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1. 发明授权

US5220059A Lipoxygenase-inhibiting compounds derived from non-steroidal antiinflammatory carboxylic acids 失效
标题翻译：从非甾体抗炎药羧酸衍生的LIPOXYGENASE抑制化合物
公开(公告)号：US5220059A
公开(公告)日：1993-06-15
申请号：US511380
申请日：1990-04-19
申请人： Dee W. Brooks , Joseph F. Dellaria, Jr. , James B. Summers, Jr.
发明人： Dee W. Brooks , Joseph F. Dellaria, Jr. , James B. Summers, Jr.
IPC分类号： A61K31/16 , A61K31/17 , A61K31/27 , A61K31/275 , A61K31/34 , A61K31/343 , A61K31/40 , A61K31/403 , A61K31/404 , A61P29/00 , A61P31/04 , A61P37/08 , A61P43/00 , C07C259/06 , C07C271/06 , C07C271/30 , C07C275/64 , C07C327/56 , C07C333/02 , C07C333/12 , C07C333/28 , C07C335/40 , C07D209/10 , C07D209/16 , C07D307/79
CPC分类号： C07C271/30 , C07C259/06 , C07C275/64 , C07C327/56 , C07C333/02 , C07C333/12 , C07C335/40 , C07D209/16 , C07C2102/08 , C07C2103/18
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is selected from (1) hydrogen; (2) --NR.sub.2 R.sub.3, --OR.sub.2 or --SR.sub.2 where R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, aryl and alkylaryl; and (3) optionally substituted C1-C8 alkyl, C2-C8 alkenyl, arylalkyl or cycloalkyl;Y is selected from sulfur and oxygen;n is an integer selected from 0 and 1;M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group; andZ is a residue of a non-steroidal antiinflammatory drug of general form Z--COOH;or a pharmaceutically acceptable salt, ester or prodrug thereof,as well as pharmaceutical compositions containing the above compounds and a method for their use as lipoxygenase inhibitors.

2. 发明授权

US4873259A Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds 失效
标题翻译：吲哚，苯并呋喃，苯并噻吩含脂氧合酶抑制化合物
公开(公告)号：US4873259A
公开(公告)日：1989-10-10
申请号：US138073
申请日：1988-01-11
申请人： James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
发明人： James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
IPC分类号： C07D209/14 , C07D307/81 , C07D333/58
CPC分类号： C07D333/58 , C07D209/14 , C07D307/81
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.sub.12 arylalkoxy, (17) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C.sub.1 to C.sub.12 arylalkyl, (22) C.sub.2 to C.sub.12 arylalkenyl, (23) C.sub.1 to C.sub.12 arylalkoxy, or (24) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl;Z is oxygen or sulfur;and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes.Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase activity.
摘要翻译：其中R 1是（1）氢，（2）C 1至C 4烷基，（3）C 2至C 4链烯基或（4）NR 2 R 3，其中R 2和R 3独立地选自（1）氢，（2）C1至C4烷基和（3）羟基，但R2和R3不同时为羟基; 其中X是氧，硫，SO 2或NR 4，其中R 4是（1）氢，（2）C 1至C 6烷基，（3）C 1至C 6烷酰基，（4）芳酰基或（5）烷基磺酰基; A选自C1至C6亚烷基和C2至C6亚烯基; n为1-5; 在（1）氢，（2）卤素，（3）羟基，（4）氰基，（5）卤代烷基，（6）C1至C12烷基，（7）C2至C12烯基，（8）C1至C12烷氧基，（9）C3至C8环烷基，（10）C1-C8硫代烷基，（11）芳基，（12）芳氧基，（13）芳酰基，（14）C1至C12芳烷基，（15）（18）芳基，（19）芳氧基，（20）芳酰基，（21）C1〜C12芳基烷基，（22）C1〜C12芳基烷氧基，（17）C1〜C12芳基烷氧基，（17））C 2至C 12芳基烯基，（23）C 1至C 12芳基烷氧基或（24）C 1至C 12芳硫基烷氧基，其中取代基选自卤素，硝基，氰基，C 1至C 12烷基，烷氧基和卤代烷基; Z是氧或硫; 和M是氢，可药用阳离子，芳酰基或C 1至C 12烷酰基，是5-和/或12-脂氧合酶的有效抑制剂。还公开了脂氧合酶抑制组合物和抑制脂氧合酶活性的方法。

3. 发明授权

US4623661A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US4623661A
公开(公告)日：1986-11-18
申请号：US727934
申请日：1985-04-26
申请人： James B. Summers, Jr.
发明人： James B. Summers, Jr.
IPC分类号： C12N9/99 , A61K31/16 , A61K31/165 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C259/06 , C07C83/10 , A61K31/185 , A61K31/205
CPC分类号： A61K31/165 , C07C2103/24 , C07C2103/26
摘要： Compounds of the formula ##STR1## where R.sub.1 is a trinuclear aromatic or biaryl group; R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl or cycloalkyl; n is 0 or 1; and M is a pharmaceutically acceptable cation, are potent inhibitors of the enzymes 5-, 12-, and 15-lipoxygenase.
摘要翻译：其中R 1是三核芳族或联芳基的式“IMAGE”的化合物; R2是氢或C1-C6烷基或环烷基; n为0或1; M是药学上可接受的阳离子，是5，12-和15-脂肪氧合酶的有效抑制剂。

4. 发明授权

US5486525A Platelet activating factor antagonists: imidazopyridine indoles 失效
标题翻译：血小板激活因子拮抗剂：咪唑并吡啶吲哚
公开(公告)号：US5486525A
公开(公告)日：1996-01-23
申请号：US347528
申请日：1994-12-05
申请人： James B. Summers, Jr. , Steven K. Davidsen , Michael L. Curtin , H. Robin Heyman , George S. Sheppard , Lianhong Xu , George M. Carrera, Jr. , Robert B. Garland
发明人： James B. Summers, Jr. , Steven K. Davidsen , Michael L. Curtin , H. Robin Heyman , George S. Sheppard , Lianhong Xu , George M. Carrera, Jr. , Robert B. Garland
IPC分类号： C07D487/04 , A61K31/41 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/505 , A61P7/02 , A61P11/00 , A61P11/16 , A61P17/00 , A61P29/00 , A61P37/08 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D403/10 , C07D471/04
摘要： The present invention relates to compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.
摘要翻译：本发明涉及作为PAF的有效拮抗剂的式“IMAGE”及其药学上可接受的盐的化合物，其可用于治疗PAF相关疾病，包括哮喘，休克，呼吸窘迫综合征，急性炎症，移植器官排斥反应，胃肠溃疡，过敏性皮肤病，延迟的细胞免疫，分娩，胎儿肺成熟和细胞分化。

5. 发明授权

US4608390A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US4608390A
公开(公告)日：1986-08-26
申请号：US727465
申请日：1985-04-26
申请人： James B. Summers, Jr.
发明人： James B. Summers, Jr.
IPC分类号： C12N9/99 , A61K31/13 , A61K31/165 , A61K31/195 , A61K31/215 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C259/06 , C07C83/10 , A61K31/04 , A61K31/185
CPC分类号： A61K31/165
摘要： Compounds of the formula ##STR1## where X is selected from hydrogen, C.sub.1 to C.sub.22 alkyl or alkenyl, or an electron withdrawing group;n=0 or 1 and m=0, 1, 2 or 3; but n and m are not O simultaneously;R.sub.1 and R.sub.2 independently are hydrogen, C.sub.1 to C.sub.6 alkyl, an electron withdrawing group, or R.sub.4 ;R.sub.3 is H, C.sub.1 to C.sub.6 alkyl or cycloalkyl, or R.sub.4 ; andR.sub.4 independently at each occurrence, has the formula ##STR2## where Y is hydrogen or an electron withdrawing group; and wherein M is a pharmaceutically acceptable cation, are potent inhibitors of lipoxygenase enzymes.
摘要翻译：其中X选自氢，C1至C22烷基或链烯基或吸电子基团的式“IMAGE”的化合物; n = 0或1，m = 0,1,2或3; 但n和m同时不是O; R1和R2独立地为氢，C1至C6烷基，吸电子基团或R4; R3是H，C1-C6烷基或环烷基，或R4; 在每次出现时独立地具有式“IMAGE”，其中Y是氢或吸电子基团; 并且其中M是药学上可接受的阳离子，是脂氧合酶的有效抑制剂。

6. 发明授权

US4897422A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US4897422A
公开(公告)日：1990-01-30
申请号：US012978
申请日：1987-02-10
申请人： James B. Summers, Jr.
发明人： James B. Summers, Jr.
IPC分类号： C12N9/99 , A61K31/165 , A61K31/17 , A61P11/00 , A61P17/00 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C259/06 , C07C275/64
CPC分类号： C07C275/64
摘要： Compounds of the formula: ##STR1## where R.sub.1 is amino or methyl; R.sub.2 is C.sub.1 -C.sub.2 alkyl; R.sub.3 is one or more substituents selected from hydrogen, halogen or trihalomethyl; R.sub.4 is one or more substituents selected from hydrogen, halogen, trihalomethyl, C.sub.1 to C.sub.4 alkoxy or C.sub.1 to C.sub.4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.6 alkoyl are inhibitors of 5- and/or 12-lipoxygenase enzymes.

7. 发明授权

US4761403A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US4761403A
公开(公告)日：1988-08-02
申请号：US849924
申请日：1986-04-09
申请人： Bruce P. Gunn , James B. Summers, Jr.
发明人： Bruce P. Gunn , James B. Summers, Jr.
IPC分类号： C07D215/60 , C07D217/24 , A61K31/695 , C07F7/10
CPC分类号： C07D215/60 , C07D217/24
摘要： Hydroxy quinol-1-one and quinol-2-one based compounds found to be potent inhibitors of 5-, 12-, and 15-lipoxygenase enzymes.
摘要翻译：羟基喹啉-1-酮和喹啉-2-酮基化合物被发现是5-，12-和15-脂氧合酶的有效抑制剂。

8. 发明授权

US5665777A Biphenyl hydroxamate inhibitors of matrix metalloproteinases 失效
标题翻译：基质金属蛋白酶联苯基异羟肟酸盐抑制剂
公开(公告)号：US5665777A
公开(公告)日：1997-09-09
申请号：US555690
申请日：1995-11-14
申请人： Stephen W. Fesik , James B. Summers, Jr. , Steven K. Davidsen , George S. Sheppard , Douglas H. Steinman , George M. Carrera, Jr. , Alan Florjancic , James H. Holms
发明人： Stephen W. Fesik , James B. Summers, Jr. , Steven K. Davidsen , George S. Sheppard , Douglas H. Steinman , George M. Carrera, Jr. , Alan Florjancic , James H. Holms
IPC分类号： A61P19/02 , A61K31/185 , A61K31/275 , A61P29/00 , A61P35/04 , A61P43/00 , C07C259/06 , C07C323/60 , A61K31/19 , C07C255/00 , C07C259/08
CPC分类号： C07C323/60 , C07C259/06
摘要： Compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof inhibit matrix metalloproteinases and TNF.alpha. secretion and are useful in the treatment of inflammatory disease states. Also disclosed are matrix metalloproteinases and TNF.alpha. secretion inhibiting compositions and a method for inhibiting matrix metalloproteinases and TNF.alpha. secretion.
摘要翻译：式“IMAGE”或其药学上可接受的盐的化合物抑制基质金属蛋白酶和TNFα分泌，并且可用于治疗炎性疾病状态。还公开了基质金属蛋白酶和TNFα分泌抑制组合物和抑制基质金属蛋白酶和TNFα分泌的方法。

9. 发明授权

US4605669A Lipoxygenase inhibiting naphthohydroxamic acids 失效
标题翻译：脂氧合酶抑制萘普肟酸
公开(公告)号：US4605669A
公开(公告)日：1986-08-12
申请号：US727464
申请日：1985-04-26
申请人： James B. Summers, Jr.
发明人： James B. Summers, Jr.
IPC分类号： C12N9/99 , A61K31/16 , A61K31/165 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C239/00 , C07C259/10 , A61K31/185 , A61K31/205 , C07C83/10
CPC分类号： A61K31/165
摘要： Compounds of the formula ##STR1## where R.sub.1 is H, or C.sub.1 to C.sub.6 alkyl; R.sub.2 is selected from C.sub.1 to C.sub.22 alkyl, cycloalkyl, aralky or alkenyl; and M is a pharmaceutically acceptable cation, are potent inhibitors of the enzymes 5-, 12- and 15-lipoxygenase.
摘要翻译：其中R1是H或C1-C6烷基的式“IMAGE”的化合物; R2选自C1至C22烷基，环烷基，芳烷基或烯基; M是药学上可接受的阳离子，是5-，12-和15-脂肪氧合酶的有效抑制剂。

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