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71. 发明授权

US4287195A Heterocyclic derivatives of [4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazol es and 1H-1,2,4-triazoles 失效
标题翻译： [4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的杂环衍生物
公开(公告)号：US4287195A
公开(公告)日：1981-09-01
申请号：US27178
申请日：1979-04-04
申请人： Jan Heeres , Robert Hendrickx
发明人： Jan Heeres , Robert Hendrickx
IPC分类号： C07D213/74 , C07D215/38 , C07D233/84 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06 , C07D521/00 , C07D419/14 , A61K31/495
CPC分类号： C07D213/74 , C07D215/38 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08 , C07D249/14 , C07D277/18 , C07D277/42 , C07D295/28 , C07D473/06
摘要： Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenloxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.
摘要翻译：可用作抗真菌和抗菌剂的[4-（哌嗪-1-基 - 苯氧基甲基）-1,3-二氧戊环-2-基甲基] -1H-咪唑和1H-1,2,4-三唑的新型杂环衍生物。

72. 发明授权

US4267179A Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidaz oles and 1H-1,2,4-triazoles 失效
标题翻译：（4-苯基哌嗪-1-基 - 芳氧基甲基-1,3-二氧戊环-2-基）甲基-1H-咪唑和1H-1,2,4-三唑的杂环衍生物
公开(公告)号：US4267179A
公开(公告)日：1981-05-12
申请号：US20383
申请日：1979-03-14
申请人： Jan Heeres , Leo J. J. Backx
发明人： Jan Heeres , Leo J. J. Backx
IPC分类号： C07D405/14 , A01N43/60 , A01N43/64 , A01N43/653 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/495 , A61K31/505 , A61P31/04 , A61P31/10 , C07D231/12 , C07D233/54 , C07D233/84 , C07D249/08 , C07D249/12 , C07D271/10 , C07D295/096 , C07D295/135 , C07D317/28 , C07D413/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , A01N43/60 , A01N43/64 , A01N43/653 , A61K31/41 , A61K31/495 , C07D233/56 , C07D233/64 , C07D233/84 , C07D249/08 , C07D249/12 , C07D271/10 , C07D295/096 , C07D295/135 , C07D317/28
摘要： Novel heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.

73. 发明授权

US4160838A Antimicrobial and plant-growth-regulating triazole derivatives 失效
标题翻译：抗菌和植物生长调节三唑衍生物
公开(公告)号：US4160838A
公开(公告)日：1979-07-10
申请号：US866317
申请日：1978-01-03
申请人： Gustaaf Van Reet , Jan Heeres , Lourens Wals
发明人： Gustaaf Van Reet , Jan Heeres , Lourens Wals
IPC分类号： A01N43/653 , C07D317/16 , C07D317/22 , C07D317/30 , C07D521/00 , A01N9/22 , C07D405/06
CPC分类号： C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08 , C07D317/16 , C07D317/22 , C07D317/30
摘要： Novel 1-(.beta.-aryl)ethyl-1H-1,2,4-triazole ketals useful for their antimicrobial and plant-growth regulating activities.
摘要翻译：新颖的1-（β-芳基）乙基-1H-1,2,4-三唑缩酮可用于其抗微生物和植物生长调节活性。

74. 发明授权

US4156008A 1-(4-Alkyl-2-aryl-1,3-dioxolan-2-ylmethyl)-1H-imidazoles 失效
标题翻译： 1-（4-烷基-2-芳基-1,3-二氧戊环-2-基甲基）-1H-咪唑
公开(公告)号：US4156008A
公开(公告)日：1979-05-22
申请号：US732829
申请日：1976-10-15
申请人： Jan Heeres
发明人： Jan Heeres
IPC分类号： A01N43/50 , C07C29/10 , C07C29/36 , C07C41/30 , C07C43/23 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30 , C07D521/00 , A61K31/415 , C07D405/06
CPC分类号： C07D233/56 , A01N43/50 , C07C29/106 , C07C29/36 , C07D231/12 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30
摘要： Novel 1-(4-alkyl-2-aryl-1,3-dioxolan-2-ylmethyl)-1H-imidazoles useful as antifungal and antibacterial agents.
摘要翻译：新颖的1-（4-烷基-2-芳基-1,3-二氧戊环-2-基甲基）-1H-咪唑可用作抗真菌和抗菌剂。

75. 发明授权

US4141908A 2-Aryl-1,3-dioxolanes 失效
标题翻译： 2-芳基-1,3-二氧戊环
公开(公告)号：US4141908A
公开(公告)日：1979-02-27
申请号：US802700
申请日：1977-06-02
申请人： Jan Heeres
发明人： Jan Heeres
IPC分类号： C07D317/22 , C07D317/10
CPC分类号： C07D317/22
摘要： Novel 1-(2-Ar-4-aryloxymethyl-1,3-dioxolan-2-ylmethyl)imidazoles, useful as antifungal and antibacterial agents.
摘要翻译：新颖的1-（2- Ar-4-芳氧基甲基-1,3-二氧戊环-2-基甲基）咪唑，可用作抗真菌剂和抗菌剂。

76. 发明授权

US4139540A 2-Aryl-2-halomethyl-4-alkenyl-1,3-dioxolanes 失效
标题翻译： 2-芳基-2-卤代甲基-4-烯基-1,3-二氧戊烷
公开(公告)号：US4139540A
公开(公告)日：1979-02-13
申请号：US774290
申请日：1977-03-04
申请人： Jan Heeres
发明人： Jan Heeres
IPC分类号： A01N43/50 , C07C29/10 , C07C29/36 , C07C41/30 , C07C43/23 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30 , C07D521/00 , C07D317/10
CPC分类号： C07D233/56 , A01N43/50 , C07C29/106 , C07C29/36 , C07D231/12 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30
摘要： Novel compounds denoted as 2-aryl-2-halomethyl-4-alkenyl-1,3-dioxolanes used as intermediates in making 1-(2-Ar-4-R-1,3-dioxolan-2-ylmethyl)imidazoles, useful as antifungal and antibacterial agents.
摘要翻译：用作制备1-（2- Ar-4-R-1,3-二氧戊环-2-基甲基）咪唑的中间体的2-芳基-2-卤代甲基-4-烯基-1,3-二氧戊环的新化合物，有用作为抗真菌剂和抗菌剂。

77. 发明授权

US3936470A 1,3-Dioxolan-2-ylmethylimidazoles 失效
标题翻译： 1,3-二氧戊环-2-基甲基咪唑
公开(公告)号：US3936470A
公开(公告)日：1976-02-03
申请号：US544157
申请日：1975-01-27
申请人： Jan Heeres
发明人： Jan Heeres
IPC分类号： A01N43/50 , C07C29/10 , C07C29/36 , C07C41/30 , C07C43/23 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30 , C07D521/00 , C07D233/60 , C07D405/10
CPC分类号： C07D233/56 , A01N43/50 , C07C29/106 , C07C29/36 , C07D231/12 , C07D249/08 , C07D303/04 , C07D303/08 , C07D303/12 , C07D303/22 , C07D317/14 , C07D317/16 , C07D317/22 , C07D317/24 , C07D317/30
摘要： Novel 1-(2-Ar.sup.1 -4-Ar.sup.2 -1,3-dioxolan-2-ylmethyl)imidazoles, 1-[2-Ar.sup.1 -4-(Ar.sup.2 -oxymethyl)-1,3-dioxolan-2-ylmethyl]imidazoles, 1-[2-Ar.sup.1 -4-(Ar.sup.2 -thiomethyl)-1,3-dioxolan-2-ylmethyl]imidazoles, and 1-[2-Ar.sup.1 -4-(Ar.sup.2 -ethyl)-1,3-dioxolan-2-ylmethyl]imidazoles, useful as antifungal and antibacterial agents.
摘要翻译： 1-（2- Ar1-4-Ar2-1,3-二氧戊环-2-基甲基）咪唑，1- [2-氨基-4-（Ar2-氧甲基）-1,3-二氧戊环-2-基甲基]咪唑，1- [2- Ar1-4-（Ar2-硫代甲基）-1,3-二氧戊环-2-基甲基]咪唑和1- [2- Ar 1-4 - （Ar 2 - 乙基）-1,3-二氧戊环-2-基] 2-基甲基]咪唑，可用作抗真菌剂和抗菌剂。

78. 发明授权

US09487518B2 HIV inhibiting bicyclic pyrimidine derivatives 有权
标题翻译： HIV抑制双环嘧啶衍生物
公开(公告)号：US09487518B2
公开(公告)日：2016-11-08
申请号：US13410779
申请日：2012-03-02
申请人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号： C07D487/04 , A61K31/519 , C07D473/00 , C07D473/34 , A61P31/18 , A61K31/52
CPC分类号： C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要： HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; and the use of these compounds for the prevention or the treatment of HIV infection.

79. 发明授权

US08946248B2 HIV inhibiting 5-substituted pyrimidines 有权
标题翻译： HIV抑制5-取代嘧啶
公开(公告)号：US08946248B2
公开(公告)日：2015-02-03
申请号：US11576315
申请日：2005-09-29
申请人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
发明人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
IPC分类号： C07D239/48 , A61K31/505 , C07D239/50
CPC分类号： C07D239/48 , C07D239/50
摘要： HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
摘要翻译：其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-;其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-; R1是氢，芳基，甲酰基，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，R2羟基，卤素，C1-6烷基，羧基，氰基，-C（= O）R6，硝基，氨基，单或二 C 1-6烷基）氨基，多卤甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（= O）p - ; R 3是H，C 1-6烷基，卤素; R4是H，C1-6烷基，卤素; R 5是硝基，氨基，单和二C 1-4烷基氨基，芳基，卤素，-CHO，-CO-R 6，-COOR 7，-NH-C（= O）H，-NH-C（= = N-O-R8; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代C 1-4烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R8是氢，C1-6烷基，芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物及其制备方法。

80. 发明授权

US08080551B2 HIV inhibiting pyrimidines derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US08080551B2
公开(公告)日：2011-12-20
申请号：US11474855
申请日：2006-06-26
申请人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号： A61K31/501 , A61K31/497 , C07D417/12 , C07D417/14 , C07D417/06 , C07D401/12 , C07D401/14 , C07D401/06 , C07D403/12 , C07D403/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D405/06 , C07D409/14 , C07D409/12 , C07D409/06 , C07D237/20 , C07F9/02 , C07D413/06 , C07D413/12 , C07D413/14 , C07C257/06 , C07C211/40 , C07C233/03 , C07C235/06 , C07C237/20 , C07C239/08 , C07C229/34 , C07C255/49 , C07C207/02
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07C255/42 , C07C257/12 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
摘要翻译：公开了具有本文定义的式（I）的HIV复制抑制剂。含有HIV复制抑制剂的药物组合物; 使用HIV复制抑制剂治疗艾滋病毒; 还公开了制备HIV复制抑制剂的方法。

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