公开(公告)号：US3895032A

公开(公告)日：1975-07-15

申请号：US33666873

申请日：1973-02-28

申请人： CIBA GEIGY CORP

发明人： CARNEY RICHARD WILLIAM JAMES

IPC分类号： C07D207/20 ,  C07D209/46 ,  C07D295/096 ,  C07D27/14

CPC分类号： C07D295/096 ,  C07D207/20 ,  C07D209/46 ,  Y10S514/824 ,  Y10S514/825

摘要： Alpha -(Cyclic tert. aminophenoxy)-alkanoic acids, e.g. those of the formula

AND FUNCTIONAL DERIVATIVES THEREOF ARE ANTI-INFLAMMATORY AND HYPOLIPIDEMIC AGENTS.

摘要翻译： α - （环状叔氨基苯氧基） - 链烷酸，例如 式R1,2 = H或烷基R1 | N-O-C-COOH | R2 AN =具有多达3个双键的单环或双环亚烷基亚氨基，其官能衍生物为抗炎和高血压剂。

公开(公告)号：US3560523A

公开(公告)日：1971-02-02

申请号：US3560523D

申请日：1967-11-01

申请人： PECHINEY SAINT GOBAIN

发明人： ETIENNE ANDRE ,  CORREIA YVES

IPC分类号： C07D207/20 ,  C07D27/14

CPC分类号： C07D207/20

摘要： 2-Y-1-PYRROLINE

IN WHICH Y IS A SUBSTITUTED ALKYL GROUP IN WHICH THE SUBSTITUENT IS NITRO,CYANO, CARBONYL AND /OR ALKYL-CARBOXYL BY REACTION OF 2-ALKOXY $1-PYRROLINE WITH A LABILE HYDROGEN COMPOUND CONTAINING THE Y GROUP.
THE INVENTION IS CONCERNED WITH THE PREPARATION OF 2SUBSTITUTED $1-PYRROLINE DERIVATIVES HAVING THE FORMULA

公开(公告)号：US3890349A

公开(公告)日：1975-06-17

申请号：US42685973

申请日：1973-12-20

申请人： LILLY CO ELI

发明人： DILLARD ROBERT D

IPC分类号： C07D207/22 ,  C07D27/14

CPC分类号： C07D207/22

摘要： 5,5-Dialkyl-3-pyrroline-2,2-dicarboxylic acid esters, useful as plant fungicides and anti-inflammatory agents, are prepared either by reacting an ethynylalkylamine with a bromomalonic ester or by heating a 2-amino-2-allenylmalonic ester with copper metal.

摘要翻译： 可用作植物杀真菌剂和抗炎剂的5,5-二烷基-3-吡咯啉-2,2-二羧酸酯通过使乙炔基烷基胺与溴马来酸酯反应或通过加热2-氨基-2-全烯丙基丙二酸 酯与铜金属。

公开(公告)号：US3632605A

公开(公告)日：1972-01-04

申请号：US3632605D

申请日：1967-07-13

申请人： RHONE POULENC SA

发明人： DEBARRE FRANCOIS ,  POIGET GILBERT

IPC分类号： C07D207/20 ,  C07D207/22 ,  C07D207/24 ,  C07D207/26 ,  C07D207/277 ,  C07D27/14

CPC分类号： C07D207/26 ,  C07D207/20 ,  C07D207/22 ,  C07D207/24 ,  C07D207/277 ,  Y10S514/96

摘要： PYRROLINE DERIVATIVES OF THE FORMULA:
WHEREIN R AND R'' ARE THE SAME OR DIFFERENT AND EACH REPRESENTS A HYDROGEN ATOM OR AN ALKYL GROUP CONTAINING 1 TO 5 CARBON ATOMS (PREFERABLY METHYL), AND THE BENZENE RING IS UNSUBSTITUTED OR CARRIES ONE OR MORE SUBSITUENTS SELECTED FORM HALOGEN ATOMS, ALKYL AND ALKOXY GROUPS CONTAINING 1 TO 5 CARBON ATOMS, AND GYDROXY, NITRO AND AMINO GROUPS, AND THEIR ACID ADDITION SALS, POSSESS PHARMACODYNAMIC PROPERTIES. THEY ACT ON THE CENTRAL NERVOUS SYSTEM, AND ARE ESPECIALLY USEFUL AS ANTI-DEPRESSANTS; FURTHERMORE, THEY SHOW A HYPERTENSIVE EFFECT.

2-(R-N(-R'')-),4-PHENYL-1-PYRROLINE

公开(公告)号：US3624081A

公开(公告)日：1971-11-30

申请号：US3624081D

申请日：1967-02-15

申请人： STERLING DRUG INC

发明人： DICKINSON WILLIAM B ,  LANG PHILIP C

IPC分类号： C07D207/22 ,  C07D27/14

CPC分类号： C07D207/22

摘要： Antibacterial 2-ethyl-1-pyrroline-3-carboxamides and derivatives thereof are prepared from either 1-(2-propynyl)-2-pyrrolidinone or 1-(1,2-propadienyl)-2-pyrrolidinone and amines in the presence of base. The carboxamides react with phenyl isocyanates to produce 1-phenylcarbamyl-2-ethyl-2-pyrroline-3-carboxamides, with either an acid halide or acid anhydride to give the corresponding 1-acyl-2-ethylidenepyrrolidine-3-carboxamides and with hydrogen to give the corresponding 2-ethyl-pyrrolidine-3-carboxamides.

公开(公告)号：US20020128490A1

公开(公告)日：2002-09-12

申请号：US09801269

申请日：2001-03-07

发明人： Jeffrey N. Johnston ,  Rajesh Viswanathan

IPC分类号： C07D29/14 ,  C07D27/14 ,  G01N033/53

CPC分类号： C07D471/04 ,  C07C251/16 ,  C07D207/16 ,  C07D209/08 ,  C07D209/36

摘要： The present invention provides methodology for carbon-nitrogen bond formation via vinyl or aryl amination. In the process of the invention, an sp2 hybridized radical is reacted with an azomethine moiety to form pyrrolidine and indole compounds. The methodology provides a facile process for the synthesis of compounds having the pyrrolidine or indole subunit and is especially advantageous for compounds having acid or base labile functional groups andor is comprised of chiral centers susceptible to acidbase epimerization.

摘要翻译： 本发明提供通过乙烯基或芳基胺化形成碳 - 氮键的方法。 在本发明的方法中，sp2杂化的基团与偶氮甲碱部分反应形成吡咯烷和吲哚化合物。 该方法为合成具有吡咯烷或吲哚亚基的化合物提供了一种简便的方法，对于具有酸或碱不稳定官能团的化合物尤其有利，并且由含有酸碱差向异构化的手性中心组成。

公开(公告)号：US20020019536A1

公开(公告)日：2002-02-14

申请号：US09275318

申请日：1999-03-24

发明人： ROLAND MAIER ,  RUDOLF HURNAUS ,  MICHAEL MARK ,  BERNHARD EISELE ,  PETER MUELLER ,  GEBHARD ADELGOSS ,  GEBHARD SCHILCHER

IPC分类号： C07D223/04 ,  C07D211/22 ,  C07D211/24 ,  C07D27/14 ,  C07C271/06 ,  C07C317/42

CPC分类号： C07D295/135 ,  C07C271/24 ,  C07C271/56 ,  C07C333/06 ,  C07C333/24 ,  C07C2601/14 ,  Y02P20/55

摘要： The present invention relates to urethanes and the thio and dithio analogues thereof of general formula 1 wherein m, n, A, X, Y and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

摘要翻译： 本发明涉及以下通式的氨基甲酸酯及其硫代和二硫类似物：其中m，n，A，X，Y和R 1至R 8如权利要求1中所定义，其对映体，非对映异构体及其盐，特别是生理上可接受的 其具有有价值的特性的酸加成盐，特别是对胆固醇生物合成的抑制作用，含有这些化合物的药物组合物，其用途和制备方法。

公开(公告)号：US3732217A

公开(公告)日：1973-05-08

申请号：US3732217D

申请日：1970-10-19

申请人： STERLING DRUG INC

发明人： DICKINSON W ,  LANG P

IPC分类号： C07D207/22 ,  C07D27/14

CPC分类号： C07D207/22

摘要： ANTIBACTERIAL 2 - ETHYL-1-PYRROLINE-3-CARBOXAMIDES AND DERIVATIVES THEREOF ARE PREPARED FROM EITHER 1-(2-PROPYNYL)-2-PYRROLIDINONE OR 1-(1,2-PROPADIENYL)-2-PYRROLIDINONE AND AMINES IN THE PRESENCE OF BASE. THE CARBOXAMIDES REACT WITH PHENYL ISOCYANATES TO PRODUCE 1-PHENYLCARBAMYL-2-ETHYL-2-PYRROLINE-3-CARBOXAMIDES, WITH EITHER AN ACID HALIDE OR ACID ANHYDRIDE TO GIVE THE CORRESPONDING 1-ACYL - 2 - ETHYLIDENEPYRROLIDINE-3-CARBOXAMIDES AND WITH HYDROGEN TO GIVE THE CORRESPONDING 2-ETHYL-PYRROLIDINE-3-CARBOXAMIDES.

公开(公告)号：US3564010A

公开(公告)日：1971-02-16

申请号：US70748468

申请日：1968-02-23

申请人： HOFFMANN LA ROCHE

发明人： BRETSCHNEIDER HERMANN ,  FRANZMAIR RUDOLF ,  KLOTZER WILHELM ,  SCHMIDT BELA

IPC分类号： C07D207/22 ,  C07D207/38 ,  C07D27/14

CPC分类号： C07D207/22 ,  C07D207/38 ,  Y10S514/884

摘要： GUANIDINO OR UREIDO OR THIOUREIDO PYRROLINES (A) PREPARED FROM 2-AMINO-$1-PYRROLINES. (B). BOTH (A) AND (B) LOWER THE BLOOD SUGAR CONTENT IN WARM BLOODED ANIMALS; HENCE, ARE USEFUL AS HYPOLGLYCEMIC AGENTS.

公开(公告)号：US20030105142A1

公开(公告)日：2003-06-05

申请号：US10192495

申请日：2002-07-11

申请人： ASTRAZENECA AB

发明人： Dearg S. Brown ,  George R. Brown

IPC分类号： C07D213/63 ,  A61K031/44 ,  A61K031/401 ,  C07D27/14

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D239/74 ,  C07D241/44 ,  C07D261/18 ,  C07D277/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

摘要： The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q1 is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and Q2 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.