AR059064A1 - Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer. - Google Patents
Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer.Info
- Publication number
- AR059064A1 AR059064A1 ARP070100212A ARP070100212A AR059064A1 AR 059064 A1 AR059064 A1 AR 059064A1 AR P070100212 A ARP070100212 A AR P070100212A AR P070100212 A ARP070100212 A AR P070100212A AR 059064 A1 AR059064 A1 AR 059064A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cr9r10
- aryl
- heteroaryl
- cycloalkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Abstract
Reivindicacion 1: Un compuesto de la formula (1) donde: A es como se muestra en la formula (2) o arilo; Y es -N(R5)R6 o -OR6; X es O, S, o -N(R7); R1 es R8, -CHR11-N(H)-R8, -CHR11-O-R8, alquinilo C2-6, hidroxialquinilo C2-6 o -C:::N; R2 es arilo o heteroarilo; R3 es -H, alquilo C1-6, que puede estar interrumpido por uno o más heteroátomos, -(CR9R10)t(arilo), -(CR9R 10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o -(CR9R10)t(heterociclilo); R4 es alquilo C1-6, que puede estar interrumpido por uno o más heteroátomos, -(CR9R10)t(arilo), -(CR9R 10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o -(CR9R10)t(heterociclilo); o R3 y R4, junto con el átomo de carbono al cual ambos están enlazados, se unen para formar un sistema de anillos carbocíclicos o heterocíclicos C3-10, o R4 y R7 se unen para formar un anillo heterocíclico C3-10; R5 es -H, alquilo C1-8, -C(O)(CR9R10)t)N(R7)2, -C(O)(CR9R10)t -C(O)2(CR9R10)t,-(CR9R10)t(arilo), -(CR9R10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o - (CR9R10)t(heterociclilo), o R4 y R5 se unen para formar un anillo heterocíclico C3-10; R6 y R7 se seleccionan, en forma independiente, de -H, alquilo C1-8, -(alquilo C1-6)arilo, o -C(O)(alquilo C1-6), o R6 y R7, junto con los átomos a los cuales están enlazados, se unen para formar un anillo heterocíclico de 5 a 6 miembros, o R5 y R6, junto con el átomo de nitrogeno al cual están enlazados, se unen para formar un anillo heterocíclico o heteroarilo de 5 a 6 miembros; R8 es -H, alquilo C1-6, - (alquilo C1-6)arilo, arilo o heteroarilo; y R9, R10 y R11 se seleccionan, en forma independiente, de -H, alquilo C1-6 o arilo; donde n es un entero de 1 a 6; m es un entero de 0 a 2; y cada t es, en forma independiente, un entero de 0 a 3; donde cada uno de los citados alquilo, arilo, heteroarilo, cicloalquilo y fracciones heterociclilo, y anillos heterocíclicos y carbocíclicos están opcional e independientemente sustituidos por 1 a 3 sustituyentes que se seleccionan de: amino, arilo, heteroarilo, cicloalquilo o heterociclilo opcionalmente sustituido por 1 a 5 sustituyentes que se seleccionan de alcoxi C1-6, alquilo C1-6 opcionalmente sustituido por halo, arilo, halo, hidroxilo, heteroarilo, hidroxialquilo C1-6, o -NHS(O)2- (alquilo C1-6); alquilo C1-6, haloalquilo C2-6, hidroxialquilo C1-6, alcoxi C1-6, alquilo C1-6, amino, alquenilo C2-6 o alquinilo C2-6, donde cada uno de los cuales puede estar interrumpido por uno o más heteroátomos, ciano, halo, hidroxilo, nitro, o -O-arilo; o una sal farmacéuticamente aceptable, hidrato o estereoisomero de éste.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US75954606P | 2006-01-18 | 2006-01-18 |
Publications (1)
Publication Number | Publication Date |
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AR059064A1 true AR059064A1 (es) | 2008-03-12 |
Family
ID=38180602
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070100212A AR059064A1 (es) | 2006-01-18 | 2007-01-18 | Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer. |
Country Status (21)
Country | Link |
---|---|
US (2) | US7514566B2 (es) |
EP (1) | EP1981884B1 (es) |
JP (1) | JP5199885B2 (es) |
KR (1) | KR20080091369A (es) |
CN (1) | CN101421265A (es) |
AR (1) | AR059064A1 (es) |
AU (1) | AU2007207743B2 (es) |
BR (1) | BRPI0706621A2 (es) |
CA (1) | CA2636077C (es) |
CR (1) | CR10211A (es) |
EA (1) | EA200801716A1 (es) |
ES (1) | ES2389062T3 (es) |
IL (1) | IL192751A0 (es) |
MY (1) | MY149143A (es) |
NO (1) | NO20083572L (es) |
PE (1) | PE20071114A1 (es) |
TW (1) | TW200738657A (es) |
UA (1) | UA91895C2 (es) |
UY (1) | UY30098A1 (es) |
WO (1) | WO2007084391A2 (es) |
ZA (1) | ZA200806386B (es) |
Families Citing this family (56)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2006044860A2 (en) | 2004-10-18 | 2006-04-27 | Amgen, Inc. | Thiadiazole compounds and methods of use |
EP1981884B1 (en) * | 2006-01-18 | 2012-06-13 | Amgen, Inc | Thiazole compounds as protein kinase b (pkb) inhibitors |
CA2678036A1 (en) * | 2007-02-13 | 2008-08-21 | Schering Corporation | Functionally selective alpha2c adrenoreceptor agonists |
CA2692713A1 (en) * | 2007-07-17 | 2009-01-22 | Amgen Inc. | Heterocyclic modulators of pkb |
AU2008276512A1 (en) * | 2007-07-17 | 2009-01-22 | Amgen Inc. | Thiadiazole modulators of PKB |
UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
JP2011525929A (ja) * | 2008-06-26 | 2011-09-29 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Akt活性の阻害剤 |
US9540322B2 (en) | 2008-08-18 | 2017-01-10 | Yale University | MIF modulators |
US9643922B2 (en) | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
CA2733554A1 (en) * | 2008-08-18 | 2010-02-25 | Yale University | Mif modulators |
LT3135672T (lt) * | 2008-10-10 | 2020-05-25 | Vm Discovery, Inc. | Kompozicijos ir būdai skirti gydyti alkoholio vartojimo sutrikimus, skausmą ir kitas ligas |
JP5770102B2 (ja) * | 2008-12-19 | 2015-08-26 | ジェネンテック, インコーポレイテッド | 複素環化合物と使用方法 |
EP2387570A1 (en) * | 2009-01-15 | 2011-11-23 | Amgen, Inc | Fluoroisoquinoline substituted thiazole compounds and methods of use |
EP2440556A1 (en) * | 2009-06-10 | 2012-04-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of phosphatidylinositol 3-kinase |
HRP20171415T4 (hr) | 2009-06-25 | 2023-03-03 | Alkermes Pharma Ireland Limited | Heterociklični spojevi za liječenje neuroloških i psiholoških poremećaja |
ES2532026T3 (es) * | 2009-10-08 | 2015-03-23 | Glaxosmithkline Llc | Combinación |
CA2777087C (en) * | 2009-10-08 | 2017-10-31 | Glaxosmithkline Llc | Combination |
CN102665720A (zh) * | 2009-10-12 | 2012-09-12 | 葛兰素史密斯克莱有限责任公司 | 组合 |
WO2011049625A1 (en) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Method for aflatoxin screening of products |
EA027123B1 (ru) | 2009-11-05 | 2017-06-30 | Ризен Фармасьютикалз С.А. | Ингибиторы киназы pi3k |
KR20130038224A (ko) * | 2010-03-15 | 2013-04-17 | 가부시키가이샤 구라레 | 티에노피리딘 유도체 및 그 제조 방법, 그리고 그것을 사용한 유기 반도체 디바이스 |
JP5578705B2 (ja) * | 2010-03-29 | 2014-08-27 | 公益財団法人相模中央化学研究所 | (アリール)ジフルオロ酢酸エステル誘導体及びその製造方法 |
US8383623B2 (en) * | 2010-04-16 | 2013-02-26 | Abbott Laboratories | Phthalazin-(2H)-one inhibitors of kinases |
WO2011130921A1 (en) * | 2010-04-23 | 2011-10-27 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
EP2579872A4 (en) * | 2010-04-23 | 2013-11-13 | Merck Sharp & Dohme | HAMMER OF ACT ACTIVITY |
JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
CN107337659A (zh) | 2011-05-04 | 2017-11-10 | 理森制药股份公司 | 作为蛋白激酶调节剂的新颖化合物 |
AU2012316055B2 (en) | 2011-09-27 | 2016-05-12 | Amgen Inc. | Heterocyclic compounds as MDM2 inhibitors for the treatment of cancer |
CN103304468A (zh) * | 2012-03-13 | 2013-09-18 | 华东师范大学 | 一种氧化吲哚的一锅法串联合成方法 |
WO2013146754A1 (ja) | 2012-03-27 | 2013-10-03 | 塩野義製薬株式会社 | Trpv4阻害活性を有する芳香族複素5員環誘導体 |
WO2013173382A1 (en) | 2012-05-15 | 2013-11-21 | Amgen Inc. | Benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein |
MY169987A (en) | 2012-07-04 | 2019-06-19 | Rhizen Pharmaceuticals Sa | Selective pi3k delta inhibitors |
CA2901696C (en) | 2013-02-19 | 2021-04-13 | Amgen Inc. | Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer |
WO2014160401A1 (en) * | 2013-03-13 | 2014-10-02 | Boston Biomedical, Inc. | 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer |
CA2906538C (en) | 2013-03-14 | 2021-02-02 | Ana Gonzalez Buenrostro | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
SG10201902429PA (en) | 2013-11-11 | 2019-04-29 | Amgen Inc | Combination therapy including an mdm2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers |
SG11201705821XA (en) * | 2015-03-02 | 2017-08-30 | Rigel Pharmaceuticals Inc | TGF-ß INHIBITORS |
WO2017151409A1 (en) | 2016-02-29 | 2017-09-08 | University Of Florida Research Foundation, Incorporated | Chemotherapeutic methods |
AR107840A1 (es) * | 2016-03-10 | 2018-06-13 | Astrazeneca Ab | INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASA g |
AU2018243770A1 (en) | 2017-03-30 | 2019-09-19 | F. Hoffmann-La Roche Ag | Isoquinolines as inhibitors of HPK1 |
JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
WO2019071147A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
AU2019230014A1 (en) | 2018-03-05 | 2020-09-17 | Alkermes Pharma Ireland Limited | Aripiprazole dosing strategy |
CA3098574A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
BR112021023277A2 (pt) | 2019-05-21 | 2022-01-04 | Amgen Inc | Formas em estado sólido |
AU2020325115A1 (en) * | 2019-08-02 | 2022-03-17 | Amgen Inc. | Pyridine derivatives as KIF18A inhibitors |
WO2021076655A1 (en) | 2019-10-15 | 2021-04-22 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
US20230028414A1 (en) | 2019-12-16 | 2023-01-26 | Amgen Inc. | Dosing regimen of kras g12c inhibitor |
CN111603466B (zh) * | 2020-06-29 | 2022-07-22 | 江南大学 | 一种乙酮类化合物在制备治疗肿瘤药物中的应用 |
CN114014787B (zh) * | 2022-01-10 | 2022-03-22 | 苏州开元民生科技股份有限公司 | 一种制备(2s,3r)-对甲砜基苯丝氨酸乙酯的不对称合成方法 |
CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
Family Cites Families (81)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3591600A (en) | 1969-07-07 | 1971-07-06 | Stauffer Chemical Co | 2-aminothiazole phosphates and phosphonates |
GB1435139A (en) | 1972-08-17 | 1976-05-12 | Sumitomo Chemical Co | Thiazole derivatives |
JPS5239827B2 (es) | 1973-11-08 | 1977-10-07 | ||
US4086239A (en) | 1977-07-01 | 1978-04-25 | Stauffer Chemical Company | Thiazole bis-phosphates and phosphonates, intermediates, and insecticidal compositions and methods |
DK150068C (da) | 1978-06-02 | 1987-06-29 | Pfizer | Analogifremgangsmaade til fremstilling af aminothiazoler |
US4297365A (en) | 1978-08-04 | 1981-10-27 | Ciba-Geigy Corporation | Benzimidazoles and pharmaceutical preparations containing such compounds |
US4451471A (en) | 1981-03-18 | 1984-05-29 | Ciba-Geigy Corporation | Certain 2,4,5-tri-substituted thiazoles, pharmaceutical compositions containing same and methods of using same |
FR2511375A1 (fr) | 1981-08-17 | 1983-02-18 | Rhone Poulenc Sante | Nouveaux derives de la cephalosporine, leur preparation et les medicaments qui les contiennent |
DE3630732A1 (de) | 1986-09-10 | 1988-03-17 | Bayer Ag | 2-cyano-2-alkoximino-acetamide |
US5232921A (en) * | 1987-03-12 | 1993-08-03 | Sanofi | Thiazole derivatives active on the cholinergic system, process for obtention and pharmaceutical compositions |
JPH0753666B2 (ja) | 1987-09-14 | 1995-06-07 | 久光製薬株式会社 | 置換ジフェニルチアゾール誘導体からなる抗炎症剤 |
FR2636628B1 (fr) | 1988-08-25 | 1990-12-28 | Sanofi Sa | Derives du thiadiazole-1,3,4, leur procede d'obtention et compositions pharmaceutiques en contenant |
US5302608A (en) | 1988-11-18 | 1994-04-12 | Takeda Chemical Industries, Ltd. | Age formation inhibitors |
US5145860A (en) | 1989-01-05 | 1992-09-08 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole compounds and pharmaceutical composition comprising the same |
US5550138A (en) | 1992-03-25 | 1996-08-27 | Takeda Chemical Industries, Ltd. | Condensed thiadiazole derivative, method of its production, and use thereof |
KR980700077A (ko) | 1994-11-29 | 1998-03-30 | 나까토미 히로타카 | 2-아미노티아졸유도체 및 그 염류로 이루어진 항균제 또는 살균제(Antibacterial Prepartion or Bactericide comprising 2-Aminothiazole Derivative or Salt Thereof |
FR2735777B1 (fr) * | 1995-06-21 | 1997-09-12 | Sanofi Sa | Derives de 4-phenylaminothiazole, leur procede de preparation et les compositions pharmaceutiques les contenant |
US6407124B1 (en) * | 1998-06-18 | 2002-06-18 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
EP1087951B9 (en) | 1998-06-18 | 2006-09-13 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
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 |
EP1150565A1 (en) | 1999-02-08 | 2001-11-07 | LION bioscience AG | Thiazole derivatives and combinatorial libraries thereof |
AUPP873799A0 (en) | 1999-02-17 | 1999-03-11 | Fujisawa Pharmaceutical Co., Ltd. | Pyridine compounds |
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 |
JP2001114690A (ja) * | 1999-08-06 | 2001-04-24 | Takeda Chem Ind Ltd | p38MAPキナーゼ阻害剤 |
EP1268474A2 (en) | 2000-03-30 | 2003-01-02 | Takeda Chemical Industries, Ltd. | Substituted 1,3-thiazole compounds, their production and use |
WO2001074793A2 (en) * | 2000-04-03 | 2001-10-11 | 3-Dimensional Pharmaceuticals, Inc. | Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1 |
US7074934B2 (en) | 2000-06-13 | 2006-07-11 | Tularik Limited | Serine protease inhibitors |
GT200100147A (es) | 2000-07-31 | 2002-06-25 | Derivados de imidazol | |
JP4689801B2 (ja) | 2000-08-09 | 2011-05-25 | ケミプロ化成株式会社 | アミノチアゾール誘導体の製造方法 |
JP2002053566A (ja) | 2000-08-11 | 2002-02-19 | Japan Tobacco Inc | チアゾール化合物及びその医薬用途 |
GB0114185D0 (en) | 2001-06-12 | 2001-08-01 | Protherics Molecular Design Lt | Compounds |
US20040097555A1 (en) | 2000-12-26 | 2004-05-20 | Shinegori Ohkawa | Concomitant drugs |
AR032653A1 (es) | 2001-02-09 | 2003-11-19 | Telik Inc | Inhibidores heterociclicos del trasportador de glicina 2 composiciones farmaceuticas, uso y metodos. |
ATE315555T1 (de) | 2001-05-11 | 2006-02-15 | Pfizer Prod Inc | Thiazolderivate und ihre verwendung als cdk- inhibitoren |
WO2002100433A1 (en) | 2001-06-11 | 2002-12-19 | Takeda Chemical Industries, Ltd. | Medicinal compositions |
AR039059A1 (es) | 2001-08-06 | 2005-02-09 | Sanofi Aventis | Compuesto derivado de acilaminotiazol, su utilizacion, procedimientos para prepararlo, composicion farmaceutica que lo comprende, y compuestos intermediarios |
JP4495963B2 (ja) * | 2001-09-28 | 2010-07-07 | サイクラセル リミテッド | 抗増殖性化合物としてのn−(4−(4−メチルチアゾール−5−イル)ピリミジン−2−イル)−n−フェニルアミン類 |
GB0123589D0 (en) | 2001-10-01 | 2001-11-21 | Syngenta Participations Ag | Organic compounds |
EP1441732A2 (en) | 2001-11-08 | 2004-08-04 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole derivative and pharmaceutical use thereof |
EP1474141A1 (en) | 2002-02-13 | 2004-11-10 | Pharmagene Laboratories Ltd | 5-ht2b receptor antagonists |
ES2292992T3 (es) * | 2002-02-28 | 2008-03-16 | F. Hoffmann-La Roche Ag | Derivados de tiazol como antagonistas del receptor npy. |
TWI314928B (en) | 2002-02-28 | 2009-09-21 | Novartis A | 5-phenylthiazole derivatives and use as pi3 kinase inhibitors |
US20040053948A1 (en) | 2002-05-10 | 2004-03-18 | Cytokinetics, Inc. | Compounds, compositions and methods |
FR2842523A1 (fr) | 2002-07-17 | 2004-01-23 | Sanofi Synthelabo | Derives d'acylaminothiazole, leur preparation et leur application en therapeutique |
EP1551815A1 (en) | 2002-10-09 | 2005-07-13 | Pfizer Products Inc. | Thiazole compounds for the treatment of neurodegenerative disorders |
JP2006514684A (ja) | 2002-10-30 | 2006-05-11 | 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 | Rockおよび他のプロテインキナーゼとして有用な組成物 |
GB0226583D0 (en) | 2002-11-14 | 2002-12-18 | Cyclacel Ltd | Compounds |
TWI335913B (en) | 2002-11-15 | 2011-01-11 | Vertex Pharma | Diaminotriazoles useful as inhibitors of protein kinases |
US20050004186A1 (en) | 2002-12-20 | 2005-01-06 | Pfizer Inc | MEK inhibiting compounds |
FR2850380B1 (fr) | 2003-01-23 | 2006-07-07 | Sanofi Synthelabo | Derives d'acylaminothiazole, leur preparation et leur utilisation en therapeutique |
JP2006182648A (ja) | 2003-04-08 | 2006-07-13 | Dai Ichi Seiyaku Co Ltd | 7員複素環誘導体 |
TW200519106A (en) * | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
ATE536353T1 (de) * | 2003-08-20 | 2011-12-15 | Vertex Pharma | 2-(4-amino-1,2,5-oxadiazol-4-yl)-imidazol- verbindungen als protein kinase inhibitoren |
KR20060088537A (ko) | 2003-09-06 | 2006-08-04 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절자 |
GB0327380D0 (en) | 2003-11-25 | 2003-12-31 | Cyclacel Ltd | Method |
GB0329275D0 (en) | 2003-12-18 | 2004-01-21 | Merck Sharp & Dohme | Therapeutic treatment |
SI1709019T1 (sl) | 2004-01-12 | 2007-10-31 | Serono Lab | Derivati tiazola in uporaba le-teh |
EP1709018B1 (fr) | 2004-01-16 | 2011-07-20 | Sanofi-Aventis | Derives d'acylaminothiazole et leur application comme inhibiteurs de beta-amyloide |
WO2005073226A1 (fr) | 2004-01-16 | 2005-08-11 | Sanofi-Aventis | Derives d’acylaminothiazole, leur preparation et leur application en therapeutique |
JP2007526324A (ja) * | 2004-03-02 | 2007-09-13 | スミスクライン・ビーチャム・コーポレイション | Akt活性のある阻害剤 |
AP2379A (en) | 2004-03-23 | 2012-03-08 | Pfizer Prod Inc | Imidazole compounds for the treatment of neurodegenerative disorders. |
CN1989131A (zh) | 2004-03-30 | 2007-06-27 | 希龙公司 | 取代的噻吩衍生物用作抗癌药 |
CA2563374A1 (en) * | 2004-04-27 | 2005-12-08 | Research Development Foundation | Antagonism of tgf-.beta.superfamily receptor signaling |
EP1758920A1 (en) | 2004-05-21 | 2007-03-07 | Mpex Pharmaceuticals, Inc. | Bacterial efflux pump inhibitors and methods of treating bacterial infections |
GB0411791D0 (en) | 2004-05-26 | 2004-06-30 | Cyclacel Ltd | Compounds |
BRPI0515012A (pt) | 2004-08-13 | 2008-07-01 | Genentech Inc | substáncia quìmica, composição e formulação farmacêutica, método de tratamento, método de inibição de pelo menos uma enzima que utiliza atp e uso |
WO2006038734A1 (en) * | 2004-10-08 | 2006-04-13 | Astellas Pharma Inc. | Pyridazinone derivatives cytokines inhibitors |
WO2006044860A2 (en) | 2004-10-18 | 2006-04-27 | Amgen, Inc. | Thiadiazole compounds and methods of use |
SE0402735D0 (sv) | 2004-11-09 | 2004-11-09 | Astrazeneca Ab | Novel compounds |
US20060178388A1 (en) | 2005-02-04 | 2006-08-10 | Wrobleski Stephen T | Phenyl-substituted pyrimidine compounds useful as kinase inhibitors |
KR100917511B1 (ko) | 2005-02-28 | 2009-09-16 | 니뽄 다바코 산교 가부시키가이샤 | Syk 저해 활성을 갖는 신규한 아미노피리딘 화합물 |
KR101386282B1 (ko) | 2005-06-17 | 2014-04-17 | 아포지 바이오테크놀로지 코포레이션 | 스핑고신 키나제 저해제 |
WO2007008541A2 (en) | 2005-07-08 | 2007-01-18 | Kalypsys, Inc. | Cellular cholesterol absorption modifiers |
DE102005048072A1 (de) | 2005-09-24 | 2007-04-05 | Bayer Cropscience Ag | Thiazole als Fungizide |
WO2007066805A1 (ja) | 2005-12-09 | 2007-06-14 | Meiji Seika Kaisha, Ltd. | リンコマイシン誘導体およびこれを有効成分とする抗菌剤 |
US7595398B2 (en) | 2005-12-12 | 2009-09-29 | Smithkline Beecham Corporation | N-(5-membered aromatic ring)-amido anti-viral compounds |
JP2009528266A (ja) | 2006-01-18 | 2009-08-06 | シェーリング コーポレイション | カンナビノイド受容体修飾因子 |
EP1981884B1 (en) * | 2006-01-18 | 2012-06-13 | Amgen, Inc | Thiazole compounds as protein kinase b (pkb) inhibitors |
AU2007207052B2 (en) | 2006-01-18 | 2012-07-12 | F. Hoffmann-La Roche Ag | CIS-4, 5-biaryl-2-heterocyclic-imidazolines as MDM2 inhibitors |
US20080242694A1 (en) | 2006-09-18 | 2008-10-02 | D Sidocky Neil R | Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith |
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2007
- 2007-01-11 EP EP07718125A patent/EP1981884B1/en active Active
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- 2007-01-11 EA EA200801716A patent/EA200801716A1/ru unknown
- 2007-01-11 CN CNA2007800097081A patent/CN101421265A/zh active Pending
- 2007-01-11 ES ES07718125T patent/ES2389062T3/es active Active
- 2007-01-11 AU AU2007207743A patent/AU2007207743B2/en not_active Ceased
- 2007-01-11 KR KR1020087019941A patent/KR20080091369A/ko not_active Application Discontinuation
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- 2007-01-11 JP JP2008551297A patent/JP5199885B2/ja not_active Expired - Fee Related
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- 2007-01-11 CA CA2636077A patent/CA2636077C/en not_active Expired - Fee Related
- 2007-01-11 WO PCT/US2007/000871 patent/WO2007084391A2/en active Application Filing
- 2007-01-17 TW TW096101796A patent/TW200738657A/zh unknown
- 2007-01-18 UY UY30098A patent/UY30098A1/es not_active Application Discontinuation
- 2007-01-18 AR ARP070100212A patent/AR059064A1/es unknown
- 2007-01-18 PE PE2007000057A patent/PE20071114A1/es not_active Application Discontinuation
- 2007-11-01 UA UAA200810455A patent/UA91895C2/ru unknown
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2008
- 2008-07-10 IL IL192751A patent/IL192751A0/en unknown
- 2008-07-23 ZA ZA200806386A patent/ZA200806386B/xx unknown
- 2008-08-18 CR CR10211A patent/CR10211A/es not_active Application Discontinuation
- 2008-08-18 NO NO20083572A patent/NO20083572L/no not_active Application Discontinuation
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Also Published As
Publication number | Publication date |
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JP2009525960A (ja) | 2009-07-16 |
UY30098A1 (es) | 2007-10-31 |
IL192751A0 (en) | 2009-02-11 |
NO20083572L (no) | 2008-10-17 |
US8084479B2 (en) | 2011-12-27 |
EP1981884A2 (en) | 2008-10-22 |
JP5199885B2 (ja) | 2013-05-15 |
US7514566B2 (en) | 2009-04-07 |
ZA200806386B (en) | 2009-11-25 |
EP1981884B1 (en) | 2012-06-13 |
ES2389062T3 (es) | 2012-10-22 |
UA91895C2 (en) | 2010-09-10 |
US20090270445A1 (en) | 2009-10-29 |
CA2636077A1 (en) | 2007-07-26 |
CN101421265A (zh) | 2009-04-29 |
AU2007207743A1 (en) | 2007-07-26 |
CR10211A (es) | 2008-10-03 |
CA2636077C (en) | 2012-01-03 |
PE20071114A1 (es) | 2008-01-10 |
AU2007207743B2 (en) | 2010-07-08 |
WO2007084391A3 (en) | 2008-03-20 |
BRPI0706621A2 (pt) | 2011-04-05 |
MY149143A (en) | 2013-07-15 |
KR20080091369A (ko) | 2008-10-10 |
US20070173506A1 (en) | 2007-07-26 |
TW200738657A (en) | 2007-10-16 |
EA200801716A1 (ru) | 2009-04-28 |
WO2007084391A2 (en) | 2007-07-26 |
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