公开(公告)号：US5321031A

公开(公告)日：1994-06-14

申请号：US950379

申请日：1992-09-23

申请人： Sundeep Dugar

发明人： Sundeep Dugar

IPC分类号： C07D295/12 ,  A61K31/165 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/10 ,  A61P43/00 ,  C07C231/10 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D221/20 ,  C07D295/125 ,  C07D295/18 ,  C07D295/185 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  A61K31/44 ,  C07C233/01 ,  C07D241/04

CPC分类号： C07D221/20 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D295/125 ,  C07D295/185 ,  C07D491/10 ,  C07C2101/14

摘要： Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

摘要翻译： 下式的酰胺：其中：R1是A，R2是B; R1为B，R2为A; 或R 1和R 2独立地选自B组; A是苯基，取代的苯基，杂芳基或取代的杂芳基; B是环烷基，取代的环烷基，杂环烷基或取代的杂环烷基; R3是1至25个碳原子的烷基链，分支或直链; 2至25个碳原子的链烯基，分支或直链; 取代的烷基链; 取代烯基链; 中断的烷基链; 中断的烯基链; 取代的中断的烷基链; 或取代的中断的烯基链; R4是氢，低级烷基，苯基，Q-取代的苯基，杂芳基或Q-取代的杂芳基; R6和R7均为H或R6，R7一起表示= O; 或其药学上可接受的盐; 可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

公开(公告)号：US5310959A

公开(公告)日：1994-05-10

申请号：US61268

申请日：1993-05-17

申请人： Braham Shroot ,  Christopher Hensby ,  Jean Maignan ,  Gerard Lang ,  Serge Restle ,  Michel Colin

发明人： Braham Shroot ,  Christopher Hensby ,  Jean Maignan ,  Gerard Lang ,  Serge Restle ,  Michel Colin

IPC分类号： A61K8/00 ,  A61K8/11 ,  A61K8/30 ,  A61K8/33 ,  A61K8/36 ,  A61K8/37 ,  A61K8/42 ,  A61K8/49 ,  A61K8/86 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/20 ,  A61K31/202 ,  A61K31/22 ,  A61K31/23 ,  A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  A61Q5/00 ,  A61Q19/00 ,  C07C17/26 ,  C07C51/353 ,  C07C57/18 ,  C07C57/68 ,  C07C67/00 ,  C07C69/606 ,  C07C231/00 ,  C07C231/02 ,  C07C233/02 ,  C07C233/09 ,  C07C233/16 ,  C07C233/20 ,  C07D295/16 ,  C07D295/18 ,  C07D295/185 ,  C07D317/20 ,  C12N9/99 ,  C07C231/100

CPC分类号： A61K8/375 ,  A61K8/42 ,  A61Q19/00 ,  A61Q19/004 ,  C07C17/26 ,  C07C57/18 ,  C07C57/68 ,  C07D295/185 ,  C07D317/20 ,  Y10S514/886

摘要： Processes for preparing 5,8,11-eicosatriynoic acid as well as esters and amides thereof involves initially preparing the acid by reacting 1-decyne with 1,4-dihalo-2-butyne in the presence of a strong base to form 1-halo-2,5-tetradecadiyne which is then reacted with 5-hexynoic acid so as to form 5,8,11-eicosatriynoic acid. This acid can then be converted to the acid chloride form and reacted with an alcohol to form an ester or converted to a potassium salt and reacted with a halide also to form an ester, or after conversion to an acid chloride reacted with an amine in the presence of a tertiary amine to form an amide, or the acid can be reacted with carbonyldiimidazole in the presence of a solvent and excess amine to form an amide.

摘要翻译： 制备5,8,11-二十碳三烯酸及其酯和酰胺的方法包括首先在强碱存在下使1-癸炔与1,4-二卤-2-丁炔反应制备酸，以形成1-卤代 -2,5-十四碳二炔，然后与5-己炔酸反应，形成5,8,11-二十碳三烯酸。 然后将该酸转化为酰氯形式并与醇反应形成酯或转化成钾盐，并与卤化物反应形成酯，或在转化为与胺反应后的酰氯中 存在叔胺以形成酰胺，或者酸可以与羰基二咪唑在溶剂和过量胺的存在下反应形成酰胺。

公开(公告)号：US5254547A

公开(公告)日：1993-10-19

申请号：US802236

申请日：1991-12-04

申请人： Zoltan Budai ,  Tibor Mezei ,  Klara Reiter nee Esses ,  Lajos Fekete ,  Karoly Magyar ,  Attila Nagy ,  Laszlo Puskas

发明人： Zoltan Budai ,  Tibor Mezei ,  Klara Reiter nee Esses ,  Lajos Fekete ,  Karoly Magyar ,  Attila Nagy ,  Laszlo Puskas

IPC分类号： A23K1/16 ,  C07D295/18 ,  C07D295/194 ,  A61K31/535

CPC分类号： C07D295/194 ,  Y10S426/807

摘要： The invention relates to new thioacid amide derivatives, a process for the preparation thereof, compositions, particularly feed additives, premixes and ready-for-use fodders, comprising the same, further to a method for increasing weight gain and improving fodder utilization of domestic animals.The new thioacid amide derivatives of the general formula (I), whereinR represents hydrogen, C.sub.1-18 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl andR.sup.1 stands for hydrogen, halogen or methoxy, with the provisos thata) at least one of R and R.sup.1 is other than hydrogen;b) if R represents ethyl, R.sup.1 is other than hydrogen; andc) if R stands for methyl, R.sup.1 is other than hydrogen or methoxy,exhibit useful weight-gain increasing and fodder-utilization improving effects and can be used in animal husbandry, particularly in pig.

公开(公告)号：US5214045A

公开(公告)日：1993-05-25

申请号：US551518

申请日：1990-07-11

申请人： Tamas Fodor ,  Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos

发明人： Tamas Fodor ,  Janos Fischer ,  Laszlo Dobay ,  Elemer Ezer ,  Judit Matuz ,  Laszlo Szporny ,  Gyorgy Hajos

IPC分类号： A61K31/16 ,  A61K31/10 ,  A61K31/195 ,  A61K31/255 ,  A61K31/425 ,  A61K31/426 ,  A61P1/04 ,  C07C317/32 ,  C07C317/44 ,  C07C323/32 ,  C07C323/54 ,  C07C323/60 ,  C07D207/16 ,  C07D277/06 ,  C07D295/16 ,  C07D295/18 ,  C07D295/185 ,  C07D295/20

CPC分类号： C07D295/185 ,  C07C317/44 ,  C07C323/54 ,  C07D207/16

摘要： Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

公开(公告)号：US5166153A

公开(公告)日：1992-11-24

申请号：US515001

申请日：1990-04-24

申请人： Friedrich Karrer

发明人： Friedrich Karrer

IPC分类号： C07D295/18 ,  A01N47/12 ,  A01N47/28 ,  A01N47/34 ,  A01N47/38 ,  C07C271/64 ,  C07C271/66 ,  C07D295/185 ,  C07D295/20

CPC分类号： C07D295/185 ,  A01N47/12 ,  A01N47/34 ,  A01N47/38 ,  C07C271/64 ,  C07C271/66

摘要： Novel N-acylated 2-[4-(halophenoxy)-phenoxy]-ethylcarbamic acid esters of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.5 alkenyl,R.sub.2 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, --CO--R.sub.7 or --NR.sub.8 R.sub.9,R.sub.3 and R.sub.4 independently of one another are hydrogen or methyl,R.sub.5 is chlorine or fluorine,R.sub.6 is either the same substituent as R.sub.5 or is hydrogen,R.sub.7 is C.sub.1 -C.sub.8 alkoxy or --NR.sub.10 R.sub.11,R.sub.8 is C.sub.1 -C.sub.4 alkyl,R.sub.9 is C.sub.1 -C.sub.4 alkyl orR.sub.8 and R.sub.9 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --,R.sub.10 is hydrogen or C.sub.1 -C.sub.4 alkyl andR.sub.11 is hydrogen or C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or phenyl substituted by halogen or by methyl, orR.sub.10 and R.sub.11 together form a C.sub.4 -C.sub.6 alkylene chain which may be interrupted by oxygen, sulfur or --NCH.sub.3 --;their preparation, their use in pest control, and pesticidal compositions that contain those carbamic acid esters as active ingredient are disclosed.

摘要翻译： 式I的新型N-酰化2-酰氯化2- [4-（卤代苯氧基） - 苯氧基] - 乙基氨基甲酸酯其中R 1是C 1 -C 8烷基或C 3 -C 5烯基，R 2是C 1 -C 8烷基，C 1 -C 8烷氧基， CO-R7或-NR8R9，R3和R4彼此独立地是氢或甲基，R5是氯或氟，R6是与R5相同的取代基或是氢，R7是C1-C8烷氧基或-NR10R11，R8是C1- C 4烷基，R 9为C 1 -C 4烷基或R 8和R 9一起形成可被氧，硫或-NCH 3 - ，R 10为氢或C 1 -C 4烷基，R 11为氢或C 1 -C 4烷基，苄基，苯基 或被卤素或甲基取代的苯基，或R 10和R 11一起形成可被氧，硫或-NCH 3 - 间隔的C 4 -C 6亚烷基链; 公开了它们的制备，其在病虫害防治中的用途和含有这些氨基甲酸酯作为活性成分的农药组合物。

公开(公告)号：US5151534A

公开(公告)日：1992-09-29

申请号：US349691

申请日：1989-05-10

申请人： Braham Shroot ,  Christopher Hensby ,  Jean Maignan ,  Gerard Lang ,  Michel Colin

发明人： Braham Shroot ,  Christopher Hensby ,  Jean Maignan ,  Gerard Lang ,  Michel Colin

IPC分类号： A61K31/16 ,  A61K8/00 ,  A61K8/04 ,  A61K8/14 ,  A61K8/30 ,  A61K8/41 ,  A61K8/46 ,  A61K8/49 ,  A61K31/165 ,  A61K31/19 ,  A61K31/22 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  A61Q5/02 ,  A61Q17/00 ,  A61Q17/04 ,  A61Q19/00 ,  C07C317/44 ,  C07C323/52 ,  C07C323/60 ,  C07C323/65 ,  C07D295/18 ,  C07H13/06

CPC分类号： A61K8/14 ,  A61K8/46 ,  A61Q19/00 ,  C07C317/44 ,  C07C323/52 ,  C07C323/60 ,  Y10S514/886 ,  Y10S514/887

摘要： Compounds corresponding to the formula: ##STR1## wherein A represents --(CH.sub.2).sub.2 or --(C.tbd.C)--;n is equal to 0, 1 or 2;R represents hydroxyl, alkoxy having the formula --OR.sub.1, or amino having the formula ##STR2## R.sub.1 represents alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or aralkyl;R.sub.2 and R.sub.3 represent hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl or benzyl;R.sub.2 and R.sub.3 form, with the nitrogen atom, a heterocyclic ring.Application of these compounds in pharmacy and cosmetics.

摘要翻译： 对应于下式的化合物：其中A表示 - （CH 2）2或 - （C 3 B）） - ; n等于0,1或2; R表示羟基，具有式-OR 1的烷氧基或具有下式的氨基R1表示烷基，单羟基烷基，多羟基烷基，芳基或芳烷基; R2和R3表示氢，烷基，单羟基烷基，多羟基烷基，芳基或苄基; R2和R3与氮原子形成杂环。 这些化合物在药房和化妆品中的应用。

公开(公告)号：US5106970A

公开(公告)日：1992-04-21

申请号：US724628

申请日：1991-07-02

申请人： Kaoru Fuji ,  Manabu Node ,  Fujie Tanaka

发明人： Kaoru Fuji ,  Manabu Node ,  Fujie Tanaka

IPC分类号： C07D295/18 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/12 ,  C07D295/185

CPC分类号： C07D295/185

摘要： Optically active 4-morpholino-2-(1-naphthylmethyl)-4-oxobutyric acid 2'-hydroxy-1,1'-binaphthalen-2-yl represented by formula (I): ##STR1## wherein * indicates an asymmetric carbon atom, which is prepared by reacting 4-morpholino-4-oxobutyric acid 2'-hydroxy-1,1'-binaphthalen-2-yl represented by formula (II): ##STR2## with a 1-halomethylnaphthalene in the presence of a base. The compound (I) is a useful intermediate for preparing pharmaceuticals such as a renin inhibitors.

公开(公告)号：US5086065A

公开(公告)日：1992-02-04

申请号：US524521

申请日：1990-05-17

申请人： Mitoshi Konno ,  Takahiko Nakae ,  Nobuyuki Hamanaka

发明人： Mitoshi Konno ,  Takahiko Nakae ,  Nobuyuki Hamanaka

IPC分类号： A61K31/19 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/425 ,  A61K31/426 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/54 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C51/09 ,  C07C59/52 ,  C07C59/64 ,  C07C59/66 ,  C07C59/68 ,  C07C59/72 ,  C07C59/90 ,  C07C69/734 ,  C07C205/34 ,  C07C205/56 ,  C07C233/47 ,  C07C233/54 ,  C07C233/55 ,  C07C233/81 ,  C07C233/87 ,  C07C235/06 ,  C07C235/16 ,  C07C235/20 ,  C07C235/32 ,  C07C235/34 ,  C07C235/38 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/78 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/32 ,  C07C311/37 ,  C07C311/48 ,  C07C311/51 ,  C07C323/19 ,  C07C405/00 ,  C07D207/26 ,  C07D207/27 ,  C07D209/08 ,  C07D209/48 ,  C07D215/08 ,  C07D217/06 ,  C07D219/02 ,  C07D275/02 ,  C07D275/03 ,  C07D277/20 ,  C07D277/42 ,  C07D277/44 ,  C07D277/46 ,  C07D279/02 ,  C07D295/10 ,  C07D295/18 ,  C07D295/185 ,  C07D333/16 ,  C12N9/99

CPC分类号： C07C69/734 ,  C07C205/34 ,  C07C205/56 ,  C07C233/47 ,  C07C233/54 ,  C07C233/81 ,  C07C235/16 ,  C07C235/20 ,  C07C235/34 ,  C07C235/42 ,  C07C235/78 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/51 ,  C07C323/19 ,  C07C405/0066 ,  C07C59/52 ,  C07C59/64 ,  C07C59/68 ,  C07C59/90 ,  C07D207/27 ,  C07D209/08 ,  C07D209/48 ,  C07D275/03 ,  C07D277/42 ,  C07D277/46 ,  C07D279/02 ,  C07D295/185 ,  C07C2101/14

摘要： The phenylalkan(en)oic acids of the formula: ##STR1## wherein A isi) --NHCO--,ii) --O--iii) --NHSO.sub.2 --,iv) --CO--v) --CH.sub.2 -- orvi) --CH(OH)--;W isi) C1-13 alkylene,ii) phenylene oriii) ##STR2## R.sup.1 is i) hydrogen,ii) C1-4 alkyl,iii) --COOH,iv) saturated or unsaturated, 4-7 membered mono-cyclic hetero ring containing one nitrogen as a hetero atom or saturated or unsaturated, 4-7 member mono-cyclic hetero ring containing one nitrogen as a hetero atom substituted by an oxo group,v) ##STR3## vi) --CH.sub.2 OH; or A, taken together with W and R.sup.1, isi) ##STR4## ii) ##STR5## iii) --N--(SO.sub.2 R.sup.6).sub.2, iv) ##STR6## or v) ##STR7## two R.sup.2 are, same or different, i) hydrogen,ii) C1-4 alkyl oriii) 4-7 membered saturated or unsaturated, mono-cyclic hetero ring containing two or three of nitrogen and sulfur in total, or two R.sup.2, taken together with a nitrogen to which they are attached, form saturated or unsaturated,i) 7-14 membered, bi- or tri-cyclic hetero ring containing one nitrogen as a hetero atom, orii) 4-7 mebered, mono-cyclic hetero ring containing two or three of nitrogen and oxygen in total;Y is ethylene or vinylene;D isi) --Z--B orii) ##STR8## Z is C3-11 alkylene or alkenylene R is ##STR9## or Z taken together with B, is C3-22 alkyl;R.sup.3 isi) hydrogen,ii) halogen,iii) C1-8 alkyl, alkoxy or alkylthio, oriv) C2-8 alkenyl, alkenyloxy or alkenylthio;n is 1-3;R.sup.4 is C1-7 alkylene;R.sup.5 isi) C1-12 alkyl,ii) C2-12 alkenyl,iii) C5-7 cycloalkyl or pp2 iv) phenethyl or phenethyl wherein the ring is substituted by one C1-4 alkoxy;Two R.sup.6 are, same or different,i) C1-7 alkyl,ii) benzyl oriii) phenyl or phenyl wherein the ring is substituted by one C1-4 alkyl; andTwo R.sup.7 are, same or different, C1-4 alky; with the proviso thati) --A--W--R.sup.1 should bind to 3- or 4- carbon in benzene ring, andii) when W phenylene or ##STR10## A should not represent --O--, --CO--, --CH.sub.2 -- or --CH(OH)--; and non-toxic salts thereof,possess an antagonistic activity on leukotriene B.sub.4, and therefore, are useful for the prevention and treatment of several diseases induced by leukotriene B.sub.4.

公开(公告)号：US5057563A

公开(公告)日：1991-10-15

申请号：US492710

申请日：1990-03-13

申请人： Ramanathan Ravichandran

发明人： Ramanathan Ravichandran

IPC分类号： C07C233/00 ,  C07D295/18 ,  C08K5/32 ,  C08K5/33 ,  C08L67/02 ,  C08L69/00

CPC分类号： C07D295/18 ,  C07C233/00 ,  C08K5/32 ,  C08K5/33 ,  C08L67/02 ,  C08L69/00

摘要： Substituted aminoxy propionamide derivatives corresponding to the formula ##STR1## said derivatives being useful as color improvers and stabilizers in various polymeric substrates.

摘要翻译： 对应于式“IMAGE”的取代的氨基羟基丙酰胺衍生物，所述衍生物可用作各种聚合物基质中的颜色改进剂和稳定剂。

公开(公告)号：US5002692A

公开(公告)日：1991-03-26

申请号：US279461

申请日：1988-12-01

申请人： George W. Gray ,  David Lacey ,  Kenneth J. Toyne ,  Richard M. Scrowston ,  Lawrence K. M. Chan ,  Madeline J. Bradshaw ,  Victoria Brimmell

发明人： George W. Gray ,  David Lacey ,  Kenneth J. Toyne ,  Richard M. Scrowston ,  Lawrence K. M. Chan ,  Madeline J. Bradshaw ,  Victoria Brimmell

IPC分类号： C07D233/60 ,  C07C67/00 ,  C07C231/00 ,  C07C233/05 ,  C07C233/07 ,  C07C241/00 ,  C07C253/00 ,  C07D207/00 ,  C07D207/325 ,  C07D211/00 ,  C07D211/16 ,  C07D231/12 ,  C07D233/66 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D295/18 ,  C09K19/12 ,  C09K19/20 ,  C09K19/30 ,  C09K19/34 ,  C09K19/46 ,  G02F1/13

CPC分类号： C07D295/18 ,  C07D231/12 ,  C09K19/126 ,  C09K19/2021 ,  C09K19/2028 ,  C09K19/3441 ,  C09K19/348 ,  C09K19/3483

摘要： Amides having the following structure: ##STR1## used in ferroelectric smectic liquid crystal mixtures, especially as pitch compensators and liquid crystal compositions containing them.

摘要翻译： 具有以下结构的酰胺：用于铁电近晶液晶混合物中的 ，特别是作为沥青补偿剂和含有它们的液晶组合物。