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1. 发明授权

US06825225B2 Bicyclic isoxazolinones as antibacterial agents 失效
标题翻译：双环异恶唑酮作为抗菌剂
公开(公告)号：US06825225B2
公开(公告)日：2004-11-30
申请号：US09991134
申请日：2001-11-14
申请人： Michael J. Genin , Michael Robert Barbachyn , Jackson B. Hester, Jr. , Paul D. Johnson , Fred L. Ciske
发明人： Michael J. Genin , Michael Robert Barbachyn , Jackson B. Hester, Jr. , Paul D. Johnson , Fred L. Ciske
IPC分类号： A61K31422
CPC分类号： C07D413/04
摘要： The present invention provides compounds of formula I useful as anti microbial agents wherein X, Y, R1, and n are as defined in thereof.
摘要翻译：本发明提供可用作抗微生物剂的式I化合物，其中X，Y，R 1和n如上所定义。

2. 发明授权

US06387896B1 Bicyclic oxazolidinones as antibacterial agents 失效
标题翻译：双环恶唑烷酮作为抗菌剂
公开(公告)号：US06387896B1
公开(公告)日：2002-05-14
申请号：US09572167
申请日：2000-05-17
申请人： Michael J. Genin , Michael Robert Barbachyn , Jackson B. Hester, Jr. , Paul D. Johnson
发明人： Michael J. Genin , Michael Robert Barbachyn , Jackson B. Hester, Jr. , Paul D. Johnson
IPC分类号： A61K3154
CPC分类号： C07D413/04
摘要： The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R1, R2 and n are as defined in thereof.
摘要翻译：本发明提供了可用作抗微生物剂的式I化合物，其中W，X，Y，R 1，R 2和n如在其中所定义。

3. 发明授权

US5708169A 5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl butyrolactone antibacterial agents 失效
标题翻译： 5-酰氨基甲基α，β-饱和和不饱和3-芳基丁内酯抗菌剂
公开(公告)号：US5708169A
公开(公告)日：1998-01-13
申请号：US708765
申请日：1996-09-05
申请人： Jackson B. Hester, Jr. , Steven Joseph Brickner , Michael Robert Barbachyn , Douglas K. Hutchinson , Dana Scott Toops
发明人： Jackson B. Hester, Jr. , Steven Joseph Brickner , Michael Robert Barbachyn , Douglas K. Hutchinson , Dana Scott Toops
IPC分类号： C07D307/58 , A61K31/00 , A61K31/34 , A61K31/341 , A61P31/00 , A61P31/04 , C07D307/28 , C07D307/52 , C07D413/10 , C07D307/33
CPC分类号： C07D307/58 , C07D307/28 , C07D307/52
摘要： The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) halogen atoms and substituted in the para position with, e.g., piperazinyl, thiomorpholinyl (and corresponding sulfoxide and sulfone), thiazolidinyl (and sulfoxide and sulfone), morpholinyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, azepinyl, troponyl, 3,7-diazabicyclo�3.3.0!octan-3-yl, bridged thiazinyl or bridged oxazinyl moieties. In those cases where a ring nitrogen is present, then this is substituted to form an amide, formamide, sulfonamide, urethane, or alkylated with a wide variety of moieties. These compounds are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci, as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.
摘要翻译：本发明提供式I的新的5-氨基甲基，α，β饱和和不饱和丁内酯抗菌剂，其特征在于3-芳基取代基，包括例如二氢吲哚基和被0（0）至二（2）个卤素原子并且在对位置被例如哌嗪基，硫代吗啉基（和相应的亚砜和砜），噻唑烷基（和亚砜和砜），吗啉基，氮杂环丁烷基，吡咯烷基，哌啶基，吡咯基，氮杂基，，7-二氮杂双环[3.3.0]辛-3-基，桥连噻嗪基或桥连的恶嗪基部分。在存在环状氮的情况下，将其取代形成酰胺，甲酰胺，磺酰胺，氨基甲酸酯或用各种部分烷基化。这些化合物对许多人类和兽医病原体有效，包括革兰氏阳性需氧细菌，如耐多发性葡萄球菌，链球菌和肠球菌，以及厌氧生物体如拟杆菌属。和梭菌属（Clostridia spp。）物种和耐酸生物，如结核分枝杆菌，鸟分枝杆菌和分枝杆菌，以及生物体如支原体属（Mycoplasma spp）。

4. 发明授权

US07049443B2 Amide-containing compound having improved solubility and method of improving the solubility of an amide-containing compound 失效
标题翻译：具有改善溶解性的含酰胺化合物和提高含酰胺化合物的溶解度的方法
公开(公告)号：US07049443B2
公开(公告)日：2006-05-23
申请号：US10194914
申请日：2002-07-12
申请人： Jackson B. Hester, Jr.
发明人： Jackson B. Hester, Jr.
IPC分类号： C07D263/04
CPC分类号： C07D263/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D411/10 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/10 , C07F9/653 , C07F9/65586 , F24C15/10
摘要： The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavailability of these oxazolidinone compounds is improved by improving the solubility thereof.
摘要翻译：本发明涉及具有改进的溶解性的新型含酰胺化合物和提高含酰胺化合物溶解度的方法。含酰胺的化合物包括恶唑烷酮化合物，并且通过改善这些恶唑烷酮化合物的溶解度来改善这些恶唑烷酮化合物的生物利用度。

5. 发明授权

US06362189B1 Oxazolidinone antibacterial agents having a thiocarbonyl functionality 失效
标题翻译：具有硫代羰基官能度的恶唑烷酮抗菌剂
公开(公告)号：US06362189B1
公开(公告)日：2002-03-26
申请号：US09712055
申请日：2000-11-14
申请人： Jackson B. Hester, Jr. , Eldon George Nidy , Salvatore Charles Perricone
发明人： Jackson B. Hester, Jr. , Eldon George Nidy , Salvatore Charles Perricone
IPC分类号： A61K31495
CPC分类号： C07D263/20 , C07D231/12 , C07D233/56 , C07D249/08 , C07D261/04 , C07D307/33 , C07D413/04 , C07D413/10 , C07D417/12 , C07D471/10
摘要： The present invention provides compounds of Formula 1 or pharmaceutical acceptable salts thereof wherein A, G and R1 are as defined in the claims which are antibacterial agents.
摘要翻译：本发明提供式1的化合物或其药学上可接受的盐，其中A，G和R 1如权利要求中所定义，其为抗菌剂。

6. 发明授权

US5155268A Antiarrhythmic N-aminoalkylene alkyl and aryl sulfonamides 失效
标题翻译：抗心律不齐的N-氨基亚烷基烷基和芳基磺酰胺
公开(公告)号：US5155268A
公开(公告)日：1992-10-13
申请号：US423499
申请日：1989-10-12
申请人： Jackson B. Hester, Jr.
发明人： Jackson B. Hester, Jr.
IPC分类号： C07C311/21 , C07D295/084 , C07D295/108 , C07D295/135 , C07D295/185
CPC分类号： C07D295/185 , C07C311/08 , C07D295/092 , C07D295/108 , C07D295/135
摘要： The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activity.
摘要翻译：本发明提供了新的磺酰苯胺和苯 - 烷基胺化合物，它们是利用新型中间体的方法的产物。新型化合物和新型中间体都可用于治疗或预防性治疗心律失常活性。

7. 发明授权

US4880781A Renin inhibitory peptides containing an N-alkyl-histidine moiety 失效
标题翻译：含有N-烷基 - 组氨酸部分的肾素抑制肽
公开(公告)号：US4880781A
公开(公告)日：1989-11-14
申请号：US147073
申请日：1988-01-20
申请人： Jackson B. Hester, Jr. , Suvit Thaisrivongs , Tomi K. Sawyer , Ruth E. TenBrink , Hossain H. Saneii , Heinrich J. Schostarez , Donald T. Pals
发明人： Jackson B. Hester, Jr. , Suvit Thaisrivongs , Tomi K. Sawyer , Ruth E. TenBrink , Hossain H. Saneii , Heinrich J. Schostarez , Donald T. Pals
IPC分类号： C07K5/02 , C12Q1/37 , G01N33/573 , G01N33/68
CPC分类号： C07K5/0227 , C12Q1/37 , G01N33/573 , G01N33/6893 , G01N2333/96472 , G01N2800/321 , Y10S530/86
摘要： The present invention provides novel renin-inhibiting peptides and novel processes and intermediates for the preparation of both novel and known renin-inhibiting peptide analogs. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.
摘要翻译：本发明提供新的肾素抑制肽和用于制备新型和已知的肾素抑制性肽类似物的新方法和中间体。这种抑制剂可用于诊断和控制肾素依赖性高血压。

8. 发明授权

US4444781A Process for inducing hypnosis 失效
标题翻译：诱发催眠的过程
公开(公告)号：US4444781A
公开(公告)日：1984-04-24
申请号：US447055
申请日：1982-12-06
申请人： Jackson B. Hester, Jr.
发明人： Jackson B. Hester, Jr.
IPC分类号： A61K31/55 , A61K31/41
CPC分类号： A61K31/55 , Y10S514/923
摘要： Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-chloro-1-methanol-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]-benzodiazepine compound of the formula: ##STR1## Including the N-oxides and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.
摘要翻译：用于治疗人和动物的治疗组合物包含以剂量单位形式的8-氯-1-甲醇-6-（邻氯苯基）-4H-三唑并[4,3-a] [1,4] - 苯并二氮杂化合物，其结构式如下：包括与药物载体结合的N-氧化物及其药学上可接受的酸加成盐。所述组合物可用作口腔，并提供诱导睡眠的过程。

9. 发明授权

US4180668A Piperidino-4H-s-triazolo[4,3-a][1,4]benzodiazepines 失效
标题翻译：哌啶基-4H-哒嗪并[4,3-a] [1,4]苯并二氮杂卓
公开(公告)号：US4180668A
公开(公告)日：1979-12-25
申请号：US804627
申请日：1977-06-08
申请人： Jackson B. Hester, Jr.
发明人： Jackson B. Hester, Jr.
IPC分类号： C07D249/08 , C07D487/04
CPC分类号： C07D249/08 , C07D487/04 , Y10S514/906
摘要： 6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety selected from the group consisting of pyrrolidino, piperidino, morpholino and 3,6-dihydro-1(2H)-pyridyl, and the pharmacologically acceptable salts thereof, are central nervous system depressant drugs which are useful in effective dosages in domestic and zoo animals for their calming and tranquilizing uses during shipment and to reduce aggressive behavior. In man these compounds are potentially useful for controlling anxiety and schizophrenia and for their sedative, muscle relaxant and anti-convulsant activity.
摘要翻译：其中R为氢或C 1至C 3 - 烷基，R 1为氢或卤素的6-氨基-4H-哒嗪并[4,3-a] [1,4]苯并二氮杂，其中R 2为氢或卤素，与它们所键合的氮原子一起形成选自吡咯烷子基，哌啶子基，吗啉代和3,6-二氢-1（2H） - 吡啶基的氮环部分，其药理学上可接受的盐是中枢神经系统抑制药物，可用于家畜和动物园动物的有效剂量，用于运送期间的镇静和镇静用途，并减少侵略行为。在这些化合物中，这些化合物可用于控制焦虑和精神分裂症以及其镇静，肌肉松弛和抗惊厥活性。

10. 发明授权

US4082761A Triazolo[4,3-a][1,4]benzodiazepinium quaternary salts 失效
标题翻译：三唑（4,3-A）+8 1,4）苯甲酸季铵盐
公开(公告)号：US4082761A
公开(公告)日：1978-04-04
申请号：US393940
申请日：1973-09-04
申请人： Jackson B. Hester, Jr.
发明人： Jackson B. Hester, Jr.
IPC分类号： A23K1/16 , C07D243/16 , C07D243/18 , C07D243/20 , C07D243/22 , C07D487/04
CPC分类号： C07D487/04 , C07D243/20 , C07D243/22
摘要： This invention relates to novel benzodiazepinium compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, hydroxy, mercapto, amino, monoalkylamino of 1 through 3 carbon atoms, arylamino wherein the aryl moiety is selected from the group consisting of unsubstituted and monosubstituted phenyl and naphthyl, alkanoylamino of 1 through 4 carbon atoms, aroylamino wherein the aroyl moiety is selected from the group consisting of unsubstituted and monosubstituted benzoyl and naphthoyl, alkanesulfonamido of 1 through 3 carbon atoms, and arylsulfonamido wherein the aryl moiety is selected from the group consisting of unsubstituted and monosubstituted phenyl and naphthyl; R.sub.1 is lower alkyl of 1 through 3 carbon atoms; R.sub.2 is selected from the group consisting of hydrogen and lower alkyl of 1 through 3 carbon atoms; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, halogen, nitro, trifluoromethyl, cyano, lower alkoxy of 1 through 3 carbon atoms and lower alkylthio of 1 through 3 carbon atoms; X.sup..crclbar. is an anion derived from a pharmacologically acceptable acid addition salt; .sup..sym. is the cation of the compound. The new compounds of Formulae VI, VII, VIII, IX, X and XI, set forth below, are included within generic Formula XIII, above. The invention also relates to inner salt compounds of the formula ##STR2## wherein Y is selected from the group consisting of hydroxy, mercapto and monosubstituted amino having an electronegative substituent selected from the group consisting of arylamino, alkanoylamino, aroylamino, alkanesulfonamide and arylsulfonamide, said terms, as well as R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and .sup..sym., having the same meaning as above, and .sup..crclbar. appearing above Y indicates that the compound is an inner salt. The invention also includes novel intermediates (III) for the production of the novel compounds of Formulae IV through XI having the formula ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 have the same meaning as above. It further relates to novel compounds (XII) prepared from those of Formula VII (wherein R' is hydrogen) and having the formula ##STR4## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 have the same meaning as above. It also relates to processes for the preparation of the novel compounds of Formulae II through XII. The systemic administration to humans and animals of the new products of Formulae IV through XII depresses their central nervous systems.

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