公开(公告)号：US08410112B2

公开(公告)日：2013-04-02

申请号：US13104291

申请日：2011-10-27

Applicant: Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

Inventor： Jean-Damien Charrier ,  Steven John Durrant ,  David Kay ,  Michael O'Donnell ,  Ronald Marcellus Alphonsus Knegtel ,  Somhairle MacCormick ,  Joanne Pinder ,  Stephen Clinton Young ,  Hayley Marie Binch ,  Thomas Cleveland ,  Lev Tyler Dewey Fanning ,  Dennis James Hurley ,  Pramod Joshi ,  Urvi Jagdishbhai Sheth ,  Alina Silina ,  Philip Michael Reaper ,  Anisa Nizarali Virani

IPC: A61K31/4965 ,  C07D403/00

CPC classification number: C07D403/14 ,  A61K31/497 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/113

Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.

Abstract translation: 本公开涉及式I的吡嗪化合物：其中L，n，R 1和R 2如说明书中所述。 这些化合物可用作ATR蛋白激酶的抑制剂。 本公开还涉及包含本公开内容的化合物的药学上可接受的组合物; 使用本公开的化合物治疗各种疾病，病症和病症的方法; 制备本公开的化合物的方法; 用于制备本公开的化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。

公开(公告)号：US20050176789A1

公开(公告)日：2005-08-11

申请号：US10936448

申请日：2004-09-07

Applicant: Sara Hadida Ruah ,  Mark Miller ,  Ashvani Singh ,  Thomas Cleveland ,  Lewis Makings ,  Matthew Hamilton ,  Peter Grootenhuis

Inventor： Sara Hadida Ruah ,  Mark Miller ,  Ashvani Singh ,  Thomas Cleveland ,  Lewis Makings ,  Matthew Hamilton ,  Peter Grootenhuis

IPC: A61K31/426 ,  A61K31/427 ,  A61P43/00 ,  C07D263/48 ,  C07D277/46 ,  C07D277/82 ,  C07D417/02 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12

CPC classification number: A61K31/426 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07D263/48 ,  C07D277/46 ,  C07D277/82 ,  C07D295/15 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  G01N33/5076

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract translation: 本发明涉及ATP结合盒（“ABC”）转运体或其片段的调节剂，包括CF跨膜调节剂（“CFTR”），其组合物及其方法。 本发明还涉及使用这种调节剂治疗ABC转运蛋白介导的疾病的方法。

公开(公告)号：US5858944A

公开(公告)日：1999-01-12

申请号：US729885

申请日：1996-10-11

Applicant: Andrea Claudette Keenan ,  Thomas Cleveland Kirk ,  Thomas Francis McCallum, III ,  Jan Edward Shulman ,  Richard James Tallent ,  Barry Weinstein

Inventor： Andrea Claudette Keenan ,  Thomas Cleveland Kirk ,  Thomas Francis McCallum, III ,  Jan Edward Shulman ,  Richard James Tallent ,  Barry Weinstein

IPC: C08F220/04 ,  C08F222/00 ,  C08F222/02 ,  C11D3/37 ,  C11D3/10

CPC classification number: C11D3/3757

Abstract: Polycarboxylate additives suitable for use in automatic dishwasher detergent compositions are prepared by polymerizing three or more monomers including monoethylenically unsaturated C.sub.3 to C.sub.6 monocarboxylic acids such as acrylic acid, monoethylenically unsaturated C.sub.4 to C.sub.6 dicarboxylic acids such as maleic acid, and monoethylenically unsaturated esters of acrylic or methacrylic acid. Automatic dishwasher detergents prepared from these additives produce low filming and spotting on washed glassware.

Abstract translation: 适用于自动洗碗机洗涤剂组合物的多羧酸盐添加剂通过聚合三种或更多种单体来制备，所述单体包括单烯属不饱和C3至C6单羧酸，例如丙烯酸，单烯属不饱和C 4 -C 6二羧酸如马来酸，和丙烯酸单烯属不饱和酯或 甲基丙烯酸。 由这些添加剂制备的自动洗碗机洗涤剂在洗涤的玻璃器皿上产生低成膜和斑点。

公开(公告)号：US09630956B2

公开(公告)日：2017-04-25

申请号：US13106476

申请日：2011-05-12

Applicant: Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

Inventor： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper ,  Matthew Paul Grote

IPC: A61K31/497 ,  A61K33/24 ,  C07D413/14 ,  C07D401/14 ,  C07D241/10

CPC classification number: C07D413/14

Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

公开(公告)号：US20120027874A1

公开(公告)日：2012-02-02

申请号：US13106476

申请日：2011-05-12

Applicant: Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

Inventor： Jean-Damien Charrier ,  Hayley Marie Binch ,  Dennis James Hurley ,  Thomas Cleveland ,  Pramod Joshi ,  Lev Tyler Dewey Fanning ,  Joanne Pinder ,  Michael O'Donnell ,  Anisa Nizarali Virani ,  Ronald Marcellus Alphonsus Knegtel ,  Steven John Durrant ,  Stephen Clinton Young ,  Pierre-Henri Storck ,  David Kay ,  Philip Michael Reaper

IPC: A61K31/497 ,  A61K33/24 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D413/14

Abstract: The present invention relates to pyrazine and pyridine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.The compounds of this invention have formula I: wherein the variables are as defined herein.

公开(公告)号：US20080207856A1

公开(公告)日：2008-08-28

申请号：US12069769

申请日：2008-02-13

Applicant: Brian Leslie Goodall ,  Thomas Cleveland Kirk ,  Lester Howard McIntosh

Inventor： Brian Leslie Goodall ,  Thomas Cleveland Kirk ,  Lester Howard McIntosh

IPC: C08F4/80

CPC classification number: C08F210/00 ,  C08F210/02 ,  C08F2/38 ,  C08F4/80 ,  C08F220/14 ,  C08F2500/03

Abstract: A polymerizable composition including a late transition metal complex, a non-polar olefin, a polar olefin, and a free radical scavenger, wherein the polymerizable composition is capable of forming a linear poly[(non-polar olefin)-(polar olefin)] substantially free of free radical addition polymer, is disclosed. A method of copolymerizing a non-polar olefin with a polar olefin, catalyzed by a late transition metal complex in the presence of a free radical scavenger, to produce a linear poly[(non-polar olefin)-(polar olefin)] substantially free of free radical addition polymer is also disclosed.

Abstract translation: 一种包含后过渡金属络合物，非极性烯烃，极性烯烃和自由基清除剂的可聚合组合物，其中所述可聚合组合物能够形成直链聚[（非极性烯烃） - （极性烯烃）] - 基本上不含自由基加成聚合物。 一种在自由基清除剂存在下，由后过渡金属配合物催化的非极性烯烃与极性烯烃共聚的方法，以产生基本上没有的线型聚[（非极性烯烃） - （极性烯烃）] 的自由基加成聚合物也被公开。

公开(公告)号：US07339075B2

公开(公告)日：2008-03-04

申请号：US11457996

申请日：2006-07-17

Applicant: Nathan Tait Allen ,  Brian Leslie Goodall ,  Thomas Cleveland Kirk ,  Lester Howard McIntosh, III

Inventor： Nathan Tait Allen ,  Brian Leslie Goodall ,  Thomas Cleveland Kirk ,  Lester Howard McIntosh, III

IPC: C07F5/02

CPC classification number: C07F9/5022

Abstract: Ligand synthesis methods for the preparation of ligands having the formula wherein Q is selected from phosphorus, arsenic and antimony; wherein X1, X2 and X3 are carbon anions; and, wherein R15 is selected from —SO3, —SO2N(R18), —CO2, —PO3, —AsO3, —SiO2, —C(CF3)2O; where R18 is selected from a hydrogen, a halogen, a hydrocarbyl group and a substituted hydrocarbyl group, are disclosed. Also disclosed are methods of complexing the ligands with late transition metals to form catalyst complexes that catalyze polymerization reactions and/or Heck coupling reactions.

Abstract translation: 用于制备具有下式的配体的配体合成方法其中Q选自磷，砷和锑; 其中X 1，X 2和X 3是碳阴离子; 和其中R 15选自-SO 3，-SO 2 N（R 18）， - CO 2，-PO 3，-AsO 3，-SiO 2，-C（CF 3）2， 3 O 2; 其中R 18选自氢，卤素，烃基和取代的烃基。 还公开了使配体与后过渡金属络合以形成催化聚合反应和/或Heck偶联反应的催化剂络合物的方法。

公开(公告)号：US20060246162A1

公开(公告)日：2006-11-02

申请号：US11118431

申请日：2005-04-29

Applicant: Thomas Cleveland ,  Stephen Boue ,  Matthew Burow ,  John McLachlan

Inventor： Thomas Cleveland ,  Stephen Boue ,  Matthew Burow ,  John McLachlan

IPC: A61K38/16 ,  A61K36/48

CPC classification number: A61K36/48

Abstract: The flavonoid family of phytochemicals, particularly those derived from soy, has received attention regarding their hormonal activity and their effects on human health and disease. The types and amounts of these compounds in soy and other plants are controlled by both constitutive expression and stress-induced biosynthesis. The health benefits of soy may therefore be dependent upon the amounts of the various hormonally active phytochemicals present. We have identified increased biosynthesis of the isoflavonoid phytoalexin compounds, Glyceollins I, II and III, in soy plants grown under stressed conditions (elicited soy), which exhibit marked anti-estrogenic effects on ER function. Here we demonstrate that specific glyceollins, isolated from elicited soy, displayed anti-estrogenic activity, suppressing basal and estrogen stimulated colony formation of ER-positive estrogen dependent breast cancer cells and inhibiting ER-dependent gene expression of progesterone receptor (PgR) and stromal derived factor-1 (SDF1/CXCL12). Examining the effects of glyceollin on in vivo tumor formation/growth we demonstrate the ability of glyceollins to significantly suppress basal and estrogen-stimulated tumor growth of ER-positive MCF-7 breast and BG-1 ovarian carcinoma cells in ovariectomized female nude mice. We further demonstrate that the effects of glyceollins on suppression of tumor growth correlate with inhibition of estrogen stimulated PgR expression. In contrast to the uterotropic activity of tamoxifen the glyceollins displayed no uterine agonist activity. The Glyceollin (I-III) compounds may represent an important component of the health effects of soy as well as represent novel anti-estrogens useful in the prevention or treatment of breast and ovarian carcinoma.

Abstract translation: 植物化学成分的黄酮类化合物，特别是那些衍生自大豆的类黄酮，已经受到关于其激素活性及其对人类健康和疾病的影响的关注。 这些化合物在大豆和其他植物中的类型和数量都受到组成型表达和应激诱导的生物合成的控制。 因此，大豆的健康益处可能取决于存在的各种激素活性植物化学物质的量。 我们已经确定了在胁迫条件下生长的大豆植物（引发的大豆）中异黄酮类植物抗坏血酸化合物Glyceollins I，II和III的生物合成的增加，其对ER功能表现出显着的抗雌激素作用。 在这里我们证明，从引出的大豆中分离的特定的果糖显示出抗雌激素活性，抑制ER阳性雌激素依赖性乳腺癌细胞的基础和雌激素刺激的集落形成，并抑制孕激素受体（PgR）和基质衍生的ER依赖性基因表达 因子-1（SDF1 / CXCL12）。 检查血糖浓度对体内肿瘤形成/生长的影响，我们证明了血清蛋白在卵巢切除的雌性裸鼠中显着抑制ER阳性MCF-7乳腺和BG-1卵巢癌细胞的基础和雌激素刺激的肿瘤生长的能力。 我们进一步证明，糖蛋白对抑制肿瘤生长的影响与抑制雌激素刺激的PgR表达有关。 与他莫昔芬的子宫活动相反，glyceollins不显示子宫激动剂活性。 Glyceollin（I-III）化合物可能代表大豆健康影响的重要组成部分，也可代表用于预防或治疗乳腺癌和卵巢癌的新型抗雌激素。

公开(公告)号：US20060054190A1

公开(公告)日：2006-03-16

申请号：US11183867

申请日：2005-07-19

Applicant: Robert Gifford ,  Lenore Buehrer ,  Thomas Cleveland

Inventor： Robert Gifford ,  Lenore Buehrer ,  Thomas Cleveland

IPC: B08B7/04 ,  B08B9/00 ,  B08B3/00 ,  B08B6/00 ,  B08B3/12

CPC classification number: B08B9/0321 ,  B01L3/5085 ,  B01L13/02 ,  B01L2200/143 ,  B01L2300/0829 ,  B01L2300/0864 ,  B01L2400/0439 ,  B01L2400/0487 ,  B08B3/12 ,  B08B9/00 ,  B08B2209/005 ,  G01N35/1004 ,  G01N2035/00554

Abstract: A plate washing system and method of cleaning pipes of the plate washing system. The plate washing system includes at least one manifold having a plurality of pipes configured to be provided within wells of a plate in order to wash the wells, at least one manifold having a plurality of pipes, a tank, an ultrasonic transducer mounted to the tank, and a control system. When tips of the pipes are positioned within the tank, the control system activates the ultrasonic transducer in order to vibrate a fluid within the tank. An additional level sensing system which can detect fluid levels in order to establish instrument function and/or the need to clean via the ultrasonic cleaning system.

Abstract translation: 一种洗板系统及其清洗系统的清洗方法。 洗板系统包括至少一个歧管，其具有多个配管，其配置成设置在板的孔内以便清洗井，至少一个歧管具有多个管，一个罐，一个安装在罐上的超声换能器 ，以及控制系统。 当管道的尖端位于罐内时，控制系统激活超声波换能器以便振荡罐内的流体。 可以检测流体水平以便建立仪器功能和/或需要通过超声波清洗系统进行清洁的附加液位检测系统。

公开(公告)号：US06569976B2

公开(公告)日：2003-05-27

申请号：US09846130

申请日：2001-05-01

Applicant: Steven Michael Baxter ,  Thomas Cleveland Kirk ,  Curtis Schwartz ,  Barry Weinstein

Inventor： Steven Michael Baxter ,  Thomas Cleveland Kirk ,  Curtis Schwartz ,  Barry Weinstein

IPC: C08J22046

CPC classification number: C08F290/062 ,  C08F220/04 ,  C08F220/12 ,  C08F220/28 ,  Y10S526/932

Abstract: Polymer compositions derived from selected monoethylenically unsaturated (C3-C6)carboxylic acid monomers, (C1-C4)alkyl (meth)acrylate ester monomers and alkoxylated (meth)acrylate monomers used in certain weight ratios to provide enhanced detergent and cleaning performance are disclosed. Polymer compositions containing from 5 to 40% of monoethylenically unsaturated (C3-C6)carboxylic acid monomer, from 35 to 65% of (C1-C4)alkyl (meth)acrylate ester monomer and from 20 to 60% of alkoxylated (meth)acrylate monomer provide improved cleaning performance in laundry detergent formulations relative to conventional polymer compositions.