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1.发明申请INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4 审中-公开用于定向递送至表达VLA-4的细胞的整合拮抗剂
公开(公告)号：WO2013110680A1
公开(公告)日：2013-08-01
申请号：PCT/EP2013/051275
申请日：2013-01-24
Applicant: F. HOFFMANN-LA ROCHE AG , GOODNOW Jr., Robert, Alan , HAMILTON, Matthew, Michael , SIDDURI, Achyutharao
CPC classification number: A61K47/545 , A61K47/54 , A61K47/60
Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.
Abstract translation: 本发明涉及式I化合物：其中R1，R2和n在详细描述和权利要求书中定义。 特别地，本发明涉及式I化合物，其用于制备和递送缀合的部分，例如小分子，肽，核酸，荧光部分和与VLA-4整联蛋白拮抗剂连接至靶细胞的聚合物 表达VLA-4。
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2.发明申请INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING ALPHA-V-BETA-3 审中-公开用于指定递送至表达ALPHA-V-BETA-3的细胞的整合拮抗剂
公开(公告)号：WO2013110578A1
公开(公告)日：2013-08-01
申请号：PCT/EP2013/051082
申请日：2013-01-22
Applicant: F. HOFFMANN-LA ROCHE AG , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , KOWALCZYK, Agnieszka , SIDDURI, Achyutharao
Inventor： GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , KOWALCZYK, Agnieszka , SIDDURI, Achyutharao
CPC classification number: C07D277/593 , A61K47/48061 , A61K47/48092 , A61K47/48215 , A61K47/545 , A61K47/549 , A61K47/60 , C07C237/52 , C07C327/32 , C07D207/452 , C07D239/14 , C07D417/12
Abstract: The invention relates to compounds of formula (I): wherein R 1 , R 2 , and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3.
Abstract translation: 本发明涉及式（I）的化合物：其中R 1，R 2和n在详细描述和权利要求书中定义。 特别地，本发明涉及用于制备和递送缀合部分的式（I）化合物，所述共轭部分例如小分子，肽，核酸，荧光部分和与α-V-β- 3整合素拮抗剂靶向表达α-V-β-3的细胞。
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公开(公告)号：WO2011057956A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/066857
申请日：2010-11-05
Applicant: F. HOFFMANN-LA ROCHE AG , BOLIN, David, Robert , HAMILTON, Matthew, Michael , MCDERMOTT, Lee, Apostle , QIAN, Yimin
IPC: C07D261/20 , C07D403/12 , A61P3/10 , A61K31/423
CPC classification number: C07D261/20 , C07D403/12
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Abstract translation: 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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公开(公告)号：WO2010056506A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/062154
申请日：2009-10-27
Applicant: VIA PHARMACEUTICALS, INC. , BOLIN, David, R. , CHEUNG, Adrian, Wai-hing , HAMILTON, Matthew, Michael , MARCOPULOUS, Nicholas , McDERMOTT, Lee, Apostle , QIAN, Yimin
Inventor： BOLIN, David, R. , CHEUNG, Adrian, Wai-hing , HAMILTON, Matthew, Michael , MARCOPULOUS, Nicholas , McDERMOTT, Lee, Apostle , QIAN, Yimin
IPC: C12Q1/48
CPC classification number: C07D401/04 , C07D213/75 , C07D213/82 , C07D277/46 , C07D277/82 , C07D295/155 , C07D295/185 , C07D295/205 , C07D333/54 , C07D401/12
Abstract: Provided herein are compounds of the formula (I): were Rl is phenyl, R2 is hyrogen, halogen or lower alkyl,X is carbon on nitrogen, and R3 is isoquinoline, -amino, or a-4- to 6-membered heterocycloalkyl ring and pharmaceutically acceptable salts thereof, which are active as DGAT inhibitors and therefore find uses in treatment of diseases associated with abnormal metabolism of triglicerides, such as, for example, obesity, type Il diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供了式（I）的化合物：R1是苯基，R2是氢，卤素或低级烷基，X是氮上的碳，R3是异喹啉， - 氨基或a-4-至6-元杂环烷基环 其药学上可接受的盐，其作为DGAT抑制剂是有活性的，因此可用于治疗与三联嘧啶的异常代谢相关的疾病，例如肥胖症，II型糖尿病和代谢综合征。
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公开(公告)号：WO2008141976A1
公开(公告)日：2008-11-27
申请号：PCT/EP2008/055843
申请日：2008-05-13
Applicant: F. HOFFMANN-LA ROCHE AG , BOLIN, David Robert , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , HAMILTON, Matthew Michael , MCDERMOTT, Lee Apostle , QIAN, Yimin , TAN, Jenny , YUN, Weiya
Inventor： BOLIN, David Robert , CHEUNG, Adrian Wai-Hing , FIROOZNIA, Fariborz , HAMILTON, Matthew Michael , MCDERMOTT, Lee Apostle , QIAN, Yimin , TAN, Jenny , YUN, Weiya
IPC: C07D231/14 , C07D263/34 , C07D277/56 , C07D307/68 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/422 , A61K31/427 , A61K31/4178 , A61K31/4192 , A61K31/4427
CPC classification number: C07D263/34 , C07D231/14 , C07D277/56 , C07D307/68 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。
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Patent Agency Ranking6.发明申请11-BETA-HYDROXYSTEROID DEHYDROGENASE-1-INHIBITOR-DIABETES-TYPE 2-1 审中-公开11-β-羟基甾体脱氢酶-1抑制剂 - 糖尿病类型2-1
公开(公告)号：WO2007025892A1
公开(公告)日：2007-03-08
申请号：PCT/EP2006/065498
申请日：2006-08-21
Applicant: F. HOFFMANN-LA ROCHE AG , BANNER, Bruce Lester , BILOTTA, Joseph Anthony , FOTOUHI, Nader , GILLESPIE, Paul , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , HAYNES, Nancy-Ellen , KOWALCZYK, Agnieszka , MAYWEG, Alexander V. , MYERS, Michael Paul , PIETRANICO-COLE, Sherrie Lynn , SCOTT, Nathan Robert , THAKKAR, Kshitij Chhabilbhai , TILLEY, Jefferson Wright
Inventor： BANNER, Bruce Lester , BILOTTA, Joseph Anthony , FOTOUHI, Nader , GILLESPIE, Paul , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , HAYNES, Nancy-Ellen , KOWALCZYK, Agnieszka , MAYWEG, Alexander V. , MYERS, Michael Paul , PIETRANICO-COLE, Sherrie Lynn , SCOTT, Nathan Robert , THAKKAR, Kshitij Chhabilbhai , TILLEY, Jefferson Wright
IPC: C07D231/54 , A61P3/00 , A61K31/4184
CPC classification number: C07D231/54
Abstract: Provided herein are compounds of the formula (I); as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供了式（I）的化合物; 以及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如II型糖尿病和代谢综合征。
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公开(公告)号：WO2011067174A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068279
申请日：2010-11-26
Inventor： BOLIN, David, Robert , HAMILTON, Matthew, Michael
IPC: A61P3/10 , C07C233/25 , C07C233/47 , C07C233/60 , A61K31/095 , A61K31/194 , A61K31/195 , A61K31/401 , C07C311/08 , C07C311/09 , C07D207/08 , C07D207/16
CPC classification number: C07C233/25 , A61K31/095 , A61K31/194 , A61K31/195 , A61K31/401 , C07C233/47 , C07C233/60 , C07C311/08 , C07C311/09 , C07C2601/08 , C07D207/08 , C07D207/16
Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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公开(公告)号：WO2009037222A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062234
申请日：2008-09-15
Applicant: F. HOFFMANN-LA ROCHE AG , BOLIN, David Robert , CAI, Jianping , CHEUNG, Adrian Wai-Hing , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , LI, Shiming , MCDERMOTT, Lee Apostle , YUN, Weiya
Inventor： BOLIN, David Robert , CAI, Jianping , CHEUNG, Adrian Wai-Hing , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , LI, Shiming , MCDERMOTT, Lee Apostle , YUN, Weiya
IPC: C07D401/14 , C07D403/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/437 , A61K31/416 , A61K31/404 , A61P3/00
CPC classification number: C07D413/12 , C07D401/14 , C07D403/12 , C07D407/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。
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9.发明申请CHITOSAN COVALENTLY LINKED WITH SMALL MOLECULE INTEGRIN ANTAGONIST FOR TARGETED DELIVERY 审中-公开CHITOSAN共同连接小分子整合剂ANAGONIST用于定向递送
公开(公告)号：WO2013110681A1
公开(公告)日：2013-08-01
申请号：PCT/EP2013/051279
申请日：2013-01-24
Applicant: F. HOFFMANN-LA ROCHE AG , CHIN, Jayne , GOODNOW Jr., Robert, Alan , HAMILTON, Matthew, Michael , SIDDURI, Achyutharao
Inventor： CHIN, Jayne , GOODNOW Jr., Robert, Alan , HAMILTON, Matthew, Michael , SIDDURI, Achyutharao
CPC classification number: A61K31/722 , A61K47/60 , A61K47/61 , C08B37/003
Abstract: The invention relates to the chitosan polymer derivatives of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Y, X 1 , X 4 , R 1 , R 2 , and n are defined in the detailed description and claims. The chitosan polymer derivatives of formula I bind to or associate with alpha-4-beta-1 (α4ß1) and alpha-V-beta-3 (α Vß3) integrin dimers and can be used in delivery formulations to deliver drugs, nucleic acids, or other therapeutic compounds to tissues or cells expressing such integrins.
Abstract translation: 本发明涉及式I的壳聚糖聚合物衍生物及其药学上可接受的盐和酯，其中Y，X 1，X 4，R 1，R 2和n在详细描述和权利要求书中定义。 式I的壳聚糖聚合物衍生物与α-4-β-1（α4β1）和α-V-β-3（αVβ3）整联蛋白二聚体结合或结合，并且可用于递送制剂中以递送药物，核酸， 或其他治疗性化合物施用于表达这种整联蛋白的组织或细胞。
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10.发明申请INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1 审中-公开用于指定递送至表达LFA-1的细胞的整合拮抗剂
公开(公告)号：WO2013110679A1
公开(公告)日：2013-08-01
申请号：PCT/EP2013/051273
申请日：2013-01-24
Applicant: F. HOFFMANN-LA ROCHE AG , GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , KOWALCZYK, Agnieszka , SIDDURI, Achyutharao
Inventor： GOODNOW JR., Robert Alan , HAMILTON, Matthew Michael , KOWALCZYK, Agnieszka , SIDDURI, Achyutharao
CPC classification number: C07D403/12 , A61K47/54 , A61K47/545 , A61K47/60 , C07C327/06 , C07C381/00 , C07D207/36 , C07D207/46 , C07D213/71 , C07H21/02
Abstract: The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2和n在详细描述和权利要求书中定义。 特别地，本发明涉及式I化合物，其用于制备和递送缀合的部分，例如与LFA-1整联蛋白拮抗剂连接至靶细胞的小分子，肽，核酸，荧光部分和聚合物 表达LFA-1。
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