专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06245774B1 Tri-substituted phenyl or pyridine derivatives 失效
公开(公告)号：US06245774B1
公开(公告)日：2001-06-12
申请号：US08492855
申请日：1995-06-20
申请人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
发明人： Graham John Warrellow , Ewan Campbell Boyd , Rikki Peter Alexander
IPC分类号： C07D21338
CPC分类号： C07D213/30 , C07D409/12
摘要： Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12C(S)—, —C(S)NR12—, —C≡C—, —NR12SO2—, or —SO2NR12—; Alk is an optionally substituted straight or branched alkyl chain optionally interrupted by an atom or group X; t is zero or an integer of value 1, 2 or 3; R3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group or an OR11 group [where R11 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group]; R4 is a hydrogen atom or an optionally substituted alkyl, —CO2R8, —CSNR9R10, —CN, —CH2CN, or —(CH2)tAr group where t is zero or an integer of value 1, 2 or 3 and Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; provided that when L is a group of type (2) or (3) above then Z is a group of type (A) or type (B) in which R4 is a —(CH2)tAr group; R5 is a group —(CH2)tAr; R6 is a hydrogen or a fluorine atom, or an optionally substituted alkyl or —CO2R8, —CONR9R10, —CSNR9R10, —CN or —CH2CN group; R7 is a hydrogen or a fluorine atom, an optionally substituted straight or branched alkyl group, or an ORc group where Rc is a hydrogen atom or an optionally substituted alkyl or alkenyl group, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where unwanted inflammatory response or muscular spasm is present.

2. 发明授权

US06646130B2 Process to chiral integrin antagonist beta-amino acid intermediate 失效
标题翻译：手性整合素拮抗剂β-氨基酸中间体的方法
公开(公告)号：US06646130B2
公开(公告)日：2003-11-11
申请号：US10197003
申请日：2002-07-17
申请人： Nelo R. Rivera , Christopher J. Welch , Yi Xiao , Nobuyoshi Yasuda
发明人： Nelo R. Rivera , Christopher J. Welch , Yi Xiao , Nobuyoshi Yasuda
IPC分类号： C07D21338
CPC分类号： C07D213/64 , C07B2200/05
摘要： The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists
摘要翻译：本发明公开了一种制备结构式I化合物的对映体富集混合物的新方法，它们是合成α-角蛋白3整联蛋白受体拮抗剂的有用中间体

3. 发明授权

US06603011B1 3-pyridinyl compounds 失效
标题翻译： 3-吡啶基化合物
公开(公告)号：US06603011B1
公开(公告)日：2003-08-05
申请号：US09642351
申请日：2000-08-21
申请人： William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
发明人： William Scott Caldwell , Gary Maurice Dull , Grayland Page Dobson
IPC分类号： C07D21338
CPC分类号： C07D213/38
摘要： Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.
摘要翻译：通过施用有效量的芳基取代的脂族胺化合物，芳基取代的烯属胺化合物或芳基取代的炔属胺化合物来治疗易患或患有中枢神经系统疾病的患者。代表性的化合物是（E）-N-甲基-5-（3-吡啶基）-4-戊烯-2-胺。

4. 发明授权

US06262268B1 Process and intermediates to a tetrahydro-[1,8]-naphthyridine 失效
标题翻译：四氢 - [1,8] - 萘啶的方法和中间体
公开(公告)号：US06262268B1
公开(公告)日：2001-07-17
申请号：US09709083
申请日：2000-11-09
申请人： Michael Palucki , David L. Hughes , Chunhua Yang , Nobuyoshi Yasuda
发明人： Michael Palucki , David L. Hughes , Chunhua Yang , Nobuyoshi Yasuda
IPC分类号： C07D21338
CPC分类号： C07D213/40 , C07D213/38 , C07D471/04
摘要： A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
摘要翻译：提供了一种制备3-（5,6,7,8-四氢 - [1,8] - 萘啶-2-基） - 丙胺的新方法，其可用于合成αphav整联蛋白受体拮抗剂。还提供了从该方法获得的有用的中间体。

5. 发明授权

US06737423B2 Substituted heterocyclo-norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and medicaments comprising them 失效
标题翻译：取代的杂环降冰片基氨基衍生物，其制备方法，它们作为药物或诊断剂的用途，以及包含它们的药物
公开(公告)号：US06737423B2
公开(公告)日：2004-05-18
申请号：US10020241
申请日：2001-12-18
申请人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Hans-Willi Jansen
发明人： Uwe Heinelt , Hans-Jochen Lang , Klaus Wirth , Hans-Willi Jansen
IPC分类号： C07D21338
CPC分类号： C07D207/335 , C07D213/38 , C07D231/12 , C07D231/16 , C07D233/56 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D261/18 , C07D277/28 , C07D307/52 , C07D333/20 , C07D333/44
摘要： Substituted heterocyclo-norbornylaminoderivatives having: a) an exo-configuration nitrogen and an endo-fused five-membered ring or six-membered ring of the formula (I) or b) an exo-configuration nitrogen and an exo-fused five-membered ring or six-membered ring of the formula (I a), wherein Rn, Het, A, B and T have the meanings given in the claims. These compounds have a variety of uses. They can be used as antihypertensives, for the reduction or prevention of is chemically induced damage, as pharmaceuticals for surgical interventions, for the treatment of ischemia of the nervous system, including stroke and cerebral edema, for the treatment of ischemia due to shock and disturbed respiratory drive, for the treatment of snoring, as a laxative, as an agent against ectoparasites, for the prevention of gallstone formation, as an antiatherosclerotic, as an agent against diabetic late complications, cancers, fibrotic disorders, endothelial dysfunction, organ hypertrophy, and organ hyperplasia. The compounds of the invention are inhibitors of the cellular sodium-proton antiporter. Additonally, the compounds of the invention influence the serum lipoproteins and can therefore be used for the prophylaxis and the regression of atherosclerotic changes.
摘要翻译：取代的杂环降冰片基氨基衍生物具有：a）外配构型氮和式（I）的内联稠合五元环或六元环，或b）外配构氮和外稠合五元环或式（Ⅰa）的六元环，其中Rn，Het，A，B和T具有权利要求中给出的含义。这些化合物具有多种用途。它们可用作抗高血压药物，用于减少或预防化学诱导的损伤，作为手术干预的药物，用于治疗神经系统缺血，包括中风和脑水肿，用于治疗由于休克和受干扰的局部缺血呼吸驱动，用作治疗打鼾，作为泻药，作为对外寄生虫的药物，用于预防胆结石形成，作为抗动脉粥样硬化，作为抗糖尿病晚期并发症，癌症，纤维化病症，内皮功能障碍，器官肥大的药剂，以及器官增生。本发明的化合物是细胞钠 - 质子逆转录酶的抑制剂。此外，本发明的化合物影响血清脂蛋白，因此可用于预防和消除动脉粥样硬化变化。

6. 发明授权

US06673934B2 Primary intermediates for oxidative coloration of hair 有权
标题翻译：头发氧化着色的主要中间体
公开(公告)号：US06673934B2
公开(公告)日：2004-01-06
申请号：US10052734
申请日：2002-01-18
申请人： Mu-Ill Lim , Yuh-Guo Pan
发明人： Mu-Ill Lim , Yuh-Guo Pan
IPC分类号： C07D21338
CPC分类号： C07D319/08 , A61K8/347 , A61K8/411 , A61K8/415 , A61K8/49 , A61K8/4926 , A61K8/494 , A61K8/4973 , A61K8/4986 , A61Q5/10 , C07D213/65 , C07D307/58 , C07D319/18 , C07D333/32
摘要： Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is hydrogen, hydroxy, nitro, amino, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy or cyclic alkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group, preferably an aromatic group selected from a furanyl, thienyl, pyridinyl, phenyl, 2,3-dihydro-benzo[1,4]dioxin-5 or -6-yl or benzo[1,3]dioxol-4 or -5-yl group; and y=1 to 3.
摘要翻译：用于头发氧化染色的染发组合物的主要中间体是式（1）的化合物：其中R是氢，羟基，硝基，氨基，卤素，C 1至C 5烷基或卤代烷基，C 1至C 5烷氧基或环烷氧基，C 1至 C5羟烷基和C1至C5羟基烷氧基; Ar是芳基，优选芳基，选自呋喃基，噻吩基，吡啶基，苯基，2,3-二氢 - 苯并[1,4]二恶英-5或-6-基或苯并[1,3] 4或5-基; y = 1〜3。

7. 发明授权

US06537994B2 Heterocyclic &bgr;3 adrenergic receptor agonists 失效
标题翻译：杂环β3肾上腺素受体激动剂
公开(公告)号：US06537994B2
公开(公告)日：2003-03-25
申请号：US09904115
申请日：2001-07-12
申请人： Mark Anthony Ashwell , William Ronald Solvibile
发明人： Mark Anthony Ashwell , William Ronald Solvibile
IPC分类号： C07D21338
CPC分类号： C07D213/74 , C07D213/75
摘要： This invention provides compounds of Formula I having the structure wherein, U, V, and W are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, glaucoma, ocular hypertension and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.
摘要翻译：本发明提供具有以下结构的式I化合物，其中U，V和W如上所定义，或其药学上可接受的盐，其可用于治疗或抑制与胰岛素抵抗或高血糖相关的代谢紊乱（通常与肥胖或葡萄糖不耐症），动脉粥样硬化，胃肠道疾病，神经源性炎症，青光眼，高眼压症和尿频; 并且特别可用于治疗或抑制II型糖尿病。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式