类号： C07D495/04 , C07D239/94 , C07D401/12 , C07D217/22 , C07D215/46 , C07D215/54 , C07D239/84 , C07D487/04 , C07D239/95 , C07D403/04 , C07D241/44 , C07D401/04 , C07D409/04
CPC分类号： C07D495/04 , C07D215/46 , C07D215/54 , C07D217/22 , C07D239/84 , C07D239/94 , C07D239/95 , C07D241/44 , C07D401/04 , C07D401/12 , C07D403/04 , C07D409/04 , C07D487/04
摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.-
公开(公告)号：US11691950B2
公开(公告)日：2023-07-04
申请号：US17339828
申请日：2021-06-04
IPC分类号： C07D217/22 , A61K47/28 , A61K9/00
CPC分类号： C07D217/22 , A61K47/28 , A61K9/0048
摘要： Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.
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公开(公告)号：US11649224B2
公开(公告)日：2023-05-16
申请号：US17313688
申请日：2021-05-06
申请人： Cornell University
发明人： Joseph P. Vacca , Dansu Li , Sarah Bettigole
IPC分类号： C07D401/04 , C07D403/04 , A61P35/00 , C07D239/84 , C07D413/04 , C07D217/22 , C07D401/12 , C07D417/04 , A61K31/517
CPC分类号： C07D403/04 , A61K31/517 , A61P35/00 , C07D217/22 , C07D239/84 , C07D401/04 , C07D401/12 , C07D413/04 , C07D417/04
摘要： Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
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公开(公告)号：US20230130470A1
公开(公告)日：2023-04-27
申请号：US17722832
申请日：2022-04-18
IPC分类号： C07D401/12 , C07D217/02 , C07D405/12 , C07D417/12 , C07D217/24 , C07D217/22 , C07D401/04 , C07D405/14 , C07C69/76 , A61P27/06 , C07D401/14 , C07D409/12
摘要： Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the disclosure are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, diseases characterized by abnormal growth, such as cancers, and inflammatory diseases. The disclosure further provides compositions containing isoquinoline amide compounds.
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公开(公告)号：US11623918B2
公开(公告)日：2023-04-11
申请号：US17529201
申请日：2021-11-17
申请人： Southern Research Institute , UAB Research Foundation , The United States Government as Represented by the Department of Veterans Affairs
发明人： Mark J. Suto , Bini Mathew , Anupam Agarwal , Amie M. Traylor
IPC分类号： C07D215/36 , C07D215/40 , C07D215/48 , C07D213/70 , C07D217/22 , C07C321/28
摘要： The present disclosure is concerned with thioquinolinone compounds for the treatment of disorders associated with heme oxygenase-1 (HO-1) signaling dysfunction such as, for example, kidney diseases (e.g., chronic kidney disease, acute kidney injury). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US20230101312A1
公开(公告)日：2023-03-30
申请号：US17801733
申请日：2021-02-23
发明人： Matthew Arnold Marx , John Michael Ketcham , Christopher Ronald Smith , John David Lawson , Aaron Craig Burns , Xiaolun Wang
IPC分类号： C07D471/04 , C07D217/22 , C07D401/04 , C07D409/12 , C07D413/14
摘要： The present invention relates to compounds that inhibit Son of sevenless homolog 1 (SOS1) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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公开(公告)号：US11427546B2
公开(公告)日：2022-08-30
申请号：US17296439
申请日：2019-12-16
发明人： Hiroyoshi Hidaka , Kengo Sumi , Takashi Izuhara
IPC分类号： C07D217/22
摘要： A stable crystal of a salt of N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide may have desirable properties for a pharmaceutical drug substance, and more specifically N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide dihydrochloride anhydride. A crystal of the anhydride may have characteristic peaks at 2θ angles of 6.8±0.1°, 10.0±0.1°, 12.7±0.1°, 14.6±0.1°, 14.8±0.1°, 16.2±0.1°, 17.4±0.1°, 17.8±0.1°, 19.5±0.1°, 20.0±0.1°, 21.6±0.1°, 24.7±0.1°, 25.5±0.1°, 25.8±0.1°, 29.8±0.1°, 39.5±0.1°, and/or 44.9±0.1° in powder X-ray diffraction spectrum.
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