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公开(公告)号：US20060229304A1
公开(公告)日：2006-10-12
申请号：US11373770
申请日：2006-03-09
Applicant: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
Inventor： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC: A61K31/538 , C07D265/36 , A61K31/138
CPC classification number: C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
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72.发明授权
公开(公告)号：US07115618B2
公开(公告)日：2006-10-03
申请号：US10812343
申请日：2004-03-30
Applicant: Michael J. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
Inventor： Michael J. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC: A61K31/36 , C07D317/50
CPC classification number: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
Abstract: α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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公开(公告)号：US07101915B1
公开(公告)日：2006-09-05
申请号：US09214277
申请日：1997-07-30
Applicant: Kenji Kawada , Mitsuaki Ohtani , Ryuji Suzuki , Akinori Arimura
Inventor： Kenji Kawada , Mitsuaki Ohtani , Ryuji Suzuki , Akinori Arimura
IPC: C07C43/205 , C07C43/225 , C07C43/23 , A61K31/075 , A61K31/09
CPC classification number: C07D213/30 , C07C15/14 , C07C43/225 , C07C43/23 , C07C43/253 , C07C43/315 , C07C45/68 , C07C47/57 , C07C47/575 , C07C59/64 , C07C59/70 , C07C65/24 , C07C65/28 , C07C69/712 , C07C69/734 , C07C69/94 , C07C205/35 , C07C205/37 , C07C217/20 , C07C217/76 , C07C217/80 , C07C229/52 , C07C233/25 , C07C233/27 , C07C233/80 , C07C235/60 , C07C251/38 , C07C251/60 , C07C255/54 , C07C271/28 , C07C275/32 , C07C281/04 , C07C281/10 , C07C307/10 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/21 , C07C311/29 , C07C317/22 , C07C327/42 , C07D215/14 , C07D239/54 , C07D295/30 , C07D307/42 , C07D309/22 , C07D317/54 , C07D319/20 , C07D333/28 , C07D333/38 , C07D333/54 , C09K2019/123
Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, CH2—, —NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
Abstract translation: 本发明提供了IgE生产的选择性抑制剂，其包含抑制从成熟B细胞分化成抗体产生细胞至产生抗体并且不抑制或弱抑制的过程中的IgE产生的化合物 同时产生的IgG，IgM和/或IgA的制备，式（I）的化合物：其中R 1 -R 13是氢， 卤素，低级烷基，低级烷氧基等，X是-O-，CH 2 - ， - NR 14 - 或-S（O） 其中Y为低级烷基，低级链烯基等，其制备方法和含有该化合物的药物组合物。
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公开(公告)号：US07087789B2
公开(公告)日：2006-08-08
申请号：US10755902
申请日：2004-01-12
Applicant: G. K. Surya Prakash , Jinbo Hu , George A. Olah
Inventor： G. K. Surya Prakash , Jinbo Hu , George A. Olah
IPC: C07C319/00
CPC classification number: C07D307/42 , C07C29/38 , C07C319/14 , C07C2603/74 , C07C323/03 , C07C33/46 , C07C31/38 , C07C35/52
Abstract: A novel, convenient and efficient method for trifluoromethylation of substrate compounds is disclosed. Particularly, alkoxide and hydroxide induced nucleophilic trifluoromethylation of carbonyl compounds, disulfides and other electrophiles, using phenyl trifluoromethyl sulfone PhSO2CF3 (or sulfoxide PhSOCF3) is disclosed. A method of both symmetrical and unsymmetrical anti-2,2-difluoropropan-1,3-diols with high diastereoselectivity (up to 94% de) is disclosed using difluoromethyl phenyl sulfone. This unusual type of high diastereoselectivity was obtained via an intramolecular charge-charge repulsion effect rather than the traditional steric control (based on the Cram's rule). Thus, difluoromethyl phenyl sulfone can be used as a novel difluoromethylene dianion species (“−CF2−”), which can couple two electrophiles (such as diphenyl disulfide or non-enolizable aldehydes) to give new difluoromethylenated products.
Abstract translation: 公开了一种用于底物化合物三氟甲基化的新颖，方便和有效的方法。 特别地，使用苯基三氟甲基砜PhSO 2 CF 3 N 3（或亚砜PhSOCF 3 N 3），烷氧基和氢氧化物诱导羰基化合物，二硫化物和其它亲电子试剂的亲核三氟甲基化 >）被公开。 使用二氟甲基苯基砜公开了具有高非对映选择性（高达94％de）的对称和不对称的2,2-二氟丙-1,3-二醇的方法。 这种不寻常类型的高非对映选择性通过分子内电荷 - 排斥效应而不是传统的空间控制获得（基于Cram的规则）。 因此，二氟甲基苯基砜可以用作新的二氟亚甲基二氧化物（“ CF2”），其可以偶合两种亲电子（如二苯基二硫化物或不可烯化的 醛），得到新的二氟亚甲基化产物。
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公开(公告)号：US20060128977A1
公开(公告)日：2006-06-15
申请号：US11273947
申请日：2005-11-15
Applicant: Alexandra Sanborn , Paul Bloom
Inventor： Alexandra Sanborn , Paul Bloom
IPC: C07D307/02
CPC classification number: C07D307/42 , C07C51/245 , C07D307/46 , C07C59/185
Abstract: A method of preparing 2,5-bis(hydroxymethyl)tetrahydrofuran comprises heating a reaction mixture comprising 2,5-(hydroxymethyl)furaldehyde, an organic solvent, and a catalyst system comprising nickel and zirconium at a temperature, for a time, and at a pressure sufficient to promote reduction of the 2,5-(hydroxymethyl)furaldehyde to 2,5-bis(hydroxymethyl)tetrahydrofuran to produce a product mixture comprising 2,5-bis(hydroxymethyl)tetrahydrofuran.
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公开(公告)号：US20060128843A1
公开(公告)日：2006-06-15
申请号：US11070063
申请日：2005-03-02
Applicant: Alexandra Sanborn , Paul Bloom
Inventor： Alexandra Sanborn , Paul Bloom
IPC: C08K5/15
CPC classification number: C07D307/42 , C07C51/245 , C07D307/46 , C07C59/185
Abstract: A method of preparing 2,5-bis(hydroxymethyl)tetrahydrofuran comprises heating a reaction mixture comprising 2,5-(hydroxymethyl)furaldehyde, an organic solvent, and a catalyst system comprising nickel and zirconium at a temperature, for a time, and at a pressure sufficient to promote reduction of the 2,5-(hydroxymethyl)furaldehyde to 2,5-bis(hydroxymethyl)tetrahydrofuran to produce a product mixture comprising 2,5-bis(hydroxymethyl)tetrahydrofuran.
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公开(公告)号：US20060084680A1
公开(公告)日：2006-04-20
申请号：US10537630
申请日：2003-12-19
Applicant: Louis-David Cantin , Soongyu Choi , Roger Clark , Martin Hentemann , Xin Ma , Joachim Rudolph , Sidney Liang , Christiana Akuche , Rico Lavoie , Libing Chen , Dyuti Majumdar , Philip Wickens
Inventor： Louis-David Cantin , Soongyu Choi , Roger Clark , Martin Hentemann , Xin Ma , Joachim Rudolph , Sidney Liang , Christiana Akuche , Rico Lavoie , Libing Chen , Dyuti Majumdar , Philip Wickens
IPC: A61K31/445 , A61K31/195 , A61K31/192
CPC classification number: C07D213/30 , C07C59/72 , C07C59/90 , C07C69/734 , C07C211/48 , C07C217/24 , C07C255/54 , C07C327/48 , C07C333/04 , C07C2602/08 , C07D209/08 , C07D213/63 , C07D213/83 , C07D213/84 , C07D215/20 , C07D231/12 , C07D239/26 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/52 , C07D249/06 , C07D249/08 , C07D261/20 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/64 , C07D277/66 , C07D285/08 , C07D307/42 , C07D307/79 , C07D333/16 , C07D405/04 , C07D417/04 , C07D513/04
Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
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公开(公告)号：US07022707B2
公开(公告)日：2006-04-04
申请号：US10874662
申请日：2004-06-23
Applicant: David Reginald Adams , Jonathan Mark Bentley , James Edward Paul Davidson , Claire Elizabeth Dawson , Ashley Roger George , Howard Langham Mansell , Patrizio Mattei , Jacques Mizrahi , Matthias Heinrich Nettekoven , Robert Mark Pratt , Stephan Roever , Jonathan Richard Anthony Roffey , Jean-Luc Specklin , Henri Stalder , Kerry Wilkinson
Inventor： David Reginald Adams , Jonathan Mark Bentley , James Edward Paul Davidson , Claire Elizabeth Dawson , Ashley Roger George , Howard Langham Mansell , Patrizio Mattei , Jacques Mizrahi , Matthias Heinrich Nettekoven , Robert Mark Pratt , Stephan Roever , Jonathan Richard Anthony Roffey , Jean-Luc Specklin , Henri Stalder , Kerry Wilkinson
IPC: A61K31/4965 , A61K31/497 , C07D295/185 , C07D295/192 , C07D241/04
CPC classification number: C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4, A1, A2 m and n are as described in the specification.
Abstract translation: 本发明是式（I）的化合物或其药学上可接受的盐，溶剂化物和酯，其中R 1至R 4，A 1， / SUP>，A＆lt; 2＆gt; m和n如说明书中所述。
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79.发明申请4-bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors 失效4-溴或4-碘苯基氨基苯并肟酸衍生物及其作为MEK抑制剂的用途
公开(公告)号：US20060052608A1
公开(公告)日：2006-03-09
申请号：US11249543
申请日：2005-10-12
Applicant: Stephen Barrett , Alexander Bridges , Annette Doherty , David Dudley , Alan Saltiel , Haile Tecle
Inventor： Stephen Barrett , Alexander Bridges , Annette Doherty , David Dudley , Alan Saltiel , Haile Tecle
IPC: C07D221/02 , C07C259/04
CPC classification number: C07D295/088 , C07C259/10 , C07D211/22 , C07D213/30 , C07D307/42 , C07D309/06 , C07D333/16
Abstract: Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
Abstract translation: 苯基氨基苯肟酸衍生物
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公开(公告)号：US06916956B2
公开(公告)日：2005-07-12
申请号：US10344157
申请日：2001-08-10
Applicant: Yuko Shinagawa , Takeo Katsushima , Takashi Nakagawa
Inventor： Yuko Shinagawa , Takeo Katsushima , Takashi Nakagawa
IPC: C07C217/28 , C07C217/60 , C07C217/76 , C07C229/38 , C07C233/25 , C07C235/42 , C07C235/60 , C07C237/30 , C07C255/54 , C07C311/21 , C07C311/29 , C07D213/30 , C07D277/24 , C07D307/42 , C07D317/58 , C07D333/16 , C07D333/56 , C07C217/10 , C07D33/16
CPC classification number: C07D213/30 , C07B2200/07 , C07C217/28 , C07C217/60 , C07C217/76 , C07C229/38 , C07C233/25 , C07C235/42 , C07C235/60 , C07C237/30 , C07C255/54 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D277/24 , C07D307/42 , C07D317/58 , C07D333/16 , C07D333/56
Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.
Abstract translation: 其中R 1为式（I）的化合物为任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有 化合物，特别是钙受体拮抗剂和骨质疏松症的治疗剂。 本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物 喜欢。 此外，还提供了化合物的中间体。
