公开(公告)号：US08067395B2

公开(公告)日：2011-11-29

申请号：US12575425

申请日：2009-10-07

Applicant: Orion D. Jankowski ,  James T. Palmer ,  Lee Honigberg

Inventor： Orion D. Jankowski ,  James T. Palmer ,  Lee Honigberg

IPC: A61K31/675

CPC classification number: C07D471/04 ,  C07F9/65685 ,  C07F9/65846

Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.

Abstract translation: 本文公开了抑制特定酪氨酸激酶活性的化合物。 公开了制备这些化合物的方法。 还公开了包含化合物的药物组合物。 提供了使用单独或与其它治疗剂组合公开的化合物用于治疗酪氨酸激酶介导的疾病或病症或酪氨酸激酶依赖性疾病或病症的方法。

公开(公告)号：US20110230446A1

公开(公告)日：2011-09-22

申请号：US13115462

申请日：2011-05-25

Applicant: Christopher I. Bayly ,  Cameron Black ,  Serge Leger ,  Chun Sing Li ,  Dan McKay ,  Chirstophe Mellon ,  Jacques Yves Gauthier ,  Vouy-Linh Truong ,  Cheuk Lau ,  Michel Therien ,  Michael J. Green ,  Bernard L. Hirschbein ,  James William Janc ,  James T. Palmer ,  Chitra Baskaran

Inventor： Christopher I. Bayly ,  Cameron Black ,  Serge Leger ,  Chun Sing Li ,  Dan McKay ,  Chirstophe Mellon ,  Jacques Yves Gauthier ,  Vouy-Linh Truong ,  Cheuk Lau ,  Michel Therien ,  Michael J. Green ,  Bernard L. Hirschbein ,  James William Janc ,  James T. Palmer ,  Chitra Baskaran

IPC: A61K31/277 ,  A61K31/495 ,  A61K31/4418 ,  A61K31/426 ,  A61K31/4174 ,  A61K31/663 ,  A61P19/08 ,  A61P19/10 ,  A61P1/02 ,  A61P19/02 ,  A61P35/00 ,  A61P19/00

CPC classification number: C07C237/20 ,  A61K31/165 ,  A61K31/18 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/495 ,  C07C255/25 ,  C07C255/29 ,  C07C255/46 ,  C07C255/58 ,  C07C259/10 ,  C07C311/37 ,  C07C317/32 ,  C07C2601/02 ,  C07C2601/14 ,  C07D209/08 ,  C07D213/38 ,  C07D213/57 ,  C07D213/64 ,  C07D213/70 ,  C07D213/89 ,  C07D215/12 ,  C07D231/12 ,  C07D233/64 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D277/30 ,  C07D295/135 ,  C07D295/155 ,  C07D307/52 ,  C07D333/20 ,  C07D401/04 ,  C07D417/04

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract translation: 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症

公开(公告)号：US06506733B1

公开(公告)日：2003-01-14

申请号：US09526300

申请日：2000-03-15

Applicant: Ann M. Buysse ,  Rohan V. Mendonca ,  James T. Palmer ,  Zong-Qiang Tian ,  Shankar Venkatraman

Inventor： Ann M. Buysse ,  Rohan V. Mendonca ,  James T. Palmer ,  Zong-Qiang Tian ,  Shankar Venkatraman

IPC: A61K3805

CPC classification number: C07C271/22 ,  C07C235/78 ,  C07C275/24 ,  C07C317/28

Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.

Abstract translation: 具有下式的化合物，并且可用作半胱氨酸蛋白酶抑制剂，特别是用于治疗组织蛋白酶K或S对组织蛋白酶K或S有助于疾病的病理学或症状性疾病的疾病如骨质疏松症或自身免疫性疾病。

公开(公告)号：US06476026B1

公开(公告)日：2002-11-05

申请号：US09526485

申请日：2000-03-15

Applicant: Clifford M. Bryant ,  James T. Palmer ,  Robert M. Rydzewski ,  Eduardo L. Setti ,  Zong-Qiang Tian ,  Shankar Venkatraman ,  Dan-Xiong Wang

Inventor： Clifford M. Bryant ,  James T. Palmer ,  Robert M. Rydzewski ,  Eduardo L. Setti ,  Zong-Qiang Tian ,  Shankar Venkatraman ,  Dan-Xiong Wang

IPC: A61K314439

CPC classification number: C07D213/70 ,  C07B2200/07 ,  C07C255/24 ,  C07C255/29 ,  C07C255/60 ,  C07C271/22 ,  C07C275/24 ,  C07C311/06 ,  C07C311/09 ,  C07C317/50 ,  C07C323/60 ,  C07C323/62 ,  C07C2601/14 ,  C07D207/16 ,  C07D209/06 ,  C07D209/26 ,  C07D209/52 ,  C07D211/60 ,  C07D213/81 ,  C07D213/82 ,  C07D233/26 ,  C07D239/28 ,  C07D277/30 ,  C07D277/42 ,  C07D277/56 ,  C07D295/155 ,  C07D295/215 ,  C07D307/68 ,  C07D333/20 ,  C07D333/38 ,  C07D417/04 ,  C07D417/12

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

公开(公告)号：US5344939A

公开(公告)日：1994-09-06

申请号：US29894

申请日：1993-03-11

Applicant: James T. Palmer

Inventor： James T. Palmer

IPC: B01J23/40 ,  C07B41/12 ,  C07B45/00 ,  C07B61/00 ,  C07C45/41 ,  C07C45/67 ,  C07C49/753 ,  C07C67/10 ,  C07C67/343 ,  C07C69/63 ,  C07C69/716 ,  C07C69/738 ,  C07C205/43 ,  C07C221/00 ,  C07C225/06 ,  C07C227/02 ,  C07C229/22 ,  C07C271/18 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C303/26 ,  C07C309/73 ,  C07C327/22 ,  C07D207/08 ,  C07D207/26 ,  C07D207/273 ,  C07D307/33 ,  C07S207/16 ,  C07C67/30 ,  C07C327/26

CPC classification number: C07D207/08 ,  C07C271/18 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C303/26 ,  C07C327/22 ,  C07C45/676 ,  C07C67/343 ,  C07C69/63 ,  C07D207/273

Abstract: The preparation of magnesium benzyl fluoromalonate and other equivalent materials, the synthetic equivalents of the --CH.sub.2 F moiety, is described. Reaction between these reagents and the in situ-formed imidazolides of various carboxylic acids gives beta-keto-alpha-fluoroesters, which upon hydrogenation and spontaneous decarboxylation yields fluoromethyl ketones in excellent yields. The overall transformation from RCOOH to RCOCH.sub.2 F is thus illustrated.

Abstract translation: 描述了氟代丙烯酸苄酯镁和其它等价物的制备，即-CH 2 F部分的合成当量。 这些试剂和各种羧酸的原位形成的咪唑化物之间的反应产生β-酮-α-氟代酯，其在氢化和自发脱羧时产生极好的产率的氟甲基酮。 因此说明了从RCOOH到RCOCH2F的整体转化。

公开(公告)号：US5210272A

公开(公告)日：1993-05-11

申请号：US744922

申请日：1991-08-14

Applicant: James T. Palmer

Inventor： James T. Palmer

IPC: C07C45/67 ,  C07C67/343 ,  C07C69/63 ,  C07C271/18 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C303/26 ,  C07C309/73 ,  C07C327/22 ,  C07D207/08 ,  C07D207/26 ,  C07D207/273

CPC classification number: C07D207/08 ,  C07C271/18 ,  C07C271/20 ,  C07C271/22 ,  C07C279/14 ,  C07C303/26 ,  C07C327/22 ,  C07C45/676 ,  C07C67/343 ,  C07C69/63 ,  C07D207/273

Abstract: The preparation of magnesium benzyl fluoromalonate and other equivalent materials, the synthetic equivalents of the --CH.sub.2 F moiety, is described. Reaction between these reagents and the in situ-formed imidazolides of various carboxylic acids gives beta-keto-alpha-fluoroesters, which upon hydrogenation and spontaneous decarboxylation yields fluoromethyl ketones in excellent yields. The overall transformation from RCOOH to RCOCH.sub.2 F is thus illustrated.

Abstract translation: 描述了氟代丙烯酸苄酯镁和其它等价物的制备，即-CH 2 F部分的合成当量。 这些试剂和各种羧酸的原位形成的咪唑化物之间的反应产生β-酮-α-氟代酯，其在氢化和自发脱羧时产生极好的产率的氟甲基酮。 因此说明了从RCOOH到RCOCH2F的整体转化。

公开(公告)号：US5008433A

公开(公告)日：1991-04-16

申请号：US505493

申请日：1990-04-06

Applicant: James T. Palmer

Inventor： James T. Palmer

IPC: C07C319/14 ,  C07C323/56 ,  C07D281/10

CPC classification number: C07C319/14 ,  C07C323/56 ,  C07D281/10

Abstract: The titled ester, especially having the (2S,3S)-configuration, which is an intermediate for the production of diltiazem, is provided. Very high yields are obtainable.

Abstract translation: 提供了特别是具有（2S，3S） - 构型的标题酯，其为生产地尔硫卓的中间体。 可获得非常高的产量。

公开(公告)号：US3627286A

公开(公告)日：1971-12-14

申请号：US3627286D

申请日：1970-10-08

Applicant: JAMES T PALMER JR

Inventor： PALMER JAMES T JR

IPC: C22B7/00 ,  F23G7/00 ,  F27B9/00

CPC classification number: C22B7/00 ,  F23G7/005 ,  Y02P10/212

Abstract: Apparatus designed primarily for burning used automobiles in the scrapping process. It includes an elongated burning tunnel having one tangent of a track for material carrying cars passing therethrough, the track having a second tangent and the tangents being connected by semicircular end sections. The track is higher at the exit end of the tunnel than at the entrance end and the cars run by gravity down the second tangent for reloading. Means is provided to propel the cars from the exit end of the tunnel to the higher end of the second tangent and from the curved section at the entrance of the tunnel to a position for loading adjacent the entrance of the tunnel.

公开(公告)号：US09181234B2

公开(公告)日：2015-11-10

申请号：US13268154

申请日：2011-10-07

Applicant: James T Palmer ,  Christopher James Lunnis ,  Daniel A Offermann ,  Lorraine Claire Axford ,  Michael Blair ,  Dale Mitchell ,  Nicholas Palmer ,  Christopher Steele ,  John Atherall ,  David Watson ,  David Haydon ,  Lloyd Czaplewski ,  David Davies ,  Ian Collins ,  Edward Malcolm Tyndall ,  Laura Andrau ,  Gary Robert William Pitt

Inventor： James T Palmer ,  Christopher James Lunnis ,  Daniel A Offermann ,  Lorraine Claire Axford ,  Michael Blair ,  Dale Mitchell ,  Nicholas Palmer ,  Christopher Steele ,  John Atherall ,  David Watson ,  David Haydon ,  Lloyd Czaplewski ,  David Davies ,  Ian Collins ,  Edward Malcolm Tyndall ,  Laura Andrau ,  Gary Robert William Pitt

IPC: C07D417/14 ,  C07D491/04 ,  C07D513/04 ,  A01N47/36

CPC classification number: C07D417/14 ,  A01N47/36 ,  C07D491/04 ,  C07D513/04

Abstract: The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

Abstract translation: 本发明提供下式的化合物及其盐：还提供了这些化合物作为抗菌剂的用途，包含它们的组合物及其制备方法。

公开(公告)号：US08461161B2

公开(公告)日：2013-06-11

申请号：US12515250

申请日：2007-11-15

Applicant: Christopher John Burns ,  Michael Francis Harte ,  James T. Palmer

Inventor： Christopher John Burns ,  Michael Francis Harte ,  James T. Palmer

IPC: A61K31/4965

CPC classification number: C07D241/20 ,  C07D213/75 ,  C07D213/82 ,  C07D241/18 ,  C07D241/24 ,  C07D241/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07F9/65583

Abstract: Compunds of the general formula wherein each of Z1-Z4 is N or CR1 wherein only two of said Z1-Z4 may be N are useful as kinase inhibitors.

Abstract translation: 通式的组合物，其中Z1-Z4各自为N或CR1，其中只有两个所述Z1-Z4可以是N可用作激酶抑制剂。