公开(公告)号：WO2008057948A3

公开(公告)日：2008-08-07

申请号：PCT/US2007083347

申请日：2007-11-01

Applicant: IRONWOOD PHARMACEUTICALS INC ,  TALLEY JOHN J ,  MARTINEZ EDUARDO J

Inventor： TALLEY JOHN J ,  MARTINEZ EDUARDO J

IPC: C07H7/04 ,  C07D205/08

CPC classification number: C07D205/08 ,  C07C47/57 ,  C07C47/575 ,  C07C249/02 ,  C07D263/24 ,  C07D263/26 ,  C07F9/4021 ,  C07F9/568 ,  C07F9/5722 ,  C07F9/65062 ,  C07F9/653 ,  C07F9/6536 ,  C07F9/6539 ,  C07H7/04 ,  C07C251/24

Abstract: Processes for preparing a 4-biphenylylazetidinone of formula are described. The processes generally proceed by either cyclizing a biphenylyl-ßaminoacyl compound or by arylating a 1-unsubstituted 4-biphenylylazetidinone with an R 1 -substituted phenyl arylating agent. Many of the processes may also be applied to the synthesis of 1,4-diphenylazetidinone deriviatives.

Abstract translation: 描述了制备式的4-联苯基氮杂环丁酮的方法。 该方法通常通过将联苯基 - β-氨基酰基化合物环化或通过用R 1 - 取代的苯基芳基化试剂将1-未取代的4-联苯基氮杂环丁烷酮芳基化来进行。 许多方法也可用于合成1,4-二苯基氮杂环丁酮衍生物。

公开(公告)号：WO2007047925A3

公开(公告)日：2007-11-22

申请号：PCT/US2006041040

申请日：2006-10-19

Applicant: UNIV NORTH CAROLINA STATE ,  BORBAS K ESZTER ,  LINDSEY JONATHAN S

Inventor： BORBAS K ESZTER ,  LINDSEY JONATHAN S

IPC: C07D487/22

CPC classification number: G01N33/582 ,  C07D487/22 ,  C07F9/5722 ,  C07F9/6524

Abstract: Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula (I) wherein: Z is a porphyrinic macrocycle, Alk 1 and Alk 2 are each independently an alkylidene chain; L is a linking group or is absent; R 1 is preferaby an ionic group or polar group; R 2 is an ionic group, polar group, bioconjugatable group, or targeting group; R 3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk 1 and Alk 2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.

Abstract translation: 描述了含有增溶基团的卟啉化合物，以及制备和使用它们的方法以及包含这些化合物的组合物。 这样的化合物的实例包括式（I）的化合物：其中：Z是卟啉大环，Alk 1和Alk 2各自独立地为亚烷基链; L是连接基团或不存在; R 1优选为离子基团或极性基团; R 2是离子基团，极性基团，生物可结合基团或靶向基团; R 3存在或不存在，并且当存在时是卤素基团，生物可结合基团或靶向基团，n是0或1（即存在CH基团，或Alk 1， 并且Alk 2直接键合到卟啉大环Z的碳上; 或其盐。

公开(公告)号：WO2007047925A2

公开(公告)日：2007-04-26

申请号：PCT/US2006/041040

申请日：2006-10-19

Applicant: NORTH CAROLINA STATE UNIVERSITY ,  BORBAS, K., Eszter ,  LINDSEY, Jonathan, S.

Inventor： BORBAS, K., Eszter ,  LINDSEY, Jonathan, S.

IPC: C07D487/22

CPC classification number: G01N33/582 ,  C07D487/22 ,  C07F9/5722 ,  C07F9/6524

Abstract: Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula (I) wherein: Z is a porphyrinic macrocycle, Alk 1 and Alk 2 are each independently an alkylidene chain; L is a linking group or is absent; R 1 is preferaby an ionic group or polar group; R 2 is an ionic group, polar group, bioconjugatable group, or targeting group; R 3 is present or absent and when present is a halo group, bioconjugatable group, or targeting group, n is O or 1 (that is, the CH group is present, or Alk 1 and Alk 2 are bonded directly to a carbon of the porphyrinic macrocycle Z); or a salt thereof.

Abstract translation: 描述含有增溶基团的卟啉化合物及其制备和使用方法以及包含这些化合物的组合物。 这些化合物的实例包括式（I）的化合物，其中：Z是卟啉大环，Alk 1和Alk 2各自独立地是亚烷基链; L是连接基团或不存在; R 1优选使用离子基团或极性基团; R 2是离子基团，极性基团，生物共轭基团或靶向基团; R 3存在或不存在，并且当存在时为卤素基团，生物共轭基团或靶向基团，n为0或1（即存在CH基团，或Alk < / SUP>和Alk 2直接键合到卟啉大环Z）的碳上; 或其盐。

公开(公告)号：WO2004111193A2

公开(公告)日：2004-12-23

申请号：PCT/US2004/018065

申请日：2004-06-08

Applicant: MERCK & CO., INC. ,  FRALEY, Mark, E. ,  GARBACCIO, Robert, M. ,  HARTMAN, George, D. ,  HOFFMAN, William, F.

Inventor： FRALEY, Mark, E. ,  GARBACCIO, Robert, M. ,  HARTMAN, George, D. ,  HOFFMAN, William, F.

IPC: C12N

CPC classification number: C07D401/12 ,  C07D207/20 ,  C07D209/48 ,  C07F9/5721 ,  C07F9/5722 ,  C07F9/65586

Abstract: The present invention relates to phosphate ester prodrugs of dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract translation: 本发明涉及二氢吡咯化合物的磷酸酯前体药物，其可用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

公开(公告)号：WO0114390A2

公开(公告)日：2001-03-01

申请号：PCT/US0022412

申请日：2000-08-16

Applicant: GUILFORD PHARMACEUTICALS

Inventor： JACKSON PAUL F ,  SLUSHER BARBARA S

IPC: C07C229/14 ,  C07C229/16 ,  C07C229/46 ,  C07C259/08 ,  C07F9/30 ,  C07F9/38 ,  C07F9/572 ,  C07F9/6561 ,  C07F9/44 ,  C07C229/50 ,  C07F9/40

CPC classification number: C07F9/5727 ,  C07C229/14 ,  C07C229/16 ,  C07C229/46 ,  C07C259/08 ,  C07C2601/02 ,  C07F9/303 ,  C07F9/383 ,  C07F9/5722 ,  C07F9/6561

Abstract: The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit angiogenesis, and to treat glutamate abnormalities, compulsive disorders, pain, diabetic neuropathy, and prostate diseases, as well as pharmaceutical compositions comprising the same.

Abstract translation: 本发明涉及代谢型谷氨酸受体配体衍生物和使用它们抑制NAALADase酶活性，影响神经元活性，抑制血管生成并治疗谷氨酸异常，强迫性障碍，疼痛，糖尿病性神经病和前列腺疾病的方法，如 以及包含其的药物组合物。

公开(公告)号：WO99054299A1

公开(公告)日：1999-10-28

申请号：PCT/US1999/007945

申请日：1999-04-12

IPC: A61K31/401 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/5377 ,  A61P31/16 ,  A61P43/00 ,  C07D207/16 ,  C07D207/32 ,  C07D207/325 ,  C07D207/327 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D521/00 ,  C07F9/572 ,  A61K31/40 ,  C07D407/04

CPC classification number: C07D207/327 ,  C07D207/16 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  C07F9/5722

Abstract: Disclosed are compounds of formula (I) which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

Abstract translation: 公开了可用于抑制致病微生物，特别是流感神经氨酸酶的神经氨酸酶的式（I）化合物。 还公开了用于预防和治疗由具有神经氨酸酶的微生物引起的疾病的组合物和方法，用于制备这些方法中使用的化合物和合成中间体的方法。

公开(公告)号：WO99026954A1

公开(公告)日：1999-06-03

申请号：PCT/NZ1998/000173

申请日：1998-11-25

IPC: A61K31/665 ,  A61K31/66 ,  A61K31/675 ,  A61K47/48 ,  A61P43/00 ,  C07F9/54 ,  C07F9/572 ,  C07F9/655

CPC classification number: C07F9/65522 ,  A61K47/54 ,  A61K47/543 ,  C07F9/54 ,  C07F9/5722

Abstract: The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3) XR.Z where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.

Abstract translation: 本发明提供线粒体靶向的抗氧化剂化合物。 本发明的化合物包含与抗氧化剂部分共价偶联的亲脂性阳离子。 在优选的实施方案中，亲脂性阳离子是三苯基鏻阳离子，并且该化合物具有式P（Ph 3）XR.Z-，其中X是连接基团，Z是阴离子，R是抗氧化剂部分 。 还提供了含有线粒体靶向抗氧化剂化合物的药物组合物，以及治疗或预防受益于减少氧化应激的患者的方法，其包括施用本发明化合物的步骤。

公开(公告)号：WO9523806A3

公开(公告)日：1995-09-28

申请号：PCT/EP9500444

申请日：1995-02-08

Applicant: PHARMACIA SPA ,  MONGELLI NICOLA ,  GRUGNOLA ANGELO ,  LOMBARDI BORGIA ANDREA ,  PESENTI ENRICO

Inventor： MONGELLI NICOLA ,  GRUGNOLA ANGELO ,  LOMBARDI BORGIA ANDREA ,  PESENTI ENRICO

IPC: A61K31/675 ,  A61P9/00 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P33/02 ,  A61P37/06 ,  C07F9/38 ,  C07F9/40 ,  C07F9/572

CPC classification number: C07F9/5722

Abstract: PCT No. PCT/EP95/00444 Sec. 371 Date Oct. 30, 1995 Sec. 102(e) Date Oct. 30, 1995 PCT Filed Feb. 8, 1995 PCT Pub. No. WO95/23806 PCT Pub. Date Sep. 8, 1995Subject of the present invention are new ureido derivatives of naphthalenephosphonic acids having the following formula (I) (I) wherein each of m and n, which are the same, is an integer of 1 to 4; each of p and q, which are the same, is an integer of 1 to 3; and each of the R groups, which are the same, is a free or esterified phosphonic acid group; and the pharmaceutically acceptable salts thereof.

公开(公告)号：WO2015066080A3

公开(公告)日：2015-06-25

申请号：PCT/US2014062729

申请日：2014-10-28

Applicant: UNIV CALIFORNIA ,  SCHWARZ RICHARD I

Inventor： SCHWARZ RICHARD I

IPC: B01D15/00

CPC classification number: C07F9/5722 ,  B01D61/145 ,  B01D61/16 ,  C07K14/465 ,  C07K14/47 ,  C07K14/4705 ,  C07K16/18

Abstract: Herein we describe, a candidate gene for the diffusible cell density signal is put through the classic test to validate its activity: ectopic expression in another cell type from another species, purification of the recombinant factor, and testing back on PAT cells to see if it acts like the original diffusible cell density signal. This classic approach is complicated by the finding that the cell type producing this protein binds a unique tissue-specific lipid cofactor and this composite molecule imparts a tissue-specific response. Previously, this mechanism was shown to rely on a diffusible factor with an affinity for the cell layer.

Abstract translation: 在本文中，我们描述了扩散细胞密度信号的候选基因通过经典测试来验证其活性：来自另一物种的另一种细胞类型的异位表达，重组因子的纯化，以及在PAT细胞上测试 像原始扩散细胞密度信号一样。 这种经典方法通过发现产生该蛋白的细胞类型结合独特的组织特异性脂质辅因子的发现而变得复杂，并且该复合分子赋予组织特异性应答。 以前，这种机制显示依赖于对细胞层具有亲和性的扩散因子。

公开(公告)号：WO2014048480A1

公开(公告)日：2014-04-03

申请号：PCT/EP2012/069141

申请日：2012-09-27

Applicant: THE UNIVERSITY OF SUSSEX

Inventor： HOFFMANN, Eva, Ran ,  VISEUX, Eddy, Michel, Elie ,  NEWCOMBE, Sonya, Clare

IPC: C07F9/50 ,  A61P35/00

CPC classification number: C07F9/5045 ,  C07C311/09 ,  C07C323/59 ,  C07F9/5022 ,  C07F9/5721 ,  C07F9/5722

Abstract: The present invention relates to gold complexes that find use in therapy, particularly in treating cancer. The compounds of the invention have formula (I) wherein L denotes a phosphine or N-heterocyclic carbene ligand; A denotes SO 2 or C(=O); R denotes hydrogen, alkyl, or haloalkyl; or optionally substituted (hetero)aryl; and G denotes hydrogen, alkyl, cycloalkyi, (hetero)aryl, A-R, or a group deriving from an a- or β-amino acid.

Abstract translation: 本发明涉及用于治疗，特别是治疗癌症的金络合物。 本发明化合物具有式（I），其中L表示膦或N-杂环卡宾配体; A表示SO2或C（= O）; R表示氢，烷基或卤代烷基; 或任选取代的（杂）芳基; 和G表示氢，烷基，环烷基，（杂）芳基，A-R或衍生自α-或β-氨基酸的基团。