HUP0202708A2 - Ciklikus protein tirozin-kináz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Ciklikus protein tirozin-kináz inhibitorok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0202708A2
HUP0202708A2 HU0202708A HUP0202708A HUP0202708A2 HU P0202708 A2 HUP0202708 A2 HU P0202708A2 HU 0202708 A HU0202708 A HU 0202708A HU P0202708 A HUP0202708 A HU P0202708A HU P0202708 A2 HUP0202708 A2 HU P0202708A2
Authority
HU
Hungary
Prior art keywords
group
amino
hydrogen
alkylene
alkenylene
Prior art date
Application number
HU0202708A
Other languages
English (en)
Inventor
Joel C. Barrish
Ping Chen
Jagabandhu Das
Arthur M. P. Doweyko
Derek J. Norris
Ramesh Padmanabha
John Wityak
Original Assignee
Bristol-Myers Squibb Co.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22440334&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0202708(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol-Myers Squibb Co. filed Critical Bristol-Myers Squibb Co.
Publication of HUP0202708A2 publication Critical patent/HUP0202708A2/hu
Publication of HUP0202708A3 publication Critical patent/HUP0202708A3/hu

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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07C237/40—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to a carbon atom of a six-membered aromatic ring
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

A találmány az általános képletű ciklikus protein tirozin-kinoázinhibitorokra, ahol bizonyos megkötésekkel Q adott esetben egy vagytöbb R1 csoporttal szubsztituált öt vagy hattagú heteroaromás vagyaromás gyűrű; Z egyes kötés, -R15C=CH vagy - (CH2)m- csoport, ahol mértéke 1 vagy 2; X1 és X2 hidrogénatom, vagy együtt oxo- vagytioxocsoport; R1 hidrogénatom vagy R6, ahol R6 alkil-, alkenil-,alkinil-, cikloalkil-, cikloalkil-alkil-, cikloalkenil-, cikloalkenil-alkil-, aril-, aralkil-, heterociklil- vagy heterociklil-alkil-csoport, amelyek mindegyike adott esetben szubsztituált; hidroxi- vagy-OR6 csoport; merkapto- vagy -SR6 csoport; karboxi-, -C(O)qR6 vagy -O-C(O)qR6 csoport, ahol q értéke 1 vagy 2; szulfo- vagy -S(O)qR6csoport; halogénatom; ciano-; nitrocsoport; -Z4-NR7R8; -Z4-N(R9)- -Z5-NR10R11; -Z4-N(R12) -Z5-R6; -P(O)(OR6)2 csoport; R2 és R3 hidrogénatomvagy R6; -Z4-R6; vagy -Z13-NR7R8 csoport; R4 és R5 hidrogénatom vagyR6; -Z4-N(R9) -Z5-NR10R11; -N(R9) Z4R6; a nitrogénatommal együtt adottesetben szubsztituált heterociklusos gyűrűt képez; R7, R8, R9, R10,R11 és R12 hidrogénatom vagy R6; R7 és R8 együtt alkilén-, alkenilén-vagy heteroalkil-csoportot alkot; vagy R9, R10 és R11 közül kettőalkilén- vagy alkeniléncsoportot alkot; R13 ciano-; nitro-; amino-;alkoxi-amino-; hidroxi-; (aril-oxi)-amino-; (alkoxi-karbonit)-amino-;[(aril-oxi)-karbonil]-amino-; (alkil-szulfonil)-amino-; (aril-szulfonil)-amino-; aril-; heteroaril-; alkoxi-; aril-oxi-csoport; R14nitro-; alkoxi-karbonil-;[(aril-oxi)-karbonil]-csoport; R15hidrogénatom; alkil-; aril-; aralkil-; cikloalkilcsoport; Z4 és Z5egyes kötés; -Z11-S(O)q-Z12-; -Z11-C(O)-Z12-; -Z11-C(S)- -Z12-; -Z11-O-Z12-; -Z11-S-Z12-, -Z11-O-C(O)-Z12-; -Z11-C(O)- -O-Z12- csoport; Z7,Z8, Z9 és Z10 hidrogénatom vagy Z6; Z7 és Z8, vagy Z6 és Z10 együttalkilén- vagy alkeniléncsoportot alkot; vagy Z7 vagyZ8 és Z9 együttalkilén- vagy alkeniléncsoportot alkot; Z11 és Z12 egyes kötés;alkilén-; alkenilén-; alkiniléncsoport; Z13 egyes kötés; -Z11-S(O)q-Z12-; -Z11-C(O) -Z12-; -Z11-C(S)-Z12-; -Z11-O-Z12-; -Z11-S-Z12-; -Z11-O-C(O)-Z12-; -Z11-C(O)-O-Z12-; -C (NR13) -; -C (CHR14) -; vagy -C[C(R14)2] - csoport - és a hatóanyagként ezeket tartalmazógyógyszerkészítményekre és protein tirozin-kinázzal kapcsolatosrendellenességek kezelésére való alkalmazásukra vonatkozik. Ó
HU0202708A 1999-04-15 2000-04-12 Cyclic protein tyrosine kinase inhibitors, pharmaceutical compositions containing them and their use HUP0202708A3 (en)

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Families Citing this family (310)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999001124A1 (en) * 1996-12-03 1999-01-14 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
BR0009721A (pt) 1999-04-15 2002-02-13 Bristol Myers Squibb Co Inibidores de tirosina quinase de proteìna cìclica
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US6114365A (en) * 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
ATE309241T1 (de) 1999-09-10 2005-11-15 Merck & Co Inc Tyrosin kinase inhibitoren
GB0001930D0 (en) 2000-01-27 2000-03-22 Novartis Ag Organic compounds
AU2001231143A1 (en) * 2000-01-27 2001-08-07 Cytovia, Inc. Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
CA2417500C (en) * 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
EP1320365A4 (en) * 2000-09-21 2004-03-17 Bristol Myers Squibb Co SUBSTITUTED AZOLE DERIVATIVES AS AN INHIBITOR OF THE CORTICOTROPIN RELEASE FACTOR
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
EP1671969A3 (en) * 2000-12-21 2006-07-26 Bristol-Myers Squibb Company Thiazolyl inhibitors of tec family tyrosine kinases
ATE318812T1 (de) 2000-12-21 2006-03-15 Bristol Myers Squibb Co Thiazolyl-inhibitoren von tyrosinkinasen der tec- familie
US7105682B2 (en) * 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
FR2820136A1 (fr) * 2001-01-26 2002-08-02 Aventis Pharma Sa Nouveaux derives de l'uree, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation
HUP0402352A2 (hu) * 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
JP2004535437A (ja) 2001-06-22 2004-11-25 メルク　エンド　カムパニー　インコーポレーテッド チロシンキナーゼ阻害剤
AUPR688101A0 (en) * 2001-08-08 2001-08-30 Luminis Pty Limited Protein domains and their ligands
EP1418917A1 (en) 2001-08-10 2004-05-19 Novartis AG Use of c-src inhibitors alone or in combination with sti571 for the treatment of leukaemia
US8101629B2 (en) 2001-08-13 2012-01-24 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US7638522B2 (en) 2001-08-13 2009-12-29 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile
WO2003015778A1 (en) * 2001-08-17 2003-02-27 Merck & Co., Inc. Tyrosine kinase inhibitors
US6677487B2 (en) * 2001-08-30 2004-01-13 Pharmacia Corporation α-haloenamine reagents
WO2003032989A1 (en) * 2001-10-18 2003-04-24 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
MXPA04004177A (es) 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Derivados de amida como inhibidores de la glicogeno cintasa cinasa 3-beta.
WO2003037891A1 (en) 2001-11-01 2003-05-08 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
US6693097B2 (en) 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
CN100349876C (zh) 2001-11-30 2007-11-21 辛塔医药品有限公司 嘧啶化合物
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
EA007987B1 (ru) 2002-03-29 2007-02-27 Чирон Корпорейшн Замещённые бензазолы и их применение в качестве ингибиторов киназы raf
AUPS251402A0 (en) * 2002-05-23 2002-06-13 Cytopia Pty Ltd Kinase inhibitors
EP1511742B1 (en) * 2002-05-23 2010-02-03 Cytopia Research Pty Ltd Kinase inhibitors
KR101169964B1 (ko) 2002-05-23 2012-08-06 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 키나아제 저해제
EP2402309A1 (en) 2002-05-24 2012-01-04 Millennium Pharmaceuticals, Inc. CCR9 inhibitors and methods of use thereof
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US6872724B2 (en) 2002-07-24 2005-03-29 Merck & Co., Inc. Polymorphs with tyrosine kinase activity
US20040127435A1 (en) * 2002-08-02 2004-07-01 Regents Of The University Of California Uses for inhibitors of inosine monophosphate dehydrogenase
WO2004014904A1 (en) * 2002-08-09 2004-02-19 Pfizer Inc. Antiproliferative 2-(heteroaryl)-aminothiazole compounds, pharmaceutical compositions and methods for their use
ES2422196T3 (es) 2002-08-09 2013-09-09 Janssen Pharmaceutica Nv Procesos para la preparación de 4-4-4-(2-cianoetenil)-2,6-dimetilfenil)amino)-2-pirimidinil)aminobenzonitrilo
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
ATE450534T1 (de) * 2002-08-23 2009-12-15 Sloan Kettering Inst Cancer Synthese von epothilonen, zwischenprodukte davon, analoga und ihre verwendung
US7537891B2 (en) * 2002-08-27 2009-05-26 Bristol-Myers Squibb Company Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells
WO2004020583A2 (en) 2002-08-27 2004-03-11 Bristol-Myers Squibb Company Polynucleotide predictor set for identifying protein tyrosine kinase modulators
WO2004041164A2 (en) * 2002-10-30 2004-05-21 Merck & Co., Inc. Kinase inhibitors
US7227035B2 (en) 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
ATE363470T1 (de) 2002-11-18 2007-06-15 Chemocentryx Inc Arylsulfonamide
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
US7169771B2 (en) 2003-02-06 2007-01-30 Bristol-Myers Squibb Company Thiazolyl-based compounds useful as kinase inhibitors
ES2598404T3 (es) 2003-02-07 2017-01-27 Janssen Pharmaceutica Nv Derivados de pirimidina para la prevención de infección por el VIH
EP1603905A1 (en) * 2003-02-10 2005-12-14 Amgen Inc. Vanilloid receptor ligands and their use in treatments
CL2004000303A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
EP2258365B1 (en) 2003-03-28 2013-05-29 Novartis Vaccines and Diagnostics, Inc. Use of organic compounds for immunopotentiation
US7427683B2 (en) 2003-04-25 2008-09-23 Ortho-Mcneil Pharmaceutical, Inc. c-fms kinase inhibitors
US7790724B2 (en) 2003-04-25 2010-09-07 Janssen Pharmaceutica N.V. c-fms kinase inhibitors
EP1631560A2 (en) 2003-04-25 2006-03-08 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
US20050113566A1 (en) * 2003-04-25 2005-05-26 Player Mark R. Inhibitors of C-FMS kinase
MXPA05013075A (es) 2003-06-03 2006-03-17 Novartis Ag Inhibidores de p-38 basados en heterociclo de 5 miembros.
JP4838121B2 (ja) 2003-06-26 2011-12-14 ノバルティス アーゲー ５員ヘテロ環を基礎とするｐ３８キナーゼ阻害剤
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
US20050009891A1 (en) * 2003-07-09 2005-01-13 Lee Francis Y. Combination of SRC Kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
EP1781659B1 (en) 2003-07-16 2008-11-05 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
EP2256106B1 (en) 2003-07-22 2015-05-06 Astex Therapeutics Limited 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
JP2007506763A (ja) * 2003-09-24 2007-03-22 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用なイミダゾール組成物
EP1669348A4 (en) 2003-09-30 2009-03-11 Eisai R&D Man Co Ltd NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND
CA2542653A1 (en) 2003-10-16 2005-04-28 Chiron Corporation Substituted benzazoles and use thereof as inhibitors of raf kinase
EP1687004A4 (en) 2003-11-10 2009-04-08 Synta Pharmaceuticals Corp PYRIDINE COMPOUNDS
AU2004289305A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Heteroaryl-Hydrazone compounds
WO2005046698A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
ES2578254T3 (es) * 2003-12-03 2016-07-22 Ym Biosciences Australia Pty Ltd Inhibidores de cinasas basados en azol
CN1878767B (zh) * 2003-12-03 2010-05-05 西托匹亚研究有限公司 唑基激酶抑制剂
EP2233174B1 (en) * 2004-01-21 2016-07-20 Emory University Compositions and use of tyrosine kinase inhibitors to treat pathogenic infection
WO2005075435A1 (en) * 2004-01-30 2005-08-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
KR20060129413A (ko) * 2004-01-30 2006-12-15 에이비 사이언스 티로신 키나제 억제제로서의2-(3-치환된-아릴)아미노-4-아릴-티아졸
US7652146B2 (en) * 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
TWI338004B (en) * 2004-02-06 2011-03-01 Bristol Myers Squibb Co Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
US7491725B2 (en) 2004-02-06 2009-02-17 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
CN1980909B (zh) * 2004-02-06 2010-08-25 布里斯托尔-迈尔斯·斯奎布公司 作为激酶抑制剂的2-氨基噻唑-5-芳香族甲酰胺的制备方法
US20050215795A1 (en) * 2004-02-06 2005-09-29 Bang-Chi Chen Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
AU2005212438A1 (en) 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7384968B2 (en) * 2004-04-01 2008-06-10 Pfizer Inc. Thiazole-amine compounds for the treatment of neurodegenerative disorders
NZ588139A (en) 2004-04-08 2012-02-24 Targegen Inc 7-Aryl-3-arylamino-benzo[1,2,4]triazine derivatives
CN1946703A (zh) * 2004-04-20 2007-04-11 特兰斯泰克制药公司 取代的噻唑和嘧啶衍生物作为黑素细胞皮质激素受体调节剂
US7550499B2 (en) * 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
CN101035525A (zh) * 2004-06-17 2007-09-12 赛特凯恩蒂克公司 用于治疗心脏疾病的经取代的脲衍生物
EP1768662A2 (en) 2004-06-24 2007-04-04 Novartis Vaccines and Diagnostics, Inc. Small molecule immunopotentiators and assays for their detection
SG156650A1 (en) * 2004-07-16 2009-11-26 Sunesis Pharmaceuticals Inc Thienopyrimidines useful as aurora kinase inhibitors
JP2008509923A (ja) 2004-08-13 2008-04-03 ジェネンテック・インコーポレーテッド Ａｔｐ利用酵素のチアゾールベースのインヒビター
US7910613B2 (en) 2004-09-22 2011-03-22 H. Lundbeck A/S 2-acylaminothiazole derivatives
US20060069101A1 (en) * 2004-09-27 2006-03-30 Kim Kyoung S Prodrugs of protein tyrosine kinase inhibitors
US7662837B2 (en) * 2004-10-22 2010-02-16 Janssen Pharmaceutica N.V. Inhibitors of c-fms kinase
US7645755B2 (en) * 2004-10-22 2010-01-12 Janssen Pharmaceutical N.V. Inhibitors of c-fms kinase
TW200628156A (en) * 2004-11-04 2006-08-16 Bristol Myers Squibb Co Combination of a SRC kinase inhibitor and a BCR-ABL inhibitor for the treatment of proliferative diseases
TW200630363A (en) 2004-11-10 2006-09-01 Synta Pharmaceuticals Corp Process for preparing trisubstituted pyrimidine compounds
AU2005304393B2 (en) 2004-11-10 2012-09-27 Synta Pharmaceuticals Corp. IL-12 modulatory compounds
TW200628463A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp Heteroaryl compounds
SE0402762D0 (sv) * 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
SE0402763D0 (sv) * 2004-11-11 2004-11-11 Astrazeneca Ab Nitro indazole derivatives
EP1827447A1 (en) 2004-11-19 2007-09-05 Synta Pharmaceuticals Corporation Pyrimidine compounds and uses thereof
JO2596B1 (en) * 2004-11-30 2011-02-27 نوفارتيس ايه جي Compositions include epothelones and tyrosine protein kinase inhibitors and their pharmaceutical uses
CA2588517A1 (en) * 2004-12-01 2006-06-08 Devgen N.V. 5-carboxamido substituted thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family
CA2593993C (en) 2004-12-30 2014-07-29 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
KR20070100894A (ko) * 2005-01-19 2007-10-12 브리스톨-마이어스 스큅 컴퍼니 혈전색전성 장애 치료용 ｐ2ｙ1 수용체 억제제로서의2-페녹시-ｎ-(1,3,4-티아디졸-2-일)피리딘-3-아민 유도체및 관련 화합물
ES2552338T3 (es) 2005-01-21 2015-11-27 Astex Therapeutics Limited Compuestos farmacéuticos
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
CN101146532B (zh) 2005-01-21 2012-05-09 阿斯泰克斯治疗有限公司 药物化合物
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
CN101106990B (zh) * 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
PE20061394A1 (es) * 2005-03-15 2006-12-15 Bristol Myers Squibb Co Metabolitos de n-(2-cloro-6-metilfenil)-2-[[6-[4-(2-hidroxietil)-1-piperazinil]-2-metil-4-pirimidinil]amino]-5-tiazolcarboxamidas
US7829585B2 (en) 2005-03-30 2010-11-09 Eisai R&D Management Co., Ltd. Antifungal agent containing pyridine derivative
US20060235006A1 (en) * 2005-04-13 2006-10-19 Lee Francis Y Combinations, methods and compositions for treating cancer
US7674912B2 (en) 2005-04-25 2010-03-09 H. Lundbeck A/S Pro-drugs of N-thiazol-2-yl-benzamide derivatives
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
HUE026040T2 (hu) * 2005-05-05 2016-05-30 Bristol-Myers Squibb Holdings Ireland SRC/ABL inhibitor formulációi
US20060281788A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
EP2664340B1 (en) 2005-06-24 2020-02-12 Duke University A direct drug delivery system based on thermally responsive biopolymers
ATE502924T1 (de) 2005-06-27 2011-04-15 Bristol Myers Squibb Co Lineare harnstoffmimetika-antagonisten des p2y1- rezeptors zur behandlung von thromboseleiden
US7700620B2 (en) * 2005-06-27 2010-04-20 Bristol-Myers Squibb Company C-linked cyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2007002634A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
MX2007016501A (es) * 2005-06-27 2008-03-06 Squibb Bristol Myers Co Antagonistas heterociclicos n-enlazados del receptor de p2y1, utiles en el tratamiento de condiciones tromboticas.
US7408069B2 (en) * 2005-08-05 2008-08-05 Bristol-Myers Squibb Company Preparation of 2-amino-thiazole-5-carboxylic-acid derivatives
EP1937270A1 (en) * 2005-09-21 2008-07-02 Brystol-Myers Squibb Company Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof
US20070123539A1 (en) 2005-10-20 2007-05-31 University Of South Florida Treatment of Restenosis and Stenosis with Dasatinib
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
KR101467723B1 (ko) 2005-11-01 2014-12-03 탈자진 인코포레이티드 키나제의 비-아릴 메타-피리미딘 억제제
AU2006309173B2 (en) 2005-11-01 2011-08-18 Array Biopharma Inc. Glucokinase activators
US20100029676A1 (en) * 2005-11-04 2010-02-04 Sawyers Charles L T315a and f317i mutations of bcr-abl kinase domain
EP1951906B1 (en) * 2005-11-10 2010-12-22 Bristol-Myers Squibb Pharma Company Moesin, caveolin 1 and yes associated protein 1 as predictive markers of response to dasatinib in breast cancers
WO2007059078A1 (en) * 2005-11-14 2007-05-24 Dana-Farber Cancer Institute Treatment of multiple myeloma with dasatinib
US20070149523A1 (en) * 2005-11-14 2007-06-28 Jan Ehlert Thiazole Analogues and Uses Thereof
WO2007059143A2 (en) * 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Methods of identifying and treating individuals exhibiting mdr-1 overexpression with protein tyrosine kinase inhibitors and combinations thereof
US7705009B2 (en) * 2005-11-22 2010-04-27 Hoffman-La Roche Inc. 4-aminopyrimidine-5-thione derivatives
CA2630860A1 (en) 2005-11-25 2007-05-31 Galapagos Sas Urea derivatives useful as calcium receptor modulators
ATE529536T1 (de) * 2005-12-01 2011-11-15 Bristol Myers Squibb Co Verfahren zur identifizierung und behandlung von komplexe karyotypen zeigenden individuen
RU2384331C2 (ru) * 2005-12-05 2010-03-20 Пфайзер Продактс Инк. Способ лечения аномального роста клеток
AU2007210159A1 (en) * 2006-01-26 2007-08-09 Foldrx Pharmaceuticals, Inc. Compounds and methods for modulating protein trafficking
EP2295432A1 (en) 2006-02-10 2011-03-16 TransTech Pharma Inc. Process for the preparation of aminobenzimidazole derivatives
WO2007106391A1 (en) * 2006-03-10 2007-09-20 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
US20070219370A1 (en) * 2006-03-15 2007-09-20 Bristol-Myers Squibb Company Process for preparing n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino] -5-thiazolecarboxamide and related metabolites thereof
US20090306094A1 (en) * 2006-03-17 2009-12-10 Bristol-Myers Squibb Company Methods Of Identifying And Treating Individuals Exhibiting Mutant Bcr/Abl Kinase Polypeptides
CA2649043C (en) 2006-04-19 2013-09-17 Astellas Pharma Inc. Azolecarboxamide derivative
CA2650057C (en) * 2006-04-20 2014-07-29 Janssen Pharmaceutica N.V. Phenyl- or pyridinyl-amide as inhibitors of c-fms kinase
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
JP5089681B2 (ja) 2006-04-20 2012-12-05 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ｃ−ｆｍｓキナーゼの阻害剤としての複素環式化合物
JP2009535311A (ja) * 2006-04-28 2009-10-01 シンジェンタ パーティシペーションズ アクチェンゲゼルシャフト 殺虫化合物
WO2007138110A2 (en) * 2006-06-01 2007-12-06 Devgen N.V. Compounds that interact with ion channels, in particular with ion channels from the kv family
JP5028484B2 (ja) * 2006-06-28 2012-09-19 グラクソ グループ リミテッド Ｇｐｒ３８受容体媒介疾患の治療に有用なピペラジニル誘導体
GB0613674D0 (en) * 2006-07-10 2006-08-16 Proskelia Sas Derivatives of urea and related diamines, methods for their manufacture, and uses therefor
US7888361B2 (en) * 2006-09-11 2011-02-15 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
SG174772A1 (en) * 2006-09-11 2011-10-28 Curis Inc Multi-functional small molecules as anti-proliferative agents
AU2007299764B2 (en) 2006-09-22 2011-10-13 Novartis Ag Method of optimizing the treatment of Philadelphia-positive leukemia with Abl tyrosine kinase inhibitors
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
US8916552B2 (en) 2006-10-12 2014-12-23 Astex Therapeutics Limited Pharmaceutical combinations
US7960569B2 (en) * 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
CA2668255A1 (en) 2006-10-31 2008-05-08 Schering Corporation Anilinopiperazine derivatives and methods of use thereof
JP5063700B2 (ja) 2006-10-31 2012-10-31 シェーリング コーポレイション アニリノピペラジン誘導体およびアニリノピペラジン誘導体を使用する方法
EP2078002B1 (en) 2006-10-31 2013-08-28 Merck Sharp & Dohme Corp. 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
ES2699585T3 (es) 2006-12-15 2019-02-11 Nantbio Inc Derivados de triazina y sus aplicaciones terapéuticas
CN101265274B (zh) * 2007-02-16 2013-09-04 中国医学科学院药物研究所 嘧啶噻唑胺衍生物、及其制法和药物组合物与用途
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
US8367686B2 (en) * 2007-06-07 2013-02-05 Intra-Cellular Therapies, Inc. Heterocycle compounds and uses thereof
JP5559043B2 (ja) * 2007-06-07 2014-07-23 イントラ−セルラー・セラピーズ・インコーポレイテッド 新規ヘテロ環化合物およびその使用
HUE026446T2 (hu) 2007-07-19 2016-05-30 Lundbeck H As 5-Tagú heterociklusos amidok és rokon vegyületek
US20090076025A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched dasatinib
AU2008305294B2 (en) * 2007-09-21 2012-11-29 Array Biopharma Inc. Pyridin-2 -yl-amino-1, 2, 4 -thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
KR20100058660A (ko) 2007-10-23 2010-06-03 테바 파마슈티컬 인더스트리즈 리미티드 다사티닙 다형체 및 이의 제조 방법
DK2206707T3 (da) 2007-10-24 2014-08-11 Astellas Pharma Inc Azolcarboxamidforbindelse eller salt deraf
EP2062578A1 (en) 2007-11-12 2009-05-27 Institut National De La Sante Et De La Recherche Medicale (Inserm) Novel use of chemical compounds for the treatment of AIDS
EP2222166B9 (en) * 2007-12-10 2012-11-07 Concert Pharmaceuticals Inc. Heterocyclic kinase inhibitors
US20110166154A1 (en) * 2008-01-25 2011-07-07 Bristol-Myers Squibb Company Identification of predictive markers of response to dasatinib in human colon cancer
RU2514192C2 (ru) * 2008-03-27 2014-04-27 Грюненталь Гмбх Гидроксиметилциклогексиламины
AU2009228642B2 (en) * 2008-03-27 2013-11-07 Grunenthal Gmbh Substituted 4-aminocyclohexane derivatives
DE102008031036A1 (de) 2008-06-30 2009-12-31 Dömling, Alexander, Priv.-Doz. Dr. Dasatinib zur Anwendung in der Organtransplantation
KR20140065017A (ko) * 2008-07-30 2014-05-28 닛토덴코 가부시키가이샤 약물 담체
WO2010025142A1 (en) * 2008-08-29 2010-03-04 Transtech Pharma, Inc. Substituted aminothiazole derivatives, pharmaceutical compositions, and methods of use
EP2966048A1 (en) 2008-10-29 2016-01-13 E. I. du Pont de Nemours and Company Treatment of tailings streams
US20100113520A1 (en) * 2008-11-05 2010-05-06 Principia Biopharma, Inc. Kinase knockdown via electrophilically enhanced inhibitors
WO2010065444A1 (en) * 2008-12-01 2010-06-10 University Of Central Florida Research Foundation, Inc. Drug composition cytotoxic for pancreatic cancer cells
WO2010120388A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
US8530492B2 (en) 2009-04-17 2013-09-10 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
WO2010139981A2 (en) * 2009-06-03 2010-12-09 Generics [Uk] Limited Processes for preparing crystalline forms
KR101457027B1 (ko) 2009-06-09 2014-10-31 캘리포니아 캐피탈 에쿼티, 엘엘씨 트리아진 유도체와 이들의 치료적 용도
JP2012529517A (ja) 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー ベンジル置換トリアジン誘導体類及びそれらの治療応用
US10640457B2 (en) 2009-12-10 2020-05-05 The Trustees Of Columbia University In The City Of New York Histone acetyltransferase activators and uses thereof
CN101812060B (zh) * 2010-02-02 2011-08-17 南京卡文迪许生物工程技术有限公司 一种简捷制备高纯度达沙替尼的新方法以及中间体化合物
CN101845045A (zh) * 2010-02-02 2010-09-29 南京卡文迪许生物工程技术有限公司 一种新的达沙替尼合成方法
EP2359813A1 (en) 2010-02-04 2011-08-24 Ratiopharm GmbH Pharmaceutical composition comprising N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamid
CN101973989B (zh) * 2010-05-17 2012-07-18 苏州波锐生物医药科技有限公司 一种噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途
MX2012013274A (es) 2010-05-21 2013-05-28 Chemilia Ab Novedosos derivados de la pirimidina.
WO2012014149A1 (en) 2010-07-30 2012-02-02 Ranbaxy Laboratories Limited N-methylformamide solvate of dasatinib
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
US9969677B2 (en) 2010-12-22 2018-05-15 The Trustees Of Columbia University In The City Of New York Histone acetyltransferase modulators and uses thereof
KR101892574B1 (ko) 2011-01-21 2018-08-28 썬 파마 어드밴스트 리서치 컴패니 리미티드 디아릴아세틸렌 히드라지드 함유 티로신 키나제 억제제
WO2012118599A1 (en) 2011-02-28 2012-09-07 Emory University C-abl tyrosine kinase inhibitors useful for inhibiting filovirus replication
BR112013023050A8 (pt) 2011-03-09 2018-09-25 G Pestell Richard antagonista de ccr5, método para determinar se um indivíduo humano tendo câncer de próstata está sofrendo de ou sob o risco de desenvolver metástase, para identificar um antagonista de ccr5, método para determinar se um indivíduo humano tendo câncer de próstata está sofrendo de ou sob o risco de desenvolver metástase, para identificar um composto candidato, para produzir in vitro células epiteliais primárias, para diagnosticar câncer de próstata, para selecionar um tratamento para um indivíduo tendo um câncer/tumor de próstata, linhagem de célula, e, modelo animal
JP5886411B2 (ja) 2011-03-24 2016-03-16 ノビガ・リサーチ・エービーＮｏｖｉｇａ Ｒｅｓｅａｒｃｈ ＡＢ 新規のピリミジン誘導体
PL2717883T3 (pl) 2011-05-02 2017-07-31 Stichting Vumc Ochrona przed zaburzeniami bariery śródbłonkowej poprzez hamowanie kinazy tyrozynowej Abl-related gene (ARG)
US9120785B2 (en) 2011-05-10 2015-09-01 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as Syk inhibitors
US9290490B2 (en) 2011-05-10 2016-03-22 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
CN102898424A (zh) * 2011-07-29 2013-01-30 江苏奥赛康药业股份有限公司 达沙替尼新的多晶型物及其制备方法
WO2013065063A1 (en) 2011-11-03 2013-05-10 Cadila Healthcare Limited Anhydrous form of dasatinib, process for its preparation and its use
US10531655B2 (en) 2011-12-02 2020-01-14 The Regents Of The University Of California Reperfusion protection solution and uses thereof
NZ630288A (en) 2012-04-20 2015-08-28 Shilpa Medicare Ltd Process for preparing dasatinib monohydrate
CN104271572A (zh) * 2012-05-11 2015-01-07 艾伯维公司 用作nampt抑制剂的噻唑羧酰胺衍生物
JP6518585B2 (ja) 2012-05-14 2019-05-22 リチャード ジー． ペステル がんの治療のためのｃｃｒ５の修飾薬の使用
KR20150020683A (ko) * 2012-06-15 2015-02-26 바스프 에스이 다사티닙 및 선택된 공-결정 형성제를 포함하는 다성분 결정
MX379717B (es) 2012-07-27 2025-03-11 Izumi Tech Llc Composiciones inhibidoras del eflujo y métodos de tratamiento mediante el uso de las mismas.
EP2882757B1 (en) 2012-08-07 2016-10-05 Janssen Pharmaceutica, N.V. Process for the preparation of heterocyclic ester derivatives
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
NZ704666A (en) 2012-08-23 2018-05-25 Alios Biopharma Inc Compounds for the treatment of paramoxyvirus viral infections
PT2892900T (pt) 2012-09-10 2017-11-06 Principia Biopharma Inc Compostos de pirazolopirimidina como inibidores de cinase
CN103788085B (zh) * 2012-10-31 2016-09-07 复旦大学 2-（喹唑啉-4-氨基）-5-噻唑甲酰胺类衍生物及其生物药物用途
CZ306598B6 (cs) 2012-12-06 2017-03-22 Zentiva, K.S. Způsob přípravy a čištění nových i známých polymorfů a solvátů dasatinibu
US9365526B2 (en) 2012-12-31 2016-06-14 Sun Pharmaceutical Industries Limited Process for the preparation of dasatinib and its intermediates
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN104151321B (zh) * 2013-05-15 2016-09-07 复旦大学 N-(2-氯-6-甲基苯基)-2[(2-甲基嘧啶-4-基)氨基]噻唑-5-甲酰胺化合物及其制备方法和用途
CA2912285C (en) * 2013-05-23 2021-07-13 Kalvista Pharmaceuticals Limited Fused 6,5 or 6,6-heteroaromatic bicyclic amide derivatives and pharmaceutical compositions thereof useful as plasma kallikrein inhibitor
CN104225611B (zh) * 2013-06-18 2017-06-30 天津键凯科技有限公司 达沙替尼与非线性构型聚乙二醇的结合物
TW201534597A (zh) * 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
WO2015011578A1 (en) * 2013-07-22 2015-01-29 Shilpa Medicare Limited Dasatinib glucuronate salt and process for preparation thereof
CN105408329A (zh) 2013-07-25 2016-03-16 巴斯夫欧洲公司 呈晶体形式的达沙替尼的盐
CA2917209A1 (en) 2013-07-25 2015-01-29 Basf Se Salts of dasatinib in amorphous form
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
CN103588758A (zh) * 2013-11-04 2014-02-19 南京大学 一类含1,4-苯并二噁烷骨架的硝基咪唑衍生物的合成、制备及其在抗癌药物中的应用
US9636340B2 (en) 2013-11-12 2017-05-02 Ayyappan K. Rajasekaran Kinase inhibitors
IN2013MU03610A (hu) 2013-12-18 2015-04-24 Dharmesh Mahendrabhai Shah
CZ306732B6 (cs) 2013-12-19 2017-05-31 Zentiva, K.S. Způsob přípravy bezvodé polymorfní formy N-6 Dasatinibu
US20170216286A1 (en) 2014-01-28 2017-08-03 Mayo Foundation For Medical Education And Research Killing senescent cells and treating senescence-associated conditions using a src inhibitor and a flavonoid
PT3107544T (pt) 2014-02-21 2021-01-05 Principia Biopharma Inc Sais e forma sólida de um inibidor de btk
AU2015200822A1 (en) 2014-03-11 2015-10-01 Cerbios-Pharma Sa Process and intermediates for the preparation of dasatinib
HU231013B1 (hu) 2014-05-26 2019-11-28 Egis Gyógyszergyár Zrt. Dasatinib sók
US20180230140A1 (en) 2014-06-30 2018-08-16 Basf Se Multicomponent crystals of dasatinib with menthol or vanillin
CN104119292A (zh) * 2014-07-23 2014-10-29 天津市炜杰科技有限公司 一种达沙替尼中间体的制备方法
CN106573928B (zh) 2014-08-26 2020-04-14 安斯泰来制药株式会社 2-氨基噻唑衍生物或其盐
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
CA2970723C (en) 2014-12-18 2023-09-05 Principia Biopharma Inc. Treatment of pemphigus
EP3932914A1 (en) 2015-03-13 2022-01-05 Valo Health, Inc. Alpha-cinnamide compounds and compositions as hdac8 inhibitors
CN104788445B (zh) * 2015-04-10 2017-06-23 山东新时代药业有限公司 一种达沙替尼中间体的合成方法
CN104974222B (zh) * 2015-06-14 2020-06-02 深圳市康尔诺生物技术有限公司 作为蛋白酪氨酸激酶抑制剂的偶联肽化合物
EP3313839A1 (en) 2015-06-24 2018-05-02 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN106749223B (zh) * 2015-11-25 2019-12-20 中国科学院广州生物医药与健康研究院 酪氨酸激酶抑制剂及其制备方法和用途
CN106866684B (zh) * 2015-12-10 2020-06-09 吴耀东 用于治疗肿瘤的大环衍生物
WO2017108605A1 (en) 2015-12-22 2017-06-29 Synthon B.V. Pharmaceutical composition comprising amorphous dasatinib
TWI620748B (zh) * 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
WO2017168454A2 (en) * 2016-04-02 2017-10-05 Sun Pharma Advanced Research Company Limited Novel compounds as btk inhibitors
HRP20201131T1 (hr) 2016-05-31 2020-10-30 Kalvista Pharmaceuticals Limited Derivati pirazola kao inhibitori kalikreina plazme
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
IL293621B2 (en) 2016-06-29 2023-09-01 Principia Biopharma Inc Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(oxane-3-yl)piperazine-1-yl)penta-2-ananitrile
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
CA3030381A1 (en) 2016-07-14 2018-01-18 Pfizer Inc. Pyrimidine carboxamides as inhibitors of vanin-1 enzyme
ES2974991T3 (es) 2016-09-19 2024-07-02 Novartis Ag Combinaciones terapéuticas que comprenden un inhibidor de RAF y un inhibidor de ERK
US20190270735A1 (en) 2016-10-29 2019-09-05 Cipla Limited Polymorphs of Dasatinib
WO2018100585A1 (en) 2016-12-01 2018-06-07 Natco Pharma Limited An improved process for the preparation of dasatinib polymorph
CN108473487B (zh) * 2016-12-13 2021-08-03 普林斯顿药物研发公司 一种蛋白激酶抑制剂
CN106674150A (zh) * 2016-12-28 2017-05-17 上海应用技术大学 具有抗肿瘤活性的达沙替尼衍生物及其应用
IT201700006157A1 (it) 2017-01-20 2018-07-20 Cerbios Pharma Sa Co-cristalli di un composto antitumorale
IT201700006145A1 (it) 2017-01-20 2018-07-20 Cerbios Pharma Sa Co-cristallo di un composto antitumorale
US11040973B2 (en) * 2017-03-29 2021-06-22 Purdue Research Foundation Inhibitors of kinase networks and uses thereof
EP3388430A1 (en) 2017-04-10 2018-10-17 Technische Universität München Compound, compound for use in the treatment of a pathological condition, a pharmaceutical composition and a method for preparing said compound
DK3391907T3 (da) 2017-04-20 2020-03-09 Iomx Therapeutics Ag Intracellulær kinase sik3, der er associeret med resistens over for antitumorimmunresponser, og anvendelser deraf
FI3618875T3 (fi) 2017-05-02 2023-07-04 Novartis Ag Raf-inhibiittoria ja trametinibia käsittävä yhdistelmähoito
BR112020000302A2 (pt) 2017-07-07 2020-07-14 Biocon Limited formas polimórficas de dasatinibe
RU2674443C1 (ru) * 2017-11-16 2018-12-10 Федеральное государственное автономное образовательное учреждение высшего образования "Белгородский государственный национальный исследовательский университет" (НИУ "БелГУ") Способ ингибирования нуклеарного фактора каппа В с использованием 5-гидрокисиникотинат 3-(2,2,2-триметилгидразиний) пропионата калия в культуре клеток
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
SMT202200112T1 (it) 2017-11-29 2022-05-12 Kalvista Pharmaceuticals Ltd Forme di dosaggio comprendenti un inibitore della callicreina plasmatica
CA3090545A1 (en) * 2018-02-28 2019-09-06 University Of Southern California Compositions and methods for modulating inflammatory and degenerative disorder
WO2019238886A1 (en) * 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting usp14
EP3807263A1 (en) * 2018-06-13 2021-04-21 Amphista Therapeutics Ltd Bifunctional molecules for targeting uchl5
KR20210021016A (ko) * 2018-06-13 2021-02-24 암피스타 테라퓨틱스 엘티디 Rpn11 표적화를 위한 이중작용성 분자
CN112423757A (zh) 2018-06-15 2021-02-26 汉达生技医药责任有限公司 激酶抑制剂的盐类及其组合物
CN108929273A (zh) * 2018-06-27 2018-12-04 合肥医工医药有限公司 一种咪唑乙基香草酸醚钠盐的制备方法
EP3643713B1 (en) 2018-10-23 2025-07-30 iOmx Therapeutics AG Heterocyclic kinase inhibitors and uses thereof
US20210393628A1 (en) * 2018-10-30 2021-12-23 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for modulating t cell exhaustion
EP3903828A4 (en) 2018-12-21 2022-10-05 Daiichi Sankyo Company, Limited ANTIBODY-DRUG CONJUGATE AND KINAS INHIBITOR COMBINATION
CN109438437B (zh) * 2018-12-24 2020-07-17 深圳市第二人民医院 一类含噻唑环的抗癌化合物
MX2021013817A (es) 2019-05-13 2021-12-14 Novartis Ag Nuevas formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinop iridin-4-il)-4-metilfenil)-2-(trifluorometil)isonicotinamida como inhibidores de raf para el tratamiento del cancer.
BR112021022682A2 (pt) 2019-05-14 2022-02-22 Provention Bio Inc Métodos e composições para prevenir diabetes do tipo 1
EP3853221B1 (en) * 2019-07-29 2024-01-31 Ascentage Pharma (Suzhou) Co., Ltd. Novel tricyclic compounds as bcr-abl inhibitors
CA3149796A1 (en) 2019-08-02 2021-02-11 Onehealthcompany, Inc. Anti-cancer agents for the treatment of canine cancers
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN112402422A (zh) * 2019-08-20 2021-02-26 湖南华纳大药厂股份有限公司 氟取代的2-氨基噻唑-5-芳香族甲酰胺的用途
CN112409349A (zh) * 2019-08-20 2021-02-26 湖南华纳大药厂股份有限公司 激酶抑制剂及其制备、药物组合物和用途
GB201913121D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913122D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913123D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913124D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
CA3154257A1 (en) 2019-10-14 2021-04-22 Principia Biopharma Inc. Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
AU2021209884A1 (en) 2020-01-22 2022-09-15 Principia Biopharma Inc. Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile
EP4093379A1 (en) 2020-01-24 2022-11-30 Nanocopoeia LLC Amorphous solid dispersions of dasatinib and uses thereof
WO2021228983A1 (en) 2020-05-13 2021-11-18 INSERM (Institut National de la Santé et de la Recherche Médicale) A pharmaceutical composition comprising an arsenic compound, an inductor of type-1 ifn and a protein kinase inhibitor for treating cancer
US12006366B2 (en) 2020-06-11 2024-06-11 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
KR20220054066A (ko) * 2020-10-23 2022-05-02 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
US11980619B2 (en) 2021-07-28 2024-05-14 Nanocopoeia, Llc Pharmaceutical compositions and crushable tablets including amorphous solid dispersions of dasatinib and uses
CA3237696A1 (en) 2021-11-08 2023-05-11 Progentos Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
WO2023204642A1 (ko) * 2022-04-20 2023-10-26 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
WO2023215825A1 (en) 2022-05-05 2023-11-09 Immatics US, Inc. Methods for improving t cell efficacy
WO2025040820A1 (en) 2023-08-23 2025-02-27 Granular Therapeutics Limited Anti-cd203c antibody conjugates and uses thereof
EP4559937A1 (en) 2023-11-24 2025-05-28 Universitat de Barcelona Cd7 targeting moieties for the treatment of cd7 positive cancer
CN117820251B (zh) * 2024-03-01 2024-05-03 南京桦冠生物技术有限公司 双α-酮酸酰胺类化合物及其组合物
CN118791413B (zh) * 2024-06-18 2025-04-18 青岛润农化工有限公司 一种丁醚脲的合成方法

Family Cites Families (130)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3709992A (en) 1966-12-07 1973-01-09 Us Rubber Co Fungicidal use of certain carboxamidothiazoles
US3547917A (en) * 1966-12-07 1970-12-15 Uniroyal Inc 2-amino-4-methylthiazole-5-carboxamides
US3725427A (en) 1966-12-07 1973-04-03 Uniroyal Ltd Certain 2,4-dimethyl-5-carboxamido-thiazoles
DE2128699A1 (de) 1971-06-09 1973-01-25 Bayer Ag Thiazylharnstoffe, verfahren zu ihrer herstellung und ihre fungizide verwendung
US3796800A (en) * 1971-11-22 1974-03-12 Uniroyal Inc Anti-inflammatory triazole compositions and methods for using same
US3896223A (en) 1971-11-22 1975-07-22 Uniroyal Inc Anti-inflammatory thiazole compositions and methods for using same
US3879531A (en) * 1972-07-17 1975-04-22 Uniroyal Inc 2-aminothiazoles compositions and methods for using them as psychotherapeutic agents
US3932633A (en) 1972-12-04 1976-01-13 Uniroyal Inc. Novel o-triazenobenzamides, in treating aggressive behavior
JPS57183768A (en) 1981-05-06 1982-11-12 Kanto Ishi Pharma Co Ltd 4-methyl-5-(o-carboxyphenyl)carbamoylthiazole derivative and its preparation
DE3205638A1 (de) 1982-02-17 1983-08-25 Hoechst Ag, 6230 Frankfurt Trisubstituierte pyrimidin-5-carbonsaeuren und deren derivate, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel
DE3220118A1 (de) * 1982-05-28 1983-12-01 Bayer Ag, 5090 Leverkusen Alkylenverbrueckte guanidinothiazolderivate, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
US4649146A (en) 1983-01-31 1987-03-10 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives and pharmaceutical composition comprising the same
US4727073A (en) 1984-10-01 1988-02-23 Fujisawa Pharmaceutical Co., Ltd. Pyrimidine derivatives and composition of the same
JPS62123180A (ja) * 1985-11-21 1987-06-04 Otsuka Pharmaceut Factory Inc ｐ−アミノフエノ−ル誘導体
JPS6339868A (ja) * 1986-08-04 1988-02-20 Otsuka Pharmaceut Factory Inc ジ低級アルキルフエノ−ル誘導体
US4837242A (en) * 1987-01-20 1989-06-06 Sumitomo Chemical Company, Limited Thiazoles and pyrazoles as fungicides
JP2552494B2 (ja) 1987-04-08 1996-11-13 ヘキストジャパン株式会社 イミダゾチアジアジン誘導体及びその製造法
GB8717068D0 (en) * 1987-07-20 1987-08-26 Fujisawa Pharmaceutical Co Nitric ester derivative
US4877441A (en) * 1987-11-06 1989-10-31 Sumitomo Chemical Company Ltd. Fungicidal substituted carboxylic acid derivatives
HU202728B (en) 1988-01-14 1991-04-29 Eszakmagyar Vegyimuevek Synergetic fungicide and acaricide compositions containing two or three active components
US4970318A (en) * 1988-05-24 1990-11-13 Pfizer Inc. Aromatic and heterocyclic carboxamide derivatives as antineoplastic agents
JPH02129171A (ja) 1988-11-08 1990-05-17 Nissan Chem Ind Ltd ピラゾールカルボキサニリド誘導体及び有害生物防除剤
JPH02275857A (ja) 1989-01-13 1990-11-09 Yoshitomi Pharmaceut Ind Ltd ピリジン誘導体
US5696270A (en) 1989-05-23 1997-12-09 Abbott Laboratories Intermediate for making retroviral protease inhibiting compounds
US5064825A (en) 1989-06-01 1991-11-12 Merck & Co., Inc. Angiotensin ii antagonists
WO1991000277A1 (en) 1989-06-30 1991-01-10 E.I. Du Pont De Nemours And Company Substituted imidazoles
TW205041B (hu) 1989-08-07 1993-05-01 Fujisawa Pharmaceutical Co
DE3934197A1 (de) 1989-10-13 1991-04-18 Bayer Ag Thiazolcarbonsaeureamid-derivate
JPH04316559A (ja) 1990-11-28 1992-11-06 Nissan Chem Ind Ltd ピラゾールカルボキサニリド誘導体及び殺菌剤
WO1993007751A1 (en) 1991-10-18 1993-04-29 Monsanto Company Fungicides for the control of take-all disease of plants
DE4138042C2 (de) 1991-11-19 1993-10-14 Biotechnolog Forschung Gmbh Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel
JPH05345780A (ja) 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
HUT63941A (en) 1992-05-15 1993-11-29 Hoechst Ag Process for producing 4-alkyl-substituted pyrimidine-5-carboxanilide derivatives, and fungicidal compositions comprising same
IL105939A0 (en) 1992-06-11 1993-10-20 Rhone Poulenc Agriculture Herbicidal compounds and compositions
DE4231517A1 (de) 1992-09-21 1994-03-24 Basf Ag Carbonsäureanilide, Verfahren zu ihrer Herstellung und sie enthaltende Mittel zur Bekämpfung von Schadpilzen
HRP921338B1 (en) 1992-10-02 2002-04-30 Monsanto Co Fungicides for the control of take-all disease of plants
EP0603595A1 (de) 1992-12-04 1994-06-29 Hoechst Aktiengesellschaft Faserreaktive Farbstoffe, Verfahren zu deren Herstellung und ihre Verwendung
KR960701023A (ko) 1993-04-07 1996-02-24 도쿠시마 슈이치 피라졸 유도체(pyrazole derivatives)
US5514643A (en) * 1993-08-16 1996-05-07 Lucky Ltd. 2-aminothiazolecarboxamide derivatives, processes for preparing the same and use thereof for controlling phytopathogenic organisms
US5728693A (en) 1993-12-29 1998-03-17 E. I. Du Pont De Nemours And Company Arthropodicidal oxadiazine-thiadiazine-or triazine-carboxanilides
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5582167A (en) * 1994-03-02 1996-12-10 Thomas Jefferson University Methods and apparatus for reducing tracheal infection using subglottic irrigation, drainage and servoregulation of endotracheal tube cuff pressure
DE69526790T2 (de) 1994-06-24 2003-03-06 Euroceltique S.A., Luxemburg/Luxembourg Verbindungen zur hemmung von phosphodiesrerase iv
US5922751A (en) 1994-06-24 1999-07-13 Euro-Celtique, S.A. Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods of using same
US6080772A (en) * 1995-06-07 2000-06-27 Sugen, Inc. Thiazole compounds and methods of modulating signal transduction
EP0850228A1 (en) 1995-09-01 1998-07-01 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
US5811428A (en) 1995-12-18 1998-09-22 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
DK0873341T3 (da) 1995-11-17 2004-01-19 Biotechnolog Forschung Gmbh Epothilonderivater, fremstilling og anvendelse
US5677097A (en) 1996-01-18 1997-10-14 Fuji Xerox Co., Ltd. Electrophotographic photoreceptor
US6011029A (en) 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
AU716123B2 (en) 1996-04-03 2000-02-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1998022461A1 (de) 1996-11-18 1998-05-28 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Epothilone c, d, e und f, deren herstellung und deren verwendung als cytostatische mittel bzw. als pflanzenschutzmittel
WO1999001124A1 (en) 1996-12-03 1999-01-14 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US6380394B1 (en) 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6187797B1 (en) * 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
EP0946528B1 (en) * 1996-12-23 2003-04-09 Bristol-Myers Squibb Pharma Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
DE59805110D1 (de) 1997-02-25 2002-09-12 Biotechnolog Forschung Gmbh Seitenkettenmodifizierte epothilone
AU7687998A (en) 1997-05-19 1998-12-11 Sugen, Inc. Heteroarylcarboxamide compounds active against protein tyrosine kinase related disorders
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
GB9801231D0 (en) 1997-06-05 1998-03-18 Merck & Co Inc A method of treating cancer
WO1998056376A1 (en) * 1997-06-13 1998-12-17 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
US5896223A (en) * 1997-06-13 1999-04-20 Tigliev; George S. Optical system having an unlimited depth of focus
AU8150398A (en) * 1997-06-19 1999-01-04 Du Pont Pharmaceuticals Company Inhibitors of factor xa with a neutral p1 specificity group
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
WO1999002224A1 (en) 1997-07-07 1999-01-21 Lewis Robert D Statistical analysis and feedback system for sports employing a projectile
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
JPH1180137A (ja) 1997-07-10 1999-03-26 Nissan Chem Ind Ltd カルバモイルテトラゾールおよび除草剤
EP1001951B1 (de) 1997-07-16 2002-09-25 Schering Aktiengesellschaft Thiazolderivate, verfahren zur herstellung und verwendung
CA2299608A1 (en) 1997-08-09 1999-02-18 Schering Aktiengesellschaft New epothilone derivatives, method for producing same and their pharmaceutical use
GEP20032896B (en) * 1997-10-27 2003-02-25 Agouron Pharma 4-Aminothiazole Derivatives, Containing Them Pharmaceutical Compositions Inhibiting Cyclin-Dependent Kinases and Methods for Treatment
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
ID24289A (id) 1997-11-10 2000-07-13 Bristol Myers Squibb Co Benzotiazol inhibitor-inhibitor protein terosin kinase
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6365749B1 (en) 1997-12-04 2002-04-02 Bristol-Myers Squibb Company Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
JP4434484B2 (ja) 1997-12-04 2010-03-17 ブリストル−マイヤーズ スクイブ カンパニー オキシラニルエポチロン化合物のオレフィン性エポチロン化合物への還元法
US6432963B1 (en) 1997-12-15 2002-08-13 Yamanouchi Pharmaceutical Co., Ltd. Pyrimidine-5-carboxamide derivatives
JPH11180965A (ja) 1997-12-24 1999-07-06 Nissan Chem Ind Ltd 新規カルバモイルテトラゾリノンおよび除草剤
EP0928793B1 (en) 1998-01-02 2002-05-15 F. Hoffmann-La Roche Ag Thiazole derivatives
EP0928790B1 (en) * 1998-01-02 2003-03-05 F. Hoffmann-La Roche Ag Thiazole derivatives
EP1058679B1 (en) 1998-02-25 2005-10-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues therof
CA2319493A1 (en) 1998-03-18 1999-09-23 Regine Bohacek Heterocyclic signal transduction inhibitors, compositions containing them
US6498257B1 (en) 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
US6399638B1 (en) 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified epothilone derivatives
AU765030B2 (en) 1998-05-05 2003-09-04 F. Hoffmann-La Roche Ag Pyrazole derivatives as p-38 map kinase inhibitors
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
DE19826988A1 (de) 1998-06-18 1999-12-23 Biotechnolog Forschung Gmbh Epothilon-Nebenkomponenten
AU4775299A (en) 1998-06-22 2000-01-10 Nicolaou, Kyriacos Costa Desmethyl epothilones
WO2000000485A1 (de) 1998-06-30 2000-01-06 Schering Aktiengesellschaft Epothilon-derivate, verfahren zu deren herstellung, zwischenprodukte und ihre pharmazeutische verwendung
CA2336848A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
GB9816533D0 (en) 1998-07-29 1998-09-30 Zeneca Ltd Preparation of heterocyclic thiols
EP1114039A1 (en) 1998-09-18 2001-07-11 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
JP3244672B2 (ja) 1998-10-13 2002-01-07 住友製薬株式会社 イソキサゾール誘導体からなる医薬
ID28356A (id) * 1998-10-22 2001-05-17 Hoffmann La Roche Turunam tiazola
GB9823871D0 (en) 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
DE69926542T2 (de) 1998-12-25 2006-04-27 Teikoku Hormone Mfg. Co., Ltd. Aminopyrazolderivate
HK1046136A1 (zh) 1999-02-10 2002-12-27 三菱制药株式会社 酰胺化合物及其药物用途
KR100342044B1 (ko) 1999-04-14 2002-06-27 김순택 녹색발광 형광체 조성물 및 이를 이용하여 제조된 음극선관
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
BR0009721A (pt) 1999-04-15 2002-02-13 Bristol Myers Squibb Co Inibidores de tirosina quinase de proteìna cìclica
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
EP1205478A4 (en) 1999-08-06 2004-06-30 Takeda Chemical Industries Ltd P38MAP KINASE INHIBITORS
US6114365A (en) 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
CZ2002534A3 (cs) 1999-08-13 2002-07-17 Vertex Pharmaceuticals Incorporated Inhibitory protein-kináz, farmaceutické prostředky, které je obsahují, a jejich pouľití
ATE309241T1 (de) 1999-09-10 2005-11-15 Merck & Co Inc Tyrosin kinase inhibitoren
EP1785134A3 (en) * 2000-01-19 2009-02-18 Synvista Therapeutics, Inc. Use of thiazole, imidazole and oxazole compounds for the treatment of disorders associated with protein aging
WO2001056567A1 (en) * 2000-02-04 2001-08-09 Novo Nordisk A/S 2,4-diaminothiazole derivatives and their use as glycogen synthase kinase-3 (gsk-3) inhibitors
US20020132836A1 (en) * 2000-10-11 2002-09-19 Chemocentryx Inc. Compounds and methods for modulating CCR4 function
AU2002213467A1 (en) * 2000-10-11 2002-04-22 Chemocentryx, Inc. Modulation of ccr4 function
US20020137755A1 (en) * 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
EP1353676A4 (en) * 2000-12-29 2006-05-31 Alteon Inc METHOD FOR THE TREATMENT OF FIBROUS OR OTHER INDICATIONS
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
WO2002094798A1 (en) 2001-05-23 2002-11-28 Nippon Soda Co.,Ltd. Process for preparation of thiazole compounds
WO2002094264A1 (en) * 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
JP4011359B2 (ja) 2002-02-15 2007-11-21 株式会社ニフコ カップホルダ装置
US20050009891A1 (en) 2003-07-09 2005-01-13 Lee Francis Y. Combination of SRC Kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
US7652146B2 (en) * 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
US7491725B2 (en) 2004-02-06 2009-02-17 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
TW200628156A (en) * 2004-11-04 2006-08-16 Bristol Myers Squibb Co Combination of a SRC kinase inhibitor and a BCR-ABL inhibitor for the treatment of proliferative diseases
US20060235006A1 (en) 2005-04-13 2006-10-19 Lee Francis Y Combinations, methods and compositions for treating cancer
HUE026040T2 (hu) * 2005-05-05 2016-05-30 Bristol-Myers Squibb Holdings Ireland SRC/ABL inhibitor formulációi
EP1937270A1 (en) * 2005-09-21 2008-07-02 Brystol-Myers Squibb Company Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof
JP4316559B2 (ja) 2005-11-30 2009-08-19 株式会社ナノクリエート 導光板及びその製造方法
US8554512B2 (en) 2006-06-13 2013-10-08 Nike, Inc. Athletic performance data system and method
US7678998B2 (en) 2007-05-21 2010-03-16 Cicoil, Llc Cable assembly
US8897586B2 (en) 2012-06-15 2014-11-25 Comcast Cable Communications, Llc Dynamic generation of a quantization matrix for compression of a digital object

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WO2000062778A1 (en) 2000-10-26
US20040024208A1 (en) 2004-02-05
DK1169038T3 (da) 2012-11-26
KR20010108500A (ko) 2001-12-07
RU2312860C2 (ru) 2007-12-20
US20040073026A1 (en) 2004-04-15
PL351126A1 (en) 2003-03-24
US7153856B2 (en) 2006-12-26
AU4233800A (en) 2000-11-02
NO20014970L (no) 2001-12-10
NO2007005I1 (no) 2007-03-27
FR13C0003I2 (fr) 2015-11-20
HK1042433A1 (en) 2002-08-16
EP2308833A3 (en) 2011-09-28
TR200102969T2 (tr) 2002-08-21
FR13C0003I1 (hu) 2013-02-01
LU92146I2 (fr) 2013-04-05
NO322470B1 (no) 2006-10-09
KR100710100B1 (ko) 2007-04-23
RU2260592C9 (ru) 2017-04-07
CZ20013677A3 (cs) 2002-06-12
US20040077875A1 (en) 2004-04-22
CN1348370A (zh) 2002-05-08
NO2019016I1 (no) 2019-04-05
CA2366932A1 (en) 2000-10-26
ZA200107204B (en) 2002-12-02
PT1169038E (pt) 2012-10-26
US6979694B2 (en) 2005-12-27
BRPI0009721B8 (pt) 2021-11-23
US20050288303A1 (en) 2005-12-29
AU779089B2 (en) 2005-01-06
JP2002542193A (ja) 2002-12-10
ID30460A (id) 2001-12-06
US20180016247A1 (en) 2018-01-18
HUP0202708A3 (en) 2004-12-28
CY2013005I1 (el) 2015-11-04
HK1244797A1 (en) 2018-08-17
US9382219B2 (en) 2016-07-05
BRPI0009721B1 (pt) 2018-11-21
EP1169038B1 (en) 2012-08-08
NO2007005I2 (hu) 2008-12-01
US20190210986A1 (en) 2019-07-11
US20140206691A1 (en) 2014-07-24
PL215901B1 (pl) 2014-02-28
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RU2005107463A (ru) 2006-08-27
CZ302788B6 (cs) 2011-11-09

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