公开(公告)号：US3853864A

公开(公告)日：1974-12-10

申请号：US31304872

申请日：1972-12-07

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  SCOTESE A

IPC分类号： A61K31/435 ,  A61P31/04 ,  C07D213/80 ,  C07D471/04

CPC分类号： C07D213/80 ,  C07D471/04

摘要： 1,7-Dialkyl-1,2-dihydro-4-hydroxy-1,8-naphthyridine-3-carboxylic acid alkyl esters are prepared by cyclization of 2-((2alkoxycarbonylethyl)alkylamino)-6-alkylnicotinic acid alkyl esters. The compounds so produced exhibit in vivo antibacterial activity.

摘要翻译： 通过使2 - [（2-烷氧基羰基乙基）烷基氨基] -6-烷基烟酸烷基酯环化制备1,1-二烷基-1,2-二氢-4-羟基-1,8-二氮杂萘-3-羧酸烷基酯 。 如此制备的化合物具有体内抗菌活性。

公开(公告)号：US3816430A

公开(公告)日：1974-06-11

申请号：US30237972

申请日：1972-10-30

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  SCOTESE A ,  BELL S

IPC分类号： C07C93/06

CPC分类号： C07D307/88

摘要： N,N''-(NAPHTHYLENEDIOXYDIETHYLENE)BIS(DI(LOWER)ALKYLAMINES) HAVE ANTI-INFLAMMATORY ACTIVITY.

公开(公告)号：US3816423A

公开(公告)日：1974-06-11

申请号：US28515372

申请日：1972-08-31

申请人： AMERICAN HOME PROD

发明人： KIM D ,  SANTILLI A

IPC分类号： C07D239/42 ,  C07D51/42

CPC分类号： C07D239/42

摘要： COMPOUNDS OF THE FORMULA:

2-(R1-PHENYL),4-R2,5-X,6-((R3,R4-PHENYL)-N(-R)-)PYRIMIDINE

IN WHICH R, R1 AND R2 ARE INDEPENDENTLY SELECTED FROM THE GROUP, CONSISTING OF -H AND LOWER ALKYL RADICALS, R3 AND R4 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF -H, LOWER ALKYL AND LOWER PERFLUOROALKYL RADICALS, X IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF -CN AND

1H-TETRAZOL-5-YL

RADICALS, AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, POSSESS CENTRAL NERVOUS SYSTEM DEPRESSANT AND ANTI-INFLAMMATORY PROPERTIES WHEN ADMINISTERED TO WARM BLOODED ANIMALS.

公开(公告)号：US3775412A

公开(公告)日：1973-11-27

申请号：US3775412D

申请日：1971-05-10

申请人： AMERICAN HOME PROD

发明人： KIM D ,  SANTILLI A

IPC分类号： C07D239/42 ,  C07D487/04 ,  C07D51/46

CPC分类号： C07D487/04 ,  C07D239/42

摘要： THE DISCLOSURE IS DIRECTED TO SUBSTITUTED 2-PHENYL-5HPYRROLO(2,3-D)PYRIMIDINE-5,6-(7H)DIONES, AND A PROCESS FOR THEIR PREPARATION, HAVING THE STRUCTURAL FORMULA:

2-R5,5,5-DI(R6-O-),6-(O=),7-R1-6,7-DIHYDRO-5H-PYRROLO-

(2,3-D)PYRIMIDINE

WHERE

R1 IS HYDROGEN OR LOWER ALKYL, R5 IS PHENYL, HALOPHENYL, LOWER ALKYLPHENYL OR LOWER ALKOXYPHENYL; AND R6 IS METHYL OR ETHYL.

THE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY AS CENTRAL NERVOUS SYSTEM DEPRESSANTS IN THAT THEY DECREASE MOTOR ACTIVITY AND DECREASE RESPIRATION IN A HOST.

公开(公告)号：US3732226A

公开(公告)日：1973-05-08

申请号：US3732226D

申请日：1971-04-23

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  KIM D

IPC分类号： C07D413/12 ,  C07D471/04 ,  C07D51/42

CPC分类号： C07D471/04 ,  C07D413/12

摘要： THE DISCLOSURE IS DIRECTED TO 5,6,7,8-TETRAHYDRO-5-OXOPYRIDO(2,3-D)PYRIMIDINE-6-CARBONITRILES AND TO CARBOXYLICACID ESTERS WHICH ARE INTERMEDIATES IN THEIR PREPARATION. BOTH THE FINAL PRODUCTS AND THE INTERMEDIATES HAVE CENTRAL NERVOUS SYSTEM ACTIVITY AS DEPRESSANTS.

公开(公告)号：US3725405A

公开(公告)日：1973-04-03

申请号：US3725405D

申请日：1970-06-18

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  KIM D

IPC分类号： C07D239/48 ,  C07D471/04 ,  C07D57/20

CPC分类号： C07D471/04 ,  C07D239/48

摘要： Novel 2,4,7-trisubstituted-pyrido(2,3-d)pyrimidine-6carboxamides have been produced which have central nervous system depressant activity and are useful pharmacological agents in the calming of animals.

摘要翻译： 已经制备了具有中枢神经系统抑制活性的新型2,4,7-三取代 - 吡啶并[2,3-d]嘧啶-6-甲酰胺，并且在动物平静中是有用的药理学试剂。

公开(公告)号：US3850931A

公开(公告)日：1974-11-26

申请号：US36419173

申请日：1973-05-25

申请人： AMERICAN HOME PROD

发明人： KIM D ,  SANTILLI A

IPC分类号： C07D239/42 ,  C07D498/04 ,  C07D51/42

CPC分类号： C07D498/04 ,  C07D239/42

摘要： 1. A COMPOUND HAVING THE FORMULA

2-(PHENYL-),4-(R5-(R6-1,2-PHENYLENE)-N(-R4)-),5-(R3-OOC-)-

PYRIMIDINE

WHERE R3 IS HYDROGEN OR LOWER ALKYL; R4 IS HYDROGEN OR LOWER ALKYL; R5 IS HYDROXY, LOWER ALKOXY, OR LOWER ALKANOYL; AND R6 IS HYDROGEN, HALOGEN, OR NITRO.

公开(公告)号：US3850928A

公开(公告)日：1974-11-26

申请号：US39496373

申请日：1973-09-04

申请人： AMERICAN HOME PROD

发明人： KIM D ,  SANTILLI A

IPC分类号： C07D239/42 ,  C07D487/04 ,  C07D51/42

CPC分类号： C07D487/04 ,  C07D239/42

摘要： 1. A COMPOUND SELECTED FROM THOSE HAVING THE STRUCTURE:

2-R2,4-R1,5-(HOOC-),6-(R4-NH-)-PYRIMIDINE

R1 IS HYDROGEN OR METHOXY; R2 IS PHENYL, HALOPHENYL, LOWER ALKYLPHENYL OR LOWER ALKOXYPHENYL; AND R4 IS LOWER ALKYL.

公开(公告)号：US3814761A

公开(公告)日：1974-06-04

申请号：US24026672

申请日：1972-03-31

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  SCOTESE A ,  TOMARELLI R

IPC分类号： C07D239/06 ,  C07D239/38 ,  C07D239/46 ,  C07D239/56 ,  C07D239/60 ,  C07D405/06 ,  C23F11/14 ,  C07D51/36

CPC分类号： C07D239/06 ,  C07D239/38 ,  C07D239/47 ,  C07D239/56 ,  C07D239/60 ,  C23F11/149

摘要： (2-PYRIMIDINYLTHIO)N ALKANOIC ACIDS, ESTERS, AMIDES AND HYDRAZIDES AS WELL AS VARIOUS 4- AND 6-SUBSTITUTED DERIVATIVES THEREOF AS DEPICTED BY THE STRUCTURAL FORMULA:

2-(Z-CO-(CH2)M-CH(-R)-S-),4-R1,5-R2,6-Y-PYRIMIDINE

IN WHICH R AND R2 ARE INDEPENDENTLY -H OR LOWER ALKYL; R1 IS -H, -HALO OR LOWER ALKOXY; Z IS -OH, OM, LOWER ALKOXY OR -(NH)P-NH2, WHEREIN P IS 0 TO 1 AND M IS AN ALKALI METAL, ALKALINE EARTH METAL OR AMMONIUM CATION; Y IS AN ARYL, AMINO OR SUBSTITUTED AMINO RADICAL; AND M IS AN INTEGER FROM 0 TO 2, EXHIBIT ANTI-LIPEMIC ACTIVITY IN WARM-BLOODED ANIMALS.

公开(公告)号：US3748352A

公开(公告)日：1973-07-24

申请号：US3748352D

申请日：1972-07-25

申请人： AMERICAN HOME PROD

发明人： SANTILLI A ,  KIM D

IPC分类号： C07D231/20 ,  C07C159/00

CPC分类号： C07D231/20

摘要： DIALKYL 2 - (1 - (3-THIOSEMICARBAZONO)ETHYL)SUCCINATES AND GLUTARATES OF THE FORMULA:

R1-NH-C(=S)-NH-N=C(-CH3)-C(-(CH2)N-COO-R3)-COO-R3

WHEREIN R1 IS HYDROGEN OR LOWER ALKYL, R3 IS LOWER ALKYL AND N IS 1 OR 2, ARE INTERMEDIATES FOR THE PREPARATION OF 5-HYDROXY-3-ALKYL-1-(THIOCARBAMOYL OR ALKYLTHIOCARBAMOYL)PYRAZOLES OF THE FORMULA:

1-(R1-NH-C(=S)-),3-CH3,4-(R2-CO-(CH2)N-),5-HO-PYRAZOLE

IN WHICH R1 IS HYDROGEN OR LOWER ALKYL R2 IS HYDROXY, AMINO OR LOWER ALKOXY, AND N IS 1 OR 2, THE LATTER COMPOUNDS BEING ACTIVE AS INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS.