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11. 发明授权

US07470797B2 Fused heterocyclic imido and amido compounds 有权
标题翻译：稠合杂环亚氨基和酰氨基化合物
公开(公告)号：US07470797B2
公开(公告)日：2008-12-30
申请号：US10917031
申请日：2004-08-12
申请人： Mark E. Salvati , Raj N. Misra
发明人： Mark E. Salvati , Raj N. Misra
IPC分类号： C07D313/06
CPC分类号： C07D487/18 , A61K31/00 , A61K31/403 , A61K31/407 , A61K31/655 , A61K31/675 , A61K45/06 , C07B2200/11 , C07D401/08 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/18 , C07D491/22 , C07D495/08 , C07D495/18 , C07D519/00 , C40B40/00 , A61K2300/00
摘要： Disclosed are fused cyclic compounds, method of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds of formula Also disclosed are fused heterocyclic imido and amido compounds of formula and stereoisomers thereof. The groups G, L, Z1, Z2, Q1, Q2, A1, A2, Y′, and W′ are defined herein.
摘要翻译：公开了稠合环状化合物，使用这些化合物治疗核激素受体相关病症如癌症和免疫疾病的方法，以及含有这些式I化合物的药物组合物。还公开了式及其立体异构体的稠合杂环亚氨基和酰氨基化合物。组G，L，Z1，Z2，Q1，Q2，A1，A2，Y'和W'在本文中定义。

12. 发明授权

US07312200B2 9-ketospinosyn derivatives 失效
标题翻译： 9-酮基链鸟苷衍生物
公开(公告)号：US07312200B2
公开(公告)日：2007-12-25
申请号：US10541442
申请日：2004-01-08
申请人： Olga Malsam , Peter Lösel , Michael E. Beck , Ulrich Ebbinghaus-Kintscher , Robert Velten , Peter Jeschke , Volker Möhrle , Rita Fröde , Günther Eberz
发明人： Olga Malsam , Peter Lösel , Michael E. Beck , Ulrich Ebbinghaus-Kintscher , Robert Velten , Peter Jeschke , Volker Möhrle , Rita Fröde , Günther Eberz
IPC分类号： A61K31/70 , C07D313/06 , C07H17/08
CPC分类号： C07D315/00 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07H17/08
摘要： The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ═N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests.
摘要翻译：本发明涉及9-酮基多杀菌素的衍生物，其被C-（O，NH或NR x） - R y部分取代， 9，其制造方法及其用于控制动物害虫的用途。

13. 发明授权

US06953782B2 11-C-substituted erythromycin derivatives 有权
标题翻译： 11-C-取代的红霉素衍生物
公开(公告)号：US06953782B2
公开(公告)日：2005-10-11
申请号：US10745856
申请日：2003-12-24
申请人： Ly Tam Phan , Yat Sun Or , Jay Judson Farmer
发明人： Ly Tam Phan , Yat Sun Or , Jay Judson Farmer
IPC分类号： A61K31/365 , A61K31/70 , A61K31/7048 , C07D313/00 , C07D313/06 , C07D313/20 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention discloses compounds of formulae I, II, III or IV or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
摘要翻译：本发明公开了式I，II，III或IV的化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。本发明还包括制备本发明化合物的方法。

14. 发明授权

US06911547B1 Process for the preparation of bicyclic diketone salts 失效
标题翻译：双环二酮盐的制备方法
公开(公告)号：US06911547B1
公开(公告)日：2005-06-28
申请号：US10408950
申请日：2003-04-08
申请人： Hermann Schneider , Christoph Lüthy
发明人： Hermann Schneider , Christoph Lüthy
IPC分类号： C07D311/94 , C07B61/00 , C07C45/51 , C07C45/57 , C07C45/60 , C07C49/443 , C07C49/733 , C07D311/00 , C07D313/06 , C07D313/08 , C07D313/02 , C07C45/27
CPC分类号： C07D311/00 , C07C45/511 , C07C45/57 , C07C45/60 , C07C49/443 , C07C49/733 , C07D313/06 , Y02P20/582
摘要： The present invention relates to a process for the preparation of bicyclic 1,3-diketone salts of formula I wherein R1, R2, R3 and R4 are each independently of the others hydrogen or C1-C4alkyl; A and E are each independently of the other C1-C2alkylene, which may be substituted once or up to four times by a C1-C4alkyl group, and M+is an alkali metal ion, alkaline earth metal ion or ammonium ion, by oxidation of a compound of formula II to a compound of formula III and subsequent conversion to a compound of formula I either in the presence of a base and a catalytic amount of a cyanide or in the presence of an alkali metal alcoholate or alkaline earth metal alcoholate, and to novel bicyclic enol lactone intermediates of formula III for use in that process.
摘要翻译：本发明涉及一种制备式I的双环1,3-二酮盐的方法，其中R 1，R 2，R 3， >和R 4各自独立地为氢或C 1 -C 4烷基; A和E各自独立于另一个C 1 -C 2亚烷基，其可以被C 1〜N取代一次或多达四次 > -C 4烷基，M + S是碱金属离子，碱土金属离子或铵离子，通过将式II化合物氧化成式式III化合物，随后在碱和催化量的氰化物的存在下或在碱金属醇盐或碱土金属醇化物的存在下转化为式I化合物，以及式III的新型双环烯醇内酯中间体用于该过程。

15. 发明申请

US20030148210A1 Polymer for photoresist and resin compositions therefor 有权
标题翻译：用于光致抗蚀剂的聚合物及其树脂组合物
公开(公告)号：US20030148210A1
公开(公告)日：2003-08-07
申请号：US10239051
申请日：2002-09-19
发明人： Yoshinori Funaki , Kiyoharu Tsutsumi , Keizo Inoue , Tomoko Adachi
IPC分类号： G03F007/039 , C08F020/28 , C07D35/14 , C07D37/93 , C07D311/94 , C07D313/06 , C07D313/20
CPC分类号： G03F7/0395 , G03F7/0397 , Y10S430/109
摘要： A polymeric compound for photoresist of the invention includes at least one monomer unit represented by following Formula (I): 1 wherein R1, R2, R3, R4 and R5 are the same or different and are each a hydrogen atom or a methyl group; m, p and q each denote an integer of from 0 to 2; and n denotes 0 or 1, where the hydroxyl group and carbonyloxy group extending from a principle chain in the formula are independently combined with either of two carbon atoms on the far-left portion of the rings. By using the polymeric compound for photoresist as a base of a photoresist, the resulting photoresist exhibits well-rounded adhesion to substrates and resistance to etching.
摘要翻译：本发明光致抗蚀剂的高分子化合物包括至少一种由下式（I）表示的单体单元：其中R1，R2，R3，R4和R5相同或不同，各自为氢原子或甲基; m，p和q分别表示0〜2的整数。并且n表示0或1，其中从式中的主链延伸的羟基和羰氧基独立地与环的最左部分的两个碳原子中的任一个结合。通过使用光致抗蚀剂的高分子化合物作为光致抗蚀剂的基底，所得到的光致抗蚀剂表现出对基底的良好的圆形粘附性和耐蚀刻性。

16. 发明申请

US20020128290A1 DERIVATIVES OF BENZOFURAN OR BENZODIOXOLE 失效
标题翻译：苯唑或BENZODIOXOLE的衍生物
公开(公告)号：US20020128290A1
公开(公告)日：2002-09-12
申请号：US08974739
申请日：1997-11-19
发明人： ETSUO OHSHIMA , TAKASHI KAWAKITA , KOJI YANAGAWA , KYOICHIRO IIDA , RIE KOIKE , YOSHISUKE NAKASATO , TOHRU MATSUZAKI , KENJI OHMORI , SOICHIRO SATO , HIDEE ISHII , HARUHIKO MANABE , MICHIO ICHIMURA , FUMIO SUZUKI
IPC分类号： A61K031/33 , A61K031/44 , C07D307/94 , C07D311/96 , C07D313/06 , C07D313/16 , C07D307/87 , C07D307/93 , C07D307/78
CPC分类号： C07D307/79 , C07D307/94 , C07D405/06 , C07D405/12 , C07D405/14
摘要： An oxygen-containing heterocyclic compound represented by following Formula (I): 1 wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, null(CH2)nnullE1nullCOnullG1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents nullC(R9)(R10)null or O; B represents O, NR11, nullC(R12)(R13)null, or nullC(R14)(R15)nullC(R16)(R17)null; D represents (i) nullC(R18)(R19)nullXnull (wherein X represents nullC(R21)(R22)null, S, or NR23), (ii) nullC(R19a)nullYnull nullY represents nullC(R24)nullZnull (wherein Z represents CONH, CONHCH2, or a bond), or Nnull, or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.
摘要翻译：由下式（I）表示的含氧杂环化合物：其中R1和R2独立地表示氢，低级烷基，氰基， - （CH2）n-E1-CO-G1（其中E1表示键，O或NH; 并且G 1表示氢，取代或未取代的低级烷基，OR 6或NR 7 R 8; n表示0〜4的整数）等。 R 1和R 2组合在一起，与邻近的碳原子一起代表饱和碳环; 或R 2，R 11或R 13组合形成单键; R3表示氢，苯基或卤素; R4代表羟基，低级烷氧基等; A表示-C（R 9）（R 10） - 或O; B表示O，NR 11，-C（R 12）（R 13） - 或-C（R 14）（R 15）-C（R 16）（R 17） - ; D表示（i）-C（R 18）（R 19）-X-（其中X表示-C（R 21）（R 22） - ，S或NR 23），（ⅱ）-C（R 19a）= Y- [Y -C（R 24）-Z-（其中Z表示CONH，CONHCH 2或键）或N]或（iii）键; R5表示芳基，芳香族杂环基，环烷基，吡啶-N-氧化物，氰基或低级烷氧基羰基; 或其药学上可接受的盐。

17. 发明申请

US20020115654A1 New compounds, their preparation and use 失效
公开(公告)号：US20020115654A1
公开(公告)日：2002-08-22
申请号：US10042051
申请日：2001-10-25
发明人： Lone Jeppesen , Paul Stanley Bury , Per Sauerberg
IPC分类号： A61K031/55 , C07D337/06 , C07D313/06
CPC分类号： C07D311/82 , C07C59/72 , C07C69/734 , C07C2603/18 , C07C2603/32 , C07D313/12 , C07D321/12 , C07D327/08
摘要： The present invention relates to compounds of the general formula (I) 1 The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

18. 发明授权

US6011058A Seco-cholestane derivatives and methods of making the same 失效
标题翻译：山梨醇胆固醇衍生物及其制备方法
公开(公告)号：US6011058A
公开(公告)日：2000-01-04
申请号：US158656
申请日：1998-09-22
申请人： Leon H. Zalkow , Hairuo Peng
发明人： Leon H. Zalkow , Hairuo Peng
IPC分类号： C07C255/31 , C07D307/16 , C07D311/94 , A61K31/335 , C07D313/06
CPC分类号： C07D311/94 , C07C255/31 , C07D307/16 , C07B2200/07 , C07B2200/09 , C07C2102/24
摘要： The present invention is directed to novel seco-cholestane derivatives, as well as to pharmaceutical compositions thereof, and methods of making the same. More particularly, the invention relates to C5- and C8-substituted seco-cholestane derivatives. The compounds of the invention can exhibit CDC25 phosphatase inhibition properties and anti-cancer activity.
摘要翻译：本发明涉及新型的分离型胆甾醇衍生物及其药物组合物及其制备方法。更具体地说，本发明涉及C5-和C8-取代的次 - 胆甾烷衍生物。本发明的化合物可以显示CDC25磷酸酶抑制性质和抗癌活性。

19. 发明授权

US5780287A Photoactivated antiviral and antitumor compositions 失效
公开(公告)号：US5780287A
公开(公告)日：1998-07-14
申请号：US474000
申请日：1995-06-07
申请人： George A. Kraus , Susan L. Carpenter , Jacob W. Petrich
发明人： George A. Kraus , Susan L. Carpenter , Jacob W. Petrich
IPC分类号： C12N15/09 , A61K31/335 , A61K31/41 , A61K31/425 , A61K38/00 , A61K38/46 , A61K41/00 , A61K45/08 , A61K48/00 , A61P31/12 , C07D277/64 , C07D277/68 , C07D313/06 , C07D417/04 , C07H21/04 , C12N5/10 , C12N9/02 , C12N7/04 , C12N7/06
CPC分类号： C07D277/68 , A61K41/0019 , A61K41/0057 , C07D277/64 , C07D313/06 , C07D417/04 , C12N9/0069 , A01K2217/05 , A61K38/00 , A61K48/00 , C12N2799/027
摘要： Disclosed herein are compounds, compositions, and methods to inactivate a virus and destroy tumor cells. The methods involve the addition into the cell of a compound containing a photosensitizing chemical and an energy donating chemical, optionally linked by a chemical tether. Also introduced into the cell are means to chemically activate the energy donating chemical which photoactivates the photosensitizing chemical which then destroys the tumor or virus. The photosensitizing chemical is preferably hypericin, porphyrin, or an analog and the energy donating chemical is preferably luciferin or an analog. Methods for synthesizing the chemicals are also disclosed. Further, the energy donating chemical is activated by an activating chemical. The expression of the activating chemical is regulated so as to target the virus-infected or tumor cells. Regulating the activating chemical is accomplished by a number of methods including construction of an expression plasmid containing a gene encoding the activating chemical under control of a promoter which is transactivated by replication of the virus or transactivated by elevated levels of proteins expressed in tumor cells.

20. 发明授权

US5731293A Esculetin derivatives, method for manufacture thereof, and pharmaceutical composition 失效
标题翻译： Esculetin衍生物，其制备方法和药物组合物
公开(公告)号：US5731293A
公开(公告)日：1998-03-24
申请号：US580364
申请日：1995-12-28
申请人： Koju Watanabe , Koichi Niimura , Toru Yamazaki , Hiroshi Maruoka
发明人： Koju Watanabe , Koichi Niimura , Toru Yamazaki , Hiroshi Maruoka
IPC分类号： C12N9/99 , A61K31/365 , A61K31/535 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/02 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P29/00 , A61P43/00 , C07D311/16 , C07H1/00 , C07H17/075 , A61K31/35 , C07D313/06 , C07H15/24
CPC分类号： C07H17/075 , C07D311/16
摘要： A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CON(R.sup.4)R.sup.5, or a monosaccharide, or acylated monosaccharide group, with the proviso that at least one of R.sup.1 and R.sup.2 is --CON(R.sup.4)R.sup.5, and R.sup.4 and R.sup.5 are, independently, a hydrogen atom, or a hydroxyl, alkyl, aryl, or aralkyl group, or R.sup.4 and R.sup.5 together with the nitrogen atom attached thereto form a 3- to 7-membered saturated cycloaliphatic amino group, and R.sup.3 is a hydrogen atom, or a hydroxyl, alkyl, aryl, aralkyl, or --COOR.sup.8 group, and R.sup.3 is at 3- or 4-position, and R.sup.8 is a hydrogen atom or an alkyl group, or a salt thereof is disclosed. The compound has a function to inhibit a matrix metalloproteinase.
摘要翻译：式（I）的化合物：其中R 1和R 2独立地为-CON（R 4）R 5，或单糖或酰化单糖基团，条件是R 1和R 2中的至少一个是-CON（R4）R5，R4和R5独立地是氢原子或羟基，烷基，芳基或芳烷基，或R4和R5与连接的氮原子一起形成3-至7- R 3为氢原子或羟基，烷基，芳基，芳烷基或-COOR 8基，R 3为3-或4-位，R 8为氢原子或烷基，或其盐。该化合物具有抑制基质金属蛋白酶的功能。

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