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公开(公告)号：US4434175A
公开(公告)日：1984-02-28
申请号：US373692
申请日：1982-05-03
IPC分类号： C07D207/32 , C07D207/337 , C07D207/34 , C07D207/36 , C07D401/06 , C07D409/06 , A61K31/405
CPC分类号： C07D207/337 , C07D207/34 , C07D207/36 , C07D401/06 , C07D409/06
摘要： 5-Aroyl-4-RO-, 5-aroyl-4-RS-, 5-aroyl-4-RSO-, 5-aroyl-4-RSO.sub.2 -, or 5-pyrrylcarbonyl-pyrrole alkanoic acid have been prepared via hydrolysis of a precursor-ester after high temperature decarboxylation or from direct acidic decarboxylation of a precursor diacid. The compounds are analgesic and anti-inflammatory agents of high activities but low ulcerogenic side effects.
摘要翻译： 5-芳酰基-4-RO-，5-芳酰基-4-RS-，5-芳酰基-4- RSO-，5-芳酰基-4-RSO 2 - 或5-吡咯烷基 - 吡咯烷酸已经通过水解 高温脱羧后的前体酯或前体二酸的直接酸性脱羧。 该化合物是具有高活性但低溃疡性副作用的止痛和抗炎药。
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2.发明授权
公开(公告)号：US5591737A
公开(公告)日：1997-01-07
申请号：US168903
申请日：1993-12-16
申请人： James B. Doherty , Conrad P. Dorn , Philippe L. Durette , Paul E. Finke , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Soumya P. Sahoo , Jeffrey J. Hale , Thomas J. Lanza , William K. Hagmann
发明人： James B. Doherty , Conrad P. Dorn , Philippe L. Durette , Paul E. Finke , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Soumya P. Sahoo , Jeffrey J. Hale , Thomas J. Lanza , William K. Hagmann
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D521/00 , A61K31/395 , A61K31/535
CPC分类号： C07D231/12 , C07D205/08 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12
摘要： New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1## wherein R.sub.4 is (a) ##STR2## or (b) ##STR3## where R.sub.x is carboxy C.sub.1-6 alkyl, benzyloxycarbonylC.sub.1-3 alkyl, or t-butoxycarbonylC.sub.1-3 alkyl,whereinQ is a covalent bond or ##STR4## wherein R.sub.5 and R.sub.6 are each individually C.sub.1-3 alkyl or hydrogen,Y is ##STR5## or a covalent bond.
摘要翻译： 描述了已经被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂的通式（I）的新的取代的氮杂环丁酮。 其中R 4是（a），或（b）其中R x是羧基C 1-6烷基，苄氧基羰基C 1-3烷基或叔丁氧基羰基C 1-3烷基，其中Q是共价键或其中 R 5和R 6各自为C 1-3烷基或氢，Y为共价键。
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3.发明授权
公开(公告)号：US4797396A
公开(公告)日：1989-01-10
申请号：US74440
申请日：1987-07-16
IPC分类号： A61K31/43 , C07D499/88 , C07D487/04 , A61K31/42
CPC分类号： A61K31/43 , C07D499/88
摘要： .beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
摘要翻译： β-内酰胺衍生物和类似物被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎/抗代谢药物。
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4.发明授权
公开(公告)号：US4711886A
公开(公告)日：1987-12-08
申请号：US627166
申请日：1984-07-02
IPC分类号： A61K31/43 , C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： A61K31/43 , C07D499/88
摘要： .beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
摘要翻译： β-内酰胺衍生物和类似物被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎/抗代谢药物。
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5.发明授权Tricyclic derivatives of substituted pyrrole acids as analgesic and anti-inflammatory agents 失效取代吡咯酸的三环衍生物作为止痛剂和抗炎剂
公开(公告)号：US4440779A
公开(公告)日：1984-04-03
申请号：US385232
申请日：1982-06-04
IPC分类号： C07D209/70 , C07D207/34 , C07D313/08 , C07D487/04 , C07D491/04 , C07D491/044 , C07D495/04 , A61K31/55 , C07D209/94
CPC分类号： C07D487/04 , C07D207/34 , C07D209/70 , C07D313/08 , C07D491/04 , C07D495/04 , Y10S514/899 , Y10S514/916
摘要： Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.
摘要翻译： 取代的吡咯酸的三环衍生物，例如取代的4,10-二氢-10-氧代-1H- [1]苯并氧杂环[4,3-b]吡咯-2-乙酸或其5-硫杂类似物已经通过 前体二酸的前体水解或脱羧。 发现这些三环化合物具有高镇痛作用和抗炎活性，但具有低溃疡性副作用。
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6.发明授权
公开(公告)号：US5229381A
公开(公告)日：1993-07-20
申请号：US761191
申请日：1991-09-20
申请人： James B. Doherty , Conrad P. Dorn , Paul E. Finke , William K. Hagmann , Malcolm MacCoss , Shrenik K. Shah
发明人： James B. Doherty , Conrad P. Dorn , Paul E. Finke , William K. Hagmann , Malcolm MacCoss , Shrenik K. Shah
IPC分类号： A61K31/395 , C07D205/08 , C07D205/085 , C07D205/09 , C07D401/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D521/00
CPC分类号： C07D231/12 , A61K31/395 , C07D205/08 , C07D205/085 , C07D205/09 , C07D233/56 , C07D249/08 , C07D401/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： New substituted azetidinones of the general formula (A') which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. ##STR1##
摘要翻译： 描述了已经被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎和抗再生剂的通式（A'）的新的取代的氮杂环丁酮。 （A）
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公开(公告)号：US4368190A
公开(公告)日：1983-01-11
申请号：US141227
申请日：1980-04-17
申请人： Tsung-Ying Shen , Philippe L. Durette , Conrad P. Dorn, Jr. , James B. Doherty , Richard T. Dean
发明人： Tsung-Ying Shen , Philippe L. Durette , Conrad P. Dorn, Jr. , James B. Doherty , Richard T. Dean
CPC分类号： C07K9/005
摘要： Immunologically active compounds of the formula: ##STR1## wherein: R.sub.1 is C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; or substituted phenyl;R.sub.2 is hydrogen; C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; substituted phenyl; phenyl C.sub.1-4 alkyl; or substituted phenyl C.sub.1-4 alkyl;R.sub.3 and R.sub.4 may be the same or different and are each independently hydrogen, provided that R.sub.3 and R.sub.4 may not both be hydrogen; or ##STR2## where X is --O--; --S--; or ##STR3## R.sub.10 is hydrogen; C.sub.1-30 alkyl; C.sub.2-30 alkenyl; C.sub.1-30 alkoxy; phenyl; C.sub.1-20 alkylsulfonyl; or cholesteryl;R.sub.11, R.sub.12, R.sub.13, R.sub.14, and R.sub.15 may be the same or different and are each independently hydrogen; C.sub.1-20 alkyl; C.sub.1-20 alkylcarbonyloxy; amino; benzyl; C.sub.1-20 alkoxymethyl; C.sub.1-20 alkylamido; or ##STR4## r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both r and t are greater than 0 or when r is 0 and R.sub.10 is amino; phenyl; substituted phenyl; 1-adamantyl; or heterocycle selected from the group consisting of 2- or 3-furyl, 2- or 3- thienyl, 2- or 3- pyrrolidinyl, 2-, 3- or 4- pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C.sub.1-20 alkylcarbonyl; and where R.sub.3 or R.sub.4 is other than hydrogen, the other of R.sub.3 and R.sub.4 may additionally be C.sub.1-4 alkylcarbonyl;R.sub.5 is hydrogen or C.sub.1-10 alkyl;R.sub.6 is hydrogen or R.sub.6 and R.sub.7 taken together are --(CH.sub.2).sub.3 --;R.sub.7 is hydrogen; C.sub.1-7 alkyl; hydroxymethyl; mercaptomethyl; benzyl; or substituted benzyl;R.sub.8 and R.sub.9 may be the same or different and are each independently COOR, or CONR'R", where R is hydrogen or C.sub.1-7 alkyl, and R' and R" are hydrogen or C.sub.1-3 alkyl;when R.sub.5 is C.sub.1-10 alkyl, the stereochemistry at asymmetric center I is D or L;when R.sub.7 is other than hydrogen, the stereochemistry at asymmetric center II is L; and the stereochemistry at asymmetric center III is D; and acid addition and quaternary salts thereof.
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公开(公告)号：US4847247A
公开(公告)日：1989-07-11
申请号：US922312
申请日：1986-10-16
IPC分类号： A61K31/43 , C07D499/00 , C07D499/21 , C07D499/44 , C07D499/48
CPC分类号： C07D499/00 , A61K31/43
摘要： Derivatives of Penicillin, their sulfoxides and sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
摘要翻译： 青霉素的衍生物，其亚砜和砜被发现是有效的弹性蛋白酶抑制剂，从而有用的抗炎/抗代谢药物。
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9.发明授权
公开(公告)号：US4637999A
公开(公告)日：1987-01-20
申请号：US490617
申请日：1983-05-02
IPC分类号： C07D501/00 , C07D501/20 , A61K31/545
CPC分类号： C07D501/00
摘要： Substituted cephalosporins are found to be potent elastase inhibitors and thereby useful antiinflammatory/antidegenerative agents.
摘要翻译： 发现取代的头孢菌素是有效的弹性蛋白酶抑制剂，从而有用的抗炎/抗代谢药物。
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公开(公告)号：US4493839A
公开(公告)日：1985-01-15
申请号：US380989
申请日：1982-05-24
IPC分类号： A61K31/40 , C07D477/10 , C07D487/04
CPC分类号： A61K31/40 , C07D477/10
摘要： Derivatives of 1-carbapenem-3-carboxylic esters are found to be potent elastase inhibitors and therefore are useful anti-inflammatory agents.
摘要翻译： 发现1-碳青霉烯-3-羧酸酯的衍生物是有效的弹性蛋白酶抑制剂，因此是有用的抗炎剂。
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