公开(公告)号：US12016896B2

公开(公告)日：2024-06-25

申请号：US17532285

申请日：2021-11-22

申请人： CORNELL UNIVERSITY

发明人： Gang Lin ,  Carl Nathan ,  Pradeep K. Singh

IPC分类号： A61K38/05 ,  A61K31/165 ,  A61K31/42 ,  A61K38/02 ,  C07C237/06 ,  C07C237/12 ,  C07C237/22 ,  C07C271/22 ,  C07C311/14 ,  C07C311/19 ,  C07D209/18 ,  C07D261/18 ,  C07K5/06

CPC分类号： A61K38/05 ,  A61K31/165 ,  A61K31/42 ,  A61K38/02 ,  C07C237/06 ,  C07C237/12 ,  C07C237/22 ,  C07C271/22 ,  C07C311/14 ,  C07C311/19 ,  C07D209/18 ,  C07D261/18 ,  C07K5/06 ,  C07C2601/02

摘要： The compounds of the present invention are represented by the following compounds having Formula I:




where the substituents R1, R4, L, M, X, Y, and s are as defined herein. The compounds of the present invention are also represented by the following compounds having Formula (Ia), Formula (Ib), or Formula (Ic):





where the substituents R1-R4, Rx, Ry, X, Y, and s are as defined herein.

These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders or for providing immunosuppression for transplanted organs or tissues.

公开(公告)号：US11951147B2

公开(公告)日：2024-04-09

申请号：US17735776

申请日：2022-05-03

申请人： Medivir AB

发明人： Stephen M. Condon ,  Yijun Deng ,  Matthew G. Laporte ,  Susan R. Rippin

IPC分类号： A61K38/05 ,  A61K31/404 ,  A61K31/555 ,  A61K38/07 ,  A61K45/06 ,  A61N5/06 ,  A61N5/10 ,  A61P35/00 ,  A61P35/04 ,  C07D403/06 ,  C07D403/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C12N5/09 ,  A61K38/00

CPC分类号： A61K38/05 ,  A61K31/404 ,  A61K31/555 ,  A61K38/07 ,  A61K45/06 ,  A61N5/062 ,  A61N5/10 ,  A61P35/00 ,  A61P35/04 ,  C07D403/06 ,  C07D403/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/06026 ,  C12N5/0693 ,  A61K38/00 ,  C12N2500/46 ,  Y02P20/55

摘要： A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

公开(公告)号：US20230265173A1

公开(公告)日：2023-08-24

申请号：US17990485

申请日：2022-11-18

申请人： ZYMEWORKS BC INC.

发明人： Geoffrey C. WINTERS ,  Alexander L. MANDEL ,  Elyse Marie Josée BOURQUE ,  James R. RICH ,  Tom Han Hsiao HSIEH

IPC分类号： C07K16/18 ,  A61K47/68 ,  C07K5/06

CPC分类号： C07K16/18 ,  A61K47/6889 ,  A61K47/6851 ,  A61K47/6817 ,  C07K5/06 ,  C07K2319/00

摘要： Sulfonamide-containing linkage systems for release of payload compounds from an attached targeting moiety in drug conjugates. The conjugates have the formula of [(P)-(L)]m-(T), wherein (P) is a payload compound, (L) is a linker, (T) is a targeting moiety and m is an integer from 1- to 10. Also provided are pharmaceutical compositions comprising such conjugates and there use in treating cancer.

公开(公告)号：US20230149500A1

公开(公告)日：2023-05-18

申请号：US17735776

申请日：2022-05-03

申请人： Medivir AB

发明人： Stephen M. CONDON ,  Yijun DENG ,  Matthew G. LAPORTE ,  Susan R. RIPPIN

IPC分类号： A61K38/05 ,  C07D403/06 ,  C07K5/062 ,  A61P35/00 ,  A61P35/04 ,  A61K38/07 ,  A61K45/06 ,  C07D403/14 ,  C07K5/02 ,  A61K31/404 ,  A61N5/06 ,  A61N5/10 ,  C07K5/06 ,  C12N5/09 ,  A61K31/555

CPC分类号： A61K38/05 ,  A61K31/404 ,  A61K31/555 ,  A61K38/07 ,  A61K45/06 ,  A61N5/10 ,  A61N5/062 ,  A61P35/00 ,  A61P35/04 ,  C07D403/06 ,  C07D403/14 ,  C07K5/02 ,  C07K5/06 ,  C07K5/06026 ,  C12N5/0693 ,  A61K38/00 ,  Y02P20/55

摘要： A SMAC mimetic and pharmaceutical compositions thereof and methods of use.

公开(公告)号：US20190241660A1

公开(公告)日：2019-08-08

申请号：US16209143

申请日：2018-12-04

申请人： INTENDET SERVICES, LLC

发明人： Brett P. GIROIR ,  Clifford H. KERN, III ,  Carola LEUSCHNER

IPC分类号： C07K16/28 ,  C07K5/06 ,  A61K35/17 ,  A61P35/00 ,  A61P31/00 ,  A61K39/00 ,  C12N5/0783

CPC分类号： C07K16/2818 ,  A61K35/17 ,  A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K38/10 ,  A61K39/0011 ,  A61K2039/5154 ,  A61K2039/5158 ,  A61P31/00 ,  A61P35/00 ,  C07K5/06 ,  C07K16/2827 ,  C12N5/0636

摘要： Presented herein are immune-stimulating peptides and uses thereof for treating cancer. The immune-stimulating peptides can be used alone, or in combination with checkpoint inhibitors and other anti-cancer therapies. The immune-stimulating peptides can also be used for expanding T-cells in vitro or ex vivo, which expanded T-cells can then be used for adoptive cell therapy.

公开(公告)号：US20190210957A1

公开(公告)日：2019-07-11

申请号：US16311747

申请日：2017-01-20

申请人： Jiangxi Normal University

发明人： Junfeng ZHAO ,  Long HU ,  Silin XU ,  Zhenguang ZHAO

IPC分类号： C07C219/20 ,  C07C213/08 ,  C07C311/17 ,  C07C303/40 ,  C07C231/02 ,  C07C233/05

CPC分类号： C07C219/20 ,  C07C213/08 ,  C07C231/02 ,  C07C233/05 ,  C07C303/40 ,  C07C311/17 ,  C07D209/20 ,  C07D231/56 ,  C07D263/22 ,  C07D307/68 ,  C07D333/68 ,  C07K5/06

摘要： Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

公开(公告)号：US20180327449A1

公开(公告)日：2018-11-15

申请号：US15974855

申请日：2018-05-09

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Marion W. WANNAMAKER ,  Robert J. DAVIES

IPC分类号： C07K5/062 ,  C07K5/083 ,  C07K5/08 ,  C07D207/16 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/06 ,  C07K5/02 ,  A61K38/00

CPC分类号： C07K5/06034 ,  A61K38/00 ,  C07D207/16 ,  C07D307/02 ,  C07D477/02 ,  C07D477/20 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06 ,  C07K5/06008 ,  C07K5/06191 ,  C07K5/08 ,  C07K5/0808 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/475

摘要： This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

公开(公告)号：US09993529B2

公开(公告)日：2018-06-12

申请号：US13507262

申请日：2012-06-15

申请人： Tzung-Horng Yang ,  Daniel Edward Vaughn ,  Michael James Labarre ,  Christopher L. Caster ,  Francois Nicol ,  Donghyun Kim

发明人： Tzung-Horng Yang ,  Daniel Edward Vaughn ,  Michael James Labarre ,  Christopher L. Caster ,  Francois Nicol ,  Donghyun Kim

IPC分类号： C07K14/62 ,  C12N9/24 ,  A61K38/28 ,  A61K47/02 ,  C07K5/06 ,  C07K5/068 ,  A61K38/47 ,  A61K9/00

CPC分类号： A61K38/28 ,  A61K9/0019 ,  A61K38/47 ,  A61K47/02 ,  C07K5/06 ,  C07K5/06086 ,  C07K14/62 ,  C12N9/2402 ,  C12Y302/01035

摘要： Provided are compositions that are stable formulations of a hyaluronan-degrading enzyme or are stable co-formulations of a fast-acting insulin and a hyaluronan degrading enzyme, including a recombinant human PH20 (rHuPH20).

公开(公告)号：US09896668B2

公开(公告)日：2018-02-20

申请号：US15251572

申请日：2016-08-30

申请人： University of South Florida ,  Yale University

发明人： Said M. Sebti ,  Jin Q. Cheng ,  Andrew D. Hamilton ,  Katherine Kayser-Bricker

IPC分类号： A61K31/132 ,  A61K31/404 ,  C07D209/04 ,  C07C255/55 ,  C12N9/12 ,  C07K5/02 ,  C07C255/50 ,  C07C255/51 ,  C07C255/60 ,  C07C279/12 ,  C07D209/14 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  C07K7/02 ,  A61K38/00

CPC分类号： C12N9/12 ,  A61K31/132 ,  A61K31/404 ,  A61K38/00 ,  C07C255/50 ,  C07C255/51 ,  C07C255/60 ,  C07C279/12 ,  C07C2601/16 ,  C07D209/04 ,  C07D209/14 ,  C07K5/02 ,  C07K5/0207 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/02 ,  C07K7/06 ,  C12N9/1205 ,  C12Y207/11001

摘要： Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.

公开(公告)号：US09868763B2

公开(公告)日：2018-01-16

申请号：US14235640

申请日：2012-07-27

申请人： David Fairlie ,  Ligong Liu ,  Mei-Kwan Yau ,  Jacky Yung Suen ,  Robert Reid ,  Rink-Jan Lohman ,  Abishek Venkatasubramanian Iyer ,  Junxian Lim ,  Lindsay Charles Brown

发明人： David Fairlie ,  Ligong Liu ,  Mei-Kwan Yau ,  Jacky Yung Suen ,  Robert Reid ,  Rink-Jan Lohman ,  Abishek Venkatasubramanian Iyer ,  Junxian Lim ,  Lindsay Charles Brown

IPC分类号： C07K5/08 ,  A61K38/05 ,  C07K5/065 ,  C07K5/02 ,  C07K5/06

CPC分类号： C07K5/08 ,  A61K38/05 ,  C07K5/02 ,  C07K5/06 ,  C07K5/06078

摘要： The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for therapies such as metabolic syndrome, obesity, type II diabetes, fibrosis and cardiovascular diseases, whether they are used alone or in combination with other treatment modalities.