公开(公告)号：CA2849711A1

公开(公告)日：2013-03-28

申请号：CA2849711

申请日：2012-09-20

Applicant: AKHAPKINA VALENTINA IVANOVNA ,  AKHAPKIN ROMAN VITALYEVICH

Inventor： AKHAPKINA VALENTINA IVANOVNA ,  AKHAPKIN ROMAN VITALYEVICH

IPC: A61K31/4015 ,  A61P3/04 ,  A61P7/10 ,  A61P9/00 ,  A61P25/00 ,  A61P37/02 ,  A61P39/06 ,  A61P43/00 ,  C07D201/00 ,  C07D201/16 ,  C07D201/18

Abstract: The invention relates to various fields of medicine, pharmaceutics and pharmacology and the chemical pharmaceutical, pharmaceutical and parapharmaceutical industry, and specifically concerns a novel class of agents which exhibit modulatory activity with a commensurate effect. The essence of the invention is that the proposed (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide product does not contain biologically inert substances which exert a negative effect on its newly discovered or significantly improved known properties and characteristics, giving rise to hitherto unknown fundamental and highly important ideas about the compound, expanding the scope of use thereof with an increase in the effectiveness and safety of use and an increase in the therapeutic index, and making it possible to produce the product and related products with the newly found properties and characteristics.

公开(公告)号：BRPI0804506A2

公开(公告)日：2011-08-30

申请号：BRPI0804506

申请日：2008-02-20

Applicant: UNIV MICHIGAN STATE

Inventor： FROST JOHN W

IPC: C07D201/00 ,  C07D201/02 ,  C07D201/08

Abstract: Catalytic processes for preparing caprolactam, pipecolinic acid, and their derivatives, from lysine or alpha-amino-epsilon-caprolactam starting materials, and products produced thereby. A process for preparing caprolactam or a derivative thereof, the process comprising contacting a reactant comprising lysine or alpha aminocaprolactam with a catalyst and a gas comprising hydrogen gas, in the presence of a solvent. The catalyst may be provided on a support material, such as a transition metal.

公开(公告)号：NO330989B1

公开(公告)日：2011-08-29

申请号：NO20053910

申请日：2005-08-22

Applicant: UCB FARCHIM SA

Inventor： ATES CELAL ,  CAVOY EMILE ,  BOUVY DIDIER

IPC: C07D295/15 ,  C07D201/00 ,  C07D271/06 ,  C07D271/07

Abstract: The present invention relates to new enantiomerically pure piperazine derivatives of formula (I) wherein Y represents hydroxy or a leaving group and n is 1, 2, 3, 4 or 5, and to their use as synthesis intermediates, especially for the preparation of pharmaceutically active compounds

公开(公告)号：UA86770C2

公开(公告)日：2009-05-25

申请号：UAA200512449

申请日：2004-05-17

Applicant: DSM IP ASSETS BV

Inventor： SMEETS THEODORUS MARIA ,  LEMMENS JOANNES ALBERTUS WILHELMUS ,  MOSTERT FRANK ,  CHENG PETER WEI-HAE

IPC: B01F5/04 ,  B01J19/26 ,  C07D201/00

Abstract: Изобретениекасаетсяспособаполучениякапролактамапутемдобавленияциклoгексаноноксимак реакционнойсмеси, котораясодержиткапролактами сернуюкислоту, спомощьюсмесительногоустройства, причемсмесительноеустройствовключает (і) трубопровод, черезкоторыйпротекаетреакционнаясмесь, и (іі) каналы, которыерасположенывокругтрубопроводаи открытыв трубопровод, ауказанныйспособвключаетпропусканиереакционнойсмесичерезтрубопроводи подачуциклогексаноноксимав реакционнуюсмесьчерезодинилибольшеизуказанныхканалов, где Re>5000, причем Re означаетчислоРейнольдса, определенноекак, где= плотность (вкг/м) реакционнойсмеси, �

公开(公告)号：ES2313126T3

公开(公告)日：2009-03-01

申请号：ES04817204

申请日：2004-10-14

Applicant: SOLVAY PHARM GMBH

Inventor： SYKES DAVID ,  MOLONEY BRIAN ,  MARRISON LESTER ,  ZIEGLER DIETER ,  MLINARIC MICHAEL ,  BOECKER CHRISTIANE

IPC: C07D201/00 ,  A61K31/353 ,  C07D311/68 ,  C07D407/12

Abstract: Compuestos de la fórmula general I, (Ver fórmula) en donde, R 1 significa alquilo C1 - 4, R 2 significa alquilo C1 - 4, R 3 significa fenilo, que está eventualmente sustituido, 1-2 veces, con halógeno, alquilo C1 - 4, alcoxi C1 - 4 o trifluorometilo; naftilo o bifenilo, R 4 significa hidrógeno; alquilo C1 - 6 o cicloalquil C3 - 7-alquilo C1 - 4, R 5 significa hidrógeno y R 6 significa alquilo C1 - 6; fenil-alquilo C1 - 4, cuyo grupo fenilo está eventualmente sustituido 1 vez con halógeno; furil-alquilo C1 - 4 o tetrahidronaftilo, o R 5 y R 6 , junto con el nitrógeno al que están unidos, forman un anillo de piperazina el cual está eventualmente sustituido con fenilo.

公开(公告)号：IL192912D0

公开(公告)日：2009-02-11

申请号：IL19291208

申请日：2008-07-20

Applicant: SQUIBB BRISTOL MYERS CO

IPC: A61K31/403 ,  A61K31/435 ,  C07C62/06 ,  C07C69/00 ,  C07C69/716 ,  C07C229/28 ,  C07C271/22 ,  C07D20060101 ,  C07D201/00 ,  C07D207/22 ,  C07D207/277 ,  C07D209/02 ,  C07D209/52 ,  C07D221/02

Abstract: Methods and compounds for production of cycloproyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

公开(公告)号：AT405547T

公开(公告)日：2008-09-15

申请号：AT04817204

申请日：2004-10-14

Applicant: SOLVAY PHARM GMBH

Inventor： SYKES DAVID ,  MOLONEY BRIAN ,  MARRISON LESTER ,  ZIEGLER DIETER ,  MLINARIC MICHAEL ,  BOECKER CHRISTIANE ,  BRUECKNER REINHARD ,  WESKE MICHAEL ,  WITTE KLAUS ,  FISCHER YVAN

IPC: C07D201/00 ,  A61K31/353 ,  C07D311/68 ,  C07D407/12

Abstract: The invention relates to compounds of general formula (I), wherein the meaning of R 1 , R 2 , R 3 , R 4 , R 5 and R 6 is given in a description, to a method for producing said compounds and to intermediate products thereof. Drugs containing the inventive compounds of formula (1) are also disclosed.

公开(公告)号：AU2002333229B2

公开(公告)日：2006-11-30

申请号：AU2002333229

申请日：2002-07-03

Applicant: SOLVAY PHARM BV

Inventor： HERREMANS ARNOLDUS H J ,  MCCREARY ANDREW C ,  SCHARRENBURG GUSTAAF J M VAN ,  COOLEN HEIN K A C ,  TULP MARTINUS TH M ,  MAARSEVEEN JAN H VAN ,  HOOGENBAND ADRIANUS VAN DEN ,  BAKKER WOUTER I IWEMA

IPC: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/08 ,  A61P3/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P11/08 ,  A61P13/02 ,  A61P13/10 ,  A61P17/00 ,  A61P17/02 ,  A61P17/04 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D201/00 ,  C07D241/00 ,  C07D241/04 ,  C07D265/00 ,  C07D401/14 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D413/14 ,  C07D471/04

Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH 3 , CF 3 , OCH 3 , halogen, cyano and 5-CF 3 -tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1-3C); n has the value 0-3; m has the value 0-2; R 1 represents NH 2 , NH-alkyl (1-3C), dialkyl (1-3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH 3 -piperazinyl; R 2 is hydrogen, alkyl (1-4C) or phenyl, or R 2 together with (CH 2 ) m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R 3 and R 4 independently represent hydrogen or methyl, or R 3 and R 4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved

公开(公告)号：DE69829867T2

公开(公告)日：2006-02-23

申请号：DE69829867

申请日：1998-09-10

Applicant: YEDA RES & DEV ,  JOHN HOPKINS UNIVERSITY BALTIM

Inventor： BACHI MARIO ,  POSNER H ,  KORSHIN EDWARD

IPC: C07D201/00 ,  C07D319/02

Abstract: PCT No. PCT/IL98/00440 Sec. 371 Date May 11, 2000 Sec. 102(e) Date May 11, 2000 PCT Filed Sep. 10, 1998 PCT Pub. No. WO99/12900 PCT Pub. Date Mar. 18, 19992,3-Dioxabicyclo[3.3.1]nonane derivatives, carrying, at position 4, a sulfur-containing functionality selected from the group consisting of sulfonyl, sulfinyl and sulfenyl, adhered to C(4) vie methylene group, represented by structural formula (A) wherein: X is hydrogen, hydroxy, alkoxy, optionally substituted by alkoxy or acyloxy, aralkoxy optionally substituted by alkoxy or aryloxy, and M is hydrogen, hydroxy, alkoxy, alkenyloxy, acyloxy, optionally substituted by acyl or acyloxy, aralokoxy, arylalkenyloxy, oxalyloxy substituted by alkoxy, di(alkyl)amino or alkyl(aryl)amino, di(aralalkyl)amino or carbonyloxy substituted by arloxy, di(alkyl)amino, di(aralkyl)amino and alkyl(aryl)amino; or X and M together represent a carbon-carbon bond or an oxygen atom; L is hydrogen or L and M together represent a carbon-carbon bond; and either Z is a radical R-S(=O)n- and Y is hydrogen, or Y is R-S(=O)n- and Z is hydrogen, wherein R is alkyl optionally substituted by alkoxy or alkoxycarbonyl, cycloalkyl, or aryl or araklkyl optionally substituted by alkyl, halogen or CF3; and n is 0, 1, or 2, are useful for the prevention and/or treatment of malaria.

公开(公告)号：BR0317139A

公开(公告)日：2005-11-29

申请号：BR0317139

申请日：2003-12-04

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： VU TRUC CHI ,  BRZOZOWSKI DAVID B ,  FOX RITA ,  GODFREY JOLLIE DUAINE JR ,  HANSON RONALD L ,  KOLOTUCHIN SERGEI V ,  MAZULLO JOHN A JR ,  PATEL RAMESH N ,  WANG JIANJI ,  WONG KWOK ,  YU JURONG ,  ZHU JASON ,  MAGNIN DAVID R ,  AUGERI DAVID J ,  HAMANN LAWRENCE G

IPC: A61K31/403 ,  A61K31/435 ,  C07C62/06 ,  C07C69/00 ,  C07C69/716 ,  C07C229/28 ,  C07C271/22 ,  C07D20060101 ,  C07D201/00 ,  C07D207/22 ,  C07D207/277 ,  C07D209/02 ,  C07D209/52 ,  C07D221/02

Abstract: Methods and compounds for production of cycloproyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.