-
公开(公告)号：US5508300A
公开(公告)日：1996-04-16
申请号：US181690
申请日：1994-01-14
申请人： Allen J. Duplantier
发明人： Allen J. Duplantier
IPC分类号： A61K31/415 , A61P9/00 , A61P11/00 , A61P17/00 , A61P27/16 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04
摘要： The compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof; wherein X.sub.1, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock etc.
摘要翻译： 式I的化合物及其药学上可接受的盐; 其中X1，R1，R2，R3和R4如本文所定义，是PDE IV的抑制剂和肿瘤坏死因子的产生。 因此，他们积极治疗炎性疾病，休克等。
-
![Benzoate salt of 4-(5-methyl-oxazolo[4,5-b]-pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane](/abs-image/US/2008/02/21/US20080045512A1/abs.jpg.150x150.jpg)
22.发明申请Benzoate salt of 4-(5-methyl-oxazolo[4,5-b]-pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane 审中-公开4-（5-甲基 - 恶唑并[4,5-b] - 吡啶-2-基）-1,4-二氮杂双环[3.2.2]壬烷的苯甲酸盐公开(公告)号：US20080045512A1
公开(公告)日：2008-02-21
申请号：US11501289
申请日：2006-08-09
IPC分类号： G06F15/00 , A61K31/5513 , C07D491/02
CPC分类号： C07D498/04
摘要： The present invention provides a benzoate salt of Formula I: Formula I is also known as 4-(5-methyloxazolo[4,5-b]pyridine-2-yl)-1,4-diazabicyclo[3.2.2]nonane. The benzoate salt of the invention is useful in the treatment of schizophrenia and Alzheimer's Disease. It is particularly of use in the treatment of cognitive deficits associated with schizophrenia, cognitive and attention deficit symptoms of Alzheimer's Disease, and neurodegeneration associated with Alzheimer's Disease.
摘要翻译： 本发明提供式I的苯甲酸盐：式I也称为4-（5-甲基恶唑并[4,5-b]吡啶-2-基）-1,4-二氮杂双环[3.2.2]壬烷。 本发明的苯甲酸盐可用于治疗精神分裂症和阿尔茨海默病。 它特别用于治疗与精神分裂症，阿尔茨海默病的认知和注意缺陷症状以及与阿尔茨海默氏病有关的神经变性相关的认知缺陷。
-
公开(公告)号：US06903128B2
公开(公告)日：2005-06-07
申请号：US10702539
申请日：2003-11-05
IPC分类号： A61K31/135 , A61K31/137 , A61K31/198 , A61K31/275 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/436 , A61K31/519 , A61K31/522 , A61K31/56 , A61K31/58 , A61K31/606 , A61K31/635 , A61K31/675 , A61K38/00 , A61K38/21 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P11/08 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P37/00 , A61P37/04 , A61P37/06 , C07C229/34 , C07C233/47 , C07C275/42 , C07C311/06 , C07D233/64 , C07D235/10 , C07D235/14 , C07D261/08 , C07D277/22 , C07D277/38 , C07D413/04 , C07D235/04 , C07D263/54
CPC分类号： C07D413/04 , C07C229/34 , C07C233/47 , C07C311/06 , C07D235/14 , C07D261/08
摘要： There is disclosed a genus of non-peptidyl compounds, wherein said compounds are VLA-4 inhibitors useful in treating inflammatory, autoimmune, and respiratory diseases, and wherein said compounds comprise a compound of Formula (1.0.0): and pharmaceutically acceptable salts and other prodrug derivatives thereof, wherein: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9; or is a member selected from the group consisiting of the following radicals: A1-NHC(═O)NH-A2-, A1-NHC(═O)O-A2-, A1-OC(═O)NH-A2-, A1-NHSO2NH-A2-, A1-NHC(═O)-A2-, A1-C(═O)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)rO-A2-, A1-O(CH2)r-A2, A1-(CH2)r-A2-, where A1 and A2 are each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9; B is a member independently selected from the group consisting of the following: E is a single bond; —O—; —NR10—; —CH═CH—; —CC—; S(═O)q; —CR11R12NR10—; or —CR11R12—; X is —O—; —C(═O)—; —S(═O)q—; or —NR10—; X1, X2 and X3 are each independently selected from the group consisting of CH, CR9 or N; Y is a single bond; —C(═O)—; —C(═S)—; or —S(═O)2—; R7 is (C1-C6) alkyl; (CH2)kOR5; (CH2)kNR6C(═O)R5; (CH2)kNR6C(═O)OR5; (CH2)kNR6SO2R5; (CH2)kNR6R5; F; CF3; OCF3; aryl, substituted with 0 to 3 R9; heterocyclyl, substituted with 0 to 3 R9; heteroaryl, substituted with 0 to 3 R9; cycloalkyl, substituted with 0 to 3 R9; or R7 may be taken together with R8 to form a cycloalkyl or heterocyclyl ring; or R7 may be taken together with R11 to form a cycloalkyl or heterocyclyl ring; and R8 is hydrogen; F; (C1-C6) alkyl or (C1-C6) alkoxy.
-
公开(公告)号：US6028086A
公开(公告)日：2000-02-22
申请号：US973725
申请日：1998-06-01
申请人： Allen J. Duplantier
发明人： Allen J. Duplantier
IPC分类号： A61K31/44 , A61K31/4409 , A61P9/02 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P27/16 , A61P37/08 , A61P43/00 , C07D213/75
CPC分类号： C07D213/75
摘要： A compound of formula (I) wherein a, b, V, W, X, Y, Z, R.sup.1 and R.sup.2 are as defined above. The compound of formula (I) and the pharmaceutically acceptable salts thereof are useful in inhibiting phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) and in the treatment of asthma, arthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and other inflammatory diseases characterized by phosphodiesterase (PDE) type IV activity as well as AIDS, sepsis, septic shock and other diseases, such as cachexia, involving the production of TNF. ##STR1##
摘要翻译： PCT No.PCT / US95 / 07208 Sec。 371日期1998年6月1日 102（e）日期1998年6月1日PCT提交1995年6月7日PCT公布。 公开号WO96 / 40636 日期：1996年12月19日其中a，b，V，W，X，Y，Z，R 1和R 2如上所定义的式（I）化合物。 式（I）化合物及其药学上可接受的盐可用于抑制IV型磷酸二酯酶（PDE）和肿瘤坏死因子（TNF）的产生以及治疗哮喘，关节炎，支气管炎，慢性阻塞性气道疾病，牛皮癣 ，过敏性鼻炎，皮炎和其他以磷酸二酯酶（PDE）IV型活性为特征的炎性疾病，以及艾滋病，败血症，败血性休克等涉及TNF产生的恶病质等疾病。
-
公开(公告)号：US5596013A
公开(公告)日：1997-01-21
申请号：US632301
申请日：1996-04-15
申请人： Allen J. Duplantier
发明人： Allen J. Duplantier
IPC分类号： A61K31/415 , A61P9/00 , A61P11/00 , A61P17/00 , A61P27/16 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号： C07D487/04
摘要： The compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof; wherein X.sub.1, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, are inhibitors of PDE IV and the production of tumor necrosis factor. As such, they are active in the treatment of inflammatory diseases, shock etc.
摘要翻译： 式I的化合物及其药学上可接受的盐; 其中X1，R1，R2，R3和R4如本文所定义，是PDE IV的抑制剂和肿瘤坏死因子的产生。 因此，他们积极治疗炎性疾病，休克等。
-
-
-
-
搜索结果
25 条记录 (耗时 0.024 秒)
