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公开(公告)号：US20220160883A1
公开(公告)日：2022-05-26
申请号：US17541636
申请日：2021-12-03
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Matthew R. Hickey , Antonio Ramirez
Abstract: The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25° C. without stirring until completion, typically within 24 hours.
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![Process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates therefor](/abs-image/US/2017/02/28/US09580420B2/abs.jpg.150x150.jpg)
2.发明授权Process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates therefor 有权制备4-（8-（2-氯苯氧基） - [1,2,4]三唑并[4,3-a]吡啶-3-基）双环[2.2.1]庚-1-醇的方法和新颖的 中间体公开(公告)号：US09580420B2
公开(公告)日：2017-02-28
申请号：US14817352
申请日：2015-08-04
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Xinhua Qian , Keming Zhu , Joerg Deerberg , Wendy Wangying Yang , Kana Yamamoto , Matthew R. Hickey
IPC: C07D213/77 , C07C35/29 , C07D471/04 , C07C29/00 , C07C51/29 , C07C61/13
CPC classification number: C07D471/04 , C07C29/00 , C07C35/29 , C07C51/29 , C07C61/13 , C07C2602/42 , C07D213/77
Abstract: A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases.
Abstract translation: 提供了制备4-（8-（2-氯苯氧基） - [1,2,4]三唑并[4,3-a]吡啶-3-基）双环[2.2.1]庚-1-醇和 在此过程中使用的新型中间体。 该化合物是在治疗各种代谢疾病中表现出活性的11-β羟基类固醇脱氢酶I型抑制剂。
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![PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE](/abs-image/US/2022/06/09/US20220177482A1/abs.jpg.150x150.jpg)
公开(公告)号：US20220177482A1
公开(公告)日：2022-06-09
申请号：US17677312
申请日：2022-02-22
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Burcu Selin Aytar , Alina Borovika , Collin Chan , Joerg Deerberg , Nathan R. Domagalski , Martin D. Eastgate , Yu Fan , Michael David Bengt Fenster , Robert V. Forest , Francisco Gonzalez-Bobes , Rebecca A. Green , Matthew R. Hickey , Nathaniel David Kopp , Thomas E. La Cruz , Kathleen Lauser , Hong Geun Lee , David K. Leahy , Helen Y. Luo , Thomas M. Razler , Scott A. Savage , Chris Sfouggatakis , Maxime C.D. Soumeillant , Serge Zaretsky , Bin Zheng , Ye Zhu
IPC: C07D487/04
Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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![PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE](/abs-image/US/2020/07/16/US20200223852A1/abs.jpg.150x150.jpg)
公开(公告)号：US20200223852A1
公开(公告)日：2020-07-16
申请号：US16631915
申请日：2018-07-19
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Burcu Selin Aytar , Alina Borovika , Collin Chan , Joerg Deerberg , Nathan R. Domagalski , Martin D. Eastgate , Yu Fan , Michael David Bengt Fenster , Robert V. Forest , Francisco Gonzalez-Bobes , Rebecca A. Green , Matthew R. Hickey , Nathaniel David Kopp , Thomas E. La Cruz , Kathleen Lauser , Hong Geun Lee , David K. Leahy , Helen Y. Luo , Thomas M. Razler , Scott A. Savage , Chris Sfouggatakis , Maxime C.D. Soumeillant , Serge Zaretsky , Bin Zheng , Ye Zhu
IPC: C07D487/04
Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolodin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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Patent Agency Ranking
公开(公告)号：US20190351065A1
公开(公告)日：2019-11-21
申请号：US15776923
申请日：2016-11-22
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Matthew R. Hickey , Antonio Ramirez
Abstract: The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25° C. without stirring until completion, typically within 24 hours.
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![PROCESS FOR THE PREPARATION OF 4-(8-(2-CHLOROPHENOXY)-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YL)BICYCLO[2.2.1]HEPTAN-1-OL AND NOVEL INTERMEDIATES THEREFOR](/abs-image/US/2016/02/11/US20160039813A1/abs.jpg.150x150.jpg)
6.发明申请PROCESS FOR THE PREPARATION OF 4-(8-(2-CHLOROPHENOXY)-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YL)BICYCLO[2.2.1]HEPTAN-1-OL AND NOVEL INTERMEDIATES THEREFOR 有权制备4-（8-（2-氯苯氧基） - [1,2,4]三唑并[4,3-A]吡啶-3-基）双氰胺[2.2.1]庚烷-1-醇和新的方法 其中间性公开(公告)号：US20160039813A1
公开(公告)日：2016-02-11
申请号：US14817352
申请日：2015-08-04
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Xinhua Qian , Keming Zhu , Joerg Deerberg , Wendy Wangying Yang , Kana Yamamoto , Matthew R. Hickey
IPC: C07D471/04 , C07C51/29 , C07D213/77 , C07C29/00 , C07C35/29 , C07C61/13
CPC classification number: C07D471/04 , C07C29/00 , C07C35/29 , C07C51/29 , C07C61/13 , C07C2602/42 , C07D213/77
Abstract: A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases.
Abstract translation: 提供了制备4-（8-（2-氯苯氧基） - [1,2,4]三唑并[4,3-a]吡啶-3-基）双环[2.2.1]庚-1-醇和 在此过程中使用的新型中间体。 该化合物是在治疗各种代谢疾病中表现出活性的11-β羟基类固醇脱氢酶I型抑制剂。
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![Process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrroldin-1-yl)cyclohexyl)acetamide](/abs-image/US/2022/02/22/US11254679B2/abs.jpg.150x150.jpg)
公开(公告)号：US11254679B2
公开(公告)日：2022-02-22
申请号：US16631915
申请日：2018-07-19
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Burcu Selin Aytar , Alina Borovika , Collin Chan , Joerg Deerberg , Nathan R. Domagalski , Martin D. Eastgate , Yu Fan , Michael David Bengt Fenster , Robert V. Forest , Francisco Gonzalez-Bobes , Rebecca A. Green , Matthew R. Hickey , Nathaniel David Kopp , Thomas E. La Cruz , Kathleen Lauser , Hong Geun Lee , David K. Leahy , Helen Y. Luo , Thomas M. Razler , Scott A. Savage , Chris Sfouggatakis , Maxime C. D. Soumeillant , Serge Zaretsky , Bin Zheng , Ye Zhu
IPC: C07D487/04
Abstract: The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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公开(公告)号：US11213589B2
公开(公告)日：2022-01-04
申请号：US16797361
申请日：2020-02-21
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Matthew R. Hickey , Antonio Ramirez
Abstract: The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25° C. without stirring until completion, typically within 24 hours.
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公开(公告)号：US20200276319A1
公开(公告)日：2020-09-03
申请号：US16797361
申请日：2020-02-21
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Matthew R. Hickey , Antonio Ramirez
Abstract: The present disclosure provides an additive system for use in protein PEGylation. The additive system includes p-aminobenzoic hydrazide used either alone or in combination with aromatic amines, such as 3,5-diaminobenzoic acid, or with ammonium salts such as ammonium chloride or ammonium acetate. The disclosed additive combination provides several benefits including increased reaction rates, higher yields and reduction in the aminoxy-PEG equivalents required to complete the conjugation reaction. Typical reactions can be run by combining the additive or additive system with a solution of a protein and aminoxy-PEG reagent. The solution is adjusted to pH 4 and held at 20-25° C. without stirring until completion, typically within 24 hours.
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