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1. 发明授权

US06380207B2 Glucocortiocoid-selective antiinflammatory agents 失效
标题翻译：糖皮质激素选择性抗炎药
公开(公告)号：US06380207B2
公开(公告)日：2002-04-30
申请号：US09023913
申请日：1998-02-13
申请人： Michael J. Coghlan , James P. Edwards , Todd K. Jones , Michael E. Kort
发明人： Michael J. Coghlan , James P. Edwards , Todd K. Jones , Michael E. Kort
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor in a mammal and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.
摘要翻译：具有式I的化合物可用于部分或完全拮抗，抑制，激动或调节哺乳动物的糖皮质激素受体并治疗哺乳动物的免疫，自身免疫和炎性疾病。还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

2. 发明授权

US06642248B2 Benzo[b]pyrano[3,2-h]acridin-7-one compounds 失效
标题翻译：苯并[b]吡喃并[3,2-h]吖啶-7-酮化合物
公开(公告)号：US06642248B2
公开(公告)日：2003-11-04
申请号：US10205566
申请日：2002-07-25
申请人： Michel Koch , François Tillequin , Sylvie Michel , Elisabeth Seguin , Abdelhakim El Omri , John Hickman , Alain Pierre , Bruno Pfeiffer , Pierre Renard
发明人： Michel Koch , François Tillequin , Sylvie Michel , Elisabeth Seguin , Abdelhakim El Omri , John Hickman , Alain Pierre , Bruno Pfeiffer , Pierre Renard
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH— or —C(O)—CH(R8)— wherein R5, R6, R7 and R8 are as defined in the description, their isomers and N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.
摘要翻译：选自式（I）的化合物：其中：X和Y表示选自氢，卤素，巯基，氰基，硝基，烷基，三卤代烷基，三卤代烷基羰基氨基，-OR a，-NR a R b，-NR a -C（O） - T1，-OC（O）-T1，-O-T2-NRaRb，-O-T2-ORa，-NRa-T2-NRaRb，-NRa-T2-ORa和-NRa-T2-CO2Ra，其中Ra，Rb，T1 ，T 2如说明书中所定义，R 1表示氢或烷基，R 2表示选自氢，-OR a，-NR a R b，-NR a -C（O）-T1，-OC（O）-T1，-O- R2-NRaRb，-O-T2-ORa，-NRa-T2-NRaRb，-NRa-T2-ORa和-NRa-T2-CO2Ra，其中Ra，Rb，T1和T2如上所定义，R3和R4代表氢或烷基，W表示式-CH（R 5）-CH（R 6） - ， - CH = C（R 7） - ， - C（R 7）= CH-或-C（O）-CH（R 8） R5，R6，R7和R8如说明书中所定义，它们的异构体和N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物，可用于治疗癌症。

3. 发明授权

US06599915B2 Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxinol[2,3f]quinoline 失效
标题翻译： 2,3-二氢-1,4-二氧杂环己烯并[2,3-f]喹啉的抗抑郁药氮杂环甲基衍生物
公开(公告)号：US06599915B2
公开(公告)日：2003-07-29
申请号：US10228744
申请日：2002-08-27
申请人： Megan Tran , Gary P. Stack
发明人： Megan Tran , Gary P. Stack
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
摘要翻译：下式的化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和心境恶劣），焦虑症，惊恐障碍，创伤后应激障碍，经前焦虑症（也称为月经前综合征），注意力缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症，神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍和相关疾病。

4. 发明授权

US06656949B1 4-anilinofuro [3,2-c] quinoline derivatives, and preparation processes and uses of the same 失效
标题翻译： 4-苯胺基呋喃并[3,2-c]喹啉衍生物及其制备方法和用途
公开(公告)号：US06656949B1
公开(公告)日：2003-12-02
申请号：US10241739
申请日：2002-09-12
申请人： Yeh-Long Chen
发明人： Yeh-Long Chen
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Disclosed herein are novel 4-anilinofuro[3,2-c]quinoline derivatives of formula (I): wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation process of these derivatives, and their uses in the manufacture of pharmaceutical compositions.
摘要翻译：本文公开了式（I）的新型4-苯胺基呋喃并[3,2-c]喹啉衍生物：其中每个取代基都给出了如说明书和权利要求中所述的定义。还公开了这些衍生物的制备方法，及其在制备药物组合物中的用途。

5. 发明授权

US06506766B1 Glucocortiocoid-selective antinflammatory agents 失效
标题翻译：糖皮质激素选择性抗炎药
公开(公告)号：US06506766B1
公开(公告)日：2003-01-14
申请号：US09610638
申请日：2000-07-05
申请人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
发明人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.
摘要翻译：具有式I的化合物可用于部分或完全拮抗，抑制，激动或调节糖皮质激素受体并在哺乳动物中治疗免疫，自身免疫和炎性疾病。还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

6. 发明授权

US06288073B1 Acronycine derivatives, preparation method and pharmaceutical compositions 失效
标题翻译： Acronycine衍生物，制备方法和药物组合物
公开(公告)号：US06288073B1
公开(公告)日：2001-09-11
申请号：US09581853
申请日：2000-06-19
申请人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
发明人： Michel Koch , François Tillequin , Sylvie Michel , Ghanem Atassi , Alain Pierre , Bruno Pfeiffer , Pierre Renard
IPC分类号： A61K314741
CPC分类号： C07D491/04 , C07D491/14
摘要： A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.
摘要翻译：选自式（I）的化合物：其中：X和Y表示氢，卤素，羟基，巯基，氰基，硝基，烷基，烷氧基，三卤代烷基，任选取代的氨基，亚甲二氧基或亚乙二氧基，烷基，R 2表示氢，羟基，烷基，烷氧基，烷基羰基氧基或任选取代的氨基，R3和R4表示氢或烷基，A表示-CH = CH-或-CH（R5）-CH（R6） - ，其中R5 和R6如说明书中所定义，它们的异构体，N-氧化物及其药学上可接受的酸或碱加成盐，以及其可用于治疗癌症的药物。

7. 发明授权

US06180640B2 Di- and tetra-hydroquinoline-indole antimicrobial agents, uses and compositions related thereto 失效
标题翻译：二 - 和四氢喹啉 - 吲哚抗菌剂，其用途和组合物
公开(公告)号：US06180640B2
公开(公告)日：2001-01-30
申请号：US09344619
申请日：1999-06-25
申请人： Gregory D. Cuny , James R. Hauske , Michael Z. Hoemann , Richard F. Rossi , Roger L. Xie
发明人： Gregory D. Cuny , James R. Hauske , Michael Z. Hoemann , Richard F. Rossi , Roger L. Xie
IPC分类号： A61K314741
CPC分类号： C07D401/04 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译：本发明提供抑制细菌微生物生长的方法和药物制剂。此外，本发明提供杀死细菌微生物的方法和药物制剂。

8. 发明授权

US06548515B1 Dihydrofuro[3,4-b]quinolin-1-one compounds 失效
标题翻译：二氢呋喃并[3,4-b]喹啉-1-酮化合物
公开(公告)号：US06548515B1
公开(公告)日：2003-04-15
申请号：US09718917
申请日：2000-11-22
申请人： Henri-Philippe Husson , Sylviane Giorgi-Renault , Christophe Tratrat , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
发明人： Henri-Philippe Husson , Sylviane Giorgi-Renault , Christophe Tratrat , Ghanem Atassi , Alain Pierre , Pierre Renard , Bruno Pfeiffer
IPC分类号： A61K314741
CPC分类号： C07D491/04 , C07D219/06 , C07D221/16 , C07D221/18 , C07D491/14 , C07D495/04
摘要： The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same are useful in the treatment of cancer.
摘要翻译：本发明涉及式（I）的化合物：其中：表示单键或双键，R 0表示氢或羟基或烷氧基，R 1和R 2相同或不同，各自表示氢或卤素或烷基，烷氧基，羟基，多卤代烷基，硝基或任选取代的氨基或其中m表示1≤= m = 4的整数，或与带有带有5至12个环成员的芳族或非芳族单环或双环基团的碳原子一起形成，并且任选地含有1或 2个选自O，S和N的杂原子，R 3表示氢或芳基，杂芳基，环烷基，任选取代的烷基或式COR7基团，其中R7表示芳基，任选取代的烷基，任选取代的氨基或OR 10，其中R 10表示芳基或任选地取代的烷基，X表示氧或硫或-CH 2 - 或-CH 2-CH 2 - ，Ar表示芳基，杂芳基或芳基烷基，其光学异构体，其水合物，溶剂合物，以及其与药学上可接受的酸的加成盐。含有它们的医药产品可用于治疗癌症。

9. 发明授权

US06268375B1 10, 11-difluoromethylenedioxycamptothecin compounds with topoisomerase I inhibition 失效
标题翻译： 10,11-二氟亚甲二氧基喜树碱化合物与拓扑异构酶I抑制
公开(公告)号：US06268375B1
公开(公告)日：2001-07-31
申请号：US09474758
申请日：1999-12-29
申请人： Monroe E. Wall , Mansukh C. Wani , Govindarajan Manikumar , Neelakantan Balasubramanian , Dolatrai Vyas
发明人： Monroe E. Wall , Mansukh C. Wani , Govindarajan Manikumar , Neelakantan Balasubramanian , Dolatrai Vyas
IPC分类号： A61K314741
CPC分类号： C07D491/22
摘要： Camptothecin compounds having a C10 11 O—(CF2)nO group where n is 1 or 2 are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.
摘要翻译：具有C10 11 O-（CF 2）n O基团的喜树碱化合物，其中n为1或2是有效的抗肿瘤化合物。这些化合物抑制酶拓扑异构酶I，并且可以将相关的拓扑异构酶I-DNA可切割复合物的DNA烷基化。

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