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公开(公告)号：US20110092520A1
公开(公告)日：2011-04-21
申请号：US12996801
申请日：2009-06-02
申请人： Shuntaro Furukawa , Taketo Ikeno , Shinji Kato , Masashi Kawasaki , Hisaki Kojima , Wataru Minagawa , Naotaka Sawada , Fuyuki Yamamoto , Sachin Lohani , Yaling Wang
发明人： Shuntaro Furukawa , Taketo Ikeno , Shinji Kato , Masashi Kawasaki , Hisaki Kojima , Wataru Minagawa , Naotaka Sawada , Fuyuki Yamamoto , Sachin Lohani , Yaling Wang
IPC分类号： A61K31/519 , C07D487/04 , C07D221/04 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2′-methyl-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-isoquinolin]-7′-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
摘要翻译： 本发明涉及一种3-（2,6-二氯苯基）-4-亚氨基-7 - [（2'-甲基-2'，3'-二氢-1'H-螺[环丙烷 -1,4'-异喹啉] -7'-基）氨基] -3,4-二氢嘧啶并[4,5-d]嘧啶-2（1H） - 酮（化合物A）或化合物A的药学上可接受的盐 以及化合物A或化合物A的药学上可接受的盐的结晶形式，其可用于治疗各种癌症作为激酶抑制剂，特别是作为威尔激酶抑制剂的领域。
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公开(公告)号：US08507504B2
公开(公告)日：2013-08-13
申请号：US12996801
申请日：2009-06-02
申请人： Shuntaro Furukawa , Taketo Ikeno , Shinji Kato , Masashi Kawasaki , Hisaki Kojima , Wataru Minagawa , Naotaka Sawada , Fuyuki Yamamoto , Sachin Lohani , Yaling Wang
发明人： Shuntaro Furukawa , Taketo Ikeno , Shinji Kato , Masashi Kawasaki , Hisaki Kojima , Wataru Minagawa , Naotaka Sawada , Fuyuki Yamamoto , Sachin Lohani , Yaling Wang
IPC分类号： C07D487/00 , A61K31/505
CPC分类号： C07D487/04
摘要： The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2′-methyl-2′,3′-dihydro-1′H-spiro[cyclopropane-1,4′-isoquinolin]-7′-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
摘要翻译： 本发明涉及一种3-（2,6-二氯苯基）-4-亚氨基-7 - [（2'-甲基-2'，3'-二氢-1'H-螺[环丙烷 -1,4'-异喹啉] -7'-基）氨基] -3,4-二氢嘧啶并[4,5-d]嘧啶-2（1H） - 酮（化合物A）或化合物A的药学上可接受的盐 以及化合物A或化合物A的药学上可接受的盐的结晶形式，其可用于治疗各种癌症作为激酶抑制剂，特别是作为威尔激酶抑制剂的领域。
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公开(公告)号：US07700611B2
公开(公告)日：2010-04-20
申请号：US11988780
申请日：2006-07-24
申请人： Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
发明人： Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D491/10
摘要： The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.
摘要翻译： 本发明涉及一种制备结晶反式-N-〔1-（2-氟苯基）-S-吡唑基〕-3-氧 - 环螺[6-氮杂苯并呋喃-1（3H），1'-环己烷〕-4 ' - 甲酰胺及其新型盐，水合物及其多晶型物。
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公开(公告)号：US20090124648A1
公开(公告)日：2009-05-14
申请号：US11988780
申请日：2006-07-24
申请人： Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
发明人： Russell R. Ferlita , Yuji Haga , Makoto Ishikawa , Keisuke Kamei , Shinji Kato , Hisaki Kojima , Aaron Moment , Nobuaki Nonoyama , Nobuya Satake , Kazuki Shigemori , Toshihiro Wada , Yaling Wang , Steven A. Weissman , Robert M. Wenslow
IPC分类号： A61K31/4355 , C07D491/048 , A61P3/04
CPC分类号： C07D491/10
摘要： The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide and novel salts, hydrates and polymorphs thereof.
摘要翻译： 本发明涉及一种制备结晶反式-N-〔1-（2-氟苯基）-S-吡唑基〕-3-氧 - 环螺[6-氮杂苯并呋喃-1（3H），1'-环己烷〕-4 ' - 甲酰胺及其新型盐，水合物及其多晶型物。
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公开(公告)号：US07074930B2
公开(公告)日：2006-07-11
申请号：US10494760
申请日：2002-11-01
申请人： Kenneth M. Wells , Nobuyoshi Yasuda , Yaling Wang
发明人： Kenneth M. Wells , Nobuyoshi Yasuda , Yaling Wang
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07C215/10 , C07D471/04
摘要： Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin αvβ3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.
摘要翻译： 3- {2-氧代-3- [3-（5,6,7,8-四氢[1,8]萘啶-2-基） - 丙基]咪唑烷-1-基} -3-（6 - 甲氧基 - 吡啶-3-基）丙酸是整联蛋白α2受体的有效拮抗剂，可用于预防和/或治疗骨质疏松症和血管再狭窄，以及与过度血管生成相关的病症，如黄斑变性，糖尿病 视网膜病变，动脉粥样硬化，炎性关节炎，癌症和转移性肿瘤生长。 本发明还涉及制备新型盐的方法以及含有盐的药物组合物和使用该盐的方法。
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公开(公告)号：US06509347B2
公开(公告)日：2003-01-21
申请号：US10167678
申请日：2002-06-11
申请人： Wei Xu , Yaling Wang
发明人： Wei Xu , Yaling Wang
IPC分类号： A61K314375
CPC分类号： C07D471/04
摘要： The present invention relates to novel crystalline forms of the integrin &agr;v&bgr;3 antagonist 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid.
摘要翻译： 本发明涉及整联蛋白α-β3拮抗剂3- {2-氧代-3- [3-（5,6,7,8-四氢 - [1,8]萘啶-2-基） - 丙基] 咪唑烷-1-基} -3（S） - （6-甲氧基 - 吡啶-3-基） - 丙酸。
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7.发明申请FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF 审中-公开四唑替代方法的形成及其选择性减少公开(公告)号：US20100041893A1
公开(公告)日：2010-02-18
申请号：US12603901
申请日：2009-10-22
申请人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
发明人： KEVIN R. CAMPOS , Artis Klapars , J. Christopher McWilliams , C. Scott Shultz , Debra J. Wallace , Alex M. Chen , Lisa F. Frey , Andrey V. Peresypkin , Yaling Wang , Robert M. Wenslow , Cheng-Yi Chen
IPC分类号： C07D211/72 , C07C233/00
CPC分类号： C07C231/18 , C07C253/14 , C07C309/73 , C07D213/64 , C07C255/56
摘要： The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
摘要翻译： 本发明涉及通过主要酰胺（IV）与结构式（III）的化合物的钯催化偶联制备烯酰胺（II）的实际方法，如下所示：除了结晶形式 通过该方法制备的化合物，特别是无水晶体形式B和分解成三种图案的晶体溶剂化物，类型1，类型2和类型3以及在该方法中产生的结晶中间体化合物。 此外，本发明涉及四取代的酰胺（II）与相应的酰胺（I）的立体选择性还原。
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公开(公告)号：US20080227786A1
公开(公告)日：2008-09-18
申请号：US10585603
申请日：2005-01-12
IPC分类号： A61K31/4985 , C07D487/02 , A61P3/10
CPC分类号： C07D487/04
摘要： Novel crystalline salts of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-&agr; amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译： （2R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3-a]吡嗪-7（8H） - 基] -1-（2,4,5-三氟苯基）丁烷-2-α胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型盐的药物组合物，制备这些盐的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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公开(公告)号：US10526611B2
公开(公告)日：2020-01-07
申请号：US15301533
申请日：2015-04-03
申请人： Stanton B Gelvin , Lan-Ying Lee , Yaling Wang
发明人： Stanton B Gelvin , Lan-Ying Lee , Yaling Wang
摘要： The present invention provides methods and compositions for enhancing the efficiency of Agrobacterium-mediated transformation of host cells, such as plant cells, wherein the host cells overexpress light-dependent short hypocotyls 10 (LSH10) protein. The methods of the invention comprise Agrobacterium-mediated transfer of T-DNA to a plant cell, wherein the T-DNA contains a DNA of interest to be inserted into a plant genome at a homologous position.
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公开(公告)号：US08637449B2
公开(公告)日：2014-01-28
申请号：US13392168
申请日：2010-08-26
IPC分类号： A61K38/00
CPC分类号： C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要翻译： 本发明涉及可用于制备式（I）的大环化合物的合成方法，其可用作丙型肝炎病毒NS3蛋白酶的抑制剂，并且可用于治疗由丙型肝炎病毒引起的病症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。
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