JP2004534010A - 新規なチロシンキナーゼ阻害剤 - Google Patents
新規なチロシンキナーゼ阻害剤 Download PDFInfo
- Publication number
- JP2004534010A JP2004534010A JP2002577817A JP2002577817A JP2004534010A JP 2004534010 A JP2004534010 A JP 2004534010A JP 2002577817 A JP2002577817 A JP 2002577817A JP 2002577817 A JP2002577817 A JP 2002577817A JP 2004534010 A JP2004534010 A JP 2004534010A
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- ethylamino
- hydroxy
- pyridin
- benzimidazol
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- 0 CC(C(C(*)*(*)C(*)**)c1nc(c(*)c(C)c(*)c2*)c2[n]1*)=* Chemical compound CC(C(C(*)*(*)C(*)**)c1nc(c(*)c(C)c(*)c2*)c2[n]1*)=* 0.000 description 22
- SECXISVLQFMRJM-UHFFFAOYSA-N CN(CCC1)C1=O Chemical compound CN(CCC1)C1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 2
- UQFQONCQIQEYPJ-UHFFFAOYSA-N C[n]1nccc1 Chemical compound C[n]1nccc1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 description 2
- NGCXHCGUQHIOLZ-UHFFFAOYSA-N C[n]1nccn1 Chemical compound C[n]1nccn1 NGCXHCGUQHIOLZ-UHFFFAOYSA-N 0.000 description 2
- MWZDIEIXRBWPLG-UHFFFAOYSA-N C[n]1ncnc1 Chemical compound C[n]1ncnc1 MWZDIEIXRBWPLG-UHFFFAOYSA-N 0.000 description 2
- VRESBNUEIKZECD-UHFFFAOYSA-N C[n]1nncn1 Chemical compound C[n]1nncn1 VRESBNUEIKZECD-UHFFFAOYSA-N 0.000 description 2
- OMAFFHIGWTVZOH-UHFFFAOYSA-N C[n]1nnnc1 Chemical compound C[n]1nnnc1 OMAFFHIGWTVZOH-UHFFFAOYSA-N 0.000 description 2
- CCXMGXOCXHRQQX-UHFFFAOYSA-N CCOC(c1cc(C)c2nc(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[nH]c2c1)=N Chemical compound CCOC(c1cc(C)c2nc(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[nH]c2c1)=N CCXMGXOCXHRQQX-UHFFFAOYSA-N 0.000 description 1
- VWIIJDNADIEEDB-UHFFFAOYSA-N CN(CCO1)C1=O Chemical compound CN(CCO1)C1=O VWIIJDNADIEEDB-UHFFFAOYSA-N 0.000 description 1
- MHYLMUJUNNWRNQ-UHFFFAOYSA-N Cc1c2N=C(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[IH]c2cc(C(NC2CCCC2)=O)c1 Chemical compound Cc1c2N=C(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[IH]c2cc(C(NC2CCCC2)=O)c1 MHYLMUJUNNWRNQ-UHFFFAOYSA-N 0.000 description 1
- UIUYQDFIVJOTTH-UHFFFAOYSA-N Cc1c2nc(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[nH]c2cc(N2CCNCC2)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3NCC(c3cccc(Cl)c3)O)[nH]c2cc(N2CCNCC2)c1 UIUYQDFIVJOTTH-UHFFFAOYSA-N 0.000 description 1
- ZAKBVBOEYCRZJE-HSZRJFAPSA-N Cc1c2nc(C(C(NC=C3)=O)=C3NC[C@H](c3cc(Cl)ccc3)O)[nH]c2cc(N2CCN(CCF)CC2)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3NC[C@H](c3cc(Cl)ccc3)O)[nH]c2cc(N2CCN(CCF)CC2)c1 ZAKBVBOEYCRZJE-HSZRJFAPSA-N 0.000 description 1
- XEJNCVPGVBIYGC-SFHVURJKSA-N Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](CC3CCCCC3)CO)[nH]c2cc(-[n]2cncc2)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](CC3CCCCC3)CO)[nH]c2cc(-[n]2cncc2)c1 XEJNCVPGVBIYGC-SFHVURJKSA-N 0.000 description 1
- WUBKSJXCBPMEJM-INIZCTEOSA-N Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc(cccc3)c3Cl)CO)[nH]c2cc(/C(/N)=N/C)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc(cccc3)c3Cl)CO)[nH]c2cc(/C(/N)=N/C)c1 WUBKSJXCBPMEJM-INIZCTEOSA-N 0.000 description 1
- QXPRTJGNGUKZMP-SFHVURJKSA-N Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc3cccc(Br)c3)CO)[nH]c2cc(-[n]2cncc2)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc3cccc(Br)c3)CO)[nH]c2cc(-[n]2cncc2)c1 QXPRTJGNGUKZMP-SFHVURJKSA-N 0.000 description 1
- NQRCKUVJMDFGCB-KRWDZBQOSA-N Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc3cccc(Cl)c3)CO)[nH]c2cc(C#N)c1 Chemical compound Cc1c2nc(C(C(NC=C3)=O)=C3N[C@@H](Cc3cccc(Cl)c3)CO)[nH]c2cc(C#N)c1 NQRCKUVJMDFGCB-KRWDZBQOSA-N 0.000 description 1
- JGEUKMABSQAXHO-UHFFFAOYSA-N Cc1cc(C#N)cc2c1nc(C(C(NC=C1)=O)=C1Cl)[nH]2 Chemical compound Cc1cc(C#N)cc2c1nc(C(C(NC=C1)=O)=C1Cl)[nH]2 JGEUKMABSQAXHO-UHFFFAOYSA-N 0.000 description 1
- GRVCMTABBYJKTD-UHFFFAOYSA-N Cc1cc(F)cc(N)c1[N+]([O-])=O Chemical compound Cc1cc(F)cc(N)c1[N+]([O-])=O GRVCMTABBYJKTD-UHFFFAOYSA-N 0.000 description 1
- OOEBTXFFPAJZJN-UHFFFAOYSA-N O=C(CCl)C(C=C(C1)C2NC1=O)=CC2Cl Chemical compound O=C(CCl)C(C=C(C1)C2NC1=O)=CC2Cl OOEBTXFFPAJZJN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27932701P | 2001-03-28 | 2001-03-28 | |
| PCT/US2002/009402 WO2002079192A1 (en) | 2001-03-28 | 2002-03-26 | Novel tyrosine kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004534010A true JP2004534010A (ja) | 2004-11-11 |
| JP2004534010A5 JP2004534010A5 (cg-RX-API-DMAC7.html) | 2005-12-22 |
Family
ID=23068491
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002577817A Withdrawn JP2004534010A (ja) | 2001-03-28 | 2002-03-26 | 新規なチロシンキナーゼ阻害剤 |
Country Status (25)
Cited By (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007026720A1 (ja) * | 2005-08-31 | 2007-03-08 | Taisho Pharmaceutical Co., Ltd. | 縮環ピラゾール誘導体 |
| WO2007145203A1 (ja) * | 2006-06-13 | 2007-12-21 | Daiichi Fine Chemical Co., Ltd. | 光学活性２－アミノ－１－（４－フルオロフェニル）エタノール |
| JP2008524233A (ja) * | 2004-12-16 | 2008-07-10 | 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 | 炎症性疾患、増殖性疾患および免疫介在性疾患の治療のためのｔｅｃファミリータンパク質キナーゼのインヒビターとして有用なピリド−２−オン |
| JP2009506123A (ja) * | 2005-08-29 | 2009-02-12 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| JP2009507792A (ja) * | 2005-08-29 | 2009-02-26 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| JP2009507790A (ja) * | 2005-08-29 | 2009-02-26 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| JP2010536813A (ja) * | 2007-08-22 | 2010-12-02 | エフ．ホフマン−ラ ロシュ アーゲー | 焦点接着キナーゼ（ｆａｋ）阻害剤としてのピリドンアミド誘導体、及び癌治療のためのその使用 |
| JP2013540820A (ja) * | 2010-11-01 | 2013-11-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロイコトリエン生成のベンゾイミダゾールインヒビター |
| JP2016522246A (ja) * | 2013-06-21 | 2016-07-28 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| JP2018511640A (ja) * | 2015-04-16 | 2018-04-26 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ３−（１ｈ−ベンズイミダゾール−２−イル）−１ｈ−ピリジン−２−オン誘導体 |
| US10231953B2 (en) | 2014-12-17 | 2019-03-19 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| US10363257B2 (en) | 2013-06-21 | 2019-07-30 | Zenith Epigenetics Ltd. | Bicyclic bromodomain inhibitors |
| US10500209B2 (en) | 2013-07-31 | 2019-12-10 | Zenith Epigenetics Ltd. | Quinazolinones as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7081454B2 (en) * | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
| EP1480514A4 (en) | 2002-03-01 | 2008-08-13 | Bristol Myers Squibb Co | TRANSGENIC NON-HUMAN MAMMALS EXPRESS CONSTITUTIVELY ACTIVATED TYROSINE KINASE RECEPTORS |
| WO2003106452A2 (en) * | 2002-06-12 | 2003-12-24 | Millennium Pharmaceuticals, Inc. | Antagonists of melanin concentrating hormone receptor |
| WO2004050033A2 (en) * | 2002-12-02 | 2004-06-17 | Arqule, Inc. | Method of treating cancers |
| EP1581539A4 (en) * | 2003-01-03 | 2007-09-19 | Bristol Myers Squibb Co | NEW TYROSINE KINASE HEMMER |
| JP2006516626A (ja) * | 2003-01-28 | 2006-07-06 | スミスクライン ビーチャム コーポレーション | 化学的化合物 |
| US7312215B2 (en) | 2003-07-29 | 2007-12-25 | Bristol-Myers Squibb Company | Benzimidazole C-2 heterocycles as kinase inhibitors |
| US8362017B2 (en) | 2003-08-29 | 2013-01-29 | Exelixis, Inc. | C-kit modulators and methods of use |
| US20050075358A1 (en) * | 2003-10-06 | 2005-04-07 | Carboni Joan M. | Methods for treating IGF1R-inhibitor induced hyperglycemia |
| WO2005061519A1 (en) | 2003-12-19 | 2005-07-07 | Takeda San Diego, Inc. | Kinase inhibitors |
| DE102004010207A1 (de) | 2004-03-02 | 2005-09-15 | Aventis Pharma S.A. | Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate |
| MXPA06011423A (es) | 2004-04-02 | 2007-01-23 | Osi Pharm Inc | Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico. |
| JP2008510734A (ja) | 2004-08-18 | 2008-04-10 | タケダ サン ディエゴ インコーポレイテッド | キナーゼ阻害剤 |
| US7582634B2 (en) | 2005-02-18 | 2009-09-01 | Wyeth | 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7538113B2 (en) | 2005-02-18 | 2009-05-26 | Wyeth | 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7534796B2 (en) | 2005-02-18 | 2009-05-19 | Wyeth | Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7531542B2 (en) | 2005-05-18 | 2009-05-12 | Wyeth | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor |
| US7582636B2 (en) | 2005-05-26 | 2009-09-01 | Wyeth | Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor |
| WO2006130657A2 (en) | 2005-05-31 | 2006-12-07 | Bristol-Myers Squibb Company | Stereoselective reduction process for the preparation of pyrrolotriazine compounds |
| US7855289B2 (en) | 2005-08-04 | 2010-12-21 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US8093401B2 (en) | 2005-08-04 | 2012-01-10 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US8088928B2 (en) | 2005-08-04 | 2012-01-03 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| PL1910384T3 (pl) | 2005-08-04 | 2013-03-29 | Sirtris Pharmaceuticals Inc | Pochodne imidazo[2,1-b]tiazolu jako związki modulujące sirtuinę |
| US8575164B2 (en) | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
| US8063225B2 (en) * | 2006-08-14 | 2011-11-22 | Chembridge Corporation | Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders |
| WO2008022747A1 (en) * | 2006-08-21 | 2008-02-28 | F. Hoffmann-La Roche Ag | Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents |
| WO2008025526A1 (en) * | 2006-08-31 | 2008-03-06 | F. Hoffmann-La Roche Ag | Indole derivatives, their manufacture and use as pharmaceutical agents |
| US8492328B2 (en) | 2007-05-17 | 2013-07-23 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators |
| TW200916472A (en) | 2007-06-20 | 2009-04-16 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
| CN101687840A (zh) * | 2007-06-25 | 2010-03-31 | 霍夫曼-拉罗奇有限公司 | 作为激酶抑制剂的苯并咪唑酰胺基衍生物 |
| US7816540B2 (en) * | 2007-12-21 | 2010-10-19 | Hoffmann-La Roche Inc. | Carboxyl- or hydroxyl-substituted benzimidazole derivatives |
| CA2712959C (en) | 2008-01-22 | 2015-06-23 | Vernalis (R & D) Ltd | Indolyl-pyridone derivatives having checkpoint kinase 1 inhibitory activity |
| WO2009143051A1 (en) | 2008-05-19 | 2009-11-26 | Osi Pharmaceuticals, Inc. | Substituted imidazopyr-and imidazotri-azines |
| PE20120057A1 (es) | 2008-12-19 | 2012-02-24 | Sirtris Pharmaceuticals Inc | Compuestos de tiazolopiridina moduladores de sirtuina |
| DE102010001064A1 (de) * | 2009-03-18 | 2010-09-23 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung |
| KR20120020099A (ko) | 2009-04-20 | 2012-03-07 | 오에스아이 파마슈티컬스, 엘엘씨 | Ｃ-피라진-메틸아민의 제조 |
| US8536180B2 (en) * | 2009-05-27 | 2013-09-17 | Abbvie Inc. | Pyrimidine inhibitors of kinase activity |
| US20120220594A1 (en) | 2009-10-30 | 2012-08-30 | Bristol-Meyers Squibb Company | Methods for treating cancer in patients having igf-1r inhibitor resistance |
| EP3170813B1 (en) * | 2010-10-06 | 2018-12-12 | GlaxoSmithKline LLC | Benzimidazole derivatives as pi3 kinase inhibitors |
| EP2766497A1 (en) | 2011-10-13 | 2014-08-20 | Bristol-Myers Squibb Company | Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors |
| CN103936719A (zh) * | 2014-05-14 | 2014-07-23 | 中国药科大学 | 苯并咪唑类衍生物制备方法及用途 |
| US11920164B2 (en) | 2014-07-30 | 2024-03-05 | Yeda Research And Development Co. Ltd. | Media for culturing naive human pluripotent stem cells |
| EP3914698B1 (en) | 2019-01-23 | 2024-12-11 | Yeda Research and Development Co. Ltd | Culture media for pluripotent stem cells |
| CN117069696B (zh) * | 2023-08-17 | 2024-04-26 | 中国药科大学 | 一种双靶点小分子抑制剂及其制备方法和应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US6162804A (en) * | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| ATE301651T1 (de) * | 1999-06-23 | 2005-08-15 | Aventis Pharma Gmbh | Substituierte benzimidazole |
| US7081454B2 (en) * | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
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2002
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- 2002-03-26 CN CNA028105168A patent/CN1514833A/zh active Pending
- 2002-03-26 HR HR20030844A patent/HRP20030844A2/hr not_active Application Discontinuation
- 2002-03-26 KR KR10-2003-7012594A patent/KR20030083016A/ko not_active Withdrawn
- 2002-03-26 SK SK12002003A patent/SK12002003A3/sk not_active Application Discontinuation
- 2002-03-26 BR BR0208373-6A patent/BR0208373A/pt not_active IP Right Cessation
- 2002-03-26 IL IL15804102A patent/IL158041A0/xx unknown
- 2002-03-26 EP EP02723631A patent/EP1381598A4/en not_active Withdrawn
- 2002-03-26 MX MXPA03008690A patent/MXPA03008690A/es unknown
- 2002-03-26 WO PCT/US2002/009402 patent/WO2002079192A1/en not_active Ceased
- 2002-03-26 PL PL02373300A patent/PL373300A1/xx not_active Application Discontinuation
- 2002-03-26 HU HU0400323A patent/HUP0400323A2/hu unknown
- 2002-03-26 CZ CZ20032615A patent/CZ20032615A3/cs unknown
- 2002-03-26 GE GE5363A patent/GEP20053660B/en unknown
- 2002-03-26 CA CA002442428A patent/CA2442428A1/en not_active Abandoned
- 2002-03-26 EE EEP200300475A patent/EE200300475A/xx unknown
- 2002-03-26 YU YU84603A patent/YU84603A/sh unknown
- 2002-03-26 RU RU2003131693/04A patent/RU2003131693A/ru not_active Application Discontinuation
- 2002-03-27 AR ARP020101167A patent/AR035804A1/es not_active Application Discontinuation
- 2002-03-27 UY UY27234A patent/UY27234A1/es not_active Application Discontinuation
- 2002-03-27 PE PE2002000244A patent/PE20021015A1/es not_active Application Discontinuation
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2003
- 2003-09-25 ZA ZA200307466A patent/ZA200307466B/en unknown
- 2003-09-26 BG BG108206A patent/BG108206A/bg unknown
- 2003-09-26 IS IS6968A patent/IS6968A/is unknown
- 2003-09-26 NO NO20034308A patent/NO20034308L/no not_active Application Discontinuation
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| JP2008524233A (ja) * | 2004-12-16 | 2008-07-10 | 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 | 炎症性疾患、増殖性疾患および免疫介在性疾患の治療のためのｔｅｃファミリータンパク質キナーゼのインヒビターとして有用なピリド−２−オン |
| JP2009062391A (ja) * | 2004-12-16 | 2009-03-26 | Vertex Pharmaceut Inc | 炎症性疾患、増殖性疾患および免疫介在性疾患の治療のためのｔｅｃファミリータンパク質キナーゼの阻害物質として有用なピリド−２−オン |
| JP2013213046A (ja) * | 2004-12-16 | 2013-10-17 | Vertex Pharmaceuticals Inc | 炎症性疾患、増殖性疾患および免疫介在性疾患の治療のためのｔｅｃファミリータンパク質キナーゼの阻害物質として有用なピリド−２−オン |
| JP2009506123A (ja) * | 2005-08-29 | 2009-02-12 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| JP2009507792A (ja) * | 2005-08-29 | 2009-02-26 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| JP2009507790A (ja) * | 2005-08-29 | 2009-02-26 | 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 | 非受容体型チロシンキナーゼのｔｅｃファミリーの阻害剤として有用な３，５−二置換ピリド−２−オン |
| WO2007026720A1 (ja) * | 2005-08-31 | 2007-03-08 | Taisho Pharmaceutical Co., Ltd. | 縮環ピラゾール誘導体 |
| WO2007145203A1 (ja) * | 2006-06-13 | 2007-12-21 | Daiichi Fine Chemical Co., Ltd. | 光学活性２－アミノ－１－（４－フルオロフェニル）エタノール |
| JP2010536813A (ja) * | 2007-08-22 | 2010-12-02 | エフ．ホフマン−ラ ロシュ アーゲー | 焦点接着キナーゼ（ｆａｋ）阻害剤としてのピリドンアミド誘導体、及び癌治療のためのその使用 |
| JP2013540820A (ja) * | 2010-11-01 | 2013-11-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロイコトリエン生成のベンゾイミダゾールインヒビター |
| JP2016522246A (ja) * | 2013-06-21 | 2016-07-28 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| US10166215B2 (en) | 2013-06-21 | 2019-01-01 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| US10226451B2 (en) | 2013-06-21 | 2019-03-12 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| US10363257B2 (en) | 2013-06-21 | 2019-07-30 | Zenith Epigenetics Ltd. | Bicyclic bromodomain inhibitors |
| US10772892B2 (en) | 2013-06-21 | 2020-09-15 | Zenith Epigenetics Ltd. | Bicyclic bromodomain inhibitors |
| US11026926B2 (en) | 2013-06-21 | 2021-06-08 | Zenith Epigenetics Ltd. | Substituted bicyclic compounds as bromodomain inhibitors |
| US11446306B2 (en) | 2013-06-21 | 2022-09-20 | Zenith Epigenetics Ltd. | Bicyclic bromodomain inhibitors |
| US10500209B2 (en) | 2013-07-31 | 2019-12-10 | Zenith Epigenetics Ltd. | Quinazolinones as bromodomain inhibitors |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| US10231953B2 (en) | 2014-12-17 | 2019-03-19 | Zenith Epigenetics Ltd. | Inhibitors of bromodomains |
| JP2018511640A (ja) * | 2015-04-16 | 2018-04-26 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ３−（１ｈ−ベンズイミダゾール−２−イル）−１ｈ−ピリジン−２−オン誘導体 |
Also Published As
| Publication number | Publication date |
|---|---|
| UY27234A1 (es) | 2002-10-31 |
| BR0208373A (pt) | 2005-02-22 |
| IS6968A (is) | 2003-09-26 |
| AR035804A1 (es) | 2004-07-14 |
| EP1381598A4 (en) | 2008-03-19 |
| PL373300A1 (en) | 2005-08-22 |
| HUP0400323A2 (hu) | 2005-11-28 |
| RU2003131693A (ru) | 2005-05-10 |
| NO20034308D0 (no) | 2003-09-26 |
| CA2442428A1 (en) | 2002-10-10 |
| SK12002003A3 (en) | 2004-10-05 |
| PE20021015A1 (es) | 2002-11-10 |
| BG108206A (bg) | 2004-11-30 |
| YU84603A (sh) | 2006-03-03 |
| KR20030083016A (ko) | 2003-10-23 |
| MXPA03008690A (es) | 2003-12-12 |
| CN1514833A (zh) | 2004-07-21 |
| GEP20053660B (en) | 2005-11-10 |
| NO20034308L (no) | 2003-11-26 |
| ZA200307466B (en) | 2005-01-13 |
| CZ20032615A3 (en) | 2004-03-17 |
| HRP20030844A2 (en) | 2005-08-31 |
| IL158041A0 (en) | 2004-03-28 |
| EP1381598A1 (en) | 2004-01-21 |
| WO2002079192A1 (en) | 2002-10-10 |
| EE200300475A (et) | 2004-02-16 |
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