公开(公告)号：US5342953A

公开(公告)日：1994-08-30

申请号：US648117

申请日：1991-01-31

Applicant: Gary F. Cooper ,  Keith E. McCarthy

Inventor： Gary F. Cooper ,  Keith E. McCarthy

IPC: A61K31/435 ,  A61K31/4365 ,  A61P7/02 ,  C07D291/04 ,  C07D495/04 ,  C07D241/04

CPC classification number: C07D291/04 ,  C07D495/04

Abstract: Compounds of the formula: ##STR1## wherein: A is oxo or dioxo;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo;are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.

Abstract translation: 下式的化合物：其中：A是氧代或二氧代; R1，R2和R3独立地是氢或1-6个碳原子的低级烷基; R4，R5，R6和R7独立地为氢，1-6个碳原子的低级烷基，烷氧基，酰基或卤素; 有利地转化为噻吩并[3,2-c]吡啶衍生物及其药学上可接受的盐，特别是噻氯匹定盐酸盐。

公开(公告)号：US5130432A

公开(公告)日：1992-07-14

申请号：US633636

申请日：1990-12-21

Applicant: Gary F. Cooper ,  Michael G. Martin

Inventor： Gary F. Cooper ,  Michael G. Martin

IPC: C07D207/08 ,  C07D515/04

CPC classification number: C07D207/08 ,  C07D515/04

Abstract: A process for preparing a cyclic amine of Formula I ##STR1## in which R.sup.1 is phenyl, optionally substituted by 1 to 3 lower alkoxy groups;R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl; andn is 1 or 2,comprises(1) converting an aminoalcohol of Formula III ##STR2## to a dioxooxathiazolidine of Formula II ##STR3## in which R.sup.2, R.sup.3, R.sup.4 and n are as defined above; and (2) reacting the dioxooxathiazolidine of Formula II with an organometallic nucleophile, R.sup.1 M*, wherein R.sup.1 is as defined above, and hydrolyzing the resulting sulfamate salt.

Abstract translation: 制备式I的环胺的方法（I）其中R 1是苯基，任选被1至3个低级烷氧基取代; R2，R3和R4独立地是氢或低级烷基; 并且n为1或2，包括（1）将式III的氨基醇（III）转化为式II的二氧代氧代噻唑烷（II），其中R 2，R 3，R 4和n如上所定义; 和（2）使式II的二氧代氧杂噻唑烷与有机金属亲核试剂R1M *反应，其中R 1如上定义，并水解所得的氨基磺酸盐。

公开(公告)号：US4929740A

公开(公告)日：1990-05-29

申请号：US217241

申请日：1988-07-11

Applicant: Gary F. Cooper

Inventor： Gary F. Cooper

IPC: C07C405/00 ,  C07F7/18

CPC classification number: C07C405/0025 ,  C07F7/1856

Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or an ether-forming group and X is hydrogen, halo, trifluoromethyl, lower alkyl, or lower akoxy, are useful intermediates for making PGE and PGF derivatives having an allenic function.

Abstract translation: 其中R1和R2是氢或醚形成基团，X是氢，卤素，三氟甲基，低级烷基或低级烷氧基的式“IMAGE”的化合物是制备具有富集功能的PGE和PGF衍生物的有用中间体。

公开(公告)号：US5248788A

公开(公告)日：1993-09-28

申请号：US467083

申请日：1990-01-18

Applicant: Gary F. Cooper ,  Colin C. Beard ,  David Y. Jackson ,  Douglas L. Wren

Inventor： Gary F. Cooper ,  Colin C. Beard ,  David Y. Jackson ,  Douglas L. Wren

IPC: C07C405/00 ,  C07D309/12 ,  C07F7/18

CPC classification number: C07C405/00 ,  C07D309/12 ,  C07F7/1856 ,  Y02P20/55

Abstract: This invention relates to a novel process for making an allenic prostanoic acid derivative in the form of a single stereoisomer, or a mixture of stereoisomers, represented by the formula (I): ##STR1## wherein R is lower alkyl, R.sup.1 is a protecting group which can be selectively removed in the presence of R.sup.2, R.sup.2 is an acid-labile, base-stable protecting group, X is --(CH.sub.2).sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--, Y is --C(R.sup.3)(OR.sup.2)CH.sub.2 --, in which --OR.sup.2 is in the .alpha. or .beta. configuration and R.sup.3 is hydrogen or methyl, Z is alkyl, or phenyl, benzyl or phenoxy each optionally substituted on the phenyl ring, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract translation: 本发明涉及以式（I）表示的单一立体异构体或立体异构体混合物形式的全氟代前列腺烷酸衍生物的制备方法：其中R为低级烷基，R 1为 在R2存在下可以选择性地除去的保护基，R2是酸不稳定的碱稳定保护基，X是 - （CH 2）2 - ，反-CH = CH-或-C 3 C 是-C（R 3）（OR 2）CH 2 - ，其中-OR 2是α或β构型，R 3是氢或甲基，Z是烷基，或苯基，苄基或苯氧基，其各自任选在苯环上取代， 波浪线表示α或β配置，条件是当一条波浪线为α时，另一条波长为β。

公开(公告)号：US5057621A

公开(公告)日：1991-10-15

申请号：US39560

申请日：1987-04-16

Applicant: Gary F. Cooper ,  John H. Fried ,  L. David Waterbury

Inventor： Gary F. Cooper ,  John H. Fried ,  L. David Waterbury

IPC: C07C405/00 ,  C07C177/00

CPC classification number: C07C405/00

Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract translation: 本发明涵盖下式的化合物，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，Y是低级烷基或者其中Z是氢，卤素，甲基，甲氧基或三氟甲基; 波浪线表示α或β配置，条件是当一条波浪线为α时，另一条波长为β。

公开(公告)号：US4778904A

公开(公告)日：1988-10-18

申请号：US2339

申请日：1987-01-09

Applicant: Gary F. Cooper

Inventor： Gary F. Cooper

IPC: C07C405/00 ,  C07F7/18 ,  C07D309/08 ,  C07C49/207

CPC classification number: C07C405/0025 ,  C07F7/1856

Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or an ether-forming group and X is hydrogen, halo, trifluoromethyl, lower alkyl, or lower alkoxy, are useful intermediates for making PGE and PGF derivatives having an allenic function.

Abstract translation: 其中R1和R2是氢或醚形成基团，X是氢，卤素，三氟甲基，低级烷基或低级烷氧基的式“IMAGE”的化合物是制备具有富集功能的PGE和PGF衍生物的有用中间体。

公开(公告)号：US5516910A

公开(公告)日：1996-05-14

申请号：US245789

申请日：1994-05-19

Applicant: Gary F. Cooper ,  Keith E. McCarthy

Inventor： Gary F. Cooper ,  Keith E. McCarthy

IPC: A61K31/435 ,  A61K31/4365 ,  A61P7/02 ,  C07D291/04 ,  C07D495/04

CPC classification number: C07D291/04 ,  C07D495/04

Abstract: Compounds of the formula: ##STR1## wherein: A is oxo or dioxo;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo;are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.

Abstract translation: 下式的化合物：其中：A是氧代或二氧代; R1，R2和R3独立地是氢或1-6个碳原子的低级烷基; R4，R5，R6和R7独立地为氢，1-6个碳原子的低级烷基，烷氧基，酰基或卤素; 有利地转化为噻吩并[3,2-c]吡啶衍生物及其药学上可接受的盐，特别是噻氯匹定盐酸盐。

公开(公告)号：US4912235A

公开(公告)日：1990-03-27

申请号：US203398

申请日：1988-06-07

Applicant: Gary F. Cooper ,  Douglas L. Wren ,  Albert R. Van Horn ,  Tsung-Tee Li ,  Colin C. Beard

Inventor： Gary F. Cooper ,  Douglas L. Wren ,  Albert R. Van Horn ,  Tsung-Tee Li ,  Colin C. Beard

IPC: C07C405/00 ,  C07F7/18 ,  C07D315/00 ,  C07C177/00

CPC classification number: C07C405/0016 ,  C07C405/00 ,  C07C405/0025 ,  C07C405/0033 ,  C07C405/0041 ,  C07F7/1856

Abstract: This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.

Abstract translation: 本发明涉及以其立体异构体或其混合物的形式制备式I化合物（I）的方法，其中R是氢，低级烷基; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线代表α或β构型，条件是当一个波浪线是α时，另一个是β，或药学上可接受的无毒的盐 其中R是氢的化合物; 用于制备这些化合物的新型中间体; 制造中间体的方法; 和其中R是甲基且X是氢的式I化合物的立体异构体及其制备方法。

公开(公告)号：US4780562A

公开(公告)日：1988-10-25

申请号：US776063

申请日：1985-09-13

Applicant: Gary F. Cooper ,  Douglas L. Wren ,  Albert R. Van Horn ,  Tsung-Tee Li ,  Colin C. Beard

Inventor： Gary F. Cooper ,  Douglas L. Wren ,  Albert R. Van Horn ,  Tsung-Tee Li ,  Colin C. Beard

IPC: C07C405/00 ,  C07C17/00

CPC classification number: C07C405/00 ,  C07C405/0016 ,  C07C405/0025 ,  C07C405/0033 ,  C07C405/0041

Abstract: This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.

Abstract translation: 本发明涉及以其立体异构体或其混合物的形式制备式I化合物（I）的方法，其中R是氢，低级烷基; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线代表α或β构型，条件是当一个波浪线是α时，另一个是β，或药学上可接受的无毒的盐 其中R是氢的化合物; 用于制备这些化合物的新型中间体; 制造中间体的方法; 和其中R是甲基且X是氢的式I化合物的立体异构体及其制备方法。

公开(公告)号：US4916238A

公开(公告)日：1990-04-10

申请号：US283644

申请日：1988-12-13

Applicant: Gary F. Cooper ,  Colin C. Beard ,  David Y. Jackson ,  Douglas L. Wren

Inventor： Gary F. Cooper ,  Colin C. Beard ,  David Y. Jackson ,  Douglas L. Wren

IPC: C07C405/00 ,  C07D309/12 ,  C07F7/18

CPC classification number: C07F7/1856 ,  C07C405/00 ,  C07D309/12 ,  Y02P20/55

Abstract: This invention relates to a novel process for making an allenic prostanoic acid derivative in the form of a single stereoisomer, or a mixture of stereosiomers, represented by the formula (I): ##STR1## wherein R is lower alkyl, R.sup.1 is a protecting group which can be selectively removed in the presence of R.sup.2, R.sup.2 is an acid-labile, base-stable protecting group, X is --(CH.sub.2).sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--, Y is --C(R.sup.3)(OR.sup.2)CH.sub.2 --, in which --OR.sup.2 is in the .alpha. or .beta. configuration and R.sup.3 is hydrogen or methyl, Z is alkyl, or phenyl, benzyl or phenoxy each optionally substituted on the phenyl ring, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..