公开(公告)号：US4191764A

公开(公告)日：1980-03-04

申请号：US946985

申请日：1978-09-29

Applicant: Colin C. Beard

Inventor： Colin C. Beard

IPC: C07C335/38 ,  C07D235/32 ,  A61K31/535 ,  C07D295/18

CPC classification number: C07D235/32 ,  C07C335/38

Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; ##STR2## is a 5, 6, 7 or 8 membered heterocyclic ring containing 1 or 2 hetero atoms; the ##STR3## substitution being at the 5(6)-position; and the pharmaceutically acceptable salts thereof. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

Abstract translation: 由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; 是含有1或2个杂原子的5,6,7或8元杂环; 替换在5（6）位置; 及其药学上可接受的盐。 这些化合物可用作杀虫剂，特别是作为驱肠虫和抗真菌剂。

公开(公告)号：US4110463A

公开(公告)日：1978-08-29

申请号：US803016

申请日：1977-06-03

Applicant: Colin C. Beard ,  Marshall B. Wallach ,  Klaus Weinhardt

Inventor： Colin C. Beard ,  Marshall B. Wallach ,  Klaus Weinhardt

IPC: A61K31/415 ,  A61P21/02 ,  C07D233/44 ,  C07D233/48 ,  C07D233/46

CPC classification number: C07C255/00 ,  C07D233/48

Abstract: Compounds represented by the formula ##STR1## wherein R is hydrogen or alkyl of 1-4 carbons, R.sup.1 is alkyl of 1-6 carbons and the naphthyl group is attached to the imidazole ring at the 1 or 2 positions of the naphthyl ring and the pharmaceutically acceptable salts thereof are useful as centrally acting skeletal muscle relaxants.

Abstract translation: 由式CHEM表示的咪唑-2-氨基甲酸酯，其中R是氢或1-4个碳的烷基，R 1是1-6个碳的烷基，萘基在咪唑环上连接1或2个 萘环的位置及其药学上可接受的盐。 这些化合物可用作中枢作用的骨骼肌松弛剂。 该化合物通过闭合式（CHEM）化合物来制备

公开(公告)号：US4011320A

公开(公告)日：1977-03-08

申请号：US664454

申请日：1976-03-08

Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

IPC: C07D487/04 ,  C07D251/72

CPC classification number: C07D487/04

Abstract: 7(8)-substituted triazinobenzimidazoles represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R' is diloweralkylaminoalkyl (C.sub.2-6) or alkyl having 1 to 18 carbon atoms; R.sup.2 is phenylsulfinyl, phenoxyethoxy, benzyloxyethoxy, methoxyethylsulfinyl, or 3-chloroprop-1-ylsulfinyl; the R.sup.2 -substitution being at the 7(8)-position; or a pharmaceutically acceptable salt thereof.The compounds are useful as pesticides, particularly as antifungal and anthelmintic agents.

公开(公告)号：US06215017B1

公开(公告)日：2001-04-10

申请号：US09497537

申请日：2000-02-03

Applicant: Charles A. Dvorak ,  Douglas L. Wren ,  Lawrence E. Fisher ,  Steven D. Axt ,  Eric R. Humphreys ,  Humberto B. Arzeno ,  Colin C. Beard ,  Sam Linh Nguyen ,  Yeun-Kwei Han ,  Christopher R. Roberts ,  Jan P. Lund ,  Paul R. Fatheree

Inventor： Charles A. Dvorak ,  Douglas L. Wren ,  Lawrence E. Fisher ,  Steven D. Axt ,  Eric R. Humphreys ,  Humberto B. Arzeno ,  Colin C. Beard ,  Sam Linh Nguyen ,  Yeun-Kwei Han ,  Christopher R. Roberts ,  Jan P. Lund ,  Paul R. Fatheree

IPC: C07C67743

CPC classification number: C07D473/00 ,  C07D473/18 ,  Y02P20/55

Abstract: Intermediates of Formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract translation: 式（III）的中间体，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基如所定义 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1的单-L-缬氨酸酯的新方法 ，3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。

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：US4080461A

公开(公告)日：1978-03-21

申请号：US729229

申请日：1976-10-04

Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

IPC: C07D235/32 ,  A61K31/415

CPC classification number: C07D235/32

Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SO.sub.2 R.sup.2, --SCN, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 where M and M' are independently O, S, ##STR2## R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; andR.sup.5 is lower alkenyl, lower alkynyl, or aralkyl. The R.sup.1 substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

Abstract translation: 由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; R1是-SOR2，-SO2R2，-SCN，-SR5，-OR5或M'（CH2）nMR7，其中M和M'独立地是O，S，R7是具有1-4个碳原子的低级烷基或芳基， n为1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，或芳烷基或芳基; 并且R 5为低级链烯基，低级炔基或芳烷基。 R1取代为5（6）位。

公开(公告)号：US4072696A

公开(公告)日：1978-02-07

申请号：US434656

申请日：1974-01-18

Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

IPC: C07C335/28 ,  C07C147/00 ,  C07C147/06 ,  C07C149/40

CPC classification number: C07C335/28

Abstract: Carbalkoxythioureidobenzene derivatives represented by the following formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SR.sup.2, --SOR.sup.2, --SO.sub.2 R.sup.2, --OR.sup.2, --SCN, --SC(O)NR.sup.3 R.sup.4, or --M'(CH.sub.2).sub.n MR.sup.7 where n is 1-4; R.sup.2 is lower alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, aralkyl or aryl, provided that when R.sup.1 is --SO.sub.2 R.sup.2, R.sup.2 is not aralkyl or phenyl; R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; Y is amino, nitro, acylamino where the acyl portion has 1 to 6 carbon atoms, --NHC(O) (CH.sub.2).sub.m COOH where m is 1-6, or --NHC(S)NHCOOR; M and M' are independently O, S or ##STR2## and R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl. The R.sup.1 substitution is either at the 4- or 5-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

Abstract translation: 由下式表示的碳烷氧基硫代脲基苯衍生物：其中R是具有1至4个碳原子的低级烷基; R1是-SR2，-SOR2，-SO2R2，-OR2，-SCN，-SC（O）NR3R4或-M'（CH2）nMR7，其中n是1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，芳烷基或芳基，条件是当R 1是-SO 2 R 2时，R 2不是芳烷基或苯基; R3和R4独立地是氢或具有1至6个碳原子的低级烷基; Y是酰基部分具有1-6个碳原子的氨基，硝基，酰基氨基，-NHC（O）（CH 2）m COOH，其中m是1-6，或-NHC（S）NHCOOR; M和M'独立地为O，S或，并且R 7为具有1至4个碳原子的低级烷基或芳基。 R1取代在4-或5-位。

公开(公告)号：US4031228A

公开(公告)日：1977-06-21

申请号：US669373

申请日：1976-03-22

Applicant: Colin C. Beard

Inventor： Colin C. Beard

IPC: A61K31/41 ,  C07D513/04 ,  A61K31/425 ,  A61K31/54

CPC classification number: C07D513/04 ,  A61K31/41

Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##STR1## where R is a lower alkyl group having 1 to 4 carbon atoms; and R.sup.1 is a fused, bicyclic heterocyclic ring moiety. The R.sup.1 S-substitution is at the 5(6)-position.The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents. The compounds are also useful as antiprotozoal agents, particularly against Trichomonas vaginalis.

Abstract translation: 由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：其中R是具有1至4个碳原子的低级烷基; 并且R 1是稠合的双环杂环部分。 R1S取代位于5（6）位。

公开(公告)号：US3935209A

公开(公告)日：1976-01-27

申请号：US441222

申请日：1974-02-11

Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

IPC: C07D235/32 ,  A23K1/16 ,  C07D213/64 ,  C07D213/643 ,  C07D213/70 ,  C07D233/84 ,  C07D239/38 ,  C07D241/18 ,  C07D249/12 ,  C07D277/34 ,  C07D277/36 ,  C07D333/34

CPC classification number: C07D213/643 ,  C07D213/70 ,  C07D233/84 ,  C07D239/38 ,  C07D241/18 ,  C07D249/12 ,  C07D277/34 ,  C07D277/36 ,  C07D333/34

Abstract: Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is a heterocyclic ring having 1-4 hetero atoms; and M is O, S, or ##EQU1## The R.sup.1 M-substitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

公开(公告)号：US06218568B1

公开(公告)日：2001-04-17

申请号：US09497538

申请日：2000-02-03

Applicant: Charles A. Dvorak ,  Douglas L. Wren ,  Lawrence E. Fisher ,  Steven D. Axt ,  Eric R. Humphreys ,  Humberto B. Arzeno ,  Colin C. Beard ,  Sam Linh Nguyen ,  Yeun-Kwei Han ,  Christopher R. Roberts ,  Jan P. Lund ,  Paul R. Fatheree

Inventor： Charles A. Dvorak ,  Douglas L. Wren ,  Lawrence E. Fisher ,  Steven D. Axt ,  Eric R. Humphreys ,  Humberto B. Arzeno ,  Colin C. Beard ,  Sam Linh Nguyen ,  Yeun-Kwei Han ,  Christopher R. Roberts ,  Jan P. Lund ,  Paul R. Fatheree

IPC: C07C67743

CPC classification number: C07D473/00 ,  C07D473/18 ,  Y02P20/55

Abstract: Process for preparing intermediates of formula (III) wherein Y1 is acyloxy, wherein acyl is of the formula R—C(O)—, wherein R is alkyl of 1-6 carbon atoms, Y2 is aralkyloxy, and Z is benzoyloxy or acyloxy, wherein acyl is as defined above. Intermediates of formula (III) are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

Abstract translation: 制备式（III）的中间体的方法，其中Y1是酰氧基，其中酰基是式RC（O） - ，其中R是1-6个碳原子的烷基，Y2是芳烷氧基，Z是苯甲酰氧基或酰氧基，其中酰基 式（III）的中间体可用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基） - 的单-L-缬氨酸酯的新方法， 甲氧基-1,3-丙二醇（更昔洛韦）。 更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。