公开(公告)号：US20090149531A1

公开(公告)日：2009-06-11

申请号：US12332324

申请日：2008-12-10

申请人： Juan Pablo PIVEL RANIERI ,  Juan Manuel Ferrer Cuesta ,  Fernando Martinez Galan ,  Juan Manuel Irache ,  Jose Luis Novella Robisco ,  Juan Jose Perez Rueda ,  Ma Paz Maria Martin ,  Julio Alvarez-Builla Gomez ,  Jaime Bermejo ,  Fernando Vidal Vanaclocha

发明人： Juan Pablo PIVEL RANIERI ,  Juan Manuel Ferrer Cuesta ,  Fernando Martinez Galan ,  Juan Manuel Irache ,  Jose Luis Novella Robisco ,  Juan Jose Perez Rueda ,  Ma Paz Maria Martin ,  Julio Alvarez-Builla Gomez ,  Jaime Bermejo ,  Fernando Vidal Vanaclocha

IPC分类号： A61K31/341 ,  C07D307/04 ,  A61P17/00

CPC分类号： A61K31/365 ,  A61K9/06

摘要： The present invention is a chemical composition including: Use of the compound with the chemical formula can be applied in pharmaceutical compositions for the treatment of psoriasis.

摘要翻译： 本发明是一种化学组合物，其包括：具有化学式的化合物的用途可用于治疗牛皮癣的药物组合物中。

公开(公告)号：US20080009496A1

公开(公告)日：2008-01-10

申请号：US11616713

申请日：2006-12-27

申请人： Richard Daifuku ,  Alexander Gall ,  Dmitri Sergueev

发明人： Richard Daifuku ,  Alexander Gall ,  Dmitri Sergueev

IPC分类号： A61K31/341 ,  A61K31/4196 ,  A61K31/53 ,  A61P31/18 ,  C07D249/12 ,  C07D307/04 ,  C07D403/02 ,  C07D403/14 ,  C07D487/02 ,  C07D487/12

CPC分类号： C07D405/12 ,  C07D487/04 ,  C07D487/16 ,  C07H13/12 ,  C07H17/02 ,  C07H19/12 ,  C07H19/23

摘要： The present invention provides compounds as well as methods of using the compounds as antiviral and anti-cancer chemotherapeutic agents.

摘要翻译： 本发明提供化合物以及使用该化合物作为抗病毒和抗癌化学治疗剂的方法。

公开(公告)号：US07049329B2

公开(公告)日：2006-05-23

申请号：US10439347

申请日：2003-05-15

申请人： Brian M. Aquila ,  Seth C. Hopkins ,  Curtis A. Lockshin ,  Fengjiang Wang

发明人： Brian M. Aquila ,  Seth C. Hopkins ,  Curtis A. Lockshin ,  Fengjiang Wang

IPC分类号： A61K31/135 ,  A61K31/34 ,  A61K31/44 ,  C07D307/04

CPC分类号： C40B40/04 ,  C07C217/58 ,  C07C2601/02 ,  C07D307/14 ,  C40B20/08 ,  C40B30/04 ,  C40B40/00 ,  C40B50/14

摘要： One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

公开(公告)号：US20050130959A1

公开(公告)日：2005-06-16

申请号：US10970344

申请日：2004-10-20

申请人： Hong Liu ,  Phillip Alper ,  Daniel Mutnick ,  Donald Karanewsky

发明人： Hong Liu ,  Phillip Alper ,  Daniel Mutnick ,  Donald Karanewsky

IPC分类号： A61K20060101 ,  A61K31/34 ,  A61K31/4025 ,  A61K31/452 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/541 ,  C07D307/04 ,  C07D307/33 ,  C07D405/12 ,  C07D407/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/02 ,  C07D45/02

CPC分类号： C07D407/12 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D235/08 ,  C07D295/215 ,  C07D307/33 ,  C07D307/68 ,  C07D405/12

摘要： The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

公开(公告)号：US5886198A

公开(公告)日：1999-03-23

申请号：US13840

申请日：1998-01-27

申请人： Daisuke Ogawa ,  Masahiro Koike ,  Yoshiyuki Yamamoto

发明人： Daisuke Ogawa ,  Masahiro Koike ,  Yoshiyuki Yamamoto

IPC分类号： C07D317/12 ,  C07D307/04

CPC分类号： C07D317/12

摘要： Cyclic formal is manufactured by cyclic reaction of an alkylene glycol and an aldehyde in a reactor, producing formal mixed with unreacted aldehyde as an impurity, which impurity is reduced in amount by connecting the reactor to a distillation tower and continuously supplying alkylene glycol to the distillation tower from which unreacted formaldehyde and a cyclic formal are being distilled, and continuously reacting them with supplied raw formaldehyde by countercurrent flow during distillation; water content in azeotropic admixture with cyclic formal can be removed by azeotropic distillation with a hydrocarbon azeotropic mixture with water, distilling water from the cyclic formal.

摘要翻译： 循环形式通过在反应器中的亚烷基二醇和醛的循环反应制备，产生与未反应的醛作为杂质混合的形式，该杂质通过将反应器连接到蒸馏塔并连续地将亚烷基二醇连续地供应至蒸馏 蒸馏出未反应的甲醛和环状缩甲醛的塔，并在蒸馏期间通过逆流流动与供应的生甲醛连续反应; 与环状甲醛共沸混合物中的水含量可以通过与烃共沸混合物与水共沸蒸馏除去，从循环甲醛蒸馏出水。

公开(公告)号：US5278313A

公开(公告)日：1994-01-11

申请号：US858907

申请日：1992-03-27

申请人： John K. Thottathil ,  Yadagiri Pendri ,  Wen-Sen Li ,  David R. Kronenthal

发明人： John K. Thottathil ,  Yadagiri Pendri ,  Wen-Sen Li ,  David R. Kronenthal

IPC分类号： C07C69/675 ,  C07C69/716 ,  C07C319/06 ,  C07D307/04 ,  C07D257/00

CPC分类号： C07C319/06 ,  C07C69/675 ,  C07C69/716

摘要： A novel, overall process for the preparation of a compound of the formula I: ##STR1## where R.sup.1 and R.sup.2 are each independently hydrogen, an alkyl group, a cycloalkyl group, an aryl group or, taken together with the carbon atom to which they are attached, form a cycloalkyl group; andR.sup.3 is hydrogen, an alkyl group, or an aryl group,or salts thereof, useful as intermediates in the preparation of HMG-CoA reductase inhibitors; novel methods within the overall process; and novel intermediates produced by those methods.

摘要翻译： 一种用于制备式I化合物的新颖的总体方法：其中R 1和R 2各自独立地为氢，烷基，环烷基，芳基或与碳原子一起 它们相连，形成环烷基; 和R3是氢，烷基或芳基，或其盐，可用作制备HMG-CoA还原酶抑制剂的中间体; 整体过程中的新颖方法; 和由这些方法生产的新型中间体。

公开(公告)号：US5030654A

公开(公告)日：1991-07-09

申请号：US354170

申请日：1989-05-19

申请人： Ian T. Barnish ,  John C. Danilewicz ,  Keith James ,  Gillian M. R. Samuels ,  Nicholas K. Terrett ,  Michael T. Williams ,  Martin J. Wythes

发明人： Ian T. Barnish ,  John C. Danilewicz ,  Keith James ,  Gillian M. R. Samuels ,  Nicholas K. Terrett ,  Michael T. Williams ,  Martin J. Wythes

IPC分类号： A61K31/16 ,  A61K31/335 ,  A61K31/395 ,  C07C235/52 ,  C07C235/82 ,  C07C237/24 ,  C07C311/01 ,  C07D207/30 ,  C07D209/46 ,  C07D213/02 ,  C07D213/56 ,  C07D231/00 ,  C07D233/00 ,  C07D235/00 ,  C07D237/00 ,  C07D239/00 ,  C07D241/12 ,  C07D261/10 ,  C07D277/36 ,  C07D277/46 ,  C07D295/00 ,  C07D295/185 ,  C07D307/04 ,  C07D307/16 ,  C07D307/68 ,  C07D309/02 ,  C07D319/00 ,  C07D321/02 ,  C07D321/08 ,  C07D321/12 ,  C07D333/34 ,  C07D521/00

CPC分类号： C07D241/12 ,  C07D209/46 ,  C07D213/56 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D261/10 ,  C07D277/36 ,  C07D277/46 ,  C07D295/185 ,  C07D307/16 ,  C07D307/68 ,  C07D321/08 ,  C07D333/34

摘要： A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

公开(公告)号：US4725302A

公开(公告)日：1988-02-16

申请号：US800179

申请日：1985-11-20

申请人： Josef Ehrenfreund

发明人： Josef Ehrenfreund

IPC分类号： A01N43/82 ,  A01N43/824 ,  A01N47/24 ,  C07D271/06 ,  C07D271/07 ,  C07D307/12 ,  C07D307/20 ,  C07D309/12 ,  C07D413/12 ,  A61K31/42 ,  C07D271/10 ,  C07D307/04 ,  C07D309/04

CPC分类号： C07D271/07 ,  A01N43/82 ,  A01N47/24 ,  C07D307/12 ,  C07D307/20 ,  C07D309/12 ,  C07D413/12

摘要： Phenylhydrazines of the formula I ##STR1## wherein R.sub.1 is --A--R--Z,A is oxygen, sulfur, ##STR2## R is C.sub.1 -C.sub.6 -alkylene, C.sub.1 -C.sub.6 -haloalkyl-C.sub.1 -C.sub.6 -alkylene, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkylene or C.sub.1 -C.sub.6 -alkylthio-C.sub.1 -C.sub.6 -alkylene,Z is halogen, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl, orR and Z together are ##STR3## R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or (C.sub.1 -C.sub.6 -alkyl).sub.2 amino,n is a number from 1-4, and R.sub.2 can be different when n is one of the numbers 2-4,R.sub.3 is halogen,R.sub.4 is hydrogen,R.sub.5 is --COOR.sub.6, orR.sub.3, R.sub.4 and R.sub.5 together form a bridge member of the formula ##STR4## and R.sub.6 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl.A process for producing these phenylhydrazines and their use for controlling pests are described.

摘要翻译： 式I的苯肼（I）其中R 1是-ARZ，A是氧，硫，R 2是C 1 -C 6亚烷基，C 1 -C 6卤代烷基-C 1 -C 6亚烷基，C 1 -C 6 - 烷氧基-C 1 -C 6亚烷基或C 1 -C 6烷硫基-C 1 -C 6亚烷基，Z为卤素，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，C 1 -C 6烷基亚磺酰基或C 1 -C 6 - C6-烷基磺酰基或R和Z一起是R 2是氢，卤素，C 1 -C 6烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷硫基或（C 1 -C 6烷基）2氨基 ，n为1-4的数，当n为2-4时，R2为可以不同，R3为卤素，R4为氢，R5为-COOR6或R3，R4和R5一起形成桥构件 式为“IMAGE”，R6为C1-C6-烷基，C2-C6-烯基或C2-C6-炔基。 描述了制备这些苯肼的方法及其用于防治害虫的用途。

公开(公告)号：US4500722A

公开(公告)日：1985-02-19

申请号：US418061

申请日：1982-09-15

申请人： David A. Thompson

发明人： David A. Thompson

IPC分类号： C10L1/30 ,  C07C45/00 ,  C07C45/77 ,  C07C49/14 ,  C07C49/92 ,  C07C67/00 ,  C07F3/02 ,  C07F3/06 ,  C07D307/04

CPC分类号： C07C45/77

摘要： Novel .beta.-diketonate complexes incorporating a tetrahydrofuran adduct, having the formula M(hfa).sub.2.nTHF wherein M is Mg or Zn and n is in the range of about 1-4 and, which offer high volatility and good chemical stability at vaporization temperatures, are described.

公开(公告)号：US4400523A

公开(公告)日：1983-08-23

申请号：US319768

申请日：1981-11-09

申请人： Manfred Jautelat ,  Dieter Arlt ,  Reinhard Lantzsch ,  Rainer Fuchs ,  Hans-Jochem Riebel ,  Rolf Schroder ,  Horst Harnisch

发明人： Manfred Jautelat ,  Dieter Arlt ,  Reinhard Lantzsch ,  Rainer Fuchs ,  Hans-Jochem Riebel ,  Rolf Schroder ,  Horst Harnisch

IPC分类号： C07C313/00 ,  A01N53/00 ,  A01N53/08 ,  A01N53/10 ,  C07C59/64 ,  C07C67/00 ,  C07C69/757 ,  C07C319/20 ,  C07C323/62 ,  C07D307/33 ,  C07D307/04 ,  C07D307/12

CPC分类号： C07D307/33 ,  A01N53/00 ,  C07C59/64

摘要： A process for the preparation of a styryl-cyclopropane-carboxylic acid ester of the formula ##STR1## in which R is C.sub.1-4 -alkyl or an alcohol radical customary in pyrethroids,R.sup.1 is alkoxy or alkylthio, either of which may be optionally substituted by halogen,R.sup.2 is hydrogen or alkoxy, orR.sup.1 and R.sup.2 together are optionally halogen-substituted alkylenedioxy, andR.sup.3 is hydrogen or chlorine, comprising reacting a compound of the formula ##STR2## with, respectively, one, two or three equivalents of a base at a temperature below 60.degree. C. The products are insecticidally active when R is the residue of a pyrethroid-type alcohol. Various syntheses are given for the starting materials which are new.

摘要翻译： 制备式IMAMA的苯乙烯基 - 环丙烷 - 羧酸酯的方法，其中R是C1-4烷基或拟除虫菊酯中通常的醇基，R 1是烷氧基或烷硫基，其中任一个可以任选被取代 通过卤素，R 2是氢或烷氧基，或者R 1和R 2一起是卤素取代的亚烷基二氧基，并且R 3是氢或氯，包括分别将下式的化合物与其反应： 一个，两个或三个当量的碱在温度低于60℃。当R是拟除虫菊酯型酒精的残留物时，产物具有杀虫活性。 给出了新的起始材料的各种合成。