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公开(公告)号：WO2010127190A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033072
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , BORCHARDT, Thomas , BRACKEMYER, Paul , CATRON, Nathaniel , HENRY, Rodger , LOU, Xiaochun , RAVN, Matthew , ZHANG, Geoff , ZHOU, Deliang
Inventor： BORCHARDT, Thomas , BRACKEMYER, Paul , CATRON, Nathaniel , HENRY, Rodger , LOU, Xiaochun , RAVN, Matthew , ZHANG, Geoff , ZHOU, Deliang
IPC: C07D295/155 , A61K31/496 , A61P35/00
CPC classification number: C07D295/155
Abstract: ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Abstract translation: ABT-263 bis-HCl及其结晶多晶型物是用于治疗特征在于过表达一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）的疾病的药物组合物的合适的活性药物成分。
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公开(公告)号：WO2008014222A1
公开(公告)日：2008-01-31
申请号：PCT/US2007/074159
申请日：2007-07-24
Applicant: ABBOTT LABORATORIES , VISWANATH, Shekhar , BARTELT, Larry , LEANNA, Robert , RASMUSSEN, Michael , DHAON, Madhup , HENRY, Rodger , BORCHARDT, Thomas , CHEN, Shuang , ZHANG, Geoff
Inventor： VISWANATH, Shekhar , BARTELT, Larry , LEANNA, Robert , RASMUSSEN, Michael , DHAON, Madhup , HENRY, Rodger , BORCHARDT, Thomas , CHEN, Shuang , ZHANG, Geoff
IPC: C07D498/18 , A61K31/395 , A61P37/06 , A61K31/4353
CPC classification number: C07D498/18
Abstract: A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula (I), which is optionally a prodrug, salt, derivative, or combination thereof: Formula (I)
Abstract translation: 雷帕霉素类似物组合物包括雷帕霉素类似物的结晶形式。 该晶体可以是水合物，脱水剂，溶剂化物或去溶剂化物。 雷帕霉素类似物可以具有式（I）的结构，其可任选地是前药，盐，衍生物或其组合：式（I）
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公开(公告)号：WO2010127198A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033085
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , ABBOTT GMBH & CO. KG , CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , GOKHALE, Rajeev , HAIGHT, Anthony R. , HEEMSTRA, Katherine , HILL, David , KNOBLOCH, Martin, Dr. , KOSTELAC, Drazen, Dr. , LAFOUNTAINE, Justin S. , LI, Yanxia , LIEPOLD, Bernd, Dr. , MARSH, Kennan , MILLER, Jonathan Mark , PACKHAEUSER, Claudia, Dr. , SANZGIRI, Yeshwant , SCHMITT, Eric , SHI, Yi , STEIGER, Norbert , TONG, Ping , WU, Huailiang , ZHANG, Geoff , ZHOU, Deliang
Inventor： CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , GOKHALE, Rajeev , HAIGHT, Anthony R. , HEEMSTRA, Katherine , HILL, David , KNOBLOCH, Martin, Dr. , KOSTELAC, Drazen, Dr. , LAFOUNTAINE, Justin S. , LI, Yanxia , LIEPOLD, Bernd, Dr. , MARSH, Kennan , MILLER, Jonathan Mark , PACKHAEUSER, Claudia, Dr. , SANZGIRI, Yeshwant , SCHMITT, Eric , SHI, Yi , STEIGER, Norbert , TONG, Ping , WU, Huailiang , ZHANG, Geoff , ZHOU, Deliang
CPC classification number: A61K31/5377 , A61K9/08 , A61K9/10 , A61K9/146 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866
Abstract: An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis -HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Abstract translation: 可口服递送的药物组合物包含作为唯一或第一活性成分的本文定义的式I化合物或其药学上可接受的盐，例如以游离碱当量分散的ABT-263游离碱或ABT-263双-HCl盐 至少约2.5重量％的组合物，在药学上可接受的载体中; 其中所述活性成分是固态形式和/或所述组合物还包含以有效抑制活性成分在其硫醚键的氧化的量分散在载体中的药学上可接受的较重硫族元素抗氧化剂。 该组合物适合于有需要的受试者的口服给药，用于治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）过表达为特征的疾病。
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公开(公告)号：WO2006015194A2
公开(公告)日：2006-02-09
申请号：PCT/US2005/026937
申请日：2005-07-29
Applicant: ABBOTT LABORATORIES , HAIGHT, Anthony , BARNES, David , ZHANG, Geoff
Inventor： HAIGHT, Anthony , BARNES, David , ZHANG, Geoff
IPC: C07D213/70
CPC classification number: C07D213/74
Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.
Abstract translation: 制备1-（6-氨基-3,5-二氟吡啶-2-基）-8-氯-6-氟-7-（3-羟基吖丁啶-1-基）-4-氧代-1,4- 二氢-3-喹啉羧酸及其治疗上可接受的盐，以及该方法中使用的中间体。
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公开(公告)号：WO2010127193A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033075
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , HAIGHT, Anthony R. , HEEMSTRA, Katherine , SANZGIRI, Yeshwant , SCHMITT, Eric , TONG, Ping , ZHANG, Geoff , ZHOU, Deliang
Inventor： CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , HAIGHT, Anthony R. , HEEMSTRA, Katherine , SANZGIRI, Yeshwant , SCHMITT, Eric , TONG, Ping , ZHANG, Geoff , ZHOU, Deliang
CPC classification number: A61K31/5377 , A61K9/0095 , A61K9/08 , A61K9/10 , A61K9/4858 , A61K47/14 , A61K47/183 , A61K47/24 , A61K47/26
Abstract: An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
Abstract translation: 可口服递送的药物组合物包含Bcl-2家族蛋白质抑制化合物，例如ABT-263，较重硫族元素抗氧化剂和基本上非水性脂质载体，其中所述化合物和所述抗氧化剂在载体中的溶液中。 该组合物适合于有需要的受试者的口服给药，用于治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）过表达为特征的疾病。
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Patent Agency Ranking6.发明申请PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED DISSOLUTION PROFILES FOR POORLY SOLUBLE DRUGS 审中-公开具有改善的溶解性溶液型号的药物组合物
公开(公告)号：WO2006110815A1
公开(公告)日：2006-10-19
申请号：PCT/US2006/013651
申请日：2006-04-11
Applicant: ABBOTT LABORATORIES , WU, Huailiang , ZHANG, Geoff
Inventor： WU, Huailiang , ZHANG, Geoff
CPC classification number: A61K47/38 , A61K9/0065 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/4866 , A61K31/00 , A61K31/33 , A61K31/47 , A61K31/4709 , A61K45/06 , A61K47/32
Abstract: Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed.
Abstract translation: 公开了具有改进的药物溶出曲线的药物组合物。
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7.发明申请FORMULATION COMPRISING A DRUG OF LOW WATER SOLUBILITY AND METHOD OF USE THEREOF 审中-公开包含低水溶性药物的配方及其使用方法
公开(公告)号：WO2007050574A1
公开(公告)日：2007-05-03
申请号：PCT/US2006/041419
申请日：2006-10-24
Applicant: ABBOTT LABORATORIES , LIPARI, John, M. , LEFEBVRE, Didier, R. , JU, Tzuchi, R. , MARSH, Kennan, C. , ZHANG, Geoff , JAYANTH, Jayanthy , PUJARA, Chetan, P. , CHESKIN, Howard, S. , VUCENOVIC, Vitomir , TONG, Ping
Inventor： LIPARI, John, M. , LEFEBVRE, Didier, R. , JU, Tzuchi, R. , MARSH, Kennan, C. , ZHANG, Geoff , JAYANTH, Jayanthy , PUJARA, Chetan, P. , CHESKIN, Howard, S. , VUCENOVIC, Vitomir , TONG, Ping
IPC: A61K9/107 , A61K47/24 , A61K31/423 , A61K31/428 , A61K31/47 , A61K31/503 , A61K31/517
CPC classification number: A61K9/10 , A61K9/0056 , A61K9/0095 , A61K9/107 , A61K9/48 , A61K31/416 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/4439 , A61K31/47 , A61K31/497 , A61K31/501 , A61K31/503 , A61K31/506 , A61K31/517 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/24 , A61K47/44
Abstract: A pharmaceutical composition comprises a drug-carrier system having a small-molecule drug of low water solubility, e.g., N [4 (3-amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), and (+)-1-(5-tert-butyl-l-y1)-3-( lH-indazol-4-yl)-urea (ABT-102), in solution in a substantially non-aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The drug-carrier system, when mixed with an aqueous phase, typically forms a non-gelling, substantially non-transparent liquid dispersion. The composition is suitable for administration by a suitable route, e.g., orally, to a subject in need thereof.
Abstract translation: 药物组合物包含具有低水溶性的小分子药物的药物载体体系，例如N [4（3-氨基-1H-吲唑-4-基）苯基] -N' - （2-氟-5 - 甲基苯基）脲（ABT-869）和（+）-1-（5-叔丁基-1-y1）-3-（1H-吲唑-4-基） - 脲（ABT-102） 在包含至少一种磷脂和药学上可接受的增溶剂的基本上非水的载体中。 当与水相混合时，药物载体体系通常形成非凝胶化的基本不透明的液体分散体。 组合物适合于通过合适途径（例如口服）给予有需要的受试者。
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8.发明公开
公开(公告)号：EP1959926A1
公开(公告)日：2008-08-27
申请号：EP06817321.0
申请日：2006-10-24
Applicant: ABBOTT LABORATORIES
Inventor： LIPARI, John, M. , LEFEBVRE, Didier, R. , JU, Tzuchi, R. , MARSH, Kennan, C. , ZHANG, Geoff , JAYANTH, Jayanthy , PUJARA, Chetan, P. , CHESKIN, Howard, S. , VUCENOVIC, Vitomir , TONG, Ping
IPC: A61K9/107 , A61K47/24 , A61K31/423 , A61K31/428 , A61K31/47 , A61K31/503 , A61K31/517
CPC classification number: A61K9/10 , A61K9/0056 , A61K9/0095 , A61K9/107 , A61K9/48 , A61K31/416 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/4439 , A61K31/47 , A61K31/497 , A61K31/501 , A61K31/503 , A61K31/506 , A61K31/517 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/24 , A61K47/44
Abstract: A pharmaceutical composition comprises a drug-carrier system having a small-molecule drug of low water solubility, e.g., N [4 (3-amino-1H-indazol-4-yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), and (+)-1-(5-tert-butyl-l-y1)-3-( lH-indazol-4-yl)-urea (ABT-102), in solution in a substantially non-aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The drug-carrier system, when mixed with an aqueous phase, typically forms a non-gelling, substantially non-transparent liquid dispersion. The composition is suitable for administration by a suitable route, e.g., orally, to a subject in need thereof.
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9.发明授权PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED DISSOLUTION PROFILES FOR POORLY SOLUBLE DRUGS 有权用于重型可溶物更高的分辨率谱的药学组合物
公开(公告)号：EP1868581B1
公开(公告)日：2012-03-14
申请号：EP06740898.9
申请日：2006-04-11
Applicant: Abbott Laboratories
Inventor： WU, Huailiang , ZHANG, Geoff
CPC classification number: A61K47/38 , A61K9/0065 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/4866 , A61K31/00 , A61K31/33 , A61K31/47 , A61K31/4709 , A61K45/06 , A61K47/32
Abstract: Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed.
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公开(公告)号：EP2424849A1
公开(公告)日：2012-03-07
申请号：EP10717392.4
申请日：2010-04-30
Applicant: Abbott Laboratories
Inventor： BORCHARDT, Thomas , BRACKEMYER, Paul , CATRON, Nathaniel , HENRY, Rodger , LOU, Xiaochun , RAVN, Matthew , ZHANG, Geoff , ZHOU, Deliang
IPC: C07D295/155 , A61K31/496 , A61P35/00
CPC classification number: C07D295/155
Abstract: ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
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