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1. 发明授权

US4824868A Propylamine derivatives useful for the treatment of dementia 失效
标题翻译：用于治疗痴呆症的丙胺衍生物
公开(公告)号：US4824868A
公开(公告)日：1989-04-25
申请号：US74581
申请日：1987-07-17
申请人： Jeffrey W. H. Watthey
发明人： Jeffrey W. H. Watthey
IPC分类号： C07C227/08 , C07C227/16 , C07D295/084 , A61K31/135
CPC分类号： C07D295/092 , C07C227/08 , C07C227/16 , Y10S514/878 , Y10S514/879
摘要： Disclosed are e.g. certain novel 2-benzyl-3-(substituted)-phenoxypropylamines, their methods of synthesis and pharmaceutical compositions. Said compounds are useful as potent and centrally active serotonin uptake inhibitors for the treatment of psychotropic disorders, particularly depression.
摘要翻译：例如，某些新的2-苄基-3-（取代的） - 苯氧基丙胺，其合成方法和药物组合物。所述化合物可用作治疗精神病症，特别是抑郁症的有效和中枢活性的5-羟色胺摄取抑制剂。

2. 发明授权

US5925367A Pest control with UV blockers and pheromones 失效
标题翻译：害虫控制与紫外线阻断剂和信息素
公开(公告)号：US5925367A
公开(公告)日：1999-07-20
申请号：US376132
申请日：1995-01-19
申请人： Max Angst , Fran.cedilla.ois Gugumus , Gunther Rist , Manfred Vogt , Jean Rody
发明人： Max Angst , Fran.cedilla.ois Gugumus , Gunther Rist , Manfred Vogt , Jean Rody
IPC分类号： A01N25/10 , A01N25/18 , A01N25/22 , A01N25/24
CPC分类号： A01N25/18 , A01N25/22 , A01N25/24 , Y10S514/972
摘要： A composition for controlling harmful insects and representatives of the order Acarina, containing as biologically active components a) a substance that modifies the behavior of the pests and b) at least one pesticidally active compound, wherein the biologically active components are contained in a flowable or viscous non-hardening matrix that is resistant to water and weather, is protected against light and is suitable for distribution in the form of droplets or droplet-like units or spots that adhere to a substrate, by means of which matrix the behavior-modifying substance is protected against UV radiation and from which it is slowly released in a biologically effective amount over a prolonged period, and wherein the pesticidally active compound can be taken up in a pesticidally effective amount from the surface of the droplets or droplet-like units or spots by the pests to be controlled; as well as a method of controlling the said pests, especially plant-destructive insects.
摘要翻译：用于控制有害昆虫的组合物和含有作为生物活性组分的蜱螨纲的代表a）改变害虫行为的物质和b）至少一种杀虫活性化合物，其中生物活性成分包含在可流动或耐水和耐候性的粘性非硬化基质被防光，适用于以液滴或液滴状单元或粘附于基底的斑点的形式分布，借助于此基质，行为修饰物质受到紫外线辐射的保护，并在长时间内以生物有效的量缓慢释放，并且其中杀虫活性化合物可以从液滴或液滴样单元或斑点的表面以杀虫有效量摄取由害虫控制; 以及控制所述害虫，特别是植物破坏性昆虫的方法。

3. 发明授权

US5837499A DNA encoding C5A receptor antagonists having substantially no agonist activity and methods of expressing same 失效
标题翻译：编码具有基本上没有激动剂活性的C5A受体拮抗剂的DNA及其表达方法
公开(公告)号：US5837499A
公开(公告)日：1998-11-17
申请号：US463377
申请日：1995-06-05
申请人： Jan van Oostrum , William C. Boyar , Nicholas G. Galakatos , Albert Schmitz , Gino Van Heeke
发明人： Jan van Oostrum , William C. Boyar , Nicholas G. Galakatos , Albert Schmitz , Gino Van Heeke
IPC分类号： G01N33/566 , A61K38/00 , A61K39/395 , A61P1/00 , A61P1/16 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P19/06 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/06 , A61P43/00 , C07H21/04 , C07K14/47 , C07K16/18 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12R1/19 , C12P21/00 , C07K14/435
CPC分类号： C07K14/472 , C07K16/18 , A61K38/00 , C07K2319/00
摘要： Disclosed are polypeptide analogues of human C5a which are C5a receptor antagonists that exhibit substantially no analphylatoxin or agonist activity, and derivatives of the analogues, and dimeric forms of the analogues or derivatives. DNA molecules encoding the polypeptides and methods of making the analogues are also provided. Pharmaceutical formulations containing a C5a analogue, are used therapeutically in the treatment of C5a-mediated diseases and inflammatory conditions in mammals, and prophylactically to prevent or reduce inflammation caused by an event which causes inflammation or aggravates an existing inflammatory condition, respectively. Further disclosed are antibodies specific to the C5a analogues, derivatives thereof, and dimers of the analogues and derivatives which exhibit substantially no cross-reactivity with human C5a. The antibodies are used to detect or quantify circulating C5a analogue or derivative, as well as to modify, e.g., neutralize, the activity of the C5a receptor antagonist in vivo.
摘要翻译：公开了人C5a的多肽类似物，其是显示基本上没有分泌毒素或激动剂活性的C5a受体拮抗剂，以及类似物的衍生物和类似物或衍生物的二聚体形式。还提供了编码多肽的DNA分子和制备类似物的方法。含有C5a类似物的药物制剂在治疗中用于治疗哺乳动物中C5a介导的疾病和炎性病症，并预防性地预防或减少由引起炎症或加重现有炎性病症的事件引起的炎症。进一步公开的是对C5a类似物，其衍生物和类似物和衍生物的二聚体特异的抗体，其表现出与人C5a基本上没有交叉反应性。所述抗体用于检测或定量循环C5a类似物或衍生物，以及修饰，例如中和体内C5a受体拮抗剂的活性。

4. 发明授权

US5728676A Use of insulin-like growth factors I and II for inhibition of inflammatory response 失效
标题翻译：使用胰岛素样生长因子I和II抑制炎症反应
公开(公告)号：US5728676A
公开(公告)日：1998-03-17
申请号：US444849
申请日：1995-05-19
申请人： Philip F. Halloran
发明人： Philip F. Halloran
IPC分类号： A61K38/27 , A61K38/00 , A61P1/16 , A61P9/00 , A61P29/00 , A61P43/00 , C07K14/65 , C12N15/12 , F04B35/04 , F04B39/00 , F04B39/10 , C07K5/00 , A61K37/26
CPC分类号： C07K14/65 , F04B39/0016 , F04B39/1073 , A61K38/00 , Y10T137/7892
摘要： The present invention relates to methods for using IGF as inhibitors of inflammatory response, ischemic injury, and organ rejection.
摘要翻译：本发明涉及使用IGF作为炎性反应，缺血性损伤和器官排斥抑制剂的方法。

5. 发明授权

US5708148A Process for the production and refolding of unfused IGF-II protein in E. coli 失效
标题翻译：在大肠杆菌中生产和重折叠未融合的IGF-II蛋白的方法
公开(公告)号：US5708148A
公开(公告)日：1998-01-13
申请号：US341275
申请日：1994-11-16
申请人： Albert Schmitz , Walter Marki
发明人： Albert Schmitz , Walter Marki
IPC分类号： C12N15/02 , A61K38/00 , A61K38/27 , C07K1/113 , C07K1/14 , C07K1/20 , C07K14/575 , C07K14/62 , C07K14/65 , C12N1/21 , C12N15/09 , C12N15/16 , C12N15/17 , C12N15/73 , C12P21/02 , C12R1/19 , C12N15/18
CPC分类号： C12N15/73 , C07K14/65 , A61K38/00
摘要： A process for the preparation of a recombinant IGF-II (rIGF-II) without a covalently attached foreign protein moiety and without N-terminal attached methionine or a derivative of methionine or of a salt of said IGF-II, rIGF-II produced by said method, hybrid vectors comprising DNA encoding said rIGF-II, hosts transformed with said vectors, and a process for the isolation of said rIGF-II from the host cell and refolding it into a biologically active form.
摘要翻译：制备不具有共价连接的外来蛋白质部分并且不具有N-末端连接的甲硫氨酸或甲硫氨酸衍生物或所述IGF-II，rIGF-II的盐的重组IGF-II（rIGF-II）的制备方法，所述方法由所述方法，包含编码所述rIGF-II的DNA的混合载体，用所述载体转化的宿主，以及从宿主细胞中分离所述rIGF-II并将其重折叠成生物活性形式的方法。

6. 发明授权

US5693807A Substituted hydroquinone derivatives 失效
标题翻译：取代氢醌衍生物
公开(公告)号：US5693807A
公开(公告)日：1997-12-02
申请号：US465628
申请日：1995-06-05
申请人： Gottfried Sedelmeier , Gerhard Fischer
发明人： Gottfried Sedelmeier , Gerhard Fischer
IPC分类号： C07D211/62 , C07D405/04 , C07F9/59 , C07D211/32
CPC分类号： C07D405/04 , C07D211/62 , C07F9/592
摘要： The invention relates to substituted hydroquinone derivatives of the general formula I ##STR1## wherein R.sub.4 is lower alkyl and either R.sub.1 is hydroxy, halogen, a group of the formula --P(=O)(R.sub.5)R.sub.6 (Ia), a group of the formula --P.sup.+ (R.sub.7)(R.sub.8)R.sub.9 X.sup.- (Ib) or a group of the formula --Si(R.sub.7)(R.sub.8)R.sub.9 (Ic), M is methylene, R.sub.2 is hydrogen or a group of the formula ##STR2## and R.sub.3 is hydrogen or halogen, or .sub.1 is hydroxy or lower alkoxy, M is carbonyl, R.sub.2 is hydrogen and R.sub.3 is halogen, each of R.sub.5 and R.sub.6, independently of the other, is lower alkyl, lower alkoxy Or N,N-di-lower alkylamino, or is benzyl, benzyloxy, phenyl or phenoxy, each of which is unsubstituted or mono- or di-substituted at the phenyl ring, to a process for the preparation of those compounds and to the use of those compounds, and to a process in which those compounds are used.
摘要翻译：本发明涉及通式Ⅰ（I）的取代氢醌衍生物，其中R 4是低级烷基，R 1是羟基，卤素，式-P（= O）（R 5）R 6（Ia）的基团，式 - +（R7）（R8）R9X-（Ib）或式-Si（R7）（R8）R9（Ic）的基团，M是亚甲基，R2是氢或式（Id），R 3为氢或卤素，或1为羟基或低级烷氧基，M为羰基，R 2为氢，R 3为卤素，R 5和R 6各自独立地为低级烷基，低级烷氧基或N，N-二低级烷基氨基，或苄基，苄氧基，苯基或苯氧基，其中每个在苯环上未被取代或单取代或二取代，制备这些化合物的方法和使用的那些化合物，以及使用这些化合物的方法。

7. 发明授权

US5688815A Hydroxypyridinones 失效
标题翻译：羟基吡啶酮
公开(公告)号：US5688815A
公开(公告)日：1997-11-18
申请号：US722820
申请日：1996-09-27
申请人： Paul Zbinden
发明人： Paul Zbinden
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4425 , A61K31/443 , A61K31/535 , A61P1/16 , A61P3/00 , A61P7/06 , C07D213/69 , C07D213/81 , C07D405/06 , C07D409/06 , C07D498/04 , C07D211/94
CPC分类号： C07D405/06 , C07D213/69 , C07D409/06
摘要： Described are 3-hydroxypyridin-4-ones of formula I ##STR1## wherein R.sub.1 -R.sub.4, A and B are as defined in the description. The compounds have valuable pharmaceutical properties and are especially effective as chelators of iron. They can be used to treat excess iron in the bodies of warm-blooded animals.
摘要翻译：描述了式I的3-羟基吡啶-4-酮其中R 1 -R 4，A和B如说明书中所定义。这些化合物具有有价值的药物性质，并且作为铁的螯合剂是特别有效的。它们可用于治疗温血动物体内的多余铁。

8. 发明授权

US5686484A Milbemycin derivatives, their preparation and their use 失效
标题翻译：米尔霉素衍生物，其制备及其用途
公开(公告)号：US5686484A
公开(公告)日：1997-11-11
申请号：US396662
申请日：1995-03-01
申请人： Yasuhiro Morisawa , Akio Saito , Satoru Naito , Toshimitsu Toyama , Susumu Kaneko , Louis-Pierre Molleyres , Jean-Claude Gehret
发明人： Yasuhiro Morisawa , Akio Saito , Satoru Naito , Toshimitsu Toyama , Susumu Kaneko , Louis-Pierre Molleyres , Jean-Claude Gehret
IPC分类号： A01N43/90 , C07D493/22 , C07H19/01 , A61K31/335 , C07D315/00
CPC分类号： C07D493/22 , A01N43/90 , C07H19/01
摘要： Compounds of formula (I): ##STR1## and of formula (I).sub.w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen atoms, halogen atoms, alkyl groups having from 1 to 4 carbon atoms, and alkoxy groups having from 1 to 4 carbon atoms; R.sup.1, R.sub.w.sup.1 and R.sub.w.sup.2 are, for example, hydrogen, halogen, cyano, nitro, optically substituted alkyl, alkoxy or alkoxyalkoxy; X or X.sub.w is hydroxy, alkanoyloxy, substituted alkanoyloxy or hydroxyimino; R.sup.3.sub.w and R.sup.4.sub.w are each hydrogen, alkyl or alkoxy; R.sup.5 and R.sup.5.sub.w are methyl, ethyl, isopropyl or sec-butyl; and salts thereof have valuable anthelmintic, acaricidal and insecticidal activities.
摘要翻译：式（I）化合物：其中：A表示具有下式之一的基团：CHR 2 CHR 3 CHR 4 CR 2 CR 3 CHR 4或（I）其中R 2，R 3和R 4独立地选自氢原子，卤素原子，具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基; R1，Rw1和Rw2是例如氢，卤素，氰基，硝基，光学取代的烷基，烷氧基或烷氧基烷氧基; X或Xw是羟基，烷酰氧基，取代的烷酰氧基或羟基亚氨基; R3w和R4w各自为氢，烷基或烷氧基; R5和R5w是甲基，乙基，异丙基或仲丁基; 其盐具有宝贵的驱虫，杀螨和杀虫活性。

9. 发明授权

US5675004A Red-shifted tris-aryl-S-triazines 失效
标题翻译：红移三芳基-S-三嗪
公开(公告)号：US5675004A
公开(公告)日：1997-10-07
申请号：US463569
申请日：1995-06-02
申请人： Tyler Arthur Stevenson
发明人： Tyler Arthur Stevenson
IPC分类号： C07D251/12 , A61K31/53 , C07D251/24 , C07D401/12 , C07D405/12 , C07F9/6558 , C08K5/3492 , C09D5/00 , C09D5/32 , C09D201/00 , C09K3/00
CPC分类号： C07D251/24 , C08K5/3492
摘要： Tris-aryl-s-triazines of formula V ##STR1## which contain from one one to three resorcinol derived moieties with at least one of said moieties substituted in the 5-position with a group such as, for example, alkyl or phenylalkyl have UV spectra which are red-shifted to the near UV range and provide excellent stabilization to polymeric substrates against the deleterious effects of actinic light.
摘要翻译：式V的三芳基-s-三嗪含有一个至三个间苯二酚衍生部分，其中至少一个所述部分在5-位被一个基团例如烷基或苯基烷基取代，紫外光谱被红色偏移到近紫外范围，并且提供对聚合物底物的极好的稳定性，以抵抗光化光的有害影响。

10. 发明授权

US5674852A Water-soluble retinoids 失效
标题翻译：水溶性类视色素
公开(公告)号：US5674852A
公开(公告)日：1997-10-07
申请号：US318870
申请日：1994-10-18
申请人： Thomas Maier , Helmut Luther
发明人： Thomas Maier , Helmut Luther
IPC分类号： C07C65/00 , A61K8/00 , A61K8/60 , A61K31/70 , A61K31/7024 , A61K49/00 , A61P17/00 , A61P17/06 , A61P17/10 , A61P35/00 , A61Q17/04 , A61Q19/00 , C07C69/00 , C07H13/04 , C07H13/06 , C07H1/00 , C07H15/00
CPC分类号： A61Q19/00 , A61K8/671 , A61Q17/04 , C07H13/06
摘要： The present invention relates to novel water-soluble sugar retinoids in which the sugar radical carries at least one sulfate group, and to their preparation and use thereof as medicaments and in cosmetic sector.
摘要翻译： PCT No.PCT / EP93 / 00878 Sec。 371日期：1994年10月18日 102（e）日期1994年10月18日PCT 1993年4月10日PCT公布。公开号WO93 / 21195 日期：1993年10月28日本发明涉及新的水溶性糖类维生素A，其中糖基含有至少一个硫酸基，并且其制备和用途作为药物和化妆品部分。

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