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51. 发明授权

US06894041B2 Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes 失效
标题翻译：可用作PDE4同功酶抑制剂的恶唑基 - 酰胺衍生物
公开(公告)号：US06894041B2
公开(公告)日：2005-05-17
申请号：US10300959
申请日：2002-11-20
申请人： Anthony Marfat , Michael William McKechney
发明人： Anthony Marfat , Michael William McKechney
IPC分类号： C07D277/20 , A61K20060101 , A61K31/357 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/4439 , A61P20060101 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/16 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D277/56 , C07D417/12 , C07D417/14 , C07D417/10 , C07D403/14
CPC分类号： C07D417/12 , C07D277/56
摘要： This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recited, optionally one carbon atom of said carbon ring system may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; and E is selected from: and all other substituents shown above are as defined in the specification.
摘要翻译：本申请涉及可用作PDE4抑制剂的化合物，用于治疗受下列通式的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病，其中Y为-C（R < > 1 _{a ） - 或 - [N <？img id =“CUSTOM-CHARACTER-00001”he =“3.13mm”wi =“2.12mm”file =“US06894041-20050517 -P00900.TIF“alt =”自定义字符“img-content =”character“img-format =”tif“？（O）>其中k是0或1; G 1是饱和或不饱和的碳环体系，其为3-至7-元单环，或为7至12元稠合多环; 条件是G 1不是如G 2所定义的不连续或限制性的联芳基部分; 其中任选地一个碳原子可以被选自N，O和S的杂原子取代; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; -G 2是饱和或不饱和的碳环体系，其为3-至7-元单环; 或者是7-12元稠合的多环; 或者是7至18元不连续或限制性的联芳基部分; 其中对于所述碳环体系中的每一个，所述碳环体系的任选一个碳原子可被选自N，O和S的杂原子代替; 其中任选地，其第二个碳原子和其另外任选的第三个碳原子可以被N取代; 并且E选自：和上述所有其它取代基如说明书中所定义。}

52. 发明授权

US06716978B2 Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors 失效
标题翻译：在PDE4抑制剂中基于吲唑生物电子替代儿茶酚的治疗活性化合物
公开(公告)号：US06716978B2
公开(公告)日：2004-04-06
申请号：US09381446
申请日：1999-09-20
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： C07D23156
CPC分类号： A61K31/416 , A61K31/496 , A61K31/497 , A61K31/517 , A61K31/52 , A61K31/525 , A61K31/5377 , A61K31/541 , C07D231/56 , Y02A50/411
摘要： This application is directed to therapeutically active compositions of matter are useful for treating or preventing inflammatory bowel disease and conditions including joint inflammation, Crohn's disease and inflammatory bowel disease; respiratory diseases such as chronic obstructive pulmonary disease (COPD) including asthma, chronic bronchitis, and pulmonary emphysema; infectious diseases including endotoxic shock and toxic shock syndrome; immune diseases including systemic lupus erythematosis and psoriasis; and other diseases including bone resorption diseases and reperfusion injury; wherein said composition of matter comprises a compound which is an inhibitor of phosphodiesterase isozyme 4 (PDE4) and wherein an indazole is one essential component of said compound's overall chemical structure, and wherein said indazole constitutes a bioisosteric replacement of a catechol component or functional derivative thereof in a known compound having the same said therapeutic activity and the same remaining said components of its overall chemical structure. Included are compounds of Formula (IA) or (IB): wherein the variable are defined as set forth in the specification.
摘要翻译：本申请涉及治疗活性组合物，其用于治疗或预防炎症性肠病和包括关节炎，克罗恩病和炎症性肠病的病症; 呼吸系统疾病如慢性阻塞性肺疾病（COPD），包括哮喘，慢性支气管炎和肺气肿; 传染病包括内毒素性休克和中毒性休克综合征; 免疫疾病包括系统性红斑狼疮和牛皮癣; 和其他疾病，包括骨吸收疾病和再灌注损伤; 其中所述物质组合物包含化合物，其是磷酸二酯酶同工酶4（PDE4）的抑制剂，其中吲唑是所述化合物的总体化学结构的一个必需组分，并且其中所述吲唑构成儿茶酚组分或其功能衍生物的生物电子替代物在具有相同治疗活性的已知化合物中，以及其总体化学结构的相同剩余部分。包括式（IA）或（IB）的化合物：其中变量如本说明书所述定义。

53. 发明授权

US6127398A Substituted indazole derivatives and related compounds 失效
标题翻译：取代的吲唑衍生物和相关化合物
公开(公告)号：US6127398A
公开(公告)日：2000-10-03
申请号：US406220
申请日：1999-09-27
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： A61K31/415 , A61K31/416 , A61P3/00 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/02 , A61P15/00 , A61P29/00 , A61P31/12 , A61P33/02 , A61P35/02 , A61P37/06 , A61P43/00 , C07D20060101 , C07D231/54 , C07D231/56 , C07D409/08 , C07D407/06
CPC分类号： C07D231/56 , C07D409/08
摘要： The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.2.sup.a and R.sub.2.sup.b are independently selected from the group consisting essentially of hydrogen and hereinafter recited substituents, provided that one, but not both of R.sub.2.sup.a and R.sub.2.sup.b must be independently selected as hydrogen, wherein said substituents comprise: ##STR2## wherein the dashed lines in formulas (Ia) and (Ib) independently and optionally represent a single or double bond, provided that in formula (Ia) both dashed lines cannot both represent double bonds at the same time; andR, R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.18 and m are as defined. The invention further relates to intermediates for the preparation of the compounds of formula I, and to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐，其中R2a和R2b独立地选自氢和下文所述的取代基，条件是R 2a和R 2b之一必须独立地选自氢，其中所述取代基包括：其中式（Ia）和（Ib）中的虚线独立地且任选地表示单键或双键，条件是在式（Ia）中，两条虚线不能同时表示双键; 并且R，R 1，R 3，R 4，R 5，R 6，R 7，R 18和m如上所定义。本发明还涉及用于制备式I化合物的中间体，以及含有式I化合物或其可接受的盐用于抑制IV型磷酸二酯酶（PDE）或其制备方法的药物组合物和在哺乳动物中产生肿瘤坏死因子（TNF）。

54. 发明授权

US6096901A Processes and intermediates for preparing 2-fluorothiophene derivatives 失效
标题翻译：制备2-氟噻吩衍生物的方法和中间体
公开(公告)号：US6096901A
公开(公告)日：2000-08-01
申请号：US450976
申请日：1999-11-30
申请人： Anthony Marfat , Robert James Chambers
发明人： Anthony Marfat , Robert James Chambers
IPC分类号： C07D333/38
CPC分类号： C07D333/38
摘要： A process for the preparation of the compound of the formula: ##STR1## wherein R.sup.1 is OH, which comprises the steps of a) treating the compound of the formula: ##STR2## with an inorganic fluoride, of the formula M.sup.2 F wherein M.sup.2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R.sup.4 P.sup.+ Z.sup.- and a compound of the formula R.sup.5 vic (COW).sub.2 wherein R.sup.4 and R.sup.5 are each selected from optionally substituted (C.sub.6 -C.sub.10) aryl and optionally substituted (C.sub.1 -C.sub.6) alkyl, and W is halo; to form the compound of the formula: ##STR3## and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, andii) treating the product of step i) with a mineral acid. A compound of the formula: ##STR4## wherein R.sup.1 is selected from the group consisting of, halo, R.sup.7 O, R.sup.7 COO and N(R.sup.8).sub.2 wherein R.sup.7 is (C.sub.1 -C.sub.6)alkyl or (C.sub.6 -C.sub.10)aryl and each R.sup.8 is selected from hydrogen and R.sup.7 with the proviso that R.sup.7 is not methyl when R.sup.1 is R.sup.7 O.
摘要翻译：一种制备下式化合物的方法，其中R1是OH，其包括以下步骤：a）用式M2F的无机氟化物处理其中M2为碱金属阳离子的式在式R4P + Z-的化合物和式的化合物R5vic（COW）2的存在下升高温度，其中R 4和R 5各自选自任选取代的（C 6 -C 10）芳基和任选取代的（C 1 -C 6）烷基，W是卤素; 形成下式的化合物：和b）I）用式MOH的碱的水溶液处理式IV的化合物，其中M是碱金属阳离子，和ii）处理步骤i的产物）与无机酸。下式的化合物：其中R 1选自卤素，R 7 O，R 7 COO和N（R 8）2，其中R 7是（C 1 -C 6）烷基或（C 6 -C 10）芳基，并且每个R 8选自氢和R 7，条件是当R 1是R 7 O时，R 7不是甲基。

55. 发明授权

US5998451A Substituted tetralins, chromans and related compounds in the treatment and related compounds in the treatment of asthma, arthritis and related diseases 失效
标题翻译：在治疗和相关化合物中治疗哮喘，关节炎和相关疾病中取代的四氢化萘，色满和相关化合物
公开(公告)号：US5998451A
公开(公告)日：1999-12-07
申请号：US696452
申请日：1991-05-06
申请人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Anthony Marfat , Lawrence S. Melvin, Jr.
IPC分类号： C07C43/253 , C07C45/62 , C07C45/63 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/74 , C07C49/747 , C07C49/755 , C07D213/30 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/38 , C07D311/22 , C07D313/08 , C07D335/02 , C07D335/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/06 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D521/00 , C07D275/02 , A01N43/78 , A01N43/80 , C07D275/04
CPC分类号： C07D213/30 , C07C43/253 , C07C45/62 , C07C45/63 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/74 , C07C49/747 , C07C49/755 , C07D215/14 , C07D215/20 , C07D215/233 , C07D215/38 , C07D231/12 , C07D233/56 , C07D249/08 , C07D311/22 , C07D313/08 , C07D335/02 , C07D335/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/06 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07C2102/08 , C07C2102/10 , Y02P20/582
摘要： Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
摘要翻译：通过抑制5-脂氧合酶和/或阻断白三烯受体的取代的四氢化萘，着色剂和相关化合物可用于预防或治疗哺乳动物中哮喘，关节炎，牛皮癣，溃疡，心肌梗塞和相关疾病状态，其药物组合物，其处理方法和可用于其合成的中间体。

56. 发明授权

US5811432A Azaoxindole derivatives 失效
标题翻译：氮杂吲哚衍生物
公开(公告)号：US5811432A
公开(公告)日：1998-09-22
申请号：US33456
申请日：1993-03-18
申请人： Anthony Marfat , Ralph P. Robinson
发明人： Anthony Marfat , Ralph P. Robinson
IPC分类号： A01N43/40 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to novel 4-, 5-, 6-, and 7-azaoxindole derivatives. The compounds are anti-inflammatory and analgesic agents and inhibitors of one or more of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. They are useful in the treatment of chronic inflammatory diseases, allergy, psoriasis, various bone diseases, and immune dysfunctions such as systemic lupus erythematosis.
摘要翻译：本发明涉及新的4-，5-，6-和7-氮杂羟基吲哚衍生物。这些化合物是一种或多种前列腺素H2合成酶，5-脂肪氧合酶和白细胞介素-1生物合成的抗炎和止痛剂和抑制剂。它们可用于治疗慢性炎性疾病，过敏，牛皮癣，各种骨骼疾病以及诸如系统性红斑狼疮的免疫功能障碍。

57. 发明授权

US5641789A Sulfonamide derivatives of benzenefused hydroxy substituted cycloalkyl and heterocyclic ring compounds 失效
标题翻译：苯磺酰胺衍生物的苯乙烯基取代的环烷基和杂环化合物
公开(公告)号：US5641789A
公开(公告)日：1997-06-24
申请号：US416681
申请日：1995-03-31
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： A61K31/18 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/47 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , A61P43/00 , C07C311/09 , C07D215/18 , C07D277/24 , C07D277/64 , C07D311/00 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14 , A61K31/35 , A61K31/38 , C07D311/22 , C07D335/06
CPC分类号： C07D405/12 , C07C311/09 , C07D215/18 , C07D277/24 , C07D277/64 , C07D405/14 , C07D417/12 , C07D417/14
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof, wherein X.sup.1, Ar, X, Y.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and n are defined below, which are inhibitors of the production of leukotrienes and/or blockers of leukotriene receptors, methods for preparing said compounds and intermediates useful in the preparation thereof, pharmaceutical compositions thereof methods of treatment therewith. The compounds of the above formula are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related diseases in mammals.
摘要翻译： PCT No.PCT / US93 / 09171 Sec。 371日期1995年3月31日 102（e）1995年3月31日PCT PCT 1993年9月30日PCT公布。公开号WO94 / 08996 日期1994年4月28日具有下式定义的式“IMAGE”及其药学上可接受的盐和前药的化合物，其中X1，Ar，X，Y1，R1，R2，R3，R5和n定义如下，其是白三烯生产抑制剂和/或白三烯受体的阻断剂，制备所述化合物的方法和用于其制备的中间体，其药物组合物的治疗方法。上述化合物可用于预防或治疗哺乳动物中的哮喘，关节炎，牛皮癣，溃疡，心肌梗塞和相关疾病。

58. 发明授权

US5248685A Substituted 1-[3-(heteroarylmethoxy)phenyl]alkanols and related compounds in the treatment of asthma 失效
标题翻译：取代的1- [3-（杂芳基甲氧基）苯基]烷醇和相关化合物治疗哮喘
公开(公告)号：US5248685A
公开(公告)日：1993-09-28
申请号：US768623
申请日：1991-09-30
申请人： James F. Eggler , Anthony Marfat , Hiroko Masamune , Lawrence S. Melvin, Jr.
发明人： James F. Eggler , Anthony Marfat , Hiroko Masamune , Lawrence S. Melvin, Jr.
IPC分类号： A61K31/085 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P11/00 , A61P11/08 , A61P29/00 , C07C33/24 , C07C43/23 , C07C45/63 , C07C45/64 , C07C45/71 , C07C45/84 , C07C49/84 , C07C69/007 , C07C69/94 , C07D20060101 , C07D213/30 , C07D213/50 , C07D213/65 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D213/30 , C07C43/23 , C07C45/63 , C07C45/71 , C07C49/84 , C07D213/50 , C07D213/65 , C07D215/14 , C07D401/12
摘要： Substituted 1-[3-(heteroarylmethoxy)phenyl]-alkanols and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction, stroke and related disease states in mammals; pharmaceutical compositions thereof; and a method of treatment therewith.
摘要翻译： PCT No.PCT / US89 / 01450 Sec。 371日期1991年9月30日 102（e）1991年9月30日PCT PCT。1989年4月7日。取代的1- [3-（杂芳基甲氧基）苯基] - 烷醇和相关化合物，其通过抑制5-脂氧合酶和/或阻断白三烯受体可用于预防或治疗哺乳动物中的哮喘，关节炎，牛皮癣，溃疡，心肌梗死，中风和相关疾病状态; 其药物组合物; 及其处理方法。

59. 发明授权

US4914101A 3,4-Dihydro-2-alkyl-3-oxo-n-aryl-2H-(1)benz o-thieno(3,2-e)-1,2-thiazine-4-carboxamide-1,1-dioxides 失效
标题翻译： 3,4-二氢-2-烷基-3-氧代 - 正 - 芳基-2H-（1）苯并噻吩并（3,2-e）-1,2-噻嗪-4-甲酰胺-1,1-二氧化物
公开(公告)号：US4914101A
公开(公告)日：1990-04-03
申请号：US382161
申请日：1989-02-06
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： A61K31/535 , A61K31/54 , A61P1/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/14 , A61P29/00 , A61P37/08 , C07D20060101 , C07D333/62 , C07D513/04
CPC分类号： C07D333/62 , C07D513/04
摘要： R.sup.1 is hydrogen, halogen or C.sub.1 to C.sub.4 alkyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkyl; and Ar is phenyl or phenyl substituted with one or more substituents selected from C.sub.1 to C.sub.4 alkyl, halo, trifluoromethyl, nitro, hydroxyl, halophenyl, or C.sub.1 to C.sub.4 alkoxy.The compounds are useful in treating inflammation or other prostaglandin or leukotriene mediated diseases.

60. 发明授权

US4761485A Synthetic method for indol-2(3H)-ones 失效
标题翻译：吲哚-2（3H） - 酮的合成方法
公开(公告)号：US4761485A
公开(公告)日：1988-08-02
申请号：US24746
申请日：1987-03-11
申请人： Anthony Marfat
发明人： Anthony Marfat
IPC分类号： C07D209/34 , A61K31/40
CPC分类号： C07D209/34
摘要： A two-step process for the synthesis of certain indol-2(3H)-ones from indoles, and the 3,3-dibromoindol-2(3H)-ones which are intermediates in that process.
摘要翻译：用于从吲哚合成某些吲哚-2（3H）酮的两步法和在该方法中作为中间体的3,3-二溴吲哚-2（3H） - 酮。

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