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1. 发明授权

US06825191B2 Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US06825191B2
公开(公告)日：2004-11-30
申请号：US10397219
申请日：2003-03-27
申请人： Tadakiyo Nakagawa , Munetaka Tokumasu , Kazumi Tashiro , Mitsuo Takahashi , Takashi Kayahara , Shunji Takehana , Yuki Kajigaya , Kaoru Yoshida , Kuniya Sakurai
发明人： Tadakiyo Nakagawa , Munetaka Tokumasu , Kazumi Tashiro , Mitsuo Takahashi , Takashi Kayahara , Shunji Takehana , Yuki Kajigaya , Kaoru Yoshida , Kuniya Sakurai
IPC分类号： C07D40114
CPC分类号： C07D401/06 , A61K31/551 , A61K31/5513 , A61K31/675 , C07D243/24 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07F9/645 , C07F9/65583
摘要： The present invention provides benzodiazepine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of inhibiting activated blood-coagulation factor X. These compounds are usable as agents for treating various diseases concerned with the activated blood-coagulation factor X.
摘要翻译：本发明提供下式的苯并二氮杂衍生物，其类似物和其药学上可接受的盐。本发明的化合物具有抑制活化凝血因子X的优异效果。这些化合物可用作治疗与活化凝血因子X有关的各种疾病的药剂。

2. 发明授权

US06514969B2 &bgr;-amyloid inhibitors, processes for preparing them, and their use in pharmaceutical compositions 有权
标题翻译： β-淀粉样蛋白抑制剂，其制备方法及其在药物组合物中的用途
公开(公告)号：US06514969B2
公开(公告)日：2003-02-04
申请号：US09911825
申请日：2001-07-24
申请人： Hans Briem , Klaus Mendla , Helmut Michael Romig , Katja Fechteler , Klaus Fuchs
发明人： Hans Briem , Klaus Mendla , Helmut Michael Romig , Katja Fechteler , Klaus Fuchs
IPC分类号： C07D40114
CPC分类号： C07D471/04
摘要： Compounds of general formula (I) wherein: A is —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—, —CH2—CO—, —CH2—CH2—CO—, or —CH═CH—CO—; Het is piperidinyl, piperazinyl, or dihydrobenzimidazolonyl; R1 is hydrogen or halogen; R2 is hydrogen, C1-C4-alkyl, CF3, or a phenyl group optionally substituted by halogen, C1-C4-alkyl, or C1-C4-alkyloxy; and R3 is hydrogen, C1-C4-alkyl, HO—C1-C4-alkyl, or C2-C4-alkenyl; or a group selected from phenyl, benzyl, and phenylethyl, each optionally substituted by halogen, CF3, C1-C4-alkyl, or C1-C4-alkyloxy; or a heterocycle selected from among morpholine, piperidine, piperazine, and dihydrobenzimidazolone, the heterocycle either linked directly or via a C1-C4-alkylene bridge, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing diseases in which a therapeutic benefit can be obtained by interfering in the process of the formation of A&bgr; or its release from cells, by inhibiting the A&bgr; activity, such as Alzheimer's disease, Parkinson's disease, and Huntington's Chorea.
摘要翻译：通式（I）的化合物，其中：A是-CH 2 - ， - CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - ， - CH 2 -CO-， - CH 2 -CH 2 - CO-或-CH = CH-CO-; Het是哌啶基，哌嗪基或二氢苯并咪唑啉酮; R1是氢或卤素; R2是氢，C1-C4-烷基，CF3或任选被卤素取代的苯基，C1- C 4 - 烷基或C 1 -C 4 - 烷氧基; 和R 3是氢，C 1 -C 4烷基，HO-C 1 -C 4烷基或C 2 -C 4 - 烯基; 或选自苯基，苄基和苯基乙基的基团，各自任选被卤素，CF 3，C 1 -C 4 - 烷基或C 1 -C 4 - 烷氧基取代; 或选自吗啉，哌啶，哌嗪和二氢苯并咪唑酮的杂环，该杂环直接或经C1-C4亚烷基桥连，或其旋光异构体，对映异构体，互变异构体，游离碱或其药理学上可接受的酸加成盐连接; 制备此类化合物的方法; 其药物组合物及其在治疗或预防通过抑制Abeta活性如阿尔茨海默氏病，帕金森氏病，帕金森氏病等疾病中可以通过干扰Aβ形成过程或其从细胞释放而获得治疗益处的疾病的用途，和亨廷顿舞蹈团。

3. 发明授权

US06440972B1 Heterocyclic compounds useful as oxido-squalene cyclase inhibitors 失效
标题翻译：可用作氧化 - 角鲨烯环化酶抑制剂的杂环化合物
公开(公告)号：US06440972B1
公开(公告)日：2002-08-27
申请号：US09367400
申请日：1999-08-13
申请人： George Robert Brown
发明人： George Robert Brown
IPC分类号： C07D40114
CPC分类号： C07D401/04 , C07D213/74 , C07D401/12
摘要： This invention concerns heterocyclic derivatives of formula (I) which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence the lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.
摘要翻译：本发明涉及可用于抑制氧化 - 角鲨烯环化酶，其制备方法和含有它们的药物组合物的式（I）的杂环衍生物。本发明还涉及能够抑制胆固醇生物合成并因此降低血浆中胆固醇水平的杂环衍生物。本发明还涉及在诸如高胆固醇血症和动脉粥样硬化的疾病和医学病症中使用这种杂环衍生物的方法。

4. 发明授权

US06410735B1 1-(4-arylpiperazin-1-y1)-&ohgr;-[N-(&agr;,&ohgr;-dicarboximido)]-alkanes useful as uro-selective &agr;1-adrenoceptor blockers 失效
标题翻译：可用作尿选择性α1-肾上腺素受体阻断剂的1-（4-芳基哌嗪-1-基） - 大豆 - [N-（α，ω-二羧酰亚氨基）] -
公开(公告)号：US06410735B1
公开(公告)日：2002-06-25
申请号：US09578088
申请日：2000-05-24
申请人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
发明人： Nitya Anand , Neelima Sinha , Sanjay Jain , Anita Mehta , Anil Kumar Saxena
IPC分类号： C07D40114
CPC分类号： C07D207/404 , A61K31/496 , C07D207/408 , C07D211/88 , C07D401/06
摘要： Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.
摘要翻译：已经发现，通过芳族系统在一个氮上取代的新颖的哌嗪衍生物，另一个氮被（2,5-二氧代吡咯烷-1-基）烷烃或（2,6-二氧代哌啶-1-基）烷烃取代，表现出选择性的α1A 肾上腺素能活动该化合物可用于治疗疾病状况，例如外周血管疾病，充血性心力衰竭，高血压，特别是良性前列腺肥大。

5. 发明授权

US06316445B1 Carboxy substituted acylic carboxamide derivatives 有权
标题翻译：羧基取代的酰基酰胺衍生物
公开(公告)号：US06316445B1
公开(公告)日：2001-11-13
申请号：US09648005
申请日：1999-05-06
申请人： Timothy P. Burkholder , George D. Maynard , Elizabeth M. Kudlacz
发明人： Timothy P. Burkholder , George D. Maynard , Elizabeth M. Kudlacz
IPC分类号： C07D40114
CPC分类号： C07D401/06 , C07D211/64 , C07D401/12 , C07D401/14 , C07D409/06
摘要： The present invention relates to novel carboxy substituted acyclic carboxamide derivatives of formula (1)): and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
摘要翻译：本发明涉及式（1））的新的羧基取代的无环羧酰胺衍生物：及其立体异构体及其药学上可接受的盐及其作为速激肽受体拮抗剂的用途。这样的拮抗剂可用于治疗速激肽介导的疾病和本文公开的病症，包括：哮喘，咳嗽和支气管炎。

6. 发明授权

US06818773B2 Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbony)]-4'-methyl-1,4-′bipiperidine 失效
标题翻译： 4 - [（Z） - （4-溴苯基）（乙氧基亚氨基）甲基] -1' - [（2,4-二甲基-1-氧化-3-吡啶基）羰基] -4'-甲基-1,4 '联哌啶
公开(公告)号：US06818773B2
公开(公告)日：2004-11-16
申请号：US10269822
申请日：2002-10-11
申请人： Minzhang Chen , Bosco Anthony D'Sa , William W. Leong , Tong Gan , George S. K. Wong , Suhan Tang , Christopher Michael Nielsen
发明人： Minzhang Chen , Bosco Anthony D'Sa , William W. Leong , Tong Gan , George S. K. Wong , Suhan Tang , Christopher Michael Nielsen
IPC分类号： C07D40114
CPC分类号： C07D213/89 , C07D211/66 , C07D401/14
摘要： In one embodiment, the present invention describes the synthesis of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine, and intermediates therefor from easily available starting materials by a simple route.
摘要翻译：在一个实施方案中，本发明描述了合成4 - [（Z） - （4-溴苯基）（乙氧基亚氨基）甲基] -1' - [（2,4-二甲基-1-氧代-3-吡啶基）羰基] -4'-甲基-1,4'-联哌啶，其中间体是通过简单的路线从容易获得的原料中获得的。

7. 发明授权

US06818631B1 Fungicidal pyrimidine derivatives 失效
标题翻译：杀真菌嘧啶衍生物
公开(公告)号：US06818631B1
公开(公告)日：2004-11-16
申请号：US10642552
申请日：2003-08-15
申请人： Yuki Nakagawa , Sergey Bobrov , Charles R. Semer, IV , Thomas A. Kucharek , Masahiro Haramoto
发明人： Yuki Nakagawa , Sergey Bobrov , Charles R. Semer, IV , Thomas A. Kucharek , Masahiro Haramoto
IPC分类号： C07D40114
CPC分类号： A01N43/647 , A01N43/54 , A01N43/653 , A01N43/713 , C07D239/34 , C07D239/36 , C07D239/38 , C07D239/52 , C07D239/56 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Fungicidal pyrimidine derivatives and the use as a fungicide of the compounds of formula (1): wherein R1 is H, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl C3-C6cycloalkyl, C1-C6alkoxy, C3-C6cycloalkoxy, C1-C6alylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, phenyl, pyridinyl or azolyl groups, (being optionally substituted by one or more substituents); or N(R4)C(O)R5, R2 is polyfluoroalkyl, R3 is fluorine, chlorine, bromine or iodine; ethenyl or ethynyl (being optionally substituted by one or more of halogen), R4 and R5 are, independently, H, C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl groups, (being optionally substituted by one or more of halogen or cyano); or R4 and R5 can join together to form a 5 or 6-membered ring, Q is a heteroaromatic ring selected from the following ring system; imidazol-1-yl, pyrazol-1-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-1-yl, benzimidazol-1-yl or tetrazol-5-yl groups, (being optionally substituted by one or more of substituents).
摘要翻译：杀真菌嘧啶衍生物和作为式（1）化合物的杀真菌剂的用途：其中R 1是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基C 3 -C 6环烷基，C 1 -C 6烷氧基，C 3 -C 6环烷氧基，C 1 -C 6芳硫基，C 1 -C 6烷基亚磺酰基，C 1 -C 6烷基磺酰基，苯基，吡啶基或唑基（任选被一个或多个取代基取代）; 或N（R 4）C（O）R 5，R 2是多氟烷基，R 3是氟，氯，溴或碘; 乙烯基或乙炔基（任选被一个或多个卤素取代），R 4和R 5独立地是H，C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基（任选地被一个或多个更多的卤素或氰基）; 或R 4和R 5可以连接在一起以形成5或6元环，Q是选自以下环系的杂芳族环; 咪唑-1-基，吡唑-1-基，1,2,3-三唑-1-基，1,2,3-三唑-2-基，1,2,4-三唑-1-基， 2,4-三唑-1-基，苯并咪唑-1-基或四唑-5-基（任选被一个或多个取代基取代）。

8. 发明授权

US06649636B1 Heteroaryl phenyl pyrazole compounds as anti-inflammatory/analgesic agents 失效
标题翻译：杂芳基苯基吡唑化合物作为抗炎/止痛剂
公开(公告)号：US06649636B1
公开(公告)日：2003-11-18
申请号：US09723608
申请日：2000-11-28
申请人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
发明人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
IPC分类号： C07D40114
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译：本发明涉及下式的化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地稠合于碳环或5至6个杂芳基 R 2是任选被卤素，氨基或烷基氨基取代的（C 1 -C 4）烷基; R 3和R 4各自为氢，卤素，任选被卤素取代的（C 1 -C 4）烷基等; X 1至X 4各自为氢，卤素，羟基，任选被卤素取代的（C 1 -C 4）烷基等。这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。

9. 发明授权

US06458793B1 Heterocyclic derivatives which inhibit factor Xa 失效
标题翻译：抑制因子Xa的杂环衍生物
公开(公告)号：US06458793B1
公开(公告)日：2002-10-01
申请号：US09463625
申请日：2000-01-28
申请人： Peter Warner , Roger James , Thorsten Nowak
发明人： Peter Warner , Roger James , Thorsten Nowak
IPC分类号： C07D40114
CPC分类号： C07D213/82
摘要： The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and more accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).
摘要翻译：本发明涉及具有抗血栓形成和抗凝血性质的杂环衍生物或其药学上可接受的盐，并且更适用于治疗人或动物的方法。本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其在制备用于制备抗血栓形成或抗凝血作用的药物（I）中的用途。

10. 发明授权

US06369068B1 Amino substituted pyrimidine containing compounds 失效
标题翻译：含氨基取代的嘧啶化合物
公开(公告)号：US06369068B1
公开(公告)日：2002-04-09
申请号：US09319859
申请日：1999-06-11
申请人： Jerry Leroy Adams , Timothy Francis Gallagher , Irennegbe Kelly Osifo , Jeffrey Charles Boehm
发明人： Jerry Leroy Adams , Timothy Francis Gallagher , Irennegbe Kelly Osifo , Jeffrey Charles Boehm
IPC分类号： C07D40114
CPC分类号： C07D401/14 , C07D401/12 , C07D403/04 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
摘要翻译：新型1,4,5-取代的咪唑化合物和用作治疗作为细胞因子抑制剂的组合物。

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