公开(公告)号：US10526363B2

公开(公告)日：2020-01-07

申请号：US15503776

申请日：2015-08-14

Applicant: Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited ,  John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

Inventor： John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

IPC: C07H19/10 ,  C07F9/58 ,  C07H19/06 ,  C07F9/24 ,  C07F9/6558

Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.

公开(公告)号：US20160122350A1

公开(公告)日：2016-05-05

申请号：US14897290

申请日：2014-06-05

Applicant: Steven P. MILLER ,  John LIMANTO ,  Yong-Li ZHONG ,  Nobuyoshi YASUDA ,  Zhijian LIU ,  MERCK SHARP & DOHME CORP.

Inventor： Steven P. Miller ,  John Limanto ,  Yong-Li Zhong ,  Nobuyoshi Yasuda ,  Zhijian Liu

IPC: C07D471/08 ,  C07D401/12

CPC classification number: C07D471/08 ,  C07D211/62 ,  C07D401/12 ,  C07D491/08 ,  Y02P20/55

Abstract: A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R4—SO2W (II-Su) in the presence of tertiary amine base, wherein PG1 and PG2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R2, R3, R4, R5, R6, R7, R8, and R9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

Abstract translation: 制备式（III）的N-保护的6-（哌啶-4-基氨基甲酰基）哌啶-3-基磺酸盐的方法：其包括使式（II）的内酯与式（II-Am）的氮杂环烷基胺 ）：然后在叔胺碱存在下与式（II-Su）的磺酰卤接触：R4-SO2W（II-Su），其中PG1和PG2是胺保护基; k，p和q分别为0,1或2，W，R2，R3，R4，R5，R6，R7，R8和R9如本文所定义。 另外的实施方案添加了一系列方法步骤，导致合成适合用作β-内酰胺酶抑制剂的7-氧代-1,6-二氮杂双环[3.2.1]辛烷。

公开(公告)号：US20090105479A1

公开(公告)日：2009-04-23

申请号：US12083931

申请日：2006-10-24

Applicant: Mark Cameron ,  Frederick W. Hartner ,  Lushi Tan ,  Nobuyoshi Yasuda ,  Naoki Yoshikawa

Inventor： Mark Cameron ,  Frederick W. Hartner ,  Lushi Tan ,  Nobuyoshi Yasuda ,  Naoki Yoshikawa

IPC: C07D471/04 ,  C07C69/75 ,  C07C25/28

CPC classification number: C07D471/04

Abstract: The invention is directed to a compound of the structural formula (22) (22) crystal form of structural formulae (21) and its free acid, pharmaceutical compositions comprising these compounds and methods of preparing and using these compounds.

Abstract translation: 本发明涉及结构式（22）（22）结构式（21）的结晶形式及其游离酸的化合物，包含这些化合物的药物组合物以及制备和使用这些化合物的方法。

公开(公告)号：US20070112030A1

公开(公告)日：2007-05-17

申请号：US10578476

申请日：2004-11-03

Applicant: Frederick Hartner ,  Lushi Tan ,  Nobuyoshi Yasuda ,  Naoki Yoshikawa

Inventor： Frederick Hartner ,  Lushi Tan ,  Nobuyoshi Yasuda ,  Naoki Yoshikawa

IPC: A61K31/445 ,  C07D211/06 ,  C07D207/00 ,  A61K31/40 ,  A61K31/198

CPC classification number: C07D303/00 ,  C07C229/50 ,  C07C2602/18 ,  C07D303/04 ,  C07D317/72

Abstract: Processes for the preparation of certain [3.1.0]hexane derivatives which are useful as mGluR agonists, and intermediates prepared during such processes.

Abstract translation: 用于制备可用作mGluR激动剂的某些[3.1.0]己烷衍生物的方法，以及在此过程中制备的中间体。

公开(公告)号：US6162911A

公开(公告)日：2000-12-19

申请号：US133201

申请日：1998-08-13

Applicant: Richard G. Ball ,  Nancy N. Tsou ,  James A. Mc Cauley ,  Chunhua Yang ,  Nobuyoshi Yasuda

Inventor： Richard G. Ball ,  Nancy N. Tsou ,  James A. Mc Cauley ,  Chunhua Yang ,  Nobuyoshi Yasuda

IPC: C07D205/08

CPC classification number: C07D205/08

Abstract: Novel crystalline carbapenem intermediate compounds of formula I: ##STR1## wherein: R.sub.1 represents CH.sub.3 or H and an efficient process for synthesis thereof are described.

Abstract translation: 式I的新型结晶碳青霉烯中间体化合物：其中：R1表示CH3或H，并描述了其有效的合成方法。

公开(公告)号：US5618934A

公开(公告)日：1997-04-08

申请号：US387307

申请日：1995-02-27

Applicant: Ann E. DeCamp ,  Edward J. J. Grabowski ,  Mark A. Huffman ,  Lyndon C. Xavier ,  Nobuyoshi Yasuda ,  Guo-Jie Ho ,  David J. Mathre

Inventor： Ann E. DeCamp ,  Edward J. J. Grabowski ,  Mark A. Huffman ,  Lyndon C. Xavier ,  Nobuyoshi Yasuda ,  Guo-Jie Ho ,  David J. Mathre

IPC: C07D477/02 ,  C07F7/18 ,  C07F5/02

CPC classification number: C07F7/1892 ,  C07D477/02

Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.

Abstract translation: 本发明涉及由结构式表示的化合物：其中Z代表带负电荷的抗衡离子。

公开(公告)号：US5442057A

公开(公告)日：1995-08-15

申请号：US226788

申请日：1994-04-12

Applicant: Ann Decamp ,  Ulf H. Dolling ,  Yulan Li ,  Dale L. Rieger ,  Nobuyoshi Yasuda ,  Lyndon C. Xavier

Inventor： Ann Decamp ,  Ulf H. Dolling ,  Yulan Li ,  Dale L. Rieger ,  Nobuyoshi Yasuda ,  Lyndon C. Xavier

IPC: C07D487/04 ,  B01J31/28 ,  C07B61/00 ,  C07D477/02 ,  C07D477/14 ,  C07F5/02 ,  C07F7/18 ,  C07D487/00

CPC classification number: C07D477/14 ,  C07D477/02 ,  C07F5/025 ,  C07F7/1852 ,  C07F7/1856

Abstract: The present invention is directed to a process of making 2-Aryl Carbapenems of Formula 1 from a compound of formula 2. ##STR1##

Abstract translation: 本发明涉及由式2的化合物制备式1的2-芳基碳原子的方法。＆lt; IMAGE＆gt; + TR＆lt; IMAGE＆gt;

公开(公告)号：US5434152A

公开(公告)日：1995-07-18

申请号：US148476

申请日：1993-11-08

Applicant: Mark A. Huffman ,  Nobuyoshi Yasuda ,  Ann E. DeCamp ,  Edward J. J. Grabowski

Inventor： Mark A. Huffman ,  Nobuyoshi Yasuda ,  Ann E. DeCamp ,  Edward J. J. Grabowski

IPC: C07D239/80 ,  C07D401/06 ,  A61K31/535 ,  A61K31/505 ,  C07D265/14 ,  C07D265/24

CPC classification number: C07D401/06 ,  C07D239/80 ,  Y02P20/55

Abstract: An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone comprises the chiral addition of 2-pyridylacetylide to N.sup.1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.

Abstract translation: （S） - （ - ） - 6-氯-4-环丙基-3,4-二氢-4 - [（2-吡啶基）乙炔基] -2（1H） - 喹唑啉酮的不对称合成包括手性添加2- 吡啶基乙酰基至N-保护的6-氯-4-环丙基-2-喹唑啉酮，随后除去保护基。

公开(公告)号：US4871730A

公开(公告)日：1989-10-03

申请号：US931978

申请日：1986-11-24

Applicant: Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

Inventor： Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D213/32 ,  C07D501/18 ,  C07D501/22 ,  C07D501/59

CPC classification number: C07D213/32

Abstract: A cephem compound of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or protected amino, R.sup.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, carboxy(lower) alkyl, protected carboxy(lower) alkyl, cyclo(lower) alkyl or cyclo (lower)alkenyl, and Z is CH or N;R.sup.2 is hydrogen, phenyl, pyridyl which may have a lower alkyl group, or cyano; andR.sup.3 is carboxy or protected carboxy; and pharmaceutically acceptable salt thereof.

Abstract translation: 其中R 1是下式的基团：其中R 5是氨基或保护的氨基，R 6是氢，低级烷基，低级烯基，低级炔基，羧基（低级）烷基， 保护的羧基（低级）烷基，环（低级）烷基或环（低级）烯基，Z是CH或N; R2是氢，苯基，可具有低级烷基的吡啶基或氰基; 并且R 3是羧基或被保护的羧基; 及其药学上可接受的盐。

公开(公告)号：US4622318A

公开(公告)日：1986-11-11

申请号：US662604

申请日：1984-10-19

Applicant: Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

Inventor： Takao Takaya ,  Zenzaburo Tozuka ,  Nobuyoshi Yasuda ,  Kohji Kawabata

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D213/32 ,  C07D501/18 ,  C07D501/22 ,  C07D501/24 ,  C07D501/36

CPC classification number: C07D213/32 ,  C07C321/00

Abstract: The invention relates to new cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or a group of the formula: ##STR2## in which R.sup.5 is amino or a protected amino group,R.sup.9 is lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkenyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or saturated 4 to 8-membered heteromonocyclic group containing one sulfur atom, andZ is N or CH,R.sup.2 is cyano, phenyl, pyridyl, lower alkylpyridyl, or tri(lower)alkylsilyl,R.sup.3 is carboxy or protected carboxy, andA is --CH.dbd.CH-- or --C.tbd.C--,and pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及具有下式的高抗微生物活性的新的头孢烯化合物：其中R 1是氨基或下式的基团：其中R 5是氨基或保护的氨基，R 9是低级烷基，低级链烯基 ，低级炔基，环（低级）烯基，羧基（低级）烷基，受保护的羧基（低级）烷基或含有一个硫原子的饱和4至8元杂单环基团，Z为N或CH，R 2为氰基，苯基，吡啶基 ，低级烷基吡啶基或三（低级）烷基甲硅烷基，R3是羧基或被保护的羧基，A是-CH = CH-或-C3BON-，及其药学上可接受的盐。