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1. 发明授权

US5006651A Phosphinic acid derivatives 失效
公开(公告)号：US5006651A
公开(公告)日：1991-04-09
申请号：US410779
申请日：1989-09-22
申请人： Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
发明人： Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
IPC分类号： A61K38/00 , C07K5/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

2. 发明授权

US4885283A Phosphinic acid derivatives 失效
标题翻译：次膦酸衍生物
公开(公告)号：US4885283A
公开(公告)日：1989-12-05
申请号：US126643
申请日：1987-12-01
申请人： Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
发明人： Michael J. Broadhurst , Balraj K. Handa , William H. Johnson , Geoffrey Lawton , Peter J. Machin
IPC分类号： A61K38/00 , C07K5/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

3. 发明授权

US4996358A Hydroxylamine bearing amino acid derivatives as collagenase inhibitors 失效
标题翻译：具有氨基酸衍生物的羟胺作为胶原酶抑制剂
公开(公告)号：US4996358A
公开(公告)日：1991-02-26
申请号：US336264
申请日：1989-04-11
申请人： Balraj K. Handa , William H. Johnson , Peter J. Machin
发明人： Balraj K. Handa , William H. Johnson , Peter J. Machin
IPC分类号： C12N9/99 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/22 , A61K31/395 , A61K38/00 , A61P29/00 , A61P43/00 , C07C67/00 , C07C231/00 , C07C237/06 , C07C237/08 , C07C237/12 , C07C237/22 , C07C259/06 , C07C313/00 , C07C323/60 , C07D207/40 , C07D225/02 , C07K1/02 , C07K5/06 , C07K5/065 , C07K5/068
CPC分类号： C07K5/06086 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , A61K38/00
摘要： Compounds of the formula ##STR1## wherein A is a group of the formula HN(OH)--CO-- or HCO--N(OH)--; R.sup.1 is a C.sub.2 -C.sub.5 -alkyl; R.sup.2 is the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R.sup.2 is not hydrogen or methyl; R.sup.3 is hydrogen, amino, hydroxy, mercapto, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -alkylthio or aryl-(C.sub.1 -C.sub.6 -alkyl), or amino-(C.sub.1 -C.sub.6 -alkyl), hydroxy-(C.sub.1 -C.sub.6 -alkyl), mercapto-(C.sub.1 -C.sub.6 -alkyl) or carboxy-(C.sub.1 -C.sub.6 -alkyl) in which the amino, hydroxy, mercapto or carboxyl group may be protected, the amino group may be acylated or the carboxyl group may be amidated; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl, di(C.sub.1 -C.sub.6 -alkoxy)-methylene, carboxyl, (C.sub.1 -C.sub.6 -alkyl)-carbonyl, (C.sub.1 -C.sub.6 -alkoxy)carbonyl, arylmethoxycarbonyl, (C.sub.1 -C.sub.6 -alkyl)aminocarbonyl or arylaminocarbonyl; and R.sup.6 is hydrogen or methyl; or R.sup.2 and R.sup.4 taken together are a group of the formula --(CH.sub.2).sub.n -- in which n is a number from 4 to 11; or R.sup.4 and R.sup.6 taken together are a trimethylene; and pharmaceutically acceptable salts of those compounds which are acidic or basic are described. The compounds of formula I possess collagenase inhibitory activity and can be used in the control or prevention of degenerative joint diseases.
摘要翻译：式（Ⅰ）化合物其中A为式HN（OH）-CO-或HCO-N（OH） - 的基团; R1是C2-C5-烷基; R2是天然α-氨基酸的表征基团，其中存在的任何官能团可以被保护，任何存在的氨基可以被酰化，并且存在的任何羧基可以被酰胺化，条件是R 2不是氢或甲基; R3是氢，氨基，羟基，巯基，C1-C6-烷基，C1-C4-烷氧基，C1-C6-烷基氨基，C1-C6-烷硫基或芳基 - （C1-C6-烷基）或氨基 - （C1- C6烷基），羟基 - （C1-C6-烷基），巯基 - （C1-C6-烷基）或羧基 - （C1-C6-烷基），其中氨基，羟基，巯基或羧基可被保护氨基可以被酰化或羧基可以酰胺化; R4是氢或甲基; R 5是氢或C 1 -C 6烷基，C 1 -C 6烷氧基-C 1 -C 6烷基，二（C 1 -C 6 - 烷氧基） - 亚甲基，羧基，（C 1 -C 6 - 烷基） - 羰基，（C 1 -C 6 - 烷氧基）羰基，芳基甲氧基羰基，（C 1 -C 6 - 烷基）氨基羰基或芳基氨基羰基; R6为氢或甲基; 或者R 2和R 4一起是式 - （CH 2）n - 的基团，其中n是4至11的数; 或R4和R6一起是三亚甲基; 和描述了那些酸性或碱性化合物的药学上可接受的盐。式I化合物具有胶原酶抑制活性，可用于控制或预防退行性关节疾病。

4. 发明授权

US5447929A Method of treating joint disorders using hydroxamic derivatives 失效
标题翻译：使用异羟肟酸衍生物治疗关节疾病的方法
公开(公告)号：US5447929A
公开(公告)日：1995-09-05
申请号：US214895
申请日：1994-03-17
申请人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
发明人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
IPC分类号： A61K31/40 , A61K20060101 , A61K31/16 , A61K31/165 , A61K31/395 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/425 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/55 , A61K33/08 , A61K38/00 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C20060101 , C07C259/10 , C07C317/44 , C07C323/04 , C07C333/24 , C07D20060101 , C07D207/26 , C07D207/27 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/18 , C07D209/48 , C07D211/88 , C07D233/72 , C07D233/74 , C07D233/96 , C07D239/52 , C07D239/54 , C07D239/88 , C07D249/12 , C07D253/06 , C07D271/06 , C07D271/07 , C07D295/18 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D407/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D491/10 , C07D491/113 , C07K5/06 , C07K5/10 , C12N9/99
CPC分类号： C07D207/27 , C07D207/404 , C07D209/48 , C07D211/88 , C07D233/74 , C07D249/12 , C07D271/07 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/06 , C07D491/10
摘要： Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.
摘要翻译：可以用于控制或预防退行性关节疾病例如类风湿性关节炎和骨关节炎或用于治疗侵入性肿瘤的胶原酶抑制剂，动脉粥样硬化或其它药学上可接受的盐，多发性硬化症。所述化合物可以通过将相应的羧酸环烷酰胺化或者使相应的苄氧基氨基甲酰基化合物脱保护来制备。

5. 发明授权

US5318964A Hydroxamic derivatives and pharmaceutical compositions 失效
标题翻译：羟肟酸衍生物和药物组合物
公开(公告)号：US5318964A
公开(公告)日：1994-06-07
申请号：US066832
申请日：1993-05-24
申请人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
发明人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
IPC分类号： A61K31/40 , A61K20060101 , A61K31/16 , A61K31/165 , A61K31/395 , A61K31/4015 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4245 , A61K31/425 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/536 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/55 , A61K33/08 , A61K38/00 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07C20060101 , C07C259/10 , C07C317/44 , C07C323/04 , C07C333/24 , C07D20060101 , C07D207/26 , C07D207/27 , C07D207/40 , C07D207/404 , C07D207/408 , C07D209/18 , C07D209/48 , C07D211/88 , C07D233/72 , C07D233/74 , C07D233/96 , C07D239/52 , C07D239/54 , C07D239/88 , C07D249/12 , C07D253/06 , C07D271/06 , C07D271/07 , C07D295/18 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D407/06 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D491/10 , C07D491/113 , C07K5/06 , C07K5/10 , C12N9/99
CPC分类号： C07D207/27 , C07D207/404 , C07D209/48 , C07D211/88 , C07D233/74 , C07D249/12 , C07D271/07 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D417/06 , C07D491/10
摘要： Hydroxamic acid derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hydroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.
摘要翻译：式（I）的羟氨肟酸衍生物及其药学上可接受的盐，其是可用于控制或预防退行性关节疾病例如类风湿性关节炎和骨关节炎或用于治疗侵袭性肿瘤的胶原酶抑制剂，动脉粥样硬化或多发性硬化症。所述化合物可以通过将相应的羧酸异羟肟化或相应的苄氧基氨基甲酰基化合物脱保护来制备。

6. 发明授权

US5304549A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US5304549A
公开(公告)日：1994-04-19
申请号：US823212
申请日：1992-01-21
申请人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
发明人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson , Geoffrey Lawton
IPC分类号： A61K31/66 , A01N37/18 , A01N57/16 , A61K20060101 , A61K31/135 , A61P9/10 , A61P29/00 , C07C20060101 , C07C235/12 , C07C237/22 , C07C259/06 , C07C279/36 , C07C281/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D295/13 , C07D295/15 , C07F9/28 , C07F9/30 , C07F9/38 , C07F9/40 , C07F9/48 , C07F9/553 , C07F9/576 , C07F9/62 , C07F9/6558 , A61K31/16 , A61K31/185 , A61K31/675 , C07C259/04 , C07F9/06 , C07C93/10
CPC分类号： C07D207/404 , C07C237/22 , C07C259/06 , C07C279/36 , C07D209/48 , C07D295/13 , C07D295/15 , C07F9/301 , C07F9/4816 , C07F9/5537 , C07F9/5765 , C07F9/65583 , Y10S514/825
摘要： Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.5 is hydrogen or halogen and their pharmaceutically acceptable salts, which are useful for the control or prevention of degenerative joint diseases or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis are described.
摘要翻译：（*化学结构*）（I）的化合物其中A是基团（*化学结构*）（a）（*化学结构*）（b）R 1是氢，氨基，被保护的氨基，酰氨基或低级烷基，被芳基，羟基，被保护的羟基，氨基，被保护的氨基，酰氨基，马来酰亚胺基，琥珀酰亚胺基，萘酰亚胺基，2,3-二氢-1,3-二氧代-1H-苯并（d，e）异喹啉-2-基，羧基，保护的羧基，氨基甲酰基，单（低级烷基）氨基甲酰基，二（低级烷基）氨基甲酰基，二（低级烷基）氨基，羧基 - 低级烷酰基氨基，吡咯烷子基或吗啉代; 氨基，氨基，胍基，羧基，被保护的羧基，氨基甲酰基，单（低级烷基）氨基甲酰基，二（低级烷基）氨基甲酰基，二（低级）烷氧基）氧膦基，二羟基氧膦基，吡咯烷子基，哌啶子基或吗啉代; R3是氢或任选被羟基，保护的羟基，氨基或被保护的氨基取代的低级烷基; R4是氢，羟基，低级烷氧基或苄氧基; 和R5是氢或卤素及其可用于控制或预防退行性关节疾病或用于治疗侵袭性肿瘤，动脉粥样硬化或多发性硬化的药学上可接受的盐。

7. 发明授权

US5614625A Hydroxamic acid derivatives with tricyclic substitution 失效
标题翻译：具有三环取代的羟肟酸衍生物
公开(公告)号：US5614625A
公开(公告)日：1997-03-25
申请号：US417317
申请日：1995-04-05
申请人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson
发明人： Michael J. Broadhurst , Paul A. Brown , William H. Johnson
IPC分类号： C07D401/06 , A61K20060101 , A61K31/16 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4178 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/535 , A61K31/5377 , A61K31/54 , A61K31/55 , A61P9/10 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C20060101 , C07C259/04 , C07C259/06 , C07D207/36 , C07D209/48 , C07D233/72 , C07D233/74 , C07D249/12 , C07D263/30 , C07D263/44 , C07D271/07 , C07D291/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D487/04 , C07D491/113 , C07D401/08
CPC分类号： C07D209/48 , A61K31/4178 , A61K31/454 , A61K31/5377 , C07D233/74 , C07D263/44 , C07D401/06 , C07D403/06 , C07D417/06 , C07D487/04 , Y02P20/55
摘要： The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino, carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.2 as an additional ring member, (c) is substituted by oxo on one or both C atoms adjacent to the linking N atom and (d) is optionally benz-fused or optionally substituted on one or more other C atoms by lower alkyl or oxo and/or on any additional N atom(s) by lower alkyl or aryl; R.sup.4 represents hydrogen, lower alkyl, aryl, aralkyl or a protecting group; m stands for 1 or 2 and n stands for 1-4, pharmaceutically acceptable salts thereof, intermediates used in the manufacture thereof, and methods of use therefor. Compounds of formula I are collagenase inhibitors useful in the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis or in the treatment of invasive tumours, atherosclerosis or multiple sclerosis.
摘要翻译：本发明提供通式为（I）的异羟肟酸衍生物，其中R 1表示环丙基，环丁基，环戊基或环己基; R2表示饱和的5-至8-元单环或桥连的N-杂环，N-杂环通过N原子连接，当其为单环时，任选地含有作为环成员的NR4，O，S，SO或SO2 羟基，低级烷基，低级烷氧基，氧代，缩酮化的氧代，氨基，单（低级烷基）氨基，二（低级烷基）氨基，羧基，低级烷氧基羰基，羟基 - 甲基，低级烷氧基甲基，氨基甲酰基，单（低级烷基） - 氨基甲酰基，二（低级烷基）氨基甲酰基或羟基亚氨基; （a）经由N原子连接的5-或6-元N-杂环，（b）任选地含有N，O和/或S，SO或SO 2作为另外的环成员，（c）是在与连接的N原子相邻的一个或两个C原子上被氧代取代，（d）任选地被苯并稠合或任选地在一个或多个其它C原子上被低级烷基或氧代和/或任何另外的N原子取代，由低级烷基或芳基取代; R4表示氢，低级烷基，芳基，芳烷基或保护基; m代表1或2，n代表1-4，其药学上可接受的盐，制备中使用的中间体及其用途。式I化合物是可用于控制或预防变性关节疾病如类风湿性关节炎和骨关节炎或用于治疗浸润性肿瘤，动脉粥样硬化或多发性硬化的胶原酶抑制剂。

8. 发明授权

US5475277A Differential torque motor 失效
标题翻译：差速马达
公开(公告)号：US5475277A
公开(公告)日：1995-12-12
申请号：US95688
申请日：1993-07-21
申请人： William H. Johnson
发明人： William H. Johnson
IPC分类号： H02K21/14 , H02K29/00 , H02P6/08 , H02K21/12
CPC分类号： H02P6/08 , H02K21/14 , H02K29/03
摘要： A PM (permanent magnet) motor is described, that uses electromagnetic current to release or pull a PM, which has increased starting torque and a large power output in a small volume. The motor includes phase units (60, FIG. 3 ) each having three electromagnets (46A-46C) and each having two PMs (44A, 44B) of Nd-B-Fe permanent magnet material. At a start position, a PM (44B) of each phase unit is centered between the cores (50B, 50C) of two electromagnets, and there is slight overlap (90, FIG. 6 ) of each of the two core faces (64B, 64C) with the PM face (62A). Each PM face has a longer circumferential length (D) than that (G) of each core face. Each PM face and each core face, has an axial length (E, FIG. 1 ) which is much larger than its circumferential length (D, G). The interface end of each electromagnet coil lies a small distance (K) from the core face.
摘要翻译：描述了使用电磁电流来释放或拉动PM的PM（永磁体）电动机，其具有增加的起动转矩和大体积的大功率输出。电动机包括各自具有三个电磁体（46A-46C）并且各自具有Nd-B-Fe永磁材料的两个PM（44A，44B）的相位单元（60）。在起始位置，每个相位单元的PM（44B）在两个电磁体的芯（50B，50C）之间居中，并且两个芯面（64B，...）中的每一个的轻微重叠（90，图6） 64C）与PM面（62A）。每个PM面具有比每个芯面的（G）更长的圆周长度（D）。每个PM面和每个芯面具有比其圆周长度（D，G）大得多的轴向长度（E，图1）。每个电磁线圈的接口端与芯面相距较小（K）。

9. 外观设计

USD348546S Plural discharge nipple type poultry watering assembly having an elongated support bar, hanger, and cup and keeper 失效
公开(公告)号：USD348546S
公开(公告)日：1994-07-05
申请号：US713334
申请日：1991-06-11
申请人： William H. Johnson
设计人： William H. Johnson

10. 外观设计

USD333894S Pathalogical waste incinerator for farm use 失效
公开(公告)号：USD333894S
公开(公告)日：1993-03-09
申请号：US767924
申请日：1991-09-30
申请人： William H. Johnson
设计人： William H. Johnson

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