公开(公告)号：US5093343A

公开(公告)日：1992-03-03

申请号：US577970

申请日：1990-09-05

Applicant: Gerhard Bonse ,  Nikolaus Muller ,  Achim Harder

Inventor： Gerhard Bonse ,  Nikolaus Muller ,  Achim Harder

IPC: A01N43/824 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/433 ,  A61P33/10 ,  C07D271/10 ,  C07D271/113 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13

CPC classification number: C07D271/113 ,  C07D285/125 ,  C07D285/13

Abstract: Substituted 1,3,4-oxa- and thiadiazolinones of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,R.sup.2 represents one or more identical or different radicals from among hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be sutstituted,R.sup.3 represents one or more identical or different radicals from among hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents O or S, andY represents O or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one, and 5-phenoxy-3-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one are disclosed as useful to combat endoparasites. Compositions containing these compounds and process for preparing them are also disclosed.The present invention relates to new substituted 1,3,4-oxa(thia)diazolinones, process for their preparation, and their use for combating endoparasites.Substituted 2-alkoxy-1,3,4-oxathiazolinones and their use against endoparasites are already known, but their actions are not always satisfactory (DE-OS (German Published Specification) 2,604,110). Previously described compounds are furthermore 2-aryloxy-1,3,4-oxadiazolinones (Pilgram, J. Heterocyclic Chem. 39, 823 (1982)); however, nothing is known about their use for combating endoparasites.The present invention relates to substituted 1,3,4-oxa-and thiadiazolinones of the formula (I) ##STR2## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogeno-alkylthio,R.sup.2 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkyl-sulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,R.sup.3 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkyl-sulphonyl, arylsulphonyl, sulphamoyl, alkyl-sulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents 0 or S, andY represents 0 or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one and 5-phenoxy-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one.The invention also relates to a process for the preparation of the new substituted 1,3,4-oxa- and thiadiazolinones of the formula ##STR3## in which R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogeno-alkylthio,R.sup.2 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, aryl-sulphonyl, sulphamoyl, alkylsulphamoyl, dialkyl-sulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,R.sup.3 represents one or more identical or different radicals from amongst hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogeno-alkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, alkylcarbonyl, carbalkoxy, alkyl-sulphonyl, arylsulphonyl, sulphamoyl, alkyl-sulphamoyl, dialkylsulphamoyl, aryl, aryloxy or arylthio, which, in turn, can be substituted,X represents O or S, andY represents O or S,with the exception of the compounds 5-phenoxy-3-(3,4-dichlorophenyl)-1,3,4-oxadiazol-2(3H)-one and 5-phenoxy-3-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-(3H)-one, characterized in that compounds of the formula (II) ##STR4## in which X, Y, R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meaning, are reacted with carbonylation reagents such as phosgene, phosgene or triphosgene, and the compounds obtained in this process, of the formula III ##STR5## in which X, Y, R.sup.1, R.sup.2 and R.sup.3 have the abovementioned meaning, are cyclized in the presence of bases.

公开(公告)号：US5077412A

公开(公告)日：1991-12-31

申请号：US414998

申请日：1989-09-29

Applicant: Josef Ehrenfreund ,  Manfred Boger ,  Odd Kristiansen ,  Jozef Drabek ,  Haukur Kristinsson

Inventor： Josef Ehrenfreund ,  Manfred Boger ,  Odd Kristiansen ,  Jozef Drabek ,  Haukur Kristinsson

IPC: A01N47/30 ,  A01N47/32 ,  A01N47/40 ,  A01N47/42 ,  C07D207/34 ,  C07D209/32 ,  C07D231/20 ,  C07D233/70 ,  C07D235/26 ,  C07D249/12 ,  C07D257/04 ,  C07D263/38 ,  C07D263/58 ,  C07D271/10 ,  C07D271/113 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D285/08 ,  C07D285/12 ,  C07D285/13 ,  C07D307/58 ,  C07D333/32 ,  C07D333/34

CPC classification number: C07D271/113 ,  A01N47/30 ,  A01N47/32 ,  A01N47/40 ,  A01N47/42 ,  C07D233/70 ,  C07D249/12 ,  C07D277/34 ,  C07D277/68 ,  C07D285/08 ,  C07D285/13

Abstract: The invention relates to novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein Z is ##STR2## or --N.dbd.C.dbd.N--; R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.10 alkenyl, C.sub.3 -C.sub.10 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.3 alkyl substituted by 1 or 2 C.sub.3 -C.sub.6 cycloalkyl radicals, or is alkoxyalkyl containing a total of 3 to 10 carbon atoms, halogen-substituted C.sub.1 -C.sub.12 alkyl, polycyclic C.sub.7 -C.sub.10 cycloalkyl, or phenyl(C.sub.1 -C.sub.5)alkyl which may be substituted in the phenyl moiety by 1 or 2 identical or different members selected from the group consisting of halogen, methoxy, ethoxy and C.sub.1 -C.sub.5 alkyl,R.sub.2 is hydrogen or C.sub.1 -C.sub.5 alkyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.3 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is a 5-membered heterocyclic radical containing 1 to 4 hetero atoms selected from the group consisting of N, O and S, which radical may be substituted at the carbon or nitrogen atoms by 1 to 3 of the substituents R.sub.6, R.sub.7 and R.sub.8, or is a 5-membered heterocyclic radical which may be fused with benzene nuclei and which contains 1 or 2 hetero atoms selected from the group consisting of N, O and S and can be substituted at the carbon or nitrogen atoms by 1 to 3 of the substituents R.sub.6, R.sub.7 and R.sub.8,R.sub.6 and R.sub.7 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, halogen-substituted C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy; halogen-substituted C.sub.1 -C.sub.4 alkoxy, phenyl, or C.sub.1 -C.sub.4 alkylthio,R.sub.8 is hydrogen or C.sub.1 -C.sub.4 alkyl, andR.sub.9 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, C.sub.3 -C.sub.4 alkynyl, alkoxyalkyl containing a total of 10 carbon atoms, or alkylthioalkyl containing a total of 10 carbon atomsand to the salts thereof with acids and bases. The invention further relates to the preparation of these compounds and to the use thereof in pest control, and to novel intermediates.

公开(公告)号：US4791208A

公开(公告)日：1988-12-13

申请号：US83556

申请日：1987-08-07

Applicant: Heinz Forster ,  Hans-Joachim Diehr ,  Fritz Maurer ,  Erich Klauke ,  Ludwig Eue ,  Hans-Joachim Santel ,  Robert R. Schmidt ,  Paul Reinecke ,  Gerd Hanssler

Inventor： Heinz Forster ,  Hans-Joachim Diehr ,  Fritz Maurer ,  Erich Klauke ,  Ludwig Eue ,  Hans-Joachim Santel ,  Robert R. Schmidt ,  Paul Reinecke ,  Gerd Hanssler

IPC: A01N43/82 ,  A01N43/824 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13 ,  C07D417/12 ,  C07D491/113

CPC classification number: C07D285/12 ,  A01N43/82 ,  C07D285/125 ,  C07D285/13

Abstract: 5-Halogenoalkyl-1,3,4-thiadiazol-2-yloxyacetamides of the formula ##STR1## in which R.sup.1 is halogenoalkyl, with the exception of trifluoromethyl, andR.sup.2 and R.sup.3 each independently is hydrogen, alkyl, alkenyl, alkinyl, in each case optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxyalkylenoxy, alkoxy, aralkyl or optionally substituted aryl, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, form an optionally substituted heterocyclic radical which can contain further hetero-atoms,which possess herbicidal and fungicidal activity. The intermediates 5-chlorodifluoromethyl- and 5-dichlorofluoromethyl-2-chloro-1,3,4- thiadiazole are also new.

Abstract translation: 其中R 1为卤代烷基，除三氟甲基以外，其中R 2和R 3各自独立地为氢，烷基，烯基，炔基，各自独立地为氢，烷基，烯基，炔基， 任选取代的环烷基或环烯基，卤代烷基，烷氧基烷基，烷氧基亚烷基氧基，烷氧基，芳烷基或任选取代的芳基，或R 2和R 3与它们所键合的氮原子一起形成任选取代的杂环基团，其可含有其它杂原子 ，具有除草和杀真菌活性。 中间体5-氯二氟甲基 - 和5-二氯氟甲基-2-氯-1,3,4-噻二唑也是新的。

公开(公告)号：US4731105A

公开(公告)日：1988-03-15

申请号：US895921

申请日：1986-08-13

Applicant: Graham P. Jones

Inventor： Graham P. Jones

IPC: C07D417/12 ,  A01N43/82 ,  A01N43/824 ,  C07D285/12 ,  C07D285/13 ,  C07D419/12

CPC classification number: C07D285/13 ,  A01N43/82

Abstract: Herbicidal thiadiazolyloxyacetamides of the formula: ##STR1## wherein: R is an optionally-substituted alkyl, cycloalkyl or aryl group; R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, alkyl, cycloalkyl, alkoxy, alkenyl, aryl, aralkyl or aryloxy, any alkyl or aryl moiety thereof being optionally substituted; or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, represent a heterocyclic or benzheterocyclic group, the hetrocyclic ring of which is 5- or 6-membered, and which may be substituted by one or more alkyl groups; and X is oxygen, sulphur or --S(O).sub.n --where n is 1 or 2,process for their preparation, and compositions containing them.

Abstract translation: 具有下式的除草噻二唑氧基乙酰胺：其中：R是任选取代的烷基，环烷基或芳基; R 1和R 2可以相同或不同，各自表示氢，烷基，环烷基，烷氧基，烯基，芳基，芳烷基或芳氧基，其任何烷基或芳基部分任选被取代; 或R 1和R 2与它们所连接的氮原子一起表示杂环或苯并杂环基，其杂环是5或6元，并且可被一个或多个烷基取代; 且X为氧，硫或-S（O）n - ，其中n为1或2，其制备方法和含有它们的组合物。

公开(公告)号：US4581175A

公开(公告)日：1986-04-08

申请号：US684639

申请日：1984-12-21

Applicant: Fritz Maurer

Inventor： Fritz Maurer

IPC: C07C333/02 ,  C07C67/00 ,  C07C325/00 ,  C07C337/02 ,  C07D285/12 ,  C07D285/13 ,  C07D491/113 ,  C07C155/02

CPC classification number: C07D285/13

Abstract: N'-Acylhydrazine-N-thiocarboxylic acid O-carbamoylmethyl esters of the formula ##STR1## in which R.sup.1 is alkyl, alkoxy, alkylthio, halogenoalkyl, aralkyl, aralkoxy, aralkylthio or optionally substituted aryl, andR.sup.2 and R.sup.3 each independently is hydrogen, alkyl, alkenyl, alkinyl, optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxy, aralkyl or optionally substituted aryl, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, are an optionally substituted heterocyclic radical,are new compounds useful in preparing known thiadiazole herbicides in high yield by ring closure.

Abstract translation: N-酰基肼-N-硫代羧酸式其中R 1为烷基，烷氧基，烷硫基，卤代烷基，芳烷基，芳烷氧基，芳烷硫基或任选取代的芳基，且R 2和R 3各自独立地为氢， 烷基，烯基，炔基，任选取代的环烷基或环烯基，卤代烷基，烷氧基烷基，烷氧基，芳烷基或任选取代的芳基，或R 2和R 3与它们所键合的氮原子一起是任选取代的杂环基， 可用于通过闭环制备高产率的已知噻二唑除草剂。

公开(公告)号：US3287463A

公开(公告)日：1966-11-22

申请号：US31195263

申请日：1963-09-27

Applicant: GEIGY AG J R

Inventor： KURT RUFENACHT

IPC: A01N43/824 ,  C07D271/10 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13 ,  F16H55/36

CPC classification number: C07D271/10 ,  A01N43/82 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13 ,  F16H55/36

公开(公告)号：US20140288040A1

公开(公告)日：2014-09-25

申请号：US14355780

申请日：2012-10-31

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Andrew James Woodhead ,  Gianni Chessari ,  Gilbert Ebai Besong ,  Maria Grazia Carr ,  Steven Douglas Hiscock ,  Michael Alistair O'Brien ,  David Charles Rees ,  Susanne Maria Saalau-Bethell ,  Hendrika Maria Gerarda Willems ,  Neil Thomas Thompson

IPC: A61K31/505 ,  A61K31/137 ,  A61K45/06 ,  C07C217/74 ,  A61K31/135 ,  C07D239/42 ,  C07C237/20 ,  A61K31/165 ,  C07D211/70 ,  A61K31/4409 ,  C07D295/027 ,  A61K31/4465 ,  A61K31/4462 ,  A61K31/397 ,  C07C217/58

CPC classification number: A61K31/505 ,  A61K31/135 ,  A61K31/137 ,  A61K31/165 ,  A61K31/397 ,  A61K31/4409 ,  A61K31/4462 ,  A61K31/4465 ,  A61K45/06 ,  C07B2200/05 ,  C07C217/58 ,  C07C217/60 ,  C07C217/62 ,  C07C217/74 ,  C07C217/90 ,  C07C225/12 ,  C07C233/18 ,  C07C233/25 ,  C07C235/46 ,  C07C237/04 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/12 ,  C07C237/20 ,  C07C243/34 ,  C07C251/48 ,  C07C255/24 ,  C07C255/29 ,  C07C255/37 ,  C07C255/46 ,  C07C255/54 ,  C07C259/06 ,  C07C271/12 ,  C07C275/36 ,  C07C311/04 ,  C07C311/08 ,  C07C311/29 ,  C07C313/06 ,  C07C317/22 ,  C07C323/25 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/14 ,  C07D207/335 ,  C07D209/08 ,  C07D209/14 ,  C07D209/44 ,  C07D211/26 ,  C07D211/56 ,  C07D211/70 ,  C07D213/38 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/84 ,  C07D217/02 ,  C07D231/12 ,  C07D233/24 ,  C07D233/64 ,  C07D237/14 ,  C07D239/34 ,  C07D239/42 ,  C07D241/18 ,  C07D241/20 ,  C07D241/24 ,  C07D243/14 ,  C07D263/32 ,  C07D265/36 ,  C07D271/10 ,  C07D277/68 ,  C07D285/13 ,  C07D295/02 ,  C07D295/027 ,  C07D295/185 ,  C07D295/192 ,  C07D305/06 ,  C07D305/08 ,  C07D307/14 ,  C07D307/22 ,  C07D307/79 ,  C07D309/06 ,  C07D309/12 ,  C07D309/14 ,  C07D319/18 ,  C07D513/04

Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0, 1, 2 or 3 heteroatom ring members selected from N, O and S; R4a is selected from halogen; cyano; C1-4 alkyl optionally substituted with one or more fluorine atoms; C1-4 alkoxy optionally substituted with one or more fluorine atoms; hydroxy-C1-4 alkyl; and C1-2 alkoxy-C1-4 alkyl; R5 is selected from hydrogen and a substituent R5a; and R5a is selected from C1-2 alkyl optionally substituted with one or more fluorine atoms; C1-3 alkoxy optionally substituted with one or more fluorine atoms; halogen; cyclopropyl; cyano; and amino. The compounds have activity against hepatitis C virus and can be used in the prevention or treatment of hepatitis C viral infections.

Abstract translation: 本发明提供式（6）化合物或其盐，N-氧化物或互变异构体，其中A为CH，CF或氮; E是CH，CF或氮; 和R 0是氢或C 1-2烷基; R1a选自CONH2; CO2H; 任选取代的非环C 1-8烃基; 和3至7个环成员的任选取代的单环碳环或杂环基，其中0,1,2,3或4为选自O，N和S的杂原子环成员; R2选自氢和基团R 2a; R2a选自任选取代的无环C 1-8烃基; 3至7个环成员的任选取代的单环碳环或杂环基，其中0,1或2个环成员是选自O，N和S的杂原子环成员; 和9或10个环成员的任选取代的双环杂环基，其中1或2个环成员是氮原子; 其中R 1和R 2中的至少一个不是氢; R3是含有0,1,2或3个选自N，O和S的杂原子环成员的任选取代的3至10元单环或双环碳环或杂环; R4a选自卤素; 氰基; 任选被一个或多个氟原子取代的C 1-4烷基; 任选被一个或多个氟原子取代的C 1-4烷氧基; 羟基-C 1-4烷基; 和C 1-2烷氧基-C 1-4烷基; R5选自氢和取代基R5a; 并且R 5a选自任选被一个或多个氟原子取代的C 1-2烷基; 任选被一个或多个氟原子取代的C 1-3烷氧基; 卤素; 环丙基 氰基; 和氨基。 该化合物具有抗丙型肝炎病毒的活性，可用于预防或治疗丙型肝炎病毒感染。

公开(公告)号：US07851635B2

公开(公告)日：2010-12-14

申请号：US10553222

申请日：2004-04-16

Applicant: Yoji Ino

Inventor： Yoji Ino

IPC: C07D285/135 ,  A61K31/41

CPC classification number: C07D285/13 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  C07D285/135

Abstract: A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, —C(═W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents —C(═Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.

Abstract translation: 一种有丝分裂驱动蛋白Eg5抑制剂，其包含由通式（I）表示的噻二唑啉衍生物或其药理学上可接受的盐作为活性成分：[其中R 1表示氢原子等，R 2表示氢原子，-C（= W）R6（其中W表示氧原子或硫原子，R6表示取代或未取代的低级烷基等）等，R3表示-C（= Z）R19（其中Z表示氧原子或硫原子 原子，R 19表示取代或未取代的低级烷基等）等，R 4表示取代或未取代的低级烷基等，R 5表示取代或未取代的芳基等〕等。

公开(公告)号：US20070179157A1

公开(公告)日：2007-08-02

申请号：US11701881

申请日：2007-02-02

Applicant: James Dunn ,  Steven Swallow ,  Zachary Sweeney

Inventor： James Dunn ,  Steven Swallow ,  Zachary Sweeney

IPC: A61K31/551 ,  A61K31/522 ,  A61K31/506 ,  A61K31/497 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/4196

CPC classification number: C07D271/113 ,  C07D249/12 ,  C07D285/13

Abstract: This invention relates to methods of treating an HIV infection with novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts, and methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I.

Abstract translation: 本发明涉及用新型式I杂环化合物治疗HIV感染的方法，其中R 1，R 2，R 4，X 1和X 2， SUP> 2 如本发明概述和药学上可接受的盐所定义，以及用式I化合物抑制或调节人类免疫缺陷病毒（HIV）逆转录酶的方法。

公开(公告)号：US07208509B2

公开(公告)日：2007-04-24

申请号：US10807766

申请日：2004-03-23

Applicant: James Patrick Dunn ,  Steven Swallow ,  Zachary Kevin Sweeney

Inventor： James Patrick Dunn ,  Steven Swallow ,  Zachary Kevin Sweeney

IPC: A61K31/433 ,  A61K31/4245 ,  A61K31/4196 ,  C07D285/13 ,  C07D249/12 ,  C07D271/113

CPC classification number: C07D271/113 ,  C07D249/12 ,  C07D285/13

Abstract: This invention relates to novel heterocyclic compounds of formula I wherein R1—R4, X1 and X2 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated

Abstract translation: 本发明涉及式I的新型杂环化合物，其中R 1，R 2，R 4，X 1和X 2， 在其总结及其药学上可接受的盐和溶剂合物中定义，用式I化合物抑制或调节人类免疫缺陷病毒（HIV）逆转录酶的方法，含有式I的药物组合物与至少一种溶剂，载体或赋形剂混合， 制备式I化合物的方法。该化合物可用于治疗涉及HIV和遗传相关病毒的疾病