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20 条记录 (耗时 0.027 秒)

    Quinoxaline compound and their preparation and use
    3.
    发明授权
    Quinoxaline compound and their preparation and use 失效
    喹啉化合物及其制备和使用

    公开(公告)号：US5081123A

    公开(公告)日：1992-01-14

    申请号：US451382

    申请日：1989-12-15

    申请人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    发明人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    IPC分类号： A61K31/495 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  C07D241/52 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06

    CPC分类号： C07D241/52 ,  C07D471/04 ,  C07D491/06

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy;R.sup.5 and R.sup.6 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.7 and R.sup.8 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.5 and r.sup.6 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

    Cycloalkyl or benzyl-6-substituted-quinoxalinediones
    4.
    发明授权
    Cycloalkyl or benzyl-6-substituted-quinoxalinediones 失效
    环烷基或苄基-6-取代的喹喔啉二酮

    公开(公告)号：US4948794A

    公开(公告)日：1990-08-14

    申请号：US268939

    申请日：1988-11-08

    申请人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    发明人： Tage Honore ,  Poul Jacobsen ,  Flemming E. Nielsen ,  Lars Naerum

    IPC分类号： A61K31/495 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  C07D20060101 ,  C07D241/38 ,  C07D241/44 ,  C07D241/52 ,  C07D403/06

    CPC分类号： C07D241/38 ,  C07D241/44 ,  C07D241/52 ,  C07D403/06

    摘要： Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, C.sup.1 or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -alkyl; orR.sup.7 and R.sup.8 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.6 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

    Protease inhibitors
    5.
    发明申请
    Protease inhibitors 审中-公开
    蛋白酶抑制剂

    公开(公告)号：US20070155803A1

    公开(公告)日：2007-07-05

    申请号：US10558782

    申请日：2004-05-27

    申请人： Jon Bondebjerg ,  Henrik Fuglsang ,  Lars Naerum

    发明人： Jon Bondebjerg ,  Henrik Fuglsang ,  Lars Naerum

    IPC分类号： A61K31/44 ,  A61K31/175 ,  C07C275/28

    CPC分类号： C07C281/06 ,  C07C2601/14 ,  C07D207/273 ,  C07D207/50 ,  C07D209/14 ,  C07D209/16 ,  C07D209/20 ,  C07D295/135 ,  C07D295/15 ,  C07D307/52 ,  C07D307/79 ,  C07D317/58 ,  C07D333/20 ,  C07D333/60 ,  C07D401/12 ,  C07K5/06078 ,  C07K5/06139 ,  C07K5/06191

    摘要： A monoacyl semicarbazide of the general formula (I): (I), or a pharmaceutically acceptable salt or ester thereof, is capable of selectively inhibiting dipeptidyl-peptidase I (DPP-I), also known as cathepsin C. A compound of the invention is useful as an active substance for the treatment of inflammation, type 2 diabetes, asthma, severe influenza, respiratory syncytial virus infection, CD8 T cell inhibition, inflammsatory bowel diseases, psoriasis, atopic dermatitis, Papillon Lefevre syndrome, Haim Munik syndrome, gum disease, periodontitis, rheumatoid arthritis, Huntington's disease, Chaga's disease, Alzheimer's disease, sepsis or for application in target cell apoptosis.

    摘要翻译： 通式（I）：（I）的单酰基氨基脲或其药学上可接受的盐或酯能够选择性抑制也称为组织蛋白酶C的二肽基肽酶I（DPP-1）。本发明的化合物 可用作治疗炎症，2型糖尿病，哮喘，严重流感，呼吸道合胞病毒感染，CD8 T细胞抑制，炎症性肠病，牛皮癣，特应性皮炎，Papillon Lefevre综合征，Haim Munik综合征，牙龈疾病的活性物质 ，牙周炎，类风湿关节炎，亨廷顿氏病，奇加氏病，阿尔茨海默氏病，败血症或用于靶细胞凋亡。

    Benzimidazole derivatives and use thereof as peptide deformylase inhibitors
    6.
    发明申请
    Benzimidazole derivatives and use thereof as peptide deformylase inhibitors 审中-公开
    苯并咪唑衍生物及其作为肽变性酶抑制剂的用途

    公开(公告)号：US20070066672A1

    公开(公告)日：2007-03-22

    申请号：US10572415

    申请日：2004-10-08

    申请人： Anders Hjelmencrantz ,  Patrizia Cali ,  Thomas Groth ,  Christian Jensen ,  Lars Naerum

    发明人： Anders Hjelmencrantz ,  Patrizia Cali ,  Thomas Groth ,  Christian Jensen ,  Lars Naerum

    IPC分类号： A61K31/4184 ,  C07D403/02 ,  C07D235/14

    CPC分类号： C07D235/14 ,  C07D405/06 ,  C07D409/06

    摘要： Benzimidazole compounds of the general formula (I) and pharmaceutically acceptable salts or esters thereof are peptide deformylase inhibitors useful in the treatment or prevention of infections and other diseases in which peptide deformylases are involved, especially in the treatment of bacterial and parasitic infections, for example infections fully or partly caused by microorganisms belonging to Staphylococcus, Enterococcus, Streptococcus, Haemophilus, Moraxella, Escherichia, Mycobacterium, Mycoplasma, Pseudomonas, Chlamydia, Rickettsia, Klebsiella, Shigella, Salmonella, Bordetella, Clostridium, helicobacter, Campylobacter, Legionella, or Neisseria.

    摘要翻译： 通式（I）的苯并咪唑化合物及其药学上可接受的盐或酯是可用于治疗或预防涉及肽变形酶的感染和其它疾病的肽去甲酰化酶抑制剂，特别是在细菌和寄生虫感染的治疗中，例如 感染完全或部分由属于葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫拉菌，埃希氏杆菌，分枝杆菌，支原体，假单胞菌，衣原体，立克次体，克雷伯氏菌，志贺氏菌，沙门氏菌，博德特氏菌，梭菌，螺杆菌，弯曲杆菌，军团菌或奈瑟球菌的微生物所致。

    Isoxazoles as peptide deformylase inhibitors
    7.
    发明申请
    Isoxazoles as peptide deformylase inhibitors 审中-公开
    异恶唑作为肽变性酶抑制剂

    公开(公告)号：US20070043062A1

    公开(公告)日：2007-02-22

    申请号：US10571361

    申请日：2004-09-10

    申请人： Patrizia Cali ,  Anders Hjelmencrantz ,  Lars Naerum

    发明人： Patrizia Cali ,  Anders Hjelmencrantz ,  Lars Naerum

    IPC分类号： A61K31/506 ,  A61K31/42 ,  C07D413/02

    CPC分类号： C07D261/18 ,  C07D413/12 ,  C07D413/14

    摘要： Isoxazole compounds of formula (I) and pharmaceutically acceptable salts or esters thereof are peptide deformylase inhibitors useful in the treatment or prevention of infections and other disease in which peptide deformylases are involved, especially in the treatment of bacterial and parasitic infections, for example infections fully or partly caused by microorganisms belonging to Staphylococcus, Enterococcus, Streptococcus, Haemophilus, Moraxella, Escherichia, Mycobacterium, Mycoplasma, Pseudomonas, Chlamydia, Rickettsia, Klebsiella, Shigella, Salmonella, Bordetella, Clostridium, Helicobacter, Campylobacter, Legionella or Neisseria.

    摘要翻译： 式（I）的异恶唑化合物及其药学上可接受的盐或酯是可用于治疗或预防涉及肽变形酶的感染和其他疾病的肽去甲酰化酶抑制剂，特别是在治疗细菌和寄生虫感染，例如完全感染 或部分由属于葡萄球菌，肠球菌，链球菌，嗜血杆菌，莫拉氏菌，大肠杆菌，分枝杆菌，支原体，假单胞菌，衣原体，立克次体，克雷伯氏菌，志贺氏菌，沙门氏菌，博德特氏菌，梭菌属，幽门螺杆菌，弯曲菌属，军团菌或奈瑟菌属的微生物所致。

    4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
    8.
    发明授权
    4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use 失效
    4,5,6,7-四氢 - 噻吩并[3,2-C]吡啶衍生物，其制备和用途

    公开(公告)号：US06177443B1

    公开(公告)日：2001-01-23

    申请号：US09035464

    申请日：1998-03-05

    申请人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergarrd ,  Lars Naerum ,  Annemarie Reinhardt Varming ,  Helle Demuth ,  Morten Heide

    发明人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergarrd ,  Lars Naerum ,  Annemarie Reinhardt Varming ,  Helle Demuth ,  Morten Heide

    IPC分类号： A61K3144

    CPC分类号： A61K31/4365 ,  A61K31/44 ,  A61K31/47

    摘要： The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a compound of formula I wherein A together with the double bond of formula I is benzene or thiophene; R1 is optionally substituted C1-6 alkyl or optionally substituted aryl; R2 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or —COR3, wherein R3 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or optionally substituted aryl; R4 and R5 independently are hydrogen, halogen, perhalomethyl, optionally substituted C1-6-alkyl, hydroxy, optionally substituted C1-6-alkoxy, nitro, cyano, amino, optionally substituted mono- or optionally substituted di-C1-6-alkylamino, acylamino, C1-6-alkoxycarbonyl, carboxy or carbamoyl; n is 0, and m is 1, and methods of treating or preventing a disease of the endocrinologic system.

    摘要翻译： 本发明涉及包含药学上可接受的载体或稀释剂和式I化合物的药物组合物，其中A与式I的双键是苯或噻吩; R1是任选取代的C 1-6烷基或任选取代的芳基; R 2是任选取代的C 1-6 - 烷基，任选取代的芳烷基或-COR 3，其中R 3是任选取代的C 1-6 - 烷基，任选取代的芳烷基或任选取代的芳基; R 4和R 5独立地是氢，卤素，全卤甲基，任选取代的C 1-6 - 烷基，羟基，任选取代的C 1-6 - 烷氧基，硝基，氰基，氨基，任选取代的单 - 或任选取代的二-C 1-6烷基氨基， 酰基氨基，C 1-6 - 烷氧基羰基，羧基或氨基甲酰基; n为0，m为1，以及治疗或预防内分泌系统疾病的方法。

    BONDED MINERAL FIBRE PRODUCT HAVING HIGH FIRE AND PUNKING RESISTANCE
    10.
    发明申请
    BONDED MINERAL FIBRE PRODUCT HAVING HIGH FIRE AND PUNKING RESISTANCE 审中-公开
    具有高火和耐冲击性的粘结矿物纤维制品

    公开(公告)号：US20130140481A1

    公开(公告)日：2013-06-06

    申请号：US13809362

    申请日：2011-07-22

    申请人： Lars Naerum ,  Povl Nissen

    发明人： Lars Naerum ,  Povl Nissen

    IPC分类号： C09K5/14

    CPC分类号： C09K5/14 ,  C03C25/26 ,  C03C25/32 ,  C03C25/34 ,  C08G69/44 ,  C08J5/24 ,  C08J2367/00 ,  C08J2377/12 ,  C08L77/06 ,  C08L2201/02 ,  C09J179/08 ,  D04H1/4209 ,  D04H1/64

    摘要： A bonded mineral fibre product exhibiting high fire resistance in accordance with Class A1 of Standard EN 13501-1 as well as improved punking resistance comprises man-made vitreous fibres (MMVF)) bound by a cured binder composition, the non-cured binder composition comprising (a) a sugar component, and either (b) a polycarboxylic acid component and an alkanolamine, or (c) a reaction product of a polycarboxylic acid component and an alkanolamine, or (d) a combination of (b) and (c), the amount of sugar component (a) being within the range of 42 to 72 percent by weight, based on the total weight (dry matter) of the binder components.

    摘要翻译： 根据EN 13501-1标准A1类别的耐火性优异的粘合矿物纤维产品以及改进的抗冲击性包括由固化的粘合剂组合物结合的人造玻璃纤维（MMVF），所述非固化粘合剂组合物包含 （a）糖组分，和（b）多元羧酸组分和链烷醇胺，或（c）多元羧酸组分和链烷醇胺的反应产物，或（d）（b）和（c） ，基于粘合剂组分的总重量（干物质），糖组分（a）的量在42至72重量％的范围内。