公开(公告)号：US07501408B2

公开(公告)日：2009-03-10

申请号：US11932679

申请日：2007-10-31

申请人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

发明人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

IPC分类号： C07D417/12 ,  C07D295/10 ,  A61K31/541

CPC分类号： C07D209/08 ,  C07D261/14 ,  C07D295/18 ,  C07D295/20

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula (I): wherein Q is thiomorpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.

摘要翻译： 本发明提供了用于选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供具有式（I）的化合物：其中Q是硫代吗啉基; A，R5，R6，R7，R8，R9和Ar为取代基。

公开(公告)号：US20080108595A1

公开(公告)日：2008-05-08

申请号：US11932679

申请日：2007-10-31

申请人： Hong Liu ,  Arnab Chatterjee ,  David Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David Woodmansee ,  Daniel Mutnick ,  Donald Karanewsky ,  Yun He

发明人： Hong Liu ,  Arnab Chatterjee ,  David Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David Woodmansee ,  Daniel Mutnick ,  Donald Karanewsky ,  Yun He

IPC分类号： C07D413/00 ,  A61K31/535 ,  C07D265/30 ,  A61K31/5377 ,  A61K31/54 ,  C07D279/12 ,  C07D241/04 ,  A61K31/495 ,  A61K31/397 ,  C07D205/04

CPC分类号： C07D209/08 ,  C07D261/14 ,  C07D295/18 ,  C07D295/20

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。

公开(公告)号：US07102000B2

公开(公告)日：2006-09-05

申请号：US10384352

申请日：2003-03-06

申请人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien A. Al-Shamma ,  Andrea Fanjul Giachino ,  Karine Jakubowicz-Jaillardon ,  Jianhua Guo ,  Mohamed Boudjelal ,  James W. Zapf

发明人： Magnus Pfahl ,  Catherine Tachdjian ,  Hussien A. Al-Shamma ,  Andrea Fanjul Giachino ,  Karine Jakubowicz-Jaillardon ,  Jianhua Guo ,  Mohamed Boudjelal ,  James W. Zapf

IPC分类号： C07D413/12 ,  C07D215/16 ,  C07D277/04

CPC分类号： C07D277/20 ,  C07D417/06 ,  C07D417/10

摘要： The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Ar5 form a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

摘要翻译： 本发明涉及式（200）的某些取代杂环，其中B，H，I，J和K与Ar 5一起形成含有至少一个酰胺残基的环，W，X ，Y和Z一起形成2,4-噻唑烷二酮，2-硫代 - 噻唑烷-4-酮，2,4-咪唑烷二酮或2-硫代 - 咪唑烷-4-酮残基; 或其药学上可接受的盐。 该化合物可用于治疗诸如2型糖尿病以及脂质和碳水化合物代谢相关疾病（包括动脉粥样硬化）的疾病。 所述化合物还可用于治疗不受控制的增殖疾病，例如一般癌症，包括乳腺癌。

公开(公告)号：US20050113356A1

公开(公告)日：2005-05-26

申请号：US10922515

申请日：2004-08-18

申请人： Hong Liu ,  Arnab Chatterjee ,  David Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David Woodmansee ,  Daniel Mutnick ,  Donald Karanewsky ,  Yun He

发明人： Hong Liu ,  Arnab Chatterjee ,  David Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David Woodmansee ,  Daniel Mutnick ,  Donald Karanewsky ,  Yun He

IPC分类号： A61K20060101 ,  A61K31/397 ,  A61K31/401 ,  A61K31/404 ,  A61K31/423 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/537 ,  A61K31/5375 ,  A61K31/54 ,  C07D209/04 ,  C07D209/08 ,  C07D261/14 ,  C07D265/30 ,  C07D295/13 ,  C07D295/18 ,  C07D295/20 ,  C07D411/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D209/08 ,  C07D261/14 ,  C07D295/18 ,  C07D295/20

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

公开(公告)号：US20230204153A1

公开(公告)日：2023-06-29

申请号：US18173832

申请日：2023-02-24

申请人： Jianhua Guo

发明人： Jianhua Guo

IPC分类号： F16M11/26 ,  F16M11/10

CPC分类号： F16M11/26 ,  F16M11/10 ,  F16M2200/028 ,  F16M11/2021

摘要： A telescopic support includes a positioning device, a panel fixing member, two fixed rods, and two lifting rods. One ends of the two lifting rods are equipped on both sides of the panel fixing member, and the other ends thereof rods are plugged into the corresponding fixed rods and move in an axial direction of the fixed rods. During the lifting process of the lifting rods, the relative positions between the lifting rods and the fixed rods are maintained via the positioning device.

公开(公告)号：US20100204200A1

公开(公告)日：2010-08-12

申请号：US12764772

申请日：2010-04-21

申请人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

发明人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

IPC分类号： A61K31/5377 ,  C07D413/12 ,  C07D295/145 ,  C07D413/14 ,  C07C245/00 ,  C07D401/12 ,  C07D403/12 ,  A61K31/5375 ,  A61K31/54 ,  A61K31/496 ,  A61K31/404

CPC分类号： C07D209/08 ,  C07D261/14 ,  C07D295/18 ,  C07D295/20

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.

摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供了具有式1的化合物：其中Q是任选取代的氮杂环丁烷基，吡咯烷基，哌啶基和二氢吲哚基; 或Q为NR25R26; A，R 5，R 6，R 7，R 8，R 9，R 25，R 26和Ar为取代基。

公开(公告)号：US20050038098A1

公开(公告)日：2005-02-17

申请号：US10827111

申请日：2004-04-19

申请人： Catherine Tachdjian ,  Jianhua Guo ,  Mohamed Boudjelal ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Qing Chen ,  James Zapf ,  Magnus Pfahl

发明人： Catherine Tachdjian ,  Jianhua Guo ,  Mohamed Boudjelal ,  Hussien Al-Shamma ,  Andrea Giachino ,  Karine Jakubowicz-Jaillardon ,  Qing Chen ,  James Zapf ,  Magnus Pfahl

IPC分类号： A61K20060101 ,  A61K31/353 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/42 ,  C07D277/04 ,  C07D49/02 ,  C07D45/02

CPC分类号： C07D417/10 ,  C07D277/34

摘要： The invention relates to novel heterocyclic compounds having the structure illustrated by Formula (I) wherein the Ar1 radicals are substituted dihydronapthalene or isochroman radicals, the Ar2 radicals are aryl or heteroaryl radicals; and HAr is a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one radical. The compounds of Formula (I) can have biological activity for advantageously regulating carbohydrate metabolism, including serum glucose level, and lipid metabolism, and can be useful for the treatment of hyperlipidemia and/or hypercholesterolemia, and Type II diabetes. The compounds of Formula (I) can also have utility in the treatment of diseases of uncontrolled proliferation, including cancer.

摘要翻译： 本发明涉及具有式（I）所示结构的新型杂环化合物，其中Ar 1基团是取代的二氢萘或异苯并二氢吡喃基，Ar 2基团是芳基或杂芳基; 并且HAr是2,4-噻唑烷二酮，2-硫代 - 噻唑烷-4-酮，2,4-咪唑烷二酮或2-硫代 - 咪唑烷-4-酮基。 式（I）的化合物可以具有有利地调节碳水化合物代谢（包括血清葡萄糖水平和脂质代谢）的生物学活性，并且可用于治疗高脂血症和/或高胆固醇血症和II型糖尿病。 式（I）化合物还可用于治疗不受控制的增殖疾病，包括癌症。

公开(公告)号：US07314872B2

公开(公告)日：2008-01-01

申请号：US10922515

申请日：2004-08-18

申请人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

发明人： Hong Liu ,  Arnab Chatterjee ,  David C. Tully ,  Phillip Alper ,  Badry Bursulaya ,  Jianhua Guo ,  David H. Woodmansee ,  Daniel Mutnick ,  Donald S. Karanewsky ,  Yun He

IPC分类号： C07D413/12 ,  C07D295/10 ,  A61K31/5377 ,  A61K31/5375

CPC分类号： C07D209/08 ,  C07D261/14 ,  C07D295/18 ,  C07D295/20

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula I: wherein Q is morpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.

摘要翻译： 本发明提供了选择性抑制组织蛋白酶S的化合物，组合物和方法。在优选的方面，组织蛋白酶S在至少一种其它组织蛋白酶同功酶的存在下被选择性地抑制。 本发明还提供了通过选择性抑制组织蛋白酶S来治疗受试者的疾病状态的方法。更具体地，本发明提供具有式I的化合物：其中Q是吗啉基; 和A，R 5，R 6，R 7，R 8，R 9， SUP>和Ar是取代基。

公开(公告)号：USD922769S1

公开(公告)日：2021-06-22

申请号：US29704465

申请日：2019-09-05

申请人： Jianhua Guo

设计人： Jianhua Guo

公开(公告)号：US20110182860A1

公开(公告)日：2011-07-28

申请号：US12677469

申请日：2009-12-11

申请人： Jianhua Guo ,  Hongxia Liu ,  Shimo Li

发明人： Jianhua Guo ,  Hongxia Liu ,  Shimo Li

IPC分类号： A01N63/00 ,  A01P1/00

CPC分类号： A01N63/00 ,  A01N2300/00

摘要： A composite biocontrol microbial agent PSX combination controls several soil-borne diseases. The PSX combination was composed of three biocontrol bacteria, which are shaking cultured in the PDA culture solution at 37° C., 180 rpm for 20 to 24 hours, then centrifugated at 4000 g for 10 min, taking the wet bacterium preserved fluid by the ratio of 1:40 to prepare the microbial agent, and then mixing at the ratio of 1:1:1, the total concentration of live bacteria in finished product being of 1×109˜1×1012 cfu/mL. The PSX combination controls soil-borne diseases of plant that occurs complexly or solely, including root knot nematode disease, bacterial wilt, verticillium wilt and blights. Its disease-preventing effect is 60-100%. Yield increase is 30-200%. The effects of preventing Fusarium wilt of banana and rice sheath blight disease are more than 50%, and have 20-80% yield increase. In addition, the PSX combination also can improve soil hardening.

摘要翻译： 复合生物控制微生物剂PSX组合控制几种土传疾病。 PSX组合由三种生物控制细菌组成，它们在PDA培养液中于37℃，180rpm振荡培养20至24小时，然后以4000g离心10分钟，将湿细菌保存液 比例为1:40，制备微生物剂，然后以1:1:1的比例混合，成品中活细菌总浓度为1×109〜1×1012cfu / mL。 PSX组合控制植物的土壤传播疾病，复发或单独发生，包括根结线虫病，细菌性枯萎病，枯萎病和枯萎病。 其防病效果为60-100％。 产量增长30-200％。 防治香蕉枯萎病和水稻纹枯病的效果超过50％，产量增加20-80％。 此外，PSX组合也可以改善土壤硬化。