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1. 发明专利

JP2014169312A Tetrahydroisoquinoline production method 审中-公开
标题翻译：四氢喹啉生产方法
公开(公告)号：JP2014169312A
公开(公告)日：2014-09-18
申请号：JP2014100580
申请日：2014-05-14
申请人： Bristol Myers Squibb Co , ブリストル−マイヤーズスクイブカンパニーBristol−Myers Squibb Company , Albany Molecular Res Inc , オールバニー・モレキュラー・リサーチ・インコーポレイテッドAlbany Molecular Research, Inc.
发明人： PAUL LOBBEN , ZHAO RULIN , WANG BEI , CHEN BANG-CHI , SHUANG LIU , HU MIN , YANG YUH-LIN ALLEN , MATTHEW ISHERWOOD , RASIDUL AMIN , CUI WENGE
IPC分类号： C07C225/06 , C07C215/30 , C07D217/04 , C07F5/04
CPC分类号： C07F5/04 , C07C215/20 , C07C217/58 , C07C223/02 , C07D217/04 , C07D237/20 , C07D401/04 , C07D413/10 , C07F5/022 , C07F5/025
摘要： PROBLEM TO BE SOLVED: To provide intermediates useful in producing tetrahydroisoquinolines, particularly 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine useful in the treatment of depression and other conditions.SOLUTION: Intermediates useful in producing tetrahydroisoquinolines are compounds represented by the specified formula (4R), where R1 is Br and H3CO.
摘要翻译：要解决的问题：提供可用于制备四氢异喹啉的中间体，特别是6 - [（4S）-2-甲基-4-（萘基）-1,2,3,4-四氢异喹啉-7-基]哒嗪-3-胺可用于治疗抑郁症和其他病症。解决方案：用于制备四氢异喹啉的中间体是指定式（4R）表示的化合物，其中R1是Br和H3CO。

2. 发明专利

JP2012188446A Process for preparing 2-aminothiazole-5-aromatic carboxamide as kinase inhibitor 审中-公开
标题翻译：制备2-氨基-5-苯甲酰胺作为激酶抑制剂的方法
公开(公告)号：JP2012188446A
公开(公告)日：2012-10-04
申请号：JP2012129253
申请日：2012-06-06
申请人： Bristol Myers Squibb Co , ブリストル−マイヤーズスクイブカンパニーBristol−Myers Squibb Company
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
IPC分类号： C07D417/12 , A61K31/506 , A61P35/00 , A61P35/02 , C07C235/28 , C07C237/42 , C07D277/56 , C07D417/14
CPC分类号： C07D417/12 , C07C235/28 , C07C237/42
摘要： PROBLEM TO BE SOLVED: To provide: a compound useful as kinase inhibitors, particularly inhibitors of protein tyrosine kinase and p38 kinase; crystalline forms thereof; and a process for preparing the same.SOLUTION: A crystalline monohydrate of the compound of formula (IV) is provided. The preparation process includes heating and dissolving the compound of formula (IV) in an ethanol/water mixture, followed by cooling, to crystallize the monohydrate out of the ethanol/water mixture. Also, the crystalline butanol solvate and the crystalline ethanol solvate of the compound of formula (IV) are provided.
摘要翻译：待解决的问题：提供：可用作激酶抑制剂的化合物，特别是蛋白酪氨酸激酶和p38激酶的抑制剂; 其结晶形式; 及其制备方法。解决方案：提供式（IV）化合物的结晶一水合物。制备方法包括将式（IV）化合物加热溶解在乙醇/水混合物中，然后冷却，使一水合物从乙醇/水混合物中结晶出来。此外，提供式（IV）化合物的结晶丁醇溶剂合物和结晶乙醇溶剂化物。版权所有（C）2013，JPO＆INPIT

3. 发明专利

JP2005139197A METHOD FOR PRODUCING 2',3'-DIDEHYDRO-3'-DEOXYTHYMIDINE (d4T) BY USING 5-METHYLURIDINE 审中-公开
标题翻译：通过使用5-甲基嘌呤制备2'，3'-二脱氢-3'-脱氧谷氨酸（d4T）的方法
公开(公告)号：JP2005139197A
公开(公告)日：2005-06-02
申请号：JP2004373339
申请日：2004-12-24
申请人： Bristol Myers Squibb Co , ブリストル−マイヤーズスクイブカンパニーBristol−Myers Squibb Company
发明人： CHEN BANG-CHI , STARK DERRON R , BAKER STEPHEN R , QUINLAN SANDRA L
IPC分类号： C07D405/04 , A61K31/505 , A61K31/513 , A61P31/12 , A61P31/18 , C07H19/06
CPC分类号： C07H19/06
摘要： PROBLEM TO BE SOLVED: To provide a method for purifying 2',3'-didehydro-3'-deoxythymidine (d4T) used as an anti-HIV (human immunodeficiency virus) pharmaceutical.
SOLUTION: This method for purifying the d4T comprises (a) reacting 5-metyluridine expressed by formula X with mesyl chloride in the presence of an organic base having a pKa value of 5.5 to 8.0, to mesylate hydroxy groups at the 2', 3', and 5' positions, and treating the mesylated compound with a hydroxide to synthesize 2,2'-anhydro-compound VIII, (b) substituting the 5'-mesyl group of the compound VIII with a benzoate anion, then hydrobrominating the substituted compound VIII, to synthesize 5'-benzoyl-2'-bromo-compound VI, and further subjecting the compound VI to reductive elimination reaction in the presence of a reduction metal, to form d4T 5'-benzoate III, (c) treating the compound III with butylamine and further treating the treated compound III with N-methylpyrrolidine and butyl acetate, to obtain d4T-NMPO solvate II, and (d) heating the d4T-NMPO solvate II in an alcoholic medium, to decompose the solvate II.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供用作抗HIV（人类免疫缺陷病毒）药物的2'，3'-二脱氢-3'-脱氧胸苷（d4T）的纯化方法。解决方案：这种纯化d4T的方法包括：（a）在pKa值为5.5-8.0的有机碱存在下，使式X表示的5-甲基尿嘧啶与甲磺酰氯反应，在2' ，3'和5'位，并用氢氧化物处理甲磺酰化的化合物以合成2,2'-脱水化合物VIII，（b）用苯甲酸根阴离子取代化合物VIII的5'-甲磺酰基，然后加入氢溴酸取代的化合物VIII，合成5'-苯甲酰基-2'-溴化合物VI，并在还原金属存在下进一步对化合物VI进行还原消除反应，形成d4T5-苯甲酸酯III，（c）用丁胺处理化合物III，并用N-甲基吡咯烷和乙酸丁酯进一步处理经处理的化合物III，得到d4T-NMPO溶剂合物II，和（d）在醇介质中加热d4T-NMPO溶剂化物II，分解溶剂化物II 。版权所有（C）2005，JPO＆NCIPI

4. 发明申请

WO2009149259A2 PROCESSES FOR PREPARING TETRAHYDROISOQUINOLINES 审中-公开
标题翻译：制备四氢喹啉的方法
公开(公告)号：WO2009149259A2
公开(公告)日：2009-12-10
申请号：PCT/US2009046259
申请日：2009-06-04
申请人： SQUIBB BRISTOL MYERS CO , ALBANY MOLECULAR RES INC , LOBBEN PAUL , ZHAO RULIN , WANG BEI , CHEN BANG-CHI , LIU SHUANG , HU MIN , YANG YUH-LIN ALLEN , ISHERWOOD MATTHEW , AMIN RASIDUL , CUI WENGE
发明人： LOBBEN PAUL , ZHAO RULIN , WANG BEI , CHEN BANG-CHI , LIU SHUANG , HU MIN , YANG YUH-LIN ALLEN , ISHERWOOD MATTHEW , AMIN RASIDUL , CUI WENGE
IPC分类号： C07D401/04
CPC分类号： C07F5/04 , C07C215/20 , C07C217/58 , C07C223/02 , C07D217/04 , C07D237/20 , C07D401/04 , C07D413/10 , C07F5/022 , C07F5/025
摘要： Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.
摘要翻译：公开了制备四氢异喹啉的方法，可用于制备四氢异喹啉的中间体，制备该中间体的方法和6 - [（4S）-2-甲基-4-（萘基）-1,2,3,4 -tetrahydroisoquinolin -7-基]哒嗪-3-胺。还公开了包含四氢异喹啉的药物组合物，使用四氢异喹啉处理抑郁症和其它病症的方法以及获得结晶形式的方法。

5. 发明专利

CA2555291C PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 未知
公开(公告)号：CA2555291C
公开(公告)日：2017-01-17
申请号：CA2555291
申请日：2005-02-04
申请人： BRISTOL MYERS SQUIBB CO
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
IPC分类号： C07D277/56 , A61P31/04 , A61P31/12 , C07C235/28 , C07C237/42 , C07D239/00 , C07D241/00 , C07D277/00 , C07D417/12 , C07D417/14
摘要： The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

7. 发明专利

RS20050789A ARIL-SUPSTITUISANA JEDINJENJA PIRAZOL-AMIDA POGODNA ZA PRIMENU KAO INHIBITORI KINAZE 未知
公开(公告)号：RS20050789A
公开(公告)日：2008-04-04
申请号：YUP20050789
申请日：2004-05-03
申请人： BRISTOL MYERS SQUIBB CO
发明人： DYCKMAN ALARIC , WROBLESKI STEPHEN , DAS JAGABANDHU , LEFTHERIS KATERINA , LIU CHUNJIAN , ZHAO RULIN , CHEN BANG-CHI
IPC分类号： C07D231/18 , A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14
摘要： Ovaj pronalazak se odnosi na jedinjenja koja imaju formulu (I), kao i na njihove farmaceutski prihvatljive soli, prolekove, solvate, izomere i/ili hidrate, gde je Q izborno supstituisani fenil, piridil, piridazinil, pirimidinil ili pirazinil prsten; R2 je alkil ili amino grupa, kao što su ovde definisane; a Z je izborno supstituisani oksadiazolil ili -C(=O)NR6, gde je R6 niži alkil ili ciklopropil. Jedinjenja su neočekivano pogodna za pripremanje lekova za lečenje stanja povezanih sa p38 kinazom i/ili pripremanje lekova za primenu u lečenju zapaljenskih poremećaja ili stanja kod pacijenta.

8. 发明专利

GEP20074236B ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 未知
公开(公告)号：GEP20074236B
公开(公告)日：2007-11-12
申请号：GEAP2004009086
申请日：2004-05-03
申请人： BRISTOL MYERS SQUIBB CO
发明人： DYCKMAN ALARIC , LIU CHUNJIAN , LEFTHERIS KATERINA , DAS JAGABANDHU , ZHAO RULIN , CHEN BANG-CHI , WROBLESKI STEPHEN T
IPC分类号： C07D231/18 , A61K20060101 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/535 , A61K31/675 , C07D20060101 , C07D231/04 , C07D231/14 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D413/14
摘要： The compounds of the formula (I) wherein values of Q, R2, Z are provided in the description, pharmaceutically-acceptable salts the¬reof, prodrugs, solvates, isomers, and/or hydrates thereof. Said compounds are useful in preparing medicaments for treating p38 kinase related conditions.

9. 发明专利

NO20071702L 未知
公开(公告)号：NO20071702L
公开(公告)日：2007-05-25
申请号：NO20071702
申请日：2007-03-30
申请人： BRISTOL MYERS SQUIBB CO
发明人： CHEN BANG-CHI , MUDRYK BOGUSLAW M , CUNIERE NICOLAS , ROSSANO LUCIUS , ZHANG HUIPING , SHAPIRO RAFAEL , OBERHOLZER MATTHEW
IPC分类号： C07D471/04
摘要： A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.

10. 发明专利

NO20071653L 未知
公开(公告)号：NO20071653L
公开(公告)日：2007-03-30
申请号：NO20071653
申请日：2007-03-28
申请人： BRISTOL MYERS SQUIBB CO
发明人： CHEN BANG-CHI , MALLEY MARY F , ZHANG HUIPING , GLEESON MARGARET M , MCGEORGE GARY
IPC分类号： C07D471/04
摘要： The instant invention provides crystalline forms of 1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1 (2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.

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