公开(公告)号：US20090253906A1

公开(公告)日：2009-10-08

申请号：US12417598

申请日：2009-04-02

申请人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

发明人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

IPC分类号： C07D413/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/14 ,  C07D409/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/14 ,  C07D417/04

CPC分类号： C07D417/04 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/502 ,  A61K31/517 ,  A61K31/53 ,  C07D217/00 ,  C07D217/04 ,  C07D217/08 ,  C07D217/12 ,  C07D217/14 ,  C07D217/16 ,  C07D217/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.

摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。

公开(公告)号：US20090048443A1

公开(公告)日：2009-02-19

申请号：US12252823

申请日：2008-10-16

申请人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

发明人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

IPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC分类号： C07D417/04 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/502 ,  A61K31/517 ,  A61K31/53 ,  C07D217/00 ,  C07D217/04 ,  C07D217/08 ,  C07D217/12 ,  C07D217/14 ,  C07D217/16 ,  C07D217/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined below in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.

摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14以下 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。

公开(公告)号：US20130005965A1

公开(公告)日：2013-01-03

申请号：US13540446

申请日：2012-07-02

申请人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

发明人： Bruce F. MOLINO ,  Shuang LIU ,  Peter R. GUZZO ,  James P. BECK

IPC分类号： C07D413/14 ,  C07D405/04 ,  C07D409/14 ,  C07D401/10 ,  C07D417/10 ,  C07D217/04 ,  C07D409/04 ,  C07D401/04

CPC分类号： C07D417/04 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/502 ,  A61K31/517 ,  A61K31/53 ,  C07D217/00 ,  C07D217/04 ,  C07D217/08 ,  C07D217/12 ,  C07D217/14 ,  C07D217/16 ,  C07D217/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.

公开(公告)号：US20120046271A1

公开(公告)日：2012-02-23

申请号：US13211678

申请日：2011-08-17

申请人： Peter R. GUZZO ,  Shuang LIU ,  Kristen N. RYAN ,  Bruce F. MOLINO ,  Russell DEORAZIO ,  Richard E. OLSON ,  John E. MACOR

发明人： Peter R. GUZZO ,  Shuang LIU ,  Kristen N. RYAN ,  Bruce F. MOLINO ,  Russell DEORAZIO ,  Richard E. OLSON ,  John E. MACOR

IPC分类号： A61K31/55 ,  C07D519/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/24 ,  A61P25/16 ,  A61P25/14 ,  C07D487/08 ,  A61P25/22

CPC分类号： C07D453/00 ,  C07D519/00

摘要： The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I): where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are as defined herein.

摘要翻译： 本发明的化合物由以下具有式（I）的2,5-亚甲基 - 和2,5-亚乙基 - 四氢苯并吖庚因衍生物表示：当n为1时，其中指定为*为R或S构型的碳原子， 取代基X和R 1 -R 7如本文所定义。

公开(公告)号：US20090118260A1

公开(公告)日：2009-05-07

申请号：US12253170

申请日：2008-10-16

申请人： Bruce F. MOLINO ,  Shuang LIU ,  Aruna SAMBANDAM ,  Peter R. GUZZO ,  Min HU ,  Congxiang ZHA ,  Kassoum NACRO ,  David D. MANNING ,  Matthew L. ISHERWOOD ,  Kristen N. FLEMING ,  Wenge CUI ,  Richard E. OLSON

发明人： Bruce F. MOLINO ,  Shuang LIU ,  Aruna SAMBANDAM ,  Peter R. GUZZO ,  Min HU ,  Congxiang ZHA ,  Kassoum NACRO ,  David D. MANNING ,  Matthew L. ISHERWOOD ,  Kristen N. FLEMING ,  Wenge CUI ,  Richard E. OLSON

IPC分类号： A61K31/55 ,  C07D487/02 ,  C07D403/02

CPC分类号： C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.

摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。

公开(公告)号：US20110312931A1

公开(公告)日：2011-12-22

申请号：US13151992

申请日：2011-06-02

申请人： Christopher L. CIOFFI ,  Mark A. WOLF ,  Peter R. GUZZO ,  Shuang LIU ,  Kashinath SADALAPURE ,  Visweswaran PARTHASARATHY ,  Jun-Ho MAENG

发明人： Christopher L. CIOFFI ,  Mark A. WOLF ,  Peter R. GUZZO ,  Shuang LIU ,  Kashinath SADALAPURE ,  Visweswaran PARTHASARATHY ,  Jun-Ho MAENG

IPC分类号： A61K31/496 ,  C07D403/12 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D401/12 ,  C07D487/08 ,  A61K31/495 ,  A61K31/454 ,  A61K31/4995 ,  A61P25/18 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  A61P25/04 ,  A61P25/30 ,  A61P25/34 ,  A61P25/08 ,  A61P25/14 ,  A61P25/06 ,  A61P27/02 ,  C07D295/26

CPC分类号： C07D295/26 ,  C07D205/04 ,  C07D207/48 ,  C07D211/58 ,  C07D213/71 ,  C07D233/84 ,  C07D241/04 ,  C07D249/04 ,  C07D309/14 ,  C07D313/04 ,  C07D405/12 ,  C07D487/08

摘要： The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.

摘要翻译： 本发明的化合物由下式（I）表示：其中取代基R 1，R 2，R 3，R 4，（R 5）m，R 6，A，X和Y如本文所定义。 该化合物可用于治疗由抑制GlyT-1产生或依赖于其的依赖性疾病的方法。

公开(公告)号：US20110237527A1

公开(公告)日：2011-09-29

申请号：US13052171

申请日：2011-03-21

申请人： Shuang LIU ,  Cheng GUO ,  Min HU ,  Douglas B. KITCHEN ,  Peter R. GUZZO ,  Russell DEORAZIO

发明人： Shuang LIU ,  Cheng GUO ,  Min HU ,  Douglas B. KITCHEN ,  Peter R. GUZZO ,  Russell DEORAZIO

IPC分类号： A61K31/706 ,  C07H7/06 ,  A61P3/10 ,  A61P27/12 ,  A61P3/06 ,  A61P3/04 ,  A61P17/02 ,  A61P9/10 ,  A61P9/12 ,  A61P19/06

CPC分类号： A61K31/706

摘要： The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.

摘要翻译： 本发明涉及作为钠依赖性葡萄糖共转运体-2（SGLT-2）抑制剂的化合物。 这些化合物用于治疗各种疾病，包括糖尿病，葡萄糖耐量降低，胰岛素抵抗，视网膜病变，肾病，神经病，白内障，高血糖症，高胰岛素血症，高胆固醇血症，游离脂肪酸或甘油血液水平升高，高脂血症，高甘油三酯血症，肥胖 伤口愈合，组织缺血，动脉粥样硬化和高血压。 这些化合物和组合物还可用于治疗和预防肾结石，高尿酸血症，痛风和低钠血症。 制备这些化合物的方法也在本发明中描述。

公开(公告)号：US20110306653A1

公开(公告)日：2011-12-15

申请号：US13107175

申请日：2011-05-13

申请人： Ichiro HIRAO ,  Michiko HIRAO ,  Shuang LIU ,  Iwao NOZAWA

发明人： Ichiro HIRAO ,  Michiko HIRAO ,  Shuang LIU ,  Iwao NOZAWA

IPC分类号： C07H21/04 ,  C12P19/34 ,  A61K31/7088

CPC分类号： A61K31/7088 ,  C12N15/111 ,  C12N15/67 ,  C12N2310/13 ,  C12N2310/14 ,  C12N2310/3519 ,  C12N2320/51 ,  C12N2310/531

摘要： This invention is intended to enhance and improve the resistance of a single- or double-stranded nucleic acid fragment comprising a base sequence of a functional nucleic acid to degradation by nucleolytic enzymes in a simple and cost-effective manner. The single- or double-stranded nucleic acid fragment comprises, ligated to at least one end thereof, hairpin-shaped DNA comprising: (A) a nucleic acid region comprising 2 to 5 arbitrary nucleotides; (B) a nucleic acid region comprising a “gna” or “gnna” base sequence, wherein each “n” represents “g”, “t”, “a”, or “c”, a base analogue, or a modified base; and (C) a nucleic acid region comprising a base sequence complementary to the nucleic acid region (A), sequentially from the 5′ end toward the 3′ end.

摘要翻译： 本发明旨在增强和改善包含功能性核酸的碱基序列的单链或双链核酸片段以简单和成本有效的方式降解核分解酶的抗性。 单链或双链核酸片段包含连接至至少一端的发夹状DNA，其包含：（A）包含2至5个任意核苷酸的核酸区; （B）包含“gna”或“gnna”碱基序列的核酸区域，其中每个“n”表示“g”，“t”，“a”或“c”，碱基类似物或修饰碱基 ; 和（C）包含与核酸区域（A）互补的碱基序列的核酸区域，从5'端到3'端依次。

公开(公告)号：US20180362504A1

公开(公告)日：2018-12-20

申请号：US16062423

申请日：2016-12-15

申请人： Joseph FOX ,  Xinqiao JIA ,  Will TROUT ,  Joel ROSENTHAL ,  Han ZHANG ,  Yinzhi FANG ,  Colin THORPE ,  Shuang LIU ,  Yixin XIE

发明人： Joseph FOX ,  Xinqiao JIA ,  Will TROUT ,  Joel ROSENTHAL ,  Han ZHANG ,  Yinzhi FANG ,  Colin THORPE ,  Shuang LIU ,  Yixin XIE

IPC分类号： C07D401/14 ,  C07D401/04 ,  C12P17/16

摘要： A method for catalytically converting a dihydrotetrazine 1 into a tetrazine 2, wherein one R group on the dihydrotetrazine 1 is a substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl, or heteroatom-containing group, and the other R group is selected from the group consisting of H and substituted or unsubstituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, carbonyl,—or heteroatom-containing groups; 1, 2 wherein the method comprises oxidizing dihydrotetrazine 1 in a reaction medium in the presence of a catalyst and a stoichiometric oxidant.

公开(公告)号：US20190247536A1

公开(公告)日：2019-08-15

申请号：US16329287

申请日：2016-12-23

申请人： Haixia SUN ,  Hong LIU ,  Han LI ,  Jian ZENG ,  Shuang LIU ,  Xin LU ,  Juncheng GUO ,  Binghan YUAN ,  Ling LI

发明人： Haixia SUN ,  Hong LIU ,  Han LI ,  Jian ZENG ,  Shuang LIU ,  Xin LU ,  Juncheng GUO ,  Binghan YUAN ,  Ling LI

IPC分类号： A61L24/06 ,  A61L24/00

CPC分类号： A61L24/06 ,  A61L24/00 ,  A61L24/001 ,  A61L2430/36

摘要： Provided are the use of poly(N-isopropylacrylamide-co-butyl methacrylate) in preparing an embolism material for blood vessels, an embolism material for blood vessels and the use thereof in preparation of drugs. The embolism material for blood vessels comprises poly(N-isopropylacrylamide-co-butyl methacrylate) and a dispersion medium consisting of an electrolyte, a contrast agent, a pH regulator and water. The concentrations of the polymer, electrolyte and contrast agent are respectively 5-30 mg/ml, 0.1-30 mg/ml and 100-350 mg/ml based on iodine. The embolism material for blood vessels is suitable for embolization therapy of tumors in hypervascular and parenchymal visceral organs.