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公开(公告)号:US11884661B2
公开(公告)日:2024-01-30
申请号:US17184179
申请日:2021-02-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Guohua Zhao , Pratik Devasthale , Xiang-Yang Ye , Kumaravel Selvakumar , Suresh Dhanusu , Palanikumar Balasubramanian , Leatte R. Guernon , Rita Civiello , Xiaojun Han , Michael Frederick Parker , Swanee E. Jacutin-Porte
IPC: C07D471/04 , C07D491/04 , C07D519/00 , A61P11/00 , A61P19/10 , A61P35/00 , A61P37/06
CPC classification number: C07D471/04 , A61P11/00 , A61P19/10 , A61P35/00 , A61P37/06 , C07D491/04 , C07D519/00
Abstract: 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.-
公开(公告)号:US20210188847A1
公开(公告)日:2021-06-24
申请号:US17184179
申请日:2021-02-24
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Guohua Zhao , Pratik Devasthale , Xiang-Yang Ye , Kumaravel Selvakumar , Suresh Dhanusu , Palanikumar Balasubramanian , Leatte R. Guernon , Rita Civiello , Xiaojun Han , Michael Frederick Parker , Swanee E. Jacutin-Porte
IPC: C07D471/04 , A61P37/06 , A61P11/00 , A61P19/10 , A61P35/00 , C07D519/00 , C07D491/04
Abstract: 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.
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3.
公开(公告)号:US12097242B2
公开(公告)日:2024-09-24
申请号:US17721569
申请日:2022-04-15
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
CPC classification number: A61K38/18 , A61K38/2221 , C07K1/1077 , C07K14/64 , A61K38/00 , A61K45/06 , A61K47/64 , A61P9/00
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US11364281B2
公开(公告)日:2022-06-21
申请号:US17198939
申请日:2021-03-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US12097241B2
公开(公告)日:2024-09-24
申请号:US17573238
申请日:2022-01-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
CPC classification number: A61K38/18 , A61K38/2221 , C07K1/1077 , C07K14/64 , A61K38/00 , A61K45/06 , A61K47/64 , A61P9/00
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US20220211812A1
公开(公告)日:2022-07-07
申请号:US17573238
申请日:2022-01-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US20210196791A1
公开(公告)日:2021-07-01
申请号:US17198939
申请日:2021-03-11
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US10968219B2
公开(公告)日:2021-04-06
申请号:US16347844
申请日:2017-11-07
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Guohua Zhao , Pratik Devasthale , Xiang-Yang Ye , Kumaravel Selvakumar , Suresh Dhanusu , Palanikumar Balasubramanian , Leatte R. Guernon , Rita Civiello , Xiaojun Han , Michael Frederick Parker , Swanee E. Jacutin-Porte
IPC: C07D471/04 , C07D491/04 , C07D519/00 , A61P11/00 , A61P19/10 , A61P35/00 , A61P37/06
Abstract: 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 ay-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号:US10266578B2
公开(公告)日:2019-04-23
申请号:US15891492
申请日:2018-02-08
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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公开(公告)号:US20220331402A1
公开(公告)日:2022-10-20
申请号:US17721569
申请日:2022-04-15
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor: Gene M. Dubowchik , Olafur S. Gudmundsson , Xiaojun Han , R. Michael Lawrence , Dasa Lipovsek , Cort S. Madsen , Claudio Mapelli , Paul E. Morin , Michael C. Myers
Abstract: The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.
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