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1.发明授权Co-processing method and formulations for HIV attachment inhibitor prodrug compound and excipients 有权用于HIV附着抑制剂前药化合物和赋形剂的协同处理方法和制剂公开(公告)号：US09248139B2
公开(公告)日：2016-02-02
申请号：US13716306
申请日：2012-12-17
Applicant: Bristol-Myers Squibb Company
Inventor： Shih-Ying Chang , Donald Kientzler , Deniz Erdemir , San Kiang , Tamar Rosenbaum
IPC: A61K31/675 , A61K9/14 , A61K9/20
CPC classification number: C07D471/04 , A61K9/14 , A61K9/146 , A61K9/2054 , A61K9/2095 , A61K31/675 , C07F9/6561
Abstract: A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried.
Abstract translation: 制备HIV附着抑制剂哌嗪三盐前药化合物的制剂的方法包括将前药化合物溶解在溶剂中以形成溶液; 向溶液中加入第一量的第一种抗溶剂; 然后将第一量的HPMC分散在溶液中; 向溶液中加入第二量的第一种反溶剂; 将第二量的HPMC分散在溶液中; 然后向溶液中加入第二种抗溶剂，以使化合物与HPMC结晶，从而形成制剂，其中第二种抗溶剂是丙酮和乙酸异丙酯（IPAC）的组合。 然后将制剂洗涤并干燥。
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公开(公告)号：US11236049B2
公开(公告)日：2022-02-01
申请号：US16624490
申请日：2018-06-29
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Jay Patrick Powers , Hilary Plake Beck , Maksim Osipov , Maureen Kay Reilly , Hunter Paul Shunatona , James Ross Walker , Mikhail Zibinsky , Tamar Rosenbaum , Ian Scott Young , Jennifer Nelson , Petinka Vlahova
IPC: C07D215/18 , A61K45/06
Abstract: The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
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3.发明申请CO-PROCESSING METHOD AND FORMULATION FOR HIV ATTACHMENT INHIBITOR PRODRUG COMPOUND AND EXCIPIENTS 审中-公开艾滋病毒联合治疗抑制剂化合物及其制剂的共同加工方法与配方公开(公告)号：US20160102093A1
公开(公告)日：2016-04-14
申请号：US14974644
申请日：2015-12-18
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Shih-Ying Chang , Donald Kientzler , Deniz Erdemir , San Kiang , Tamar Rosenbaum
IPC: C07D471/04 , C07F9/6561
CPC classification number: C07D471/04 , A61K9/14 , A61K9/146 , A61K9/2054 , A61K9/2095 , A61K31/675 , C07F9/6561
Abstract: A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried.
Abstract translation: 制备HIV附着抑制剂哌嗪三盐前药化合物的制剂的方法包括将前药化合物溶解在溶剂中以形成溶液; 向溶液中加入第一量的第一种抗溶剂; 然后将第一量的HPMC分散在溶液中; 向溶液中加入第二量的第一种反溶剂; 将第二量的HPMC分散在溶液中; 然后向溶液中加入第二种抗溶剂，以使化合物与HPMC结晶，从而形成制剂，其中第二种抗溶剂是丙酮和乙酸异丙酯（IPAC）的组合。 然后将制剂洗涤并干燥。
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4.发明申请Co-Processing Method and Formulations for HIV Attachment Inhibitor Prodrug Compound and Excipients 有权HIV附着抑制剂前药化合物和赋形剂的共加工方法和配方公开(公告)号：US20130164345A1
公开(公告)日：2013-06-27
申请号：US13716306
申请日：2012-12-17
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Shih-Ying Chang , Donald Kientzler , Deniz Erdemir , San Kiang , Tamar Rosenbaum
IPC: A61K31/675 , A61K9/14
CPC classification number: C07D471/04 , A61K9/14 , A61K9/146 , A61K9/2054 , A61K9/2095 , A61K31/675 , C07F9/6561
Abstract: A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried.
Abstract translation: 制备HIV附着抑制剂哌嗪三盐前药化合物的制剂的方法包括将前药化合物溶解在溶剂中以形成溶液; 向溶液中加入第一量的第一种抗溶剂; 然后将第一量的HPMC分散在溶液中; 向溶液中加入第二量的第一种反溶剂; 将第二量的HPMC分散在溶液中; 然后向溶液中加入第二种抗溶剂，以使化合物与HPMC结晶，从而形成制剂，其中第二种抗溶剂是丙酮和乙酸异丙酯（IPAC）的组合。 然后将制剂洗涤并干燥。
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