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1. 发明授权

US4652551A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US4652551A
公开(公告)日：1987-03-24
申请号：US735504
申请日：1985-05-17
申请人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
发明人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , A61K31/165 , A61K37/43 , C07C103/19 , C07K5/06 , C07K5/08
CPC分类号： C07K5/06078 , C07K5/0227 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxyl, loweralkyl or arylalkyl; R.sub.1, R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is CH.sub.2 ; R.sub.6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; and X and R.sub.6 when taken together may be a vinylic group.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A为N-保护基团时，B为NH，当n为0时，B为氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X为CH 2; R6是低级烷基，环烷基，环烷基烷基，芳基或芳基烷基; 并且X和R 6一起可以是乙烯基。

2. 发明授权

US4645759A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US4645759A
公开(公告)日：1987-02-24
申请号：US735491
申请日：1985-05-17
申请人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
发明人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , A61K37/43 , C07K5/08
CPC分类号： C07K5/06078 , C07K5/0227 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R.sub.1, R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO or SO.sub.2 ; and R.sub.6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R.sub.6 may be an N-protecting group when X is NH.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A是N-保护基时，B是NH，当n是0时，B是氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是NH，O，S，SO或SO 2; 并且R 6为低级烷基，环烷基，环烷基烷基，芳基，芳烷基或N-保护基，条件是当X为NH时，R 6可为N-保护基。

3. 发明授权

US06797718B2 Ether substituted imidazopyridines 失效
公开(公告)号：US06797718B2
公开(公告)日：2004-09-28
申请号：US10456308
申请日：2003-06-06
申请人： Joseph F. Dellaria , Kyle J. Lindstrom , Luke T. Dressel , Philip D. Heppner , John R. Jacobsen , Matthew R. Radmer , Doris Stoermer
发明人： Joseph F. Dellaria , Kyle J. Lindstrom , Luke T. Dressel , Philip D. Heppner , John R. Jacobsen , Matthew R. Radmer , Doris Stoermer
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

4. 发明授权

US06664260B2 Heterocyclic ether substituted imidazoquinolines 失效
公开(公告)号：US06664260B2
公开(公告)日：2003-12-16
申请号：US10011921
申请日：2001-12-06
申请人： Leslie J. Charles , Joseph F. Dellaria , George W. Griesgraber , Philip D. Heppner , Karl J. Manske , John W. Mickelson , Michael J. Rice
发明人： Leslie J. Charles , Joseph F. Dellaria , George W. Griesgraber , Philip D. Heppner , Karl J. Manske , John W. Mickelson , Michael J. Rice
IPC分类号： A61K314745
CPC分类号： C07D471/04
摘要： Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and heterocyclyl or heteroaryl functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

5. 发明授权

US06525064B1 Sulfonamido substituted imidazopyridines 失效
标题翻译：磺酰胺取代的咪唑并吡啶
公开(公告)号：US06525064B1
公开(公告)日：2003-02-25
申请号：US10165002
申请日：2002-06-07
申请人： Joseph F. Dellaria , Chad A. Haraldson , Philip D. Heppner , Kyle J. Lindstrom , Bryon A. Merrill
发明人： Joseph F. Dellaria , Chad A. Haraldson , Philip D. Heppner , Kyle J. Lindstrom , Bryon A. Merrill
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： Imidazopyridine compounds that contain sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.
摘要翻译：在1位含有磺酰胺官能团的咪唑并吡啶化合物可用作免疫应答调节剂。本发明的化合物和组合物可以诱导各种细胞因子的生物合成，并且可用于治疗各种病症，包括病毒性疾病和肿瘤性疾病。

6. 发明授权

US5514702A Arylamidoalkyl-N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的芳酰胺基烷基-N-羟基脲化合物
公开(公告)号：US5514702A
公开(公告)日：1996-05-07
申请号：US178237
申请日：1994-01-10
申请人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
发明人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
IPC分类号： A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P29/00 , A61P43/00 , C07C275/64 , C07C311/13 , C07C311/18 , C07C311/27 , C07C311/29 , C07C311/35 , C07C311/41 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/48 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/88 , C07D239/26 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/56 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/84 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/36 , C07D333/38 , C07D333/54 , C07D333/56 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07D333/32 , C07D333/34
CPC分类号： C07D213/64 , C07C275/64 , C07C311/18 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D215/48 , C07D277/56 , C07D307/68 , C07D307/85 , C07D333/20 , C07D333/38 , C07D333/70 , C07D405/12
摘要： The present invention provides certain (substituted carbocyclic aryl)amidoalkyl- and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
摘要翻译： PCT No.PCT / US92 / 05715 Sec。 371日期1994年1月10日 102（e）日期1994年1月10日PCT提交1992年7月7日PCT公布。出版物WO93 / 02037 日期：1993年2月4日。本发明提供了某些（取代的碳环芳基）酰氨基烷基 - 和（取代的杂环芳基）酰氨基烷基-N-羟基脲化合物，其抑制脂氧合酶活性，因此可用于治疗过敏性和炎性疾病状态。

7. 发明授权

US5432194A (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and aryalkynylarylurea inhibitors of 5-lipoxygenase 失效
标题翻译：（4-烷氧基吡喃-4-基）取代的芳基烷基芳基 - 芳烯基芳基和芳氧基炔基芳基脲抑制剂5-脂氧合酶
公开(公告)号：US5432194A
公开(公告)日：1995-07-11
申请号：US236001
申请日：1994-05-09
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
IPC分类号： C07D309/12 , C07D405/12 , A61K31/35 , C07D309/10
CPC分类号： C07D405/12 , C07D309/12
摘要： Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：其中W选自其中Q是氧或硫的结构的化合物，R6和R7是氢或烷基，或R6和R7与它们所连接的氮原子一起定义为烷基，卤代烷基，任选取代的苯基，羟基烷基，氨基烷基，羧基烷基，（烷氧基羰基）烷基和（烷基氨基羰基）烷基; Z是-CH 2 - ，氧，硫或-NR 9，其中R 9是氢或烷基，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基，R 1，R 2，R 3和R 4独立地选自烷基卤素，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y选自氧，-NR10，其中R10是氢或烷基，和其中n = 0,1或2，R5是烷基，抑制白三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

8. 发明授权

US5354865A Phenylmethyl derivatives having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的苯甲基衍生物
公开(公告)号：US5354865A
公开(公告)日：1994-10-11
申请号：US942870
申请日：1992-09-10
申请人： Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
发明人： Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
IPC分类号： C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10 , C07D405/12 , C07D235/26 , C07D215/227 , C07D265/36
CPC分类号： C07D405/12 , C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10
摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, benzo[b]thienyl, A.sub.1 is propynylene, methylene, or a valence bond, X is O, S, SO.sub.2, or NR.sub.2, Y is selected from alkyl, haloalkyl, alkoxy, halogen, and hydrogen, A.sub.2 is selected from ##STR2## and methylene where Z is OR.sub.5 or NHR.sub.5 where R.sub.5 is hydrogen or alkyl, R.sub.1 is hydrogen, alkyl, or OR.sub.5, and m and n are integers having a value of 1 or 2 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：其中Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基，苯并[b]噻吩基，A 1是亚丙炔基，亚甲基或价键，X是O，S，SO 2或NR 2， Y选自烷基，卤代烷基，烷氧基，卤素和氢，A2选自：其中Z是OR 5或亚甲基，其中R 5是氢或烷基，R 1是氢，烷基或OR 5，和m和n 是具有1或2值的整数是脂氧合酶的有效抑制剂，因此抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

9. 发明授权

US5214204A Arylamidoalkyl-N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
标题翻译：具有LIPOXYGENASE抑制活性的ARYLAMIDOALKYL-N-HYDROXYUREA化合物
公开(公告)号：US5214204A
公开(公告)日：1993-05-25
申请号：US732520
申请日：1991-07-19
申请人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
发明人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
IPC分类号： A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P29/00 , A61P43/00 , C07C275/64 , C07C311/13 , C07C311/18 , C07C311/27 , C07C311/29 , C07C311/35 , C07C311/41 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/48 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/88 , C07D239/26 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/56 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/84 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/36 , C07D333/38 , C07D333/54 , C07D333/56 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D213/64 , C07C275/64 , C07C311/18 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D215/48 , C07D277/56 , C07D307/68 , C07D307/85 , C07D333/20 , C07D333/38 , C07D333/70 , C07D405/12
摘要： The present invention provides certain (substituted carbocyclic aryl)amidoalkyl-and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
摘要翻译：本发明提供某些（取代的碳环芳基）酰氨基烷基 - 和（取代的杂环芳基）酰氨基烷基-N-羟基脲化合物，其抑制脂氧合酶活性并因此可用于治疗过敏性和炎性疾病状态。

10. 发明申请

US20100069427A9 Oxime and Hydroxylamine Substituted Imidazo[4,5-c] Ring Compounds and Methods 失效
标题翻译：肟和羟胺取代的咪唑并[4,5-c]环化合物和方法
公开(公告)号：US20100069427A9
公开(公告)日：2010-03-18
申请号：US11884153
申请日：2006-02-10
申请人： Tushar A. Kshirsagar , Gregory D. Lundquist, JR. , Joseph F. Dellaria , Matthew R. Radmer , Bernhard M. Zimmermann
发明人： Tushar A. Kshirsagar , Gregory D. Lundquist, JR. , Joseph F. Dellaria , Matthew R. Radmer , Bernhard M. Zimmermann
IPC分类号： A61K31/437 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04 , C07D471/14
摘要： Imidazo[4,5-c] ring compounds, (e.g. imidazo[4,5-c]pyridines, imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydro imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridine, and 6,7,8,9-tetrahydro imidazo[4,5-c]naphthyridine compounds) having an oxime or hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
摘要翻译：咪唑并[4,5-c]环化合物（例如咪唑并[4,5-c]吡啶，咪唑并[4,5-c]喹啉，6,7,8,9-四氢咪唑并[4,5-c] 喹啉，咪唑并[4,5-c]萘啶和6,7,8,9-四氢咪唑并[4,5-c]萘啶化合物），其中2-位具有肟或羟胺取代基，药物组合物含有化合物，中间体和制备方法以及这些化合物作为免疫调节剂的用途，用于调节动物中的细胞因子生物合成和治疗包括病毒和肿瘤疾病在内的疾病。

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