JP2010520228A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010520228A5 JP2010520228A5 JP2009551895A JP2009551895A JP2010520228A5 JP 2010520228 A5 JP2010520228 A5 JP 2010520228A5 JP 2009551895 A JP2009551895 A JP 2009551895A JP 2009551895 A JP2009551895 A JP 2009551895A JP 2010520228 A5 JP2010520228 A5 JP 2010520228A5
- Authority
- JP
- Japan
- Prior art keywords
- butoxycarbonylamino
- piperidine
- tert
- cis
- benzyl
- 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.)
- Granted
Links
- XEKOWRVHYACXOJ-UHFFFAOYSA-N acetic acid ethyl ester Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M Lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
- RBQORQMAZDTPPY-UHFFFAOYSA-M N1(CC(CCC1)C(=O)[O-])C(=O)ONC(=O)OC(C)(C)C Chemical compound N1(CC(CCC1)C(=O)[O-])C(=O)ONC(=O)OC(C)(C)C RBQORQMAZDTPPY-UHFFFAOYSA-M 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000012267 brine Substances 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- VLKZOEOYAKHREP-UHFFFAOYSA-N hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 2
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 2
- 238000007069 methylation reaction Methods 0.000 description 2
- YMWUJEATGCHHMB-UHFFFAOYSA-N methylene dichloride Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 230000002194 synthesizing Effects 0.000 description 2
- 125000006633 tert-butoxycarbonylamino group Chemical group 0.000 description 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- HDSNVAURSXRRHB-LSDHHAIUSA-N (3S,5R)-5-[(2-methylpropan-2-yl)oxycarbonylamino]-1-phenylmethoxycarbonylpiperidine-3-carboxylic acid Chemical compound C1[C@H](NC(=O)OC(C)(C)C)C[C@H](C(O)=O)CN1C(=O)OCC1=CC=CC=C1 HDSNVAURSXRRHB-LSDHHAIUSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- PSHKMPUSSFXUIA-UHFFFAOYSA-N N,N-dimethylpyridin-2-amine Chemical compound CN(C)C1=CC=CC=N1 PSHKMPUSSFXUIA-UHFFFAOYSA-N 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M NaHCO3 Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 238000007792 addition Methods 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000008079 hexane Substances 0.000 description 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- YOQDYZUWIQVZSF-UHFFFAOYSA-N sodium borohydride Substances [BH4-].[Na+] YOQDYZUWIQVZSF-UHFFFAOYSA-N 0.000 description 1
- ODGROJYWQXFQOZ-UHFFFAOYSA-N sodium;boron(1-) Chemical compound [B-].[Na+] ODGROJYWQXFQOZ-UHFFFAOYSA-N 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
Description
cis−(+/−)−1−ベンジル 3−メチル 5−(tert−ブトキシカルボニルアミノ)ピペリジン−1,3−ジカルボキシレートの合成
ジクロロメタン中の濃度0.25Mのcis−(+/−)−1−(ベンジルオキシカルボニル)−5−(tert−ブトキシカルボニルアミノ)ピペリジン−3−カルボン酸(1.0当量)、メタノール(20当量)およびEDC(1.3当量)の溶液に、0℃で、ジメチルアミノピリジン(0.1当量)を加えた。48時間撹拌した後、該反応物を室温まで昇温し、揮発成分を真空で除去した。酢酸エチルを添加した後、H2O(3×)で、1N HClで、NaHCO3(飽和)で、そして塩水で洗浄し、該溶液をMgSO4で乾燥し、濾過し、濃縮し、カラムクロマトグラフィーによって精製し(25% 酢酸エチル/ヘキサン)、cis−(+/−)−1−ベンジル 3−メチル 5−(tert−ブトキシカルボニルアミノ)ピペリジン−1,3−ジカルボキシレートを得た。
LCMS (m/z): 293.1 (MH-Boc+ );
LC Rt = 4.09分。
LCMS (m/z): 293.1 (MH-Boc+ );
LC Rt = 4.09分。
cis−(+/−)−ベンジル 3−(tert−ブトキシカルボニルアミノ)−5−(ヒドロキシメチル)ピペリジン−1−カルボキシレートの合成
THF中の濃度0.08Mのcis−(+/−)−1−ベンジル 3−メチル 5−(tert−ブトキシカルボニルアミノ)ピペリジン−1,3−ジカルボキシレート(1.0当量)の溶液を0℃で冷却し、次いでLiCl(2.3当量)および水素化ホウ素ナトリウム(2.3当量)を加えた。該反応物を室温まで温めながら、20時間撹拌した後、pHを、1M クエン酸で、pH 4〜5に調節した。真空で揮発成分を除去した後、該生成物をジクロロメタン中に抽出し、H2Oで、そして塩水で洗浄し、MgSO4で乾燥した。濾過し、真空で揮発成分を除去した後、cis−(+/−)−ベンジル 3−(tert−ブトキシカルボニルアミノ)−5−(ヒドロキシメチル)ピペリジン−1−カルボキシレートを、白色の泡状固体として得た。
LCMS (m/z): 265.0 (MH-Boc+ );
LC Rt = 3.37分。
LCMS (m/z): 265.0 (MH-Boc+ );
LC Rt = 3.37分。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US89244407P | 2007-03-01 | 2007-03-01 | |
US60/892,444 | 2007-03-01 | ||
US2377708P | 2008-01-25 | 2008-01-25 | |
US61/023,777 | 2008-01-25 | ||
PCT/US2008/055724 WO2008106692A1 (en) | 2007-03-01 | 2008-03-03 | Pim kinase inhibitors and methods of their use |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2010520228A JP2010520228A (ja) | 2010-06-10 |
JP2010520228A5 true JP2010520228A5 (ja) | 2011-03-17 |
JP5330274B2 JP5330274B2 (ja) | 2013-10-30 |
Family
ID=39433847
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009551895A Active JP5330274B2 (ja) | 2007-03-01 | 2008-03-03 | Pimキナーゼ阻害剤およびその使用方法 |
Country Status (12)
Country | Link |
---|---|
US (1) | US8822497B2 (ja) |
EP (1) | EP2132177B1 (ja) |
JP (1) | JP5330274B2 (ja) |
KR (1) | KR101514853B1 (ja) |
CN (1) | CN101679266B (ja) |
AU (1) | AU2008221263B2 (ja) |
BR (1) | BRPI0808523A2 (ja) |
CA (1) | CA2679659C (ja) |
EA (1) | EA019951B1 (ja) |
ES (1) | ES2431163T3 (ja) |
MX (1) | MX2009009304A (ja) |
WO (1) | WO2008106692A1 (ja) |
Families Citing this family (147)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8088928B2 (en) | 2005-08-04 | 2012-01-03 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
US7855289B2 (en) | 2005-08-04 | 2010-12-21 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
US20070037865A1 (en) | 2005-08-04 | 2007-02-15 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
US8093401B2 (en) | 2005-08-04 | 2012-01-10 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
ES2612196T3 (es) | 2005-12-13 | 2017-05-12 | Incyte Holdings Corporation | Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus |
WO2008054702A1 (en) | 2006-10-31 | 2008-05-08 | Schering Corporation | Anilinopiperazine derivatives and methods of use thereof |
AU2007314305B2 (en) | 2006-10-31 | 2013-01-24 | Merck Sharp & Dohme Corp. | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
US20140249135A1 (en) * | 2007-03-01 | 2014-09-04 | Novartis Ag | Pim kinase inhibitors and methods of their use |
AU2008247102B2 (en) | 2007-05-03 | 2011-11-24 | Pfizer Limited | 2 -pyridine carboxamide derivatives as sodium channel modulators |
MX342814B (es) | 2007-06-13 | 2016-10-13 | Incyte Holdings Corp | Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
TW200918542A (en) | 2007-06-20 | 2009-05-01 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
CL2008001822A1 (es) | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras. |
CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
AR067585A1 (es) * | 2007-07-19 | 2009-10-14 | Schering Corp | Compuestos heterociclicos de amidas como inhibidores de la proteincinasa |
WO2009020198A1 (ja) * | 2007-08-03 | 2009-02-12 | Kinopharma, Inc. | 抗dnaウイルス作用を有するアニリン誘導体 |
CN101918371A (zh) * | 2007-11-01 | 2010-12-15 | 西特里斯药业公司 | 作为瑟土因调节剂的酰胺衍生物 |
UY31679A1 (es) * | 2008-03-03 | 2009-09-30 | Inhibidores de cinasa pim y metodos para su uso | |
AR071717A1 (es) | 2008-05-13 | 2010-07-07 | Array Biopharma Inc | Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer. |
AU2011265439B2 (en) * | 2008-09-02 | 2012-09-20 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
PL2344474T3 (pl) * | 2008-09-02 | 2016-03-31 | Novartis Ag | Pochodne pikolinamidu jako inhibitory kinaz |
UY32146A (es) | 2008-09-29 | 2010-04-30 | Boehringer Ingelheim Int | Derivados de las 5-[4-(1,5-dimetil-1h-pirazol-4-il)-1,2,3-triazol-1-il]-6-metil-nicotinamidas n-(sustituidas) y de las n-{5-[4-(1,5-dimetil-1h-pirazol-4-il)-1,2,3-triazol-1-il]-6-metil-piridin-3-il}-benzamidas sustituidas y composiciones conteniéndolos |
US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
WO2010054398A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
MX2011006555A (es) | 2008-12-19 | 2011-08-03 | Sirtris Pharmaceuticals Inc | Compuestos de tiazolopiridina moduladores de sirtuina. |
EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
KR20120030447A (ko) | 2009-05-22 | 2012-03-28 | 인사이트 코포레이션 | Jak 저해물질로서 3-[4-(7h-피롤로[2,3-d]피리미딘-4-일)-1h-피라졸-1-일]옥탄- 또는 헵탄-니트릴 |
CA2762174C (en) | 2009-05-22 | 2018-02-20 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
AR077328A1 (es) | 2009-07-24 | 2011-08-17 | Novartis Ag | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos |
US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
US8435976B2 (en) | 2009-09-08 | 2013-05-07 | F. Hoffmann-La Roche | 4-substituted pyridin-3-yl-carboxamide compounds and methods of use |
US20110183938A1 (en) | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
WO2011089416A1 (en) * | 2010-01-19 | 2011-07-28 | Astrazeneca Ab | Pyrazine derivatives |
US8470820B2 (en) | 2010-01-22 | 2013-06-25 | Hoffman-La Roche Inc. | Nitrogen-containing heteroaryl derivatives |
RS60680B1 (sr) | 2010-03-10 | 2020-09-30 | Incyte Holdings Corp | Piperidin-4-il azetidin derivati kao inhibitori jak1 |
CN102791691B (zh) * | 2010-03-12 | 2015-06-03 | 日本曹达株式会社 | 含有吡啶环的化合物、及卤代甲基吡啶衍生物以及四唑基肟衍生物的制造方法 |
JP5871897B2 (ja) | 2010-03-26 | 2016-03-01 | 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 | ピリジルトリアゾール |
EP2556066B1 (en) | 2010-04-07 | 2016-10-19 | F.Hoffmann-La Roche Ag | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
WO2011143425A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
EP2569289A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
NZ603478A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | 2 -aminopyridine derivatives useful as inhibitors of atr kinase |
JP2013526538A (ja) | 2010-05-12 | 2013-06-24 | 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 | Atrキナーゼ阻害剤として有用な化合物 |
MX2012013081A (es) | 2010-05-12 | 2013-05-09 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa atr. |
WO2011143423A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
SG10201503983QA (en) | 2010-05-21 | 2015-06-29 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
US8703768B2 (en) | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
EP2585468A1 (en) | 2010-06-23 | 2013-05-01 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
WO2012004217A1 (en) * | 2010-07-06 | 2012-01-12 | Novartis Ag | Cyclic ether compounds useful as kinase inhibitors |
EP2640725B1 (en) | 2010-11-19 | 2015-01-07 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
TW201249845A (en) | 2010-11-19 | 2012-12-16 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
US8524897B2 (en) | 2011-01-12 | 2013-09-03 | Novartis Ag | Crystalline oxazine derivative |
JP5715710B2 (ja) | 2011-01-13 | 2015-05-13 | ノバルティス アーゲー | 新規複素環誘導体および神経障害の処置におけるそれらの使用 |
US8987307B2 (en) | 2011-03-03 | 2015-03-24 | Hoffmann-La Roche Inc. | 3-amino-pyridines as GPBAR1 agonists |
UY33930A (es) | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
CN103429572A (zh) * | 2011-03-04 | 2013-12-04 | 诺瓦提斯公司 | 作为激酶抑制剂的四取代的环己基化合物 |
WO2012138938A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
JP2014516941A (ja) | 2011-04-29 | 2014-07-17 | アムジェン インコーポレイテッド | Pim阻害剤としての二環式ピリダジン化合物 |
US9321727B2 (en) * | 2011-06-10 | 2016-04-26 | Hoffmann-La Roche Inc. | Pyridine derivatives as agonists of the CB2 receptor |
MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
EP2734517B1 (en) * | 2011-07-18 | 2017-08-30 | Merck Patent GmbH | Benzamides |
JP6105578B2 (ja) | 2011-07-21 | 2017-03-29 | トレロ ファーマシューティカルズ, インコーポレイテッド | 複素環式プロテインキナーゼ阻害剤 |
US9458151B2 (en) | 2011-08-11 | 2016-10-04 | Jikai Biosciences, Inc. | Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
US9452995B2 (en) | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyridine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
US9453003B2 (en) | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyrimidine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
CN102924446B (zh) | 2011-08-11 | 2015-08-26 | 上海吉铠医药科技有限公司 | Pim激酶抑制剂及其制备方法与在制药中的应用 |
TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
AR088061A1 (es) * | 2011-09-27 | 2014-05-07 | Hoffmann La Roche | Compuestos de pirazol-4-il-heterociclil-carboxamida y metodos de uso |
US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
ES2751741T3 (es) | 2011-09-30 | 2020-04-01 | Vertex Pharma | Procedimiento para fabricar compuestos útiles como inhibidores de la quinasa ATR |
MX2014003785A (es) | 2011-09-30 | 2014-07-24 | Vertex Phamaceuticals Inc | Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr. |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
MX2014003796A (es) | 2011-09-30 | 2015-01-16 | Vertex Pharma | Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2013071090A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2013071085A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
CA2869309C (en) | 2012-04-05 | 2021-02-09 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
AR091079A1 (es) | 2012-05-18 | 2014-12-30 | Incyte Corp | Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak |
KR20150013548A (ko) * | 2012-05-21 | 2015-02-05 | 노파르티스 아게 | 키나제 억제제로서의 신규 고리-치환된 n-피리디닐 아미드 |
WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
HUE049611T2 (hu) * | 2012-09-26 | 2020-09-28 | Hoffmann La Roche | Ciklikus éter-pirazol-4-il-heterociklil-karboxamid vegyületek és felhasználási módszerek |
WO2014055756A1 (en) | 2012-10-04 | 2014-04-10 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
WO2014062604A1 (en) | 2012-10-16 | 2014-04-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
RS62329B1 (sr) | 2012-11-15 | 2021-10-29 | Incyte Holdings Corp | Dozni oblici ruksolitiniba sa produženim vremenom oslobađanja |
EP3808749B1 (en) | 2012-12-07 | 2023-03-08 | Vertex Pharmaceuticals Incorporated | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of atr kinase for the treatment of cancer diseases |
WO2014093230A2 (en) * | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
JP6437452B2 (ja) * | 2013-01-14 | 2018-12-12 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pimキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物 |
HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
ES2900492T3 (es) | 2013-03-06 | 2022-03-17 | Incyte Holdings Corp | Procesos y productos intermedios para elaborar un inhibidor de JAK |
US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EA201690357A1 (ru) | 2013-08-07 | 2016-07-29 | Инсайт Корпорейшн | Лекарственные формы с замедленным высвобождением для ингибитора jak1 |
JP6449880B2 (ja) * | 2013-08-08 | 2019-01-09 | 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 | 新規ピラジンアミド化合物 |
JP2016528298A (ja) | 2013-08-23 | 2016-09-15 | インサイト・コーポレイションIncyte Corporation | Pimキナーゼ阻害剤として有用なフロピリジン及びチエノピリジンカルボキシアミド化合物 |
HUE046727T2 (hu) | 2013-12-06 | 2020-03-30 | Vertex Pharma | Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai |
UY36034A (es) | 2014-03-18 | 2015-09-30 | Astrazeneca Ab | Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos |
US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
EP3152212B9 (en) | 2014-06-05 | 2020-05-27 | Vertex Pharmaceuticals Inc. | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
JP6936007B2 (ja) | 2014-06-17 | 2021-09-15 | 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Vertex Pharmaceuticals Incorporated | Chk1阻害剤とatr阻害剤との組み合わせを使用してがんを処置する方法 |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
JO3589B1 (ar) * | 2014-08-06 | 2020-07-05 | Novartis Ag | مثبطات كيناز البروتين c وطرق استخداماتها |
SG11201706756VA (en) | 2015-03-10 | 2017-09-28 | Aduro Biotech Inc | Compositions and methods for activating "stimulator of interferon gene" -dependent signalling |
WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
CN105130959B (zh) * | 2015-09-18 | 2018-08-03 | 上海吉铠医药科技有限公司 | 嘧啶衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
CN105218523B (zh) * | 2015-09-18 | 2019-08-23 | 上海吉铠医药科技有限公司 | 吡啶衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
RU2605400C1 (ru) * | 2015-11-13 | 2016-12-20 | ЗАО "Р-Фарм" | ПРОИЗВОДНЫЕ 1-(3-АМИНОФЕНИЛ)-6,8-ДИМЕТИЛ-5-(4-ИОД-2-ФТОР-ФЕНИЛАМИНО)-3-ЦИКЛОПРОПИЛ-1H,6H-ПИРИДО[4,3-d]ПИРИМИДИН-2,4,7-ТРИОНА В КАЧЕСТВЕ ИНГИБИТОРОВ МЕК1/2 |
WO2017147701A1 (en) | 2016-03-01 | 2017-09-08 | Ontario Institute For Cancer Research (Oicr) | Inhibitors of wdr5 protein-protein binding |
US11319299B2 (en) * | 2016-03-01 | 2022-05-03 | Propellon Therapeutics Inc. | Substituted carboxamides as inhibitors of WDR5 protein-protein binding |
EP3432886B1 (en) | 2016-03-25 | 2021-06-02 | University of Maryland, Baltimore County | Pim kinase inhibitors in combination with rna splicing modulators/inhibitors for treatment of cancers |
WO2017211303A1 (en) | 2016-06-07 | 2017-12-14 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
EP3507367A4 (en) | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
WO2018049214A1 (en) | 2016-09-09 | 2018-03-15 | Incyte Corporation | Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer |
EA202190196A1 (ru) | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
PL3621615T3 (pl) | 2017-05-12 | 2024-03-25 | Enanta Pharmaceuticals, Inc. | Inhibitory regulujące sygnał apoptozy kinazy 1 i sposoby ich stosowania |
AU2018341084B2 (en) | 2017-09-27 | 2023-04-13 | Exonate Limited | SRPK1 inhibitors |
AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
WO2019144012A1 (en) * | 2018-01-18 | 2019-07-25 | Emory University | Mast1 and uses for diagnosing and treating cancer |
SG11202007164UA (en) | 2018-01-30 | 2020-08-28 | Incyte Corp | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
SI3755703T1 (sl) * | 2018-02-20 | 2022-11-30 | Incyte Corporation | N-(fenil)-2-(fenil)pirimidin-4-karboksamidni derivati in sorodne spojine kot zaviralci HPK1 za zravljenje raka |
DK3773593T3 (da) | 2018-03-30 | 2024-05-27 | Incyte Corp | Behandling af hidradenitis suppurativa under anvendelse af JAK-inhibitorer |
US20210113562A1 (en) | 2018-04-13 | 2021-04-22 | Sumitomo Dainippon Pharma Oncology, Inc. | Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer |
WO2019213244A1 (en) | 2018-05-02 | 2019-11-07 | Enanta Pharmaceuticals, Inc. | Tetrazole containing apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof |
EP3802518A1 (en) * | 2018-05-25 | 2021-04-14 | Silverback Therapeutics, Inc. | Amino-pyrazinecarboxamide compounds, conjugates, and uses thereof |
US10899755B2 (en) | 2018-08-08 | 2021-01-26 | Incyte Corporation | Benzothiazole compounds and uses thereof |
WO2020167990A1 (en) | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
US20220169660A1 (en) * | 2019-03-06 | 2022-06-02 | Silverback Therapeutics, Inc. | Cyclic amino-pyrazinecarboxamide compounds and uses thereof |
CN114222747A (zh) * | 2019-04-29 | 2022-03-22 | 斯奈普生物公司 | Pim激酶抑制剂组合物及其用途 |
CN110452180A (zh) * | 2019-06-25 | 2019-11-15 | 南京普锐达医药科技有限公司 | 一种合成2-氯-5-氨基-6-嘧啶甲酸乙酯的方法 |
EP4010338A1 (en) | 2019-08-06 | 2022-06-15 | Incyte Corporation | Solid forms of an hpk1 inhibitor |
CN117229215A (zh) * | 2019-09-10 | 2023-12-15 | 四川科伦博泰生物医药股份有限公司 | 联芳基类化合物,包含其的药物组合物,其制备方法及其用途 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
CN115385864A (zh) * | 2022-08-10 | 2022-11-25 | 杭州国瑞生物科技有限公司 | 一种苏沃雷生中间体的制备方法 |
WO2024059207A2 (en) * | 2022-09-15 | 2024-03-21 | Vanderbilt University | Pyrazoloether analogs as mglu5 negative allosteric modulators and methods of making and using the same |
WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (143)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
US4294926A (en) | 1979-06-15 | 1981-10-13 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
US4319039A (en) | 1979-06-15 | 1982-03-09 | Merck & Co., Inc. | Preparation of ammonium salt of hypocholesteremic fermentation product |
US4444784A (en) | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
JPS5889191A (ja) | 1981-11-20 | 1983-05-27 | Sankyo Co Ltd | 3−ヒドロキシ−ml−236b誘導体の製造法 |
WO1984002131A1 (en) | 1982-11-22 | 1984-06-07 | Sandoz Ag | Analogs of mevalolactone and derivatives thereof, processes for their production, pharmaceutical compositions containing them and their use as pharmaceuticals |
US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
US4911165A (en) | 1983-01-12 | 1990-03-27 | Ethicon, Inc. | Pliabilized polypropylene surgical filaments |
US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
US4782084A (en) | 1987-06-29 | 1988-11-01 | Merck & Co., Inc. | HMG-COA reductase inhibitors |
US4885314A (en) | 1987-06-29 | 1989-12-05 | Merck & Co., Inc. | Novel HMG-CoA reductase inhibitors |
US4820850A (en) | 1987-07-10 | 1989-04-11 | Merck & Co., Inc. | Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof |
US5180589A (en) | 1988-03-31 | 1993-01-19 | E. R. Squibb & Sons, Inc. | Pravastatin pharmaceuatical compositions having good stability |
US5030447A (en) | 1988-03-31 | 1991-07-09 | E. R. Squibb & Sons, Inc. | Pharmaceutical compositions having good stability |
US4916239A (en) | 1988-07-19 | 1990-04-10 | Merck & Co., Inc. | Process for the lactonization of mevinic acids and analogs thereof |
US5118853A (en) | 1988-10-13 | 1992-06-02 | Sandoz Ltd. | Processes for the synthesis of 3-disubstituted aminoacroleins |
US5290946A (en) | 1988-10-13 | 1994-03-01 | Sandoz Ltd. | Processes for the synthesis of 3-(substituted indolyl-2-yl)propenaldehydes |
US4929437A (en) | 1989-02-02 | 1990-05-29 | Merck & Co., Inc. | Coenzyme Q10 with HMG-CoA reductase inhibitors |
US5189164A (en) | 1989-05-22 | 1993-02-23 | Sandoz Ltd. | Processes for the synthesis of syn-(E)-3,5-dihydroxy-7-substituted hept-6-enoic and heptanoic acids and derivatives and intermediates thereof |
FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
US5420245A (en) | 1990-04-18 | 1995-05-30 | Board Of Regents, The University Of Texas | Tetrapeptide-based inhibitors of farnesyl transferase |
HU9203780D0 (en) | 1991-12-12 | 1993-03-29 | Sandoz Ag | Stabilized pharmaceutical products of hmg-coa reductase inhibitor and method for producing them |
US5604260A (en) | 1992-12-11 | 1997-02-18 | Merck Frosst Canada Inc. | 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2 |
EP0604181A1 (en) | 1992-12-21 | 1994-06-29 | Eli Lilly And Company | Antitumor compositions and method of treatment |
ATE160345T1 (de) | 1993-01-15 | 1997-12-15 | Searle & Co | 3,4-diarylthiophene und analoga davon, sowie deren verwendung als entzündungshemmende mittel |
WO1994019357A1 (en) | 1993-02-23 | 1994-09-01 | Merrell Dow Pharmaceuticals Inc. | Farnesyl:protein transferase inhibitors as anticancer agents |
US5298627A (en) | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
US5409944A (en) | 1993-03-12 | 1995-04-25 | Merck Frosst Canada, Inc. | Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase |
CA2118985A1 (en) | 1993-04-02 | 1994-10-03 | Dinesh V. Patel | Heterocyclic inhibitors of farnesyl protein transferase |
CA2160786A1 (en) | 1993-05-14 | 1994-11-24 | James C. Marsters, Jr. | Ras farnesyl transferase inhibitors |
US5602098A (en) | 1993-05-18 | 1997-02-11 | University Of Pittsburgh | Inhibition of farnesyltransferase |
US5380738A (en) | 1993-05-21 | 1995-01-10 | Monsanto Company | 2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents |
US5436265A (en) | 1993-11-12 | 1995-07-25 | Merck Frosst Canada, Inc. | 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents |
US5474995A (en) | 1993-06-24 | 1995-12-12 | Merck Frosst Canada, Inc. | Phenyl heterocycles as cox-2 inhibitors |
GB9602877D0 (en) | 1996-02-13 | 1996-04-10 | Merck Frosst Canada Inc | 3,4-Diaryl-2-hydroxy-2,5- dihydrofurans as prodrugs to cox-2 inhibitors |
WO1995008542A1 (fr) | 1993-09-22 | 1995-03-30 | Kyowa Hakko Kogyo Co., Ltd. | Inhibiteur de la farnesyl-transferase |
IL111258A0 (en) | 1993-10-15 | 1994-12-29 | Schering Corp | Tricyclic carbamate compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
US5661152A (en) | 1993-10-15 | 1997-08-26 | Schering Corporation | Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
MY134819A (en) | 1993-10-15 | 2007-12-31 | Schering Corp | Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
US5721236A (en) | 1993-10-15 | 1998-02-24 | Schering Corporation | Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
US5719148A (en) | 1993-10-15 | 1998-02-17 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
IL111235A (en) | 1993-10-15 | 2001-03-19 | Schering Plough Corp | Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them |
EP0725790B1 (en) | 1993-10-25 | 2001-04-18 | PARKE DAVIS & COMPANY | Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase |
US5344991A (en) | 1993-10-29 | 1994-09-06 | G.D. Searle & Co. | 1,2 diarylcyclopentenyl compounds for the treatment of inflammation |
EP0677039B1 (en) | 1993-11-04 | 1999-03-10 | Abbott Laboratories | Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase |
US5783593A (en) | 1993-11-04 | 1998-07-21 | Abbott Laboratories | Inhibitors of squalene synthetase and protein farnesyltransferase |
JP3597863B2 (ja) | 1993-11-05 | 2004-12-08 | ワーナー−ランバート・コンパニー | タンパク質:ファルネシルトランスフェラーゼの置換されたジ‐およびトリペプチド阻害剤 |
US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
US5484799A (en) | 1993-12-09 | 1996-01-16 | Abbott Laboratories | Antifungal dorrigocin derivatives |
US5393790A (en) | 1994-02-10 | 1995-02-28 | G.D. Searle & Co. | Substituted spiro compounds for the treatment of inflammation |
WO1995024612A1 (de) | 1994-03-07 | 1995-09-14 | International Business Machines Corporation | Verfahren und vorrichtung zur schnellen interpolation von zwischenwerten aus periodischen phasenverschobenen signalen und zur erkennung von defekten in einem drehkörper |
AU2122795A (en) | 1994-03-15 | 1995-10-03 | Eisai Co. Ltd. | Isoprenyl transferase inhibitors |
IL113196A0 (en) | 1994-03-31 | 1995-06-29 | Bristol Myers Squibb Co | Imidazole derivatives and pharmaceutical compositions containing the same |
US5523430A (en) | 1994-04-14 | 1996-06-04 | Bristol-Myers Squibb Company | Protein farnesyl transferase inhibitors |
US5510510A (en) | 1994-05-10 | 1996-04-23 | Bristol-Meyers Squibb Company | Inhibitors of farnesyl protein transferase |
FR2720396B1 (fr) * | 1994-05-27 | 1996-06-28 | Adir | Nouveaux N-pyridyl carboxamides et dérivés leur procédé de préparation et les compositions pharmaceutiques qui les contiennent. |
US5563255A (en) | 1994-05-31 | 1996-10-08 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
CZ361996A3 (en) | 1994-06-10 | 1997-04-16 | Rhone Poulenc Rorer Sa | Inhibitors of farnesyl-transferase, process of their preparation and pharmaceutical compositions containing thereof |
US5571792A (en) | 1994-06-30 | 1996-11-05 | Warner-Lambert Company | Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase |
WO1996005529A1 (en) | 1994-08-09 | 1996-02-22 | Micron Optics, Inc. | Temperature compensated fiber fabry-perot filters |
CA2155448A1 (en) | 1994-08-11 | 1996-02-12 | Katerina Leftheris | Inhibitors of farnesyl protein transferase |
DE69514367T2 (de) | 1994-08-11 | 2000-07-27 | Banyu Pharma Co Ltd | Substituierte amidderivate |
WO1996005169A1 (fr) | 1994-08-12 | 1996-02-22 | Banyu Pharmaceutical Co., Ltd. | Derive d'acide amique n,n-bisubstitue |
DE4429506B4 (de) | 1994-08-19 | 2007-09-13 | Degussa Gmbh | Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe |
DE4429653C2 (de) | 1994-08-20 | 1997-04-03 | Anton Dr More | Konverter und Verfahren zum Frischen von Metallschmelzen insbesondere von Roheisen zu Stahl |
EP0740853B1 (en) | 1994-11-22 | 1999-01-13 | Koninklijke Philips Electronics N.V. | Semiconductor device with a carrier body on which a substrate with a semiconductor element is fastened by means of a glue layer and on which a pattern of conductor tracks is fastened |
JPH10510261A (ja) | 1994-12-09 | 1998-10-06 | ワーナー−ランバート・カンパニー | タンパク質:ファルネシルトランスフェラーゼの置換テトラーおよびペンタペプチド阻害剤 |
WO1996021701A2 (en) | 1995-01-09 | 1996-07-18 | Magla International Ltd. | Wear resistant image printing on latex surfaces |
EP0794789A4 (en) | 1995-01-12 | 1999-05-26 | Univ Pittsburgh | PRENYL TRANSFERASE INHIBITORS |
FR2729390A1 (fr) | 1995-01-18 | 1996-07-19 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
FR2730491B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
FR2730492B1 (fr) | 1995-02-09 | 1997-03-14 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
US5633272A (en) | 1995-02-13 | 1997-05-27 | Talley; John J. | Substituted isoxazoles for the treatment of inflammation |
US5700806A (en) | 1995-03-24 | 1997-12-23 | Schering Corporation | Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
US5684013A (en) | 1995-03-24 | 1997-11-04 | Schering Corporation | Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases |
IL117580A0 (en) | 1995-03-29 | 1996-07-23 | Merck & Co Inc | Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them |
IL117798A (en) | 1995-04-07 | 2001-11-25 | Schering Plough Corp | Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them |
US5712280A (en) | 1995-04-07 | 1998-01-27 | Schering Corporation | Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases |
CA2217351C (en) | 1995-04-07 | 2003-03-18 | Schering Corporation | Carbonyl-piperazinyl and piperidinyl compounds which inhibit farnesyl protein transferase |
US5891872A (en) | 1995-04-07 | 1999-04-06 | Schering Corporation | Tricyclic compounds |
US5831115A (en) | 1995-04-21 | 1998-11-03 | Abbott Laboratories | Inhibitors of squalene synthase and protein farnesyltransferase |
IL118101A0 (en) | 1995-05-03 | 1996-09-12 | Abbott Lab | Inhibitors of farnesyltransferase |
US5919780A (en) | 1995-06-16 | 1999-07-06 | Warner Lambert Company | Tricyclic inhibitors of protein farnesyltransferase |
FR2736641B1 (fr) | 1995-07-10 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
AT402617B (de) | 1995-07-11 | 1997-07-25 | Datacon Schweitzer & Zeindl Gm | Anlage zum automatisierten, hermetischen anlage zum automatisierten, hermetischen verschliessen von gehäusen verschliessen von gehäusen |
FR2736638B1 (fr) | 1995-07-12 | 1997-08-22 | Rhone Poulenc Rorer Sa | Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent |
CH690163A5 (fr) | 1995-07-28 | 2000-05-31 | Symphar Sa | Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers. |
US6020343A (en) | 1995-10-13 | 2000-02-01 | Merck Frosst Canada, Inc. | (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors |
WO1997017070A1 (en) | 1995-11-06 | 1997-05-15 | University Of Pittsburgh | Inhibitors of protein isoprenyl transferases |
DK1186606T4 (da) | 1995-11-17 | 2011-12-05 | Biotechnolog Forschung Gmbh | Epothilonderivater, deres fremstilling og anvendelse |
AU704139B2 (en) | 1995-11-22 | 1999-04-15 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
WO1997021701A1 (en) | 1995-12-08 | 1997-06-19 | Janssen Pharmaceutica N.V. | Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives |
ES2248826T3 (es) | 1995-12-22 | 2006-03-16 | Schering Corporation | Amidas triciclicas utiles para la inhibicion de la funcion de la proteina g y para el tratamiento de enfermedades proliferativas. |
AU1529997A (en) | 1996-01-16 | 1997-08-11 | Warner-Lambert Company | Substituted histidine inhibitors of protein farnesyltransferase |
US6673927B2 (en) | 1996-02-16 | 2004-01-06 | Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. | Farnesyl transferase inhibitors |
EP0944388A4 (en) | 1996-04-03 | 2001-08-16 | Merck & Co Inc | INHIBITORS OF FARNESYL PROTEIN TRANSFERASE |
EP0892791B1 (en) | 1996-04-12 | 2003-03-05 | G.D. Searle & Co. | N-[[4-(5-METHYL-3-PHENYLISOXAZOL-4-YL]PHENYL]SULFONYLPROPYLAMIDE and its SODIUMSALT AS PRODRUGS OF COX-2 INHIBITORS |
EA199801031A1 (ru) | 1996-05-22 | 1999-06-24 | Варнер-Ламберт Компани | Ингибиторы протеинфарнезилтрансферазы |
JP2000514456A (ja) | 1996-07-15 | 2000-10-31 | ブリストル―マイヤーズ・スクイブ・カンパニー | ファルネシルプロテイントランスフェラーゼのチアジオキソベンゾジアゼピン阻害剤 |
US5861419A (en) | 1996-07-18 | 1999-01-19 | Merck Frosst Canad, Inc. | Substituted pyridines as selective cyclooxygenase-2 inhibitors |
CA2273083C (en) | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
AU5719598A (en) | 1996-12-30 | 1998-07-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
JP2002511054A (ja) | 1996-12-30 | 2002-04-09 | メルク エンド カンパニー インコーポレーテッド | ファルネシル蛋白トランスフェラーゼ阻害薬 |
WO2000044777A1 (en) | 1999-01-29 | 2000-08-03 | Imclone Systems Incorporated | Antibodies specific to kdr and uses thereof |
GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
AU4972900A (en) | 1999-04-08 | 2000-11-14 | Arch Development Corporation | Use of anti-vegf antibody to enhance radiation in cancer therapy |
US6545004B1 (en) | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
AU774748B2 (en) | 1999-10-27 | 2004-07-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
WO2001055155A1 (fr) | 2000-01-26 | 2001-08-02 | Meiji Seika Kaisha, Ltd. | Nouveaux derives de carbapenem de type sel quaternaire |
WO2001055115A1 (en) * | 2000-01-27 | 2001-08-02 | Cytovia, Inc. | Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof |
MXPA03008560A (es) * | 2001-03-22 | 2004-06-30 | Abbot Gmbh & Co Kg | Pirazolopirimidinas como agentes terapeuticos. |
US20040106540A1 (en) | 2001-04-10 | 2004-06-03 | Barnett Stanley F | Method of treating cancer |
WO2002083139A1 (en) | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
US6958334B2 (en) | 2001-04-10 | 2005-10-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
AU2002252614B2 (en) | 2001-04-10 | 2006-09-14 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
WO2003013526A1 (en) | 2001-08-08 | 2003-02-20 | Merck & Co. Inc. | Anticoagulant compounds |
WO2003039460A2 (en) | 2001-11-07 | 2003-05-15 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
WO2003049679A2 (en) | 2001-12-06 | 2003-06-19 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
US7244723B2 (en) | 2001-12-06 | 2007-07-17 | Merck & Co., Inc. | Substituted furopyrimidinones as a mitotic kinesin inhibitors |
ATE372341T1 (de) | 2001-12-06 | 2007-09-15 | Merck & Co Inc | Inhibitoren von mitotischem kinesin |
JP4464136B2 (ja) | 2001-12-06 | 2010-05-19 | メルク・シャープ・エンド・ドーム・コーポレイション | 有糸分裂キネシン阻害薬 |
DE60231439D1 (de) | 2001-12-06 | 2009-04-16 | Merck & Co Inc | Mitotische kinesinhemmer |
GB0209715D0 (en) * | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
TW200424174A (en) * | 2003-02-06 | 2004-11-16 | Hoffmann La Roche | New TP diamide |
CN1747933A (zh) * | 2003-02-06 | 2006-03-15 | 霍夫曼-拉罗奇有限公司 | 新单乙酰代邻-苯二胺类衍生物 |
WO2005028467A1 (en) | 2003-09-15 | 2005-03-31 | Anadys Pharmaceuticals, Inc. | Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds |
KR100557093B1 (ko) * | 2003-10-07 | 2006-03-03 | 한미약품 주식회사 | 다약제 내성 저해 활성을 갖는 테트라졸 유도체 및 그의제조방법 |
PE20050444A1 (es) * | 2003-10-31 | 2005-08-09 | Takeda Pharmaceutical | Compuestos de piridina como inhibidores de la peptidasa |
JP4473698B2 (ja) * | 2003-10-31 | 2010-06-02 | 武田薬品工業株式会社 | ピリジン化合物 |
JP2007513184A (ja) | 2003-12-04 | 2007-05-24 | 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キノキサリン |
US20060004197A1 (en) | 2004-07-02 | 2006-01-05 | Thomas Thrash | Sulfonamide-based compounds as protein tyrosine kinase inhibitors |
JP2008519850A (ja) * | 2004-11-10 | 2008-06-12 | シンタ ファーマシューティカルズ コーポレーション | Il−12調節化合物 |
CR9465A (es) * | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
US20070037865A1 (en) * | 2005-08-04 | 2007-02-15 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
DE102005048824A1 (de) * | 2005-10-10 | 2007-04-12 | Bayer Healthcare Ag | Behandlung und Prophylaxe von Mikroangiopathien |
GB0520657D0 (en) * | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
TWI372752B (en) * | 2005-12-22 | 2012-09-21 | Nihon Nohyaku Co Ltd | Pyrazinecarboxamide derivatives and plant disease controlling agents containing the same |
EP1973885A1 (en) * | 2005-12-22 | 2008-10-01 | Crystalgenomics, Inc. | Aminopyrimidine derivatives inhibiting protein kinase activity, method for the preparation thereof and pharmaceutical composition containing same |
CN101466686A (zh) * | 2006-04-20 | 2009-06-24 | 詹森药业有限公司 | C-fms激酶抑制剂 |
KR20140008295A (ko) * | 2010-08-26 | 2014-01-21 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 돌연변이 델타-9 연장효소 및 다중불포화 지방산의 제조에서의 그들의 용도 |
UY33930A (es) * | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
-
2008
- 2008-03-03 AU AU2008221263A patent/AU2008221263B2/en active Active
- 2008-03-03 CN CN200880011679.7A patent/CN101679266B/zh active Active
- 2008-03-03 US US12/449,701 patent/US8822497B2/en active Active
- 2008-03-03 ES ES08731299T patent/ES2431163T3/es active Active
- 2008-03-03 BR BRPI0808523-4A patent/BRPI0808523A2/pt not_active Application Discontinuation
- 2008-03-03 MX MX2009009304A patent/MX2009009304A/es active IP Right Grant
- 2008-03-03 WO PCT/US2008/055724 patent/WO2008106692A1/en active Application Filing
- 2008-03-03 CA CA2679659A patent/CA2679659C/en active Active
- 2008-03-03 EP EP08731299.7A patent/EP2132177B1/en active Active
- 2008-03-03 EA EA200901144A patent/EA019951B1/ru not_active IP Right Cessation
- 2008-03-03 JP JP2009551895A patent/JP5330274B2/ja active Active
- 2008-03-03 KR KR1020097020450A patent/KR101514853B1/ko active IP Right Grant
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP2010520228A5 (ja) | ||
JP2018502909A5 (ja) | ||
RU2011106794A (ru) | Способы экстракции и очистки промежуточного продукта получения сукралозы | |
CN103145698A (zh) | 一种利伐沙班中间体的制备方法及利伐沙班的新合成方法 | |
EP2697209A1 (en) | Method for the preparation of substituted oxazolidinones | |
JP6248202B2 (ja) | シロドシン及びその中間体の製造方法 | |
KR101744046B1 (ko) | 실로도신 합성에 유용한 중간체의 제조방법 | |
KR102078158B1 (ko) | 에제티미브의 제조방법 및 그 중간체 | |
CN103450065B (zh) | 制备依泽替米贝的方法 | |
JP5017101B2 (ja) | 不斉四置換炭素原子含有化合物の製法 | |
MX2008000821A (es) | Nuevos derivados de piperidina. | |
JP2009256298A (ja) | ピペリジン−3−イルカーバメート化合物の光学分割方法およびその中間体 | |
JP7373241B2 (ja) | ピリミジニルビピリジン化合物の製造方法及びそのための中間体 | |
KR101698124B1 (ko) | 3-(메틸아미노)-3-((r)-피롤리딘-3-일)프로판니트릴 또는 이의 염의 제조방법 | |
TW200613283A (en) | 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one | |
Ha et al. | A Novel synthetic method for Bepotastine, a histamine H1 receptor antagonist | |
RU2011153767A (ru) | Способ получения флупиртина | |
CN107474008A (zh) | 一种α‑甲酰基四氢吡啶类化合物的合成方法 | |
JP2014193873A (ja) | ビフェニル−2−イルカルバミン酸エステルの調製方法 | |
JPWO2014069351A1 (ja) | 光学活性二環式ウレア化合物の製造方法 | |
CN102898289B (zh) | 一种医药中间体 2-(4-苯甲氧基苯基)乙醇的合成方法 | |
CN104672132B (zh) | 阿加曲班中间体的合成方法 | |
WO2013011999A1 (ja) | 光学活性2-メチルプロリン誘導体の製造法 | |
CN102060746B (zh) | 3-(取代二氢异吲哚酮-2-基)-2,6-哌啶二酮的合成方法及其中间体 | |
KR101303813B1 (ko) | 라세믹 오메프라졸로부터 에스오메프라졸의 개선된제조방법 |