公开(公告)号：EP2069299A2

公开(公告)日：2009-06-17

申请号：EP07813133.1

申请日：2007-07-19

申请人： Pharmacofore, Inc.

发明人： JENKINS, Thomas, E.

IPC分类号： C07D211/22 ,  C07C211/01 ,  C07C211/45 ,  C07D207/12 ,  C07D211/46 ,  C07D223/04 ,  A61K31/4453 ,  A61P23/00

CPC分类号： C07D211/22 ,  C07C219/14 ,  C07C219/22 ,  C07C229/60 ,  C07C229/64 ,  C07D207/12 ,  C07D211/46 ,  C07D223/04

摘要： In one embodiment the invention provides novel compounds of Formula (I) as well as prodrugs, salts, hydrates, solvates and N-oxides thereof. The invention also provides pharmaceutical compositions that include such compounds as well as methods for making and methods for using such compounds in medical therapy.

公开(公告)号：EP1586553B1

公开(公告)日：2009-04-22

申请号：EP05006414.6

申请日：2005-03-23

申请人： DAISO CO., LTD.

发明人： Yaegashi, Keisuke ,  Mikami, Masafumi

IPC分类号： C07C209/68 ,  C07C213/08 ,  C07D207/12

CPC分类号： C07D207/12 ,  C07C213/00 ,  C07C215/08

公开(公告)号：EP1701939B1

公开(公告)日：2009-02-25

申请号：EP04806187.3

申请日：2004-12-22

申请人： Somanta Limited

发明人： PATTERSON, Laurence, Hylton ,  PORS, Klaus ,  TEESDALE-SPITTLE, Paul, Henry

IPC分类号： C07D207/06 ,  C07D211/22 ,  C07D211/46 ,  C07D207/12 ,  C07D207/08 ,  C07D211/18 ,  C07D211/38 ,  C07D207/10 ,  C07D207/46 ,  C07D211/94 ,  A61K31/445 ,  A61P35/00

CPC分类号： C07D207/08 ,  C07D207/06 ,  C07D207/10 ,  C07D207/12 ,  C07D207/46 ,  C07D211/18 ,  C07D211/22 ,  C07D211/38 ,  C07D211/46 ,  C07D211/94

摘要： Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, -NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.

公开(公告)号：EP1928821B1

公开(公告)日：2009-01-07

申请号：EP06795581.5

申请日：2006-09-01

申请人： Pfizer Limited

发明人： GLOSSOP, Paul, Alan ,  MANTELL, Simon, John ,  STRANG, Ross, Sinclair ,  WATSON, Christine, Anne, Louise ,  WOOD, Anthony

IPC分类号： C07D207/12 ,  C07D413/12 ,  C07D211/46 ,  C07D205/04 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4409 ,  A61P37/00

CPC分类号： C07D207/12 ,  C07D205/02 ,  C07D205/04 ,  C07D207/04 ,  C07D211/26 ,  C07D211/46 ,  C07D413/12

摘要： The invention relates to compounds of Formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.

公开(公告)号：EP1051397B1

公开(公告)日：2008-12-31

申请号：EP99904421.7

申请日：1999-01-29

申请人： Aventis Pharmaceuticals Inc.

发明人： HULME, Christopher ,  MORTON, George, C. ,  SALVINO, Joseph, M. ,  LABAUDINIERE, Richard, F. ,  MASON, Helen, J. ,  MORRISSETTE, Matthew, M. ,  MA, Liang ,  CHERRIER, Marie-Pierre

IPC分类号： C07D205/00 ,  C07D205/08 ,  C07D243/12 ,  C07D243/24 ,  C07D241/04 ,  C07D241/36 ,  C07D231/00 ,  C07D233/22 ,  C07D207/00 ,  C07D207/12 ,  C07D401/00 ,  C07D241/08

CPC分类号： C07D207/273 ,  C07C231/14 ,  C07C269/06 ,  C07C2601/02 ,  C07C2601/16 ,  C07D231/12 ,  C07D233/28 ,  C07D233/56 ,  C07D233/64 ,  C07D241/18 ,  C07D241/44 ,  C07D243/24 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07F9/645 ,  C40B40/00 ,  Y02P20/55 ,  C07C237/22 ,  C07C271/28

摘要： The present invention relates to a method for preparing an N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound of formula (I) wherein Ra is (II); Raa is hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rb is hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rca and Rcb are independently hydrogen, optionally substituted aliphatic or optionally substituted aromatic; Rd is (III); and Rda is optionally substituted aliphatic or optionally substituted aromatic; and Raa is substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Rb, Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rb is substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Raa, Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rca and Rcb are independently substituted with a primary or secondary protected amine that upon deprotection can react with the *ab or *db carbon, or at least one of Raa, Rb, Rca, Rcb or Rda where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring; or Rda is substituted with a primary or secondary protected amine that upon deprotection can react with at least one of Rca or Rcb where each is at least substituted with an activated carboxylic acid to form a 5-7 membered cyclic ring, provided that when Raa is substituted with a primary or secondary protected amine that upon deprotection can react with Rb at least substituted with an activated carboxylic acid, then Raa is other than substituted aliphatic, comprising reacting the following four compounds: a carbonyl compound of formula (IV), an amine compound of formula NH2Rb, an isonitrile compound of formula NCRda, and an acid compound of formula RaCO2H, to produce the N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound, and the N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound. The invention is also directed to a method for cyclizing N-[(aliphatic or aromatic)carbonyl]-2-aminoacetamide compound to a cyclic compound selected from the group consisting of a 1,4-benzodiazepine-2,5-dione derivative, diketopiperazine derivative, ketopiperazine derivative, lactam derivative, 1,4-benzodiazapine derivative and dihydroquinoxalinones derivative, and the cyclized compound.

摘要翻译： 本发明涉及一种用于N个制备 - [（脂肪族或芳香族）羰基]式（I）-2-氨基乙酰胺化合物worin R a是（II）; RAA是氢，任选取代的脂或任选取代的芳族的; R b是氢，任选取代的脂或任选取代的芳族的; RCA和RCB是unabhängig氢，任选substituiertem脂肪族或芳香族OPTIONALLY substituiertem; R d是（III）; 和RDA任选substituiertem脂肪族或芳香族OPTIONALLY substituiertem; 和拉加与伯或仲保护的胺取代的并在去保护后能够与* AB或*分贝碳反应，或R b，RCA或RCB，其中每个是至少substituiertem与活化的羧酸，以形成一个5中的至少一个 -7元环; 或R b与伯或仲保护的胺取代的在去保护并可以通过* AB或*分贝碳反应，或拉加，RCA或RCB，其中每个是至少substituiertem与活化的羧酸，以形成一个5中的至少一个 -7元环; 或RCA和RCB是unabhängigsubstituiertem与伯或仲保护的胺并在去保护后能够与* AB或*分贝碳反应，或拉加，RB，RCA，RCB或RDA中的至少一个，其中每个是至少substituiertem与 活化的羧酸形成5-7元环; 或RDA是用伯或仲胺保护基取代并在去保护后能够与RCA或RCB中的至少一个，其中每个是至少substituiertem与活化的羧酸，以形成5-7元环状环反应，提供并当拉加是 与伯或仲胺保护时substituiertem脱保护确实可以与RB反应至少substituiertem与活化的羧酸，然后拉加比substituiertem脂肪族其他方法，包括将下列四种化合物：式的羰基化合物（IV）为胺 式NH2Rb的化合物，以异腈式NCRda的化合物，并在式RaCO2H的酸化合物，以产生N - [（脂肪族或芳香族）羰基] -2-氨基乙酰胺化合物，以及N - [（脂肪族或芳香族）羰基 ] -2-氨基乙酰胺化合物。 因此，本发明涉及用于环化N A方法 - [（脂肪族或芳香族）羰基] -2-氨基乙酰胺化合物由1,4-苯并二氮杂-2,5-二酮衍生物，二酮哌嗪从组中选择的环式化合物 衍生物，ketopiperazine衍生物，内酰胺衍生物，1,4-苯二氮衍生物和dihydroquinoxalinones衍生物，环化化合物。

公开(公告)号：EP1996545A1

公开(公告)日：2008-12-03

申请号：EP07758126.2

申请日：2007-03-08

申请人： Boehringer Ingelheim International GmbH ,  Boehringer Ingelheim Pharma GmbH & Co. KG

发明人： DE LOMBAERT, Stephane ,  ELDRUP, Anne, Bettina ,  KOWALSKI, Jennifer, A. ,  MUGGE, Ingo, Andreas ,  SOLEYMANZADEH, Fariba ,  SWINAMER, Alan, David ,  TAYLOR, Steven, John

IPC分类号： C07D207/12 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/62 ,  C07D295/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  A61K31/4545 ,  A61P9/00

CPC分类号： C07D295/215 ,  C07D207/12 ,  C07D211/22 ,  C07D211/46 ,  C07D211/58 ,  C07D211/62 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12

摘要： Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.

公开(公告)号：EP1984330A1

公开(公告)日：2008-10-29

申请号：EP07705135.7

申请日：2007-02-07

申请人： AstraZeneca AB

发明人： ARNOULD, Jean-Claude ,  DELOUVRIE, Benedicte ,  KETTLE, Jason, Grant

IPC分类号： C07D205/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/48 ,  C07D211/46 ,  C07D211/96 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06 ,  A61K31/166 ,  A61K31/18 ,  A61K31/33 ,  C07C233/87 ,  C07C311/32

CPC分类号： C07D205/04 ,  C07C233/87 ,  C07C311/04 ,  C07D207/08 ,  C07D207/12 ,  C07D207/48 ,  C07D211/46 ,  C07D211/96 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D413/06

摘要： The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.

摘要翻译： 本发明涉及抑制α5β1功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，它们作为药物的用途，以及它们在制备用于治疗温血动物例如 人类患有显着血管生成或血管成分的疾病，例如用于治疗实体瘤。 本发明还涉及抑制α5b1的化合物，并且还表现出针对其他整联蛋白的适当选择性特征。

公开(公告)号：EP1605934A4

公开(公告)日：2008-10-08

申请号：EP04758116

申请日：2004-03-23

申请人： DU PONT

发明人： MANZER LEO ERNEST

IPC分类号： C07D207/26 ,  C07D207/267 ,  A61K31/4015 ,  A01N43/36 ,  C07D207/12

CPC分类号： C07D207/267

公开(公告)号：EP1950198A1

公开(公告)日：2008-07-30

申请号：EP06822568.9

申请日：2006-10-30

申请人： Toray Fine Chemicals Co., Ltd.

发明人： MORIMOTO, Masao ,  YAMAKAWA, Atsushi

IPC分类号： C07D207/12

CPC分类号： C07D207/12

摘要： Provided are: a process for production of a benzyloxypyrrolidine derivative in high yield and safety, and a process for production of a hydrochloride powder of a benzyloxypyrrolidine derivative in high yield and safety; the process for production of a benzyloxypyrrolidine derivative expressed by the general formula (2) [Chemical formula 2], in reacting a pyrrolidinol derivative represented by the general formula (1) [Chemical formula 1 with a benzyl halide derivative in the presence of an alkali metal hydroxide, wherein the reaction is carried out in either of the following conditions A or B; condition A: an aprotic polar solvent, and condition B: an aliphatic ether solvent containing a phase transfer catalyst:

摘要翻译： 本发明提供一种以高收率和安全性生产苄氧基吡咯烷衍生物的方法以及以高收率和安全性生产苄氧基吡咯烷衍生物的盐酸盐粉末的方法; （1）表示的吡咯烷醇衍生物[化学式1]与苄基卤化物衍生物在碱存在下反应，生产由通式（2）[化学式2]表示的苄氧基吡咯烷衍生物的方法 金属氢氧化物，其中反应在下列任一条件下进行：A或B; 条件A：非质子传递极性溶剂，条件B：含有相转移催化剂的脂族醚溶剂：

公开(公告)号：EP1693364A4

公开(公告)日：2008-06-18

申请号：EP04788396

申请日：2004-09-30

申请人： DAIICHI SEIYAKU CO

发明人： FUJITA MASAO ,  KITAGAWA YUTAKA ,  MUTO MAKOTO

IPC分类号： C07D207/09 ,  C07B53/00 ,  C07D207/12 ,  C07D207/16 ,  C07D207/20

CPC分类号： C07D207/20 ,  C07B2200/07 ,  C07D207/09 ,  C07D207/12 ,  C07D207/16 ,  Y02P20/55

摘要： Provided are a process for the production of intermediates from which optically active cyclopropylamine derivatives (6) can be easily synthesized by a short operation without optical resolution; and such intermediates. A process for the production of optically active compounds represented by the general formula (4) or salts thereof: (4) (wherein R1 is an amino-protecting group), characterized by reacting an optically active compound represented by the general formula (3): (3) (wherein R1 is as defined above) with a reagent prepared from both a titanium(IV) reagent and an alkylmetal compound, if necessary, in the presence of a Lewis acid.