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1. 发明申请

US20030220496A1 Novel intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的新型中间体
公开(公告)号：US20030220496A1
公开(公告)日：2003-11-27
申请号：US10364641
申请日：2003-02-12
申请人： Merrell Pharmaceuticals, Inc.
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D265/30 , C07C049/786 , C07D211/20
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1 wherein W represents nullC(nullO)null or nullCH(OH)null; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is nullCOOH or nullCOOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are ta to form a second bond between the carbon R1 and R2 or where R1 represented hydrox integer 0.
摘要翻译：本发明涉及可用于制备下式其中W代表-C（= O） - 或-CH（OH） - 的某些抗组氨酸哌啶衍生物的新中间体和方法; R1代表氢或羟基; R2表示氢; R1和R2一起形成带有R1和R2的碳原子之间的第二个键; n为1〜5的整数， m为整数0或1; R3是-COOH或-COO烷基，其中烷基部分具有1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其中R1和R2为ta R1和R2或其中R1表示为“整数0。

2. 发明申请

US20040127555A1 Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as Alzheimer's disease, type 2 diabetes, and parkinson's disease 有权
标题翻译：用于治疗淀粉样蛋白病和突触核蛋白病如阿尔茨海默病，2型糖尿病和帕金森病的化合物，组合物和方法
公开(公告)号：US20040127555A1
公开(公告)日：2004-07-01
申请号：US10452851
申请日：2003-05-30
发明人： Alan D. Snow , Beth P. Nguyen , Gerardo M. Castillo , Virginia J. Sanders , Thomas P. Lake , Lesley Larsen , Rex T. Weavers , Stephen D. Lorimer , David S. Larsen , David L. Coffen , Charlotte Coffen
IPC分类号： A61K031/34 , A61K031/137 , C07C049/786 , A61K031/075 , A61K031/12 , A61K031/095
CPC分类号： C07C49/248 , A61K31/047 , C07C39/15 , C07C39/16 , C07C39/17 , C07C45/62 , C07C45/64 , C07C49/83 , C07C49/835 , C07C69/017 , C07C215/50 , C07C231/02 , C07C235/34 , C07C235/38 , C07C235/48 , C07C235/54 , C07C235/56 , C07C237/22 , C07C275/34 , C07D207/16 , C07D211/74 , C07D213/30 , C07D213/69 , C07D213/85 , C07D221/08 , C07D221/18 , C07D231/06 , C07D241/08 , C07D263/38 , C07D265/38 , C07D295/096 , C07D295/192 , C07D311/60 , C07D317/50 , C07D317/54 , C07D317/58 , C07D317/60 , C07D317/66 , C07D317/68 , C07D333/16 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D451/06 , C07D471/04 , C07D487/08 , C07D491/08
摘要： Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Anull amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
摘要翻译：双 - 和三 - 二羟基芳基化合物及其亚甲二氧基类似物和药学上可接受的酯，其合成，含有它们的药物组合物及其在治疗淀粉样蛋白病，尤其是Aβ淀粉样变性中的用途，例如在阿尔茨海默病，IAPP淀粉样变性在2型糖尿病中观察到，以及突触核蛋白病，例如在帕金森病中观察到的，以及用于这种治疗的药物的制造。

3. 发明申请

US20040176644A1 Process for producing 2-phenylacetophenone derivatives and precursons therefor 失效
标题翻译：制备2-苯基苯乙酮衍生物及其前体的方法
公开(公告)号：US20040176644A1
公开(公告)日：2004-09-09
申请号：US10485615
申请日：2004-01-30
发明人： Takeshi Ohshima , Shigeyuki Nishimura , Takayoshi Ando
IPC分类号： C07C049/786
CPC分类号： C07C49/813 , C07C45/42 , C07C45/516
摘要： A process for producing 2-phenylacetophenone derivatives represented by the formula (I): 1 (wherein X is an alkyl group or a haloalkyl group, and Y is a hydrogen atom, a halogen atom or an alkyl group which may be substituted), which comprises reacting a compound represented by the formula (II): 2 (wherein X and Y are as defined above, and R is a hydrogen atom or an alkyl group) with an acid.
摘要翻译：一种制备由式（I）表示的2-苯基苯乙酮衍生物的方法：（其中X是烷基或卤代烷基，Y是氢原子，卤原子或可被取代的烷基），其包括与式（II）表示的化合物（其中X和Y如上定义，R是氢原子或烷基）与酸反应。

4. 发明申请

US20040158093A1 Process for preparing a biaryl compound 有权
标题翻译：制备联芳基化合物的方法
公开(公告)号：US20040158093A1
公开(公告)日：2004-08-12
申请号：US10774498
申请日：2004-02-10
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Hiroshi Ueda , Isao Kurimoto
IPC分类号： C07C049/786 , C07C255/10
CPC分类号： C07C269/06 , C07B37/04 , C07B2200/07 , C07C271/22 , C07D333/24
摘要： A process for preparing an optically active biaryl compound the formula (4): 1 wherein R*, R2, R3, n1, n2 and * are as defined hereinafter, which comprises reacting an aromatic sulfonic acid ester compound of the formula (1): 2 wherein R1 is a substituted or unsubstituted alkyl or aryl group, R2 is the same or different and represents a fluorine atom, a cyano group, a nitro group, a substituted or unsubstituted linear or branched alkyl group, etc., R* is the same or different and represents a substituent having at least one asymmetric carbon, or the substituents on the adjacent carbon atoms of the benzene ring may be bound each other and taken together with the benzene ring to form a fused polycyclic aromatic ring, and provided that R1 is not a trifluoromethyl group, a nonafluorobutyl group or a pentafluorophenyl group, with an organic boron compound of the formula (2): 3 wherein R3 is a substituted or unsubstituted aryl or heteroaryl group, and Q1 and Q2 are the same or different and each is a hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, etc., at 70null C. or below in the presence of a nickel catalyst and a base.
摘要翻译：制备式（4）的光学活性联芳基化合物的方法：其中R *，R 2，R 3，n 1，n 2和*如下文所定义，其包括使芳族磺酸酯化合物式（1）：其中R 1是取代或未取代的烷基或芳基，R 2相同或不同，表示氟原子，氰基，硝基，取代或未取代的直链或支链烷基等，R *相同或不同，表示具有至少一个不对称碳的取代基，或苯环的相邻碳原子上的取代基可以彼此结合并与苯环一起形成稠合多环芳环，并且R 1不是三氟甲基，九氟丁基或五氟苯基，与式（2）的有机硼化合物反应：其中R 3是取代或未取代的芳基或杂芳基，Q 1和Q 2相同或不同在镍催化剂和碱的存在下，在70℃以下，分别为羟基，碳原子数为1〜4的烷氧基等。

5. 发明申请

US20040082815A1 Benzophenones, the production thereof and their use for controlling plant pathogenic fungi 失效
标题翻译：二苯甲酮，其生产及其用于控制植物致病真菌的用途
公开(公告)号：US20040082815A1
公开(公告)日：2004-04-29
申请号：US10469688
申请日：2003-09-03
发明人： Thomas Grote , Andreas Gypser , Joachim Rheinheimer , Ingo Rose , Peter Schafer , Frank Schieweck , Norbert Gotz , Karl Eicken , Eberhard Ammermann , Siegfried Strathmann , Gisela Lorenz , Reinhard Stierl
IPC分类号： C07C049/786
CPC分类号： C07C49/84 , A01N35/04 , C07C45/46
摘要： The invention relates to benzophenones of formula (I), in which the substituents have the following meanings: X represents halogen; R1 represents hydrogen, halogen, C1-C6 alkyl, halo-C1-C2 alkyl, C1-C4 alkoxy, oxyhalomethyl or nitro, and; R2 represents hydrogen, C1-C6 alkyl, benzyl, cyclohexylmethyl or C3-C6 alkenyl. The invention also relates to the production of these benzophenones and to their use as fungicides. 1
摘要翻译：本发明涉及式（I）的二苯甲酮，其中取代基具有以下含义：X表示卤素; R 1表示氢，卤素，C 1 -C 6烷基，卤代-C 1 -C 2烷基，C 1 -C 4烷氧基，氧卤甲基或硝基， R 2表示氢，C 1 -C 6烷基，苄基，环己基甲基或C 3 -C 6烯基。本发明还涉及这些二苯甲酮的制备及其作为杀真菌剂的用途。

6. 发明申请

US20040176645A1 Process for stereoselective synthesis of prostacyclin derivatives 有权
公开(公告)号：US20040176645A1
公开(公告)日：2004-09-09
申请号：US10648191
申请日：2003-08-27
申请人： United Therapeutics Corporation
发明人： Robert M. Moriarty , Hitesh Bxatra
IPC分类号： C07C049/786
CPC分类号： C07C45/71 , C07C39/17 , C07C45/67 , C07C45/80 , C07C2603/12 , C07C47/565 , C07C47/575
摘要： An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

7. 发明申请

US20030220304A1 Hydroxyphenstatin and the prodrugs thereof 有权
标题翻译：羟泼尼松坦及其前药
公开(公告)号：US20030220304A1
公开(公告)日：2003-11-27
申请号：US10258676
申请日：2003-04-24
发明人： George R. Pettit , Matthew P Grealish
IPC分类号： A61K031/66 , C07C049/786 , A61K031/12
CPC分类号： C07C49/84 , A61K31/12 , A61K31/38 , A61K31/66 , C07C45/292 , C07C45/30 , C07C45/45 , C07C45/46 , C07C45/673 , C07F9/12 , C07C47/575
摘要： The benzophenone derivative of combretastatin A-1, designated nullhydroxyphenstatinnull, was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted to a sodium phosphate prodrug by dibenzyl phosphite phosphorylation and subsequent benzyl cleavage: Hydroxyphenstatin and the prodrugs thereof were found to be a potent inhibitor of tubulin polymerization and to demonstrate surprisingly effective anti neoplastic activity against a series of human cancer cells and murine P388 lymphocytic leukemia cells.
摘要翻译：通过将受保护的溴苯和苯甲醛进行组合形成二氧化碳来合成康培定A-1的二苯甲酮衍生物，命名为“羟苯苯达汀”，随后氧化成酮。羟基苯达不稳定剂通过亚磷酸二苄酯磷酸化和随后的苄基裂解转化为磷酸钠前体药物：羟基苯达氨他汀及其前药被发现是微管蛋白聚合的有效抑制剂，并且对一系列人类癌细胞和鼠P388表现出出人意料的有效的抗肿瘤活性淋巴细胞白血病细胞。

8. 发明申请

US20020103389A1 Klainetins and their derivatives, method for their preparation and use thereof 失效
标题翻译：蛇毒素及其衍生物，其制备方法和用途
公开(公告)号：US20020103389A1
公开(公告)日：2002-08-01
申请号：US10000450
申请日：2001-12-04
发明人： Sabine Haag , Herbert Kogler , Ziyu Li , Laszlo Vertesy
IPC分类号： C07D311/74 , C07C323/22 , C07C049/786
CPC分类号： C07D311/32 , C07C45/78 , C07C49/84
摘要： The invention relates to compounds of formula I 1 in which R1, R2, R3, R4, R5, X1, X2, X3, X4, X5 and Y are defined in the specification. The compounds of formula I and II inhibit cyclin-dependent kinases (CDKs) and other kinases (KDR), have cytostatic actions, and are suitable for treating tumors. The compounds of formula I and II are obtainable by extracting the plant Uvaria klaineri, PLA 100484, by cell cultures of the plant Uvaria klaineri, or by chemical synthesis. The invention relates to a method for preparing the compounds of formula I and II, to the use of the compounds for producing a pharmaceutical for the treatment of malignant disorders and of diseases which may be treated by inhibition of CDKs and KDR, and also to pharmaceutical compositions comprising at least one compound of the formula I or II.
摘要翻译：本发明涉及其中R1，R2，R3，R4，R5，X1，X2，X3，X4，X5和Y在本说明书中定义的式I化合物。式I和II的化合物抑制细胞周期蛋白依赖性激酶（CDKs）和其他激酶（KDR），具有细胞抑制作用，并且适用于治疗肿瘤。式I和II化合物可以通过植物Uvaria klaineri的细胞培养物提取植物Uvaria klaineri，PLA 100484，或通过化学合成获得。本发明涉及一种制备式I和II化合物的方法，该化合物用于制备用于治疗恶性疾病的药物和可通过抑制CDK和KDR治疗的疾病，以及制剂组合物，其包含至少一种式I或II的化合物。

9. 发明申请

US20010005509A1 Foot cream composition 审中-公开
标题翻译：足霜组合物
公开(公告)号：US20010005509A1
公开(公告)日：2001-06-28
申请号：US09753900
申请日：2001-01-03
发明人： Marie Harbeck
IPC分类号： A61K035/78 , A01N065/00 , A61K047/00 , A01N025/00 , C01B035/10 , C07C035/18 , C07C049/76 , C07C049/84 , C07C049/82 , C07C049/786
CPC分类号： A61K8/19 , A01N65/00 , A61K8/31 , A61K8/345 , A61K8/35 , A61K8/361 , A61K8/671 , A61K8/678 , A61K8/922 , A61K8/927 , A61K9/0014 , A61K9/06 , A61K36/185 , A61K36/286 , A61K36/53 , A61K36/55 , A61K36/736 , A61K47/22 , A61K47/44 , A61Q19/00 , A61Q19/007 , A61K2300/00 , A01N2300/00
摘要： An improved, and useful, topical transdermal delivery composition for the alleviation and treatment of dermatitis, eczema, lupus, dry, cracked, flaking, peeling, and itching skin infirmites of the foot, which has as its constituents, safflower oil, flaxseed oil, vitamin A, tocopheryl linoleate, and tincture of benzoin to restore organic oil lipids that are essential for the health of the dermal areas of the foot.
摘要翻译：一种用于缓解和治疗皮肤炎，湿疹，狼疮，干燥，破裂，剥落，剥离和瘙痒的足部皮肤软化症的改进和有用的局部透皮递送组合物，其具有红花油，亚麻籽油，维生素A，亚油酸生育酚酯和安息香酊，以恢复对脚皮肤区域的健康至关重要的有机油脂质。

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