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1. 发明授权

US06417367B1 Methods of making quinoline amides 失效
标题翻译：制备喹啉酰胺的方法
公开(公告)号：US06417367B1
公开(公告)日：2002-07-09
申请号：US09924665
申请日：2001-08-08
申请人： Norma J. Tom , David C. Whritenour
发明人： Norma J. Tom , David C. Whritenour
IPC分类号： C07D21514
CPC分类号： C07D215/38
摘要： The present invention relates to methods of making quinoline amides of Formula I below, which are microsomal triglyceride transfer protein inhibitors and can be used as medicines. The present invention also relates to compounds that are used to make quinoline amides of Formula I and methods of making these compounds.
摘要翻译：本发明涉及制备式I的喹啉酰胺的方法，它们是微粒体甘油三酯转移蛋白抑制剂，可用作药物。本发明还涉及用于制备式I的喹啉酰胺的化合物及其制备方法这些化合物。

2. 发明授权

US06437135B1 Process for producing quinolinecarbaldehyde 有权
标题翻译：制备喹啉甲醛的方法
公开(公告)号：US06437135B1
公开(公告)日：2002-08-20
申请号：US09868904
申请日：2001-07-09
申请人： Hiroo Matsumoto , Takanori Shimizu , Yasutaka Takada
发明人： Hiroo Matsumoto , Takanori Shimizu , Yasutaka Takada
IPC分类号： C07D21514
CPC分类号： C07D215/14
摘要： A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde, which entails oxidizing 2-cyclopropyl-4-(4-fluorophenyl)-3-hydroxymethylquinoline with a salt of a hypohalogenous acid in the presence of a quaternary ammonium salt.
摘要翻译：一种2-环丙基-4-（4-氟苯基） - 喹啉-3-甲醛的制备方法，该方法需要在存在下用次卤酸的盐氧化2-环丙基-4-（4-氟苯基）-3-羟甲基喹啉的季铵盐。

3. 发明授权

US06291677B1 Compounds having activity as inhibitors of cytochrome P450RAI 失效
标题翻译：具有细胞色素P450RAI抑制剂活性的化合物
公开(公告)号：US06291677B1
公开(公告)日：2001-09-18
申请号：US09651001
申请日：2000-08-29
申请人： Jayasree Vasudevan , Alan T. Johnson , Dehua Huang , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Alan T. Johnson , Dehua Huang , Roshantha A. Chandraratna
IPC分类号： C07D21514
CPC分类号： C07D221/20 , C07C59/72 , C07C65/28 , C07D215/14 , C07D217/04 , C07D311/58
摘要： Compounds having Formula 7 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
摘要翻译：具有式7的化合物，其中符号具有本说明书中定义的含义是细胞色素P450RAI（视黄酸诱导型）酶的抑制剂，并且用于治疗响应于类视黄醇治疗的疾病。

4. 发明授权

US06562976B2 4-phenyltetrahydrochinoline utilized as an inhibitor of the cholesterol ester transfer protein 失效
公开(公告)号：US06562976B2
公开(公告)日：2003-05-13
申请号：US10122546
申请日：2002-04-15
申请人： Gunter Schmidt , Jürgen Stoltefuss , Michael Lögers , Arndt Brandes , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt
发明人： Gunter Schmidt , Jürgen Stoltefuss , Michael Lögers , Arndt Brandes , Carsten Schmeck , Klaus-Dieter Bremm , Hilmar Bischoff , Delf Schmidt
IPC分类号： C07D21514
CPC分类号： C07D221/20 , C07D215/20 , C07D401/06 , C07D417/06
摘要： The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by customary methods. The tetrahydroquinolines are suitable as active compounds in medicaments, in particular in medicaments. for the treatment of arteriosclerosis and dyslipidaemias.

5. 发明授权

US06359135B1 Compounds having activity as inhibitors of cytochrome P450RAI 失效
公开(公告)号：US06359135B1
公开(公告)日：2002-03-19
申请号：US09829098
申请日：2001-04-09
申请人： Jayasree Vasudevan , Alan T. Johnson , Dehua Huang , Roshantha A. Chandraratna
发明人： Jayasree Vasudevan , Alan T. Johnson , Dehua Huang , Roshantha A. Chandraratna
IPC分类号： C07D21514
CPC分类号： C07D221/20 , A61K31/192 , A61K31/195 , A61K31/353 , A61K31/382 , A61K31/47 , A61K31/472 , A61K31/4747 , C07C59/72 , C07C65/28 , C07D215/14 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D311/96 , C07D333/40 , C07D335/04 , C07D335/06 , C07D409/06
摘要： Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

6. 发明授权

US06331549B1 1-aminoethylquinoline derivatives for treating urinary incontinence 失效
标题翻译：用于治疗尿失禁的1-氨基乙基喹啉衍生物
公开(公告)号：US06331549B1
公开(公告)日：2001-12-18
申请号：US09831442
申请日：2001-05-09
申请人： Christophe Philippo , Patrick Mougenot , Gérard Defosse , Alain Braun , Philippe Bovy
发明人： Christophe Philippo , Patrick Mougenot , Gérard Defosse , Alain Braun , Philippe Bovy
IPC分类号： C07D21514
CPC分类号： C07D215/14 , C07D215/18 , C07D219/02
摘要： The invention relates to 1-aminoethylquinoline derivatives, to pharmaceutical compositions containing them, to therapeutic methods of using them and to processes for preparing them.
摘要翻译：本发明涉及1-氨基乙基喹啉衍生物，含有它们的药物组合物，其使用方法及其制备方法。

7. 发明授权

US06673801B1 Dihydroxyhexanoic acid derivatives 失效
标题翻译：二羟基己酸衍生物
公开(公告)号：US06673801B1
公开(公告)日：2004-01-06
申请号：US09403218
申请日：2000-03-02
申请人： John Charles Kath , Mathew Frank Brown , Christopher Stanley Poss
发明人： John Charles Kath , Mathew Frank Brown , Christopher Stanley Poss
IPC分类号： C07D21514
CPC分类号： C07D241/52 , C07D215/54 , C07D241/44 , C07D409/12
摘要： Dihydroxyhexanoic acid derivatives of the general formula are useful to treat inflammation and other immune disorders.
摘要翻译：通式的二羟基己酸衍生物可用于治疗炎症和其他免疫疾病。

8. 发明授权

US06579987B2 Diaryl-enynes 失效
标题翻译：二芳基烯
公开(公告)号：US06579987B2
公开(公告)日：2003-06-17
申请号：US10324195
申请日：2002-12-20
申请人： Ian Egle , Jennifer Frey , Methvin Isaac
发明人： Ian Egle , Jennifer Frey , Methvin Isaac
IPC分类号： C07D21514
CPC分类号： C07D207/325 , C07C229/14 , C07C323/32 , C07C2601/14 , C07C2602/08 , C07D215/12 , C07D317/58 , C07D333/20 , C07D333/52
摘要： Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selected from the group consisting of H, alkyl and benzyl; R3 is selected from the group consisting of CO2R, CONRR′, CONH(OH), COSR, SO2NRR′, PO(OR)(OR′) and tetrazolyl, wherein R and R′ are independently selected from the group consisting of H and alkyl; and a salt, solvate or hydrate thereof.
摘要翻译：本发明提供式I化合物：其中：Ar 1和Ar 2独立地选自被至多5个独立地选自烷基，烷氧基，环烷基，环烷氧基，杂环烷基，杂环烷氧基，烷酰基芳烷氧基取代的烷氧基，环烷氧基取代的烷氧基，环烷氧基取代的烷氧基，杂环烷基取代的烷基，杂环烷氧基取代的烷基，杂环烷基取代的烷氧基，杂环烷氧基取代的烷氧基，，硫代芳基，芳烷硫基，硫代芳基 - 烷基，芳烷硫基烷基，卤素，NO2，CF3，CN，OH，亚烷基二氧基，SO2NRR'，NRR'，CO2R（其中R和R'独立地选自H和烷基），和可以如上所述取代的第二芳基; R 1选自H和烷基; R 2选自C 存在H，烷基和苄基; R 3选自CO 2 R，CONRR'，CONH（OH），COSR，SO 2 NRR'，PO（OR）（OR'）和四唑基，其中R和R' 由H和烷基组成的组;及其盐，溶剂合物或水合物。

9. 发明授权

US06469028B1 Synthesis and use of retinoid compounds having negative hormone and/or anatgonist activities 失效
标题翻译：合成和使用具有负激素和/或阴离子活性的类视黄醇化合物
公开(公告)号：US06469028B1
公开(公告)日：2002-10-22
申请号：US09821673
申请日：2001-03-28
申请人： Elliott S. Klein , Alan T. Johnson , Andrew M. Standeven , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Sunil Nagpal , Vidyasagar Vuligonda , Min Teng , Roshantha A. Chandraratna
发明人： Elliott S. Klein , Alan T. Johnson , Andrew M. Standeven , Richard L. Beard , Samuel J. Gillett , Tien T. Duong , Sunil Nagpal , Vidyasagar Vuligonda , Min Teng , Roshantha A. Chandraratna
IPC分类号： C07D21514
CPC分类号： C07D335/06 , C07C57/50 , C07C63/33 , C07C63/49 , C07C63/66 , C07C63/72 , C07C63/74 , C07C65/19 , C07C65/28 , C07C65/38 , C07C69/618 , C07C69/76 , C07C69/90 , C07C69/94 , C07C233/81 , C07C245/10 , C07C327/48 , C07C2602/10 , C07D213/55 , C07D277/30 , C07D307/54 , C07D333/24 , C07D409/04 , C07D417/04 , C07F7/081
摘要： Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
摘要翻译：芳基取代的和芳基和（3-氧代-1-丙烯基）取代的苯并吡喃，苯并噻喃，1,2-二氢喹啉和5,6-二氢萘衍生物具有类视黄醇阴性激素和/或拮抗剂样生物活性。本发明的RAR拮抗剂可以施用于包括人在内的哺乳动物，以预防或减少RAR激动剂在结合受体位点上的作用。具体来说，RAR激动剂与类视黄醇药物一起施用或共同施用以预防或改善由类维生素A或维生素A或维生素A前体引起的毒性或副作用。类视黄醇阴性激素可用于增强其他类维生素A和核受体激动剂的活性。例如，称为AGN 193109的类视黄醇阴性激素有效地增加了体外反式激活测定中其他类维生素A和类固醇激素的有效性。另外，反式激活测定可用于鉴定具有负激素活性的化合物。这些测定是基于负激素下调修饰的具有组成型转录激活子结构域的嵌合维甲酸受体的活性的能力。

10. 发明授权

US06410733B1 Amidine inhibitors of serine proteases 失效
标题翻译：丝氨酸蛋白酶的脒抑制剂
公开(公告)号：US06410733B1
公开(公告)日：2002-06-25
申请号：US09947424
申请日：2001-09-05
申请人： Richard M. Pastor , Dean R. Artis , Alan G. Olivero
发明人： Richard M. Pastor , Dean R. Artis , Alan G. Olivero
IPC分类号： C07D21514
CPC分类号： C07D401/06 , C07D207/16 , C07D207/48 , C07D401/12 , C07D403/12
摘要： Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
摘要翻译：提供丝氨酸蛋白酶的抑制剂，其具有式（I），其中X，R 1，R 2，R 3，R 4和R 5如本文所定义。特别地，化合物结合因子VIIa，组织因子/因子Xa复合物，凝血酶，胰蛋白酶，纤溶酶和激肽释放酶，并具有抗凝活性。包含该化合物的药物组合物可用于在体内抑制静脉和/或动脉血栓的形成。

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