公开(公告)号：US10246469B2

公开(公告)日：2019-04-02

申请号：US15763281

申请日：2016-09-29

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D237/08 ,  C07D239/26 ,  C07D213/34 ,  A61K31/50 ,  A61K31/51 ,  A61K31/505 ,  A61K31/506 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/28 ,  C07D513/04 ,  A61P25/18 ,  A61P25/16 ,  C07D213/74

摘要： The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

公开(公告)号：US20170051059A1

公开(公告)日：2017-02-23

申请号：US15122455

申请日：2015-03-19

申请人： Bristol-Myers Squibb Company

发明人： Anish SURI ,  Steven G. NADLER ,  Christian P. LARSEN ,  Andrew Briane ADAMS

IPC分类号： C07K16/28 ,  A61K39/395 ,  A61K38/17 ,  C07K14/705

CPC分类号： C07K16/2818 ,  A61K38/00 ,  A61K38/1774 ,  A61K39/39541 ,  A61K39/3955 ,  A61K2039/505 ,  A61K2039/507 ,  A61K2039/54 ,  A61K2039/545 ,  C07K14/70521 ,  C07K14/70575 ,  C07K16/2875 ,  C07K2317/21 ,  C07K2317/40 ,  C07K2317/56 ,  C07K2317/569 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92 ,  C07K2317/94 ,  C07K2319/30 ,  A61K2300/00

摘要： Methods of treating renal transplant rejection using anti-CD40L domain antibodies are provided. The anti-CD40L dAbs are less likely to cause platelet aggregation and thus cause thromboembolism. Appropriate anti-CD40L dAbs doses and administration regimens are also provided. Combination treatments for transplant rejection, particularly renal transplant rejection, using anti-CD40L dAbs, a CTLA4 mutant molecule (e.g., belatacept) and/or anti-CD28 optionally with conventional immunosuppressive renal transplant therapy are provided.

摘要翻译： 提供了使用抗CD40L结构域抗体治疗肾移植排斥的方法。 抗CD40L dAb不太可能引起血小板聚集，从而引起血栓栓塞。 还提供了适当的抗CD40L dAb剂量和给药方案。 提供了使用抗CD40L dAb，CTLA4突变分子（例如belatacept）和/或任选用常规免疫抑制性肾移植治疗的抗CD28的移植排斥特别是肾移植排斥的组合治疗。

公开(公告)号：US09765018B2

公开(公告)日：2017-09-19

申请号：US14897668

申请日：2014-07-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Jay A. Markwalder ,  Steven P. Seitz ,  James Aaron Balog ,  Audris Huang ,  Sunil Kumar Mandal ,  David K. Williams ,  Amy C. Hart ,  Jennifer Inghrim

IPC分类号： C07C275/42 ,  C07C311/51 ,  C07D213/75 ,  C07D257/04 ,  C07D401/04 ,  A61K31/18 ,  A61K31/41 ,  A61K31/44 ,  C07D213/79 ,  C07D307/86 ,  A61K31/196 ,  A61K31/277 ,  A61K31/343 ,  A61K31/4418 ,  A61K31/444 ,  A61K45/06 ,  C07C311/09 ,  C07D307/79

CPC分类号： C07C275/42 ,  A61K31/18 ,  A61K31/196 ,  A61K31/277 ,  A61K31/343 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/444 ,  A61K45/06 ,  C07C311/09 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D213/75 ,  C07D213/79 ,  C07D257/04 ,  C07D307/79 ,  C07D307/86 ,  C07D401/04

摘要： There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US10253027B2

公开(公告)日：2019-04-09

申请号：US14902868

申请日：2014-07-01

申请人： Bristol-Myers Squibb Company

发明人： Richard A. Hartz ,  Vijay T. Ahuja ,  Joanne J. Bronson ,  Carolyn Diane Dzierba ,  John E. Macor ,  Susheel Jethanand Nara ,  Ramkumar Rajamani

IPC分类号： C07D487/04 ,  C07D409/10 ,  C07D233/61 ,  C07D401/12 ,  C07D401/10 ,  C07D263/32 ,  C07D213/56 ,  C07D285/12 ,  C07D277/30 ,  C07D213/73 ,  C07D213/65 ,  C07D249/08 ,  C07D233/54 ,  C07D249/06 ,  C07D237/08 ,  C07D213/72 ,  C07D213/16 ,  C07D285/08 ,  C07D231/12 ,  C07D213/62 ,  C07D277/20 ,  C07D213/61 ,  C07D263/30 ,  C07D413/12 ,  C07D417/12

摘要： The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

公开(公告)号：US20170137514A1

公开(公告)日：2017-05-18

申请号：US15296290

申请日：2016-10-18

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Nils LONBERG ,  Mohan SRINIVASAN

IPC分类号： C07K16/28 ,  A61K39/395

CPC分类号： C07K16/2803 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/6849 ,  A61K2039/507 ,  C07K16/18 ,  C07K16/28 ,  C07K16/2818 ,  C07K16/2827 ,  C07K16/3061 ,  C07K2317/14 ,  C07K2317/21 ,  C07K2317/565 ,  C07K2317/75 ,  C07K2317/76 ,  C07K2317/92 ,  C07K2317/94

摘要： The present invention provides isolated monoclonal antibodies that specifically bind LAG-3, and have optimized functional properties compared to previously described anti-LAG-3 antibodies, such as antibody 25F7 (US 2011/0150892 A1). These properties include reduced deamidation sites, while still retaining high affinity binding to human LAG-3, and physical (i.e., thermal and chemical) stability. Nucleic acid molecules encoding the antibodies of the invention, expression vectors, host cells and methods for expressing the antibodies of the invention are also provided, as well as immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies. The present invention also provides methods for detecting LAG-3, as well as methods for treating stimulating immune responses using an anti-LAG-3 antibody of the invention. Combination therapy, in which the antibodies are co-administered with at least one additional immunostimulatory antibody, is also provided.

公开(公告)号：US20040171876A1

公开(公告)日：2004-09-02

申请号：US10788728

申请日：2004-02-26

申请人： Bristol-Myers Squibb Company ,  Bristol-Myers Squibb Company to Women First Healthcare, Inc.

发明人： Jingyang Zhu ,  Scott T. Chadwick ,  Benjamin A. Price ,  Shannon X. Zhao ,  Carrie A. Costello ,  Purushotham Vemishetti

IPC分类号： C07C229/02

CPC分类号： C07C255/29 ,  C07C227/10 ,  C07C227/16 ,  C07C227/18 ,  C07C227/22 ,  C07C227/40 ,  C07C227/42 ,  C07C253/30 ,  C07C255/28 ,  C07C229/26

摘要： Provided are processes and synthetic intermediates useful for the preparation of null-difluoromethylornithine (DFMO) having the formula 1

公开(公告)号：US20200339662A1

公开(公告)日：2020-10-29

申请号：US16813094

申请日：2020-03-09

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Jonathan DAVIS ,  Dasa LIPOVSEK ,  Ray CAMPHAUSEN

IPC分类号： C07K14/78 ,  C07K16/24 ,  C07K16/28 ,  C07K14/47 ,  G01N33/68 ,  C12N15/10

摘要： Fibronectin type III (10Fn3) binding domains having novel designs that are associated with reduced immunogenicity are provided. The application describes alternative 10Fn3 binding domains in which certain immunogenic regions are not modified when producing a binder in order to maintain recognition as a self antigen by the host organism. The application also describes 10Fn3 binding domains in which HLA anchor regions have been destroyed thereby reducing the immunogenic contribution of the adjoining region. Also provided are 10Fn3 domains having novel combinations of modified regions that can bind to a desired target with high affinity.

公开(公告)号：US09790169B2

公开(公告)日：2017-10-17

申请号：US15088211

申请日：2016-04-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： James Aaron Balog ,  Emily Charlotte Cherney ,  Weiwei Guo ,  Audris Huang ,  Jay A. Markwalder ,  Steven P. Seitz ,  Weifang Shan ,  David K. Williams ,  Natesan Murugesan ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Ramesh Kumar Sistla ,  Srinivas Cheruku ,  Srinivasan Thangathirupathy ,  Yadagiri Kanyaboina ,  Nagalakshmi Pulicharla

IPC分类号： C07C229/42 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/395 ,  C07C255/58 ,  C07C275/40 ,  C07D205/04 ,  C07D211/14 ,  C07D239/47 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D309/04 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D309/14 ,  C07D407/12 ,  C07D487/08 ,  C07D265/30 ,  C07D207/08 ,  C07D211/08 ,  C07D307/22 ,  C07C255/57 ,  C07C235/38 ,  C07C235/56

CPC分类号： C07C275/40 ,  A61K31/17 ,  A61K31/196 ,  A61K31/277 ,  A61K31/351 ,  A61K31/382 ,  A61K31/397 ,  A61K31/428 ,  A61K31/437 ,  A61K31/445 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/538 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  C07C229/42 ,  C07C233/81 ,  C07C235/38 ,  C07C235/56 ,  C07C255/57 ,  C07C255/58 ,  C07C275/30 ,  C07C275/42 ,  C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D211/08 ,  C07D211/14 ,  C07D239/34 ,  C07D239/47 ,  C07D265/30 ,  C07D265/36 ,  C07D277/64 ,  C07D295/155 ,  C07D307/22 ,  C07D309/04 ,  C07D309/14 ,  C07D317/46 ,  C07D335/02 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08

摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

公开(公告)号：US20230140430A1

公开(公告)日：2023-05-04

申请号：US17792887

申请日：2021-01-26

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Matthew COX ,  Liqi HE ,  Sanjeev GANGWAR ,  Ashvinikumar V. GAVAI ,  Matthias BROEKEMA ,  Qiang CONG ,  Daniel O'MALLEY ,  Yam B. POUDEL ,  Christine M. TARBY

IPC分类号： C07D519/00 ,  A61K45/06

摘要： Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

公开(公告)号：US11639353B2

公开(公告)日：2023-05-02

申请号：US17212210

申请日：2021-03-25

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Pratik Devasthale ,  Fang Moore ,  Guohua Zhao ,  Susan Nicole Pieniazek ,  Kumaravel Selvakumar ,  Suresh Dhanusu ,  Manoranjan Panda ,  Lawrence R. Marcin

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P1/16 ,  A61P13/12 ,  A61P11/00 ,  A61P35/00

摘要： The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to αv-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αv-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.