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A N T I A T H E R O S C L E R O T I C A G E N T C O M P O S I T I O N S
Tadashi Sasaki, Yoshihiro Fujikawa, Ryozo Sakoda, Mitsuaki Sakashita, Morihide Hibi, Tokyo, Japan assigned to Nissan Chemical Industries Ltd
3,5-Dimethyl-4,6-diphenyl-tetrahydro-2H- 1,3,5-thiadiazine-2-thione having the formula: See Patent for Chemical Structure for use as an active therapeutic agent.
3 - V I N Y L A N D 3 - T H Y I N Y L - B E T A - C A R B O L I N E S , A N D T H E I R U S E
AS B E N Z O D I A Z E P I N E R E C E P T O R A N T A G O N I S T S O R
A G O N I S T S
Dieter Seidelmann, Andreas Huth, Ralph Schmiechen, Rudolf Wiechert, Herbert Schneider, David N Stephens, Berlin, Federal Republic Of Germany assigned to Schering Ak- tiengesellschaft
Compounds of formula 1 See Patent./br Chem- ical Structure (l) wherein RI is hydrogen or a protecting group, R2 is -CH double bondCR24 or -C triple bondCR4, R4 is hydrogen or halogen, R3 is hydrogen, lower alkyl or lower alkoxyalkyl, RA is, inter alia, hydrogen, OR7, lower alkyl, which optionally is substituted with aryl, lower alkoxy or NR5R6, R5 and R6 can be the same or different and in each case is hydro- gen, lower alkyl or together with the nitrogen atom a 5-6 member ring, which can contain another heteroatom, R7 is lower alkyl, op- tionally substituted aryl or aralkyl, and each compound can contain one or more RA radicals which are not hydrogen, have valuable pharma- cological properties.
PYRIDO(3,4-B)INDOLES HAVING ANTIHYPERTENSIVE
Magid A Abou-Gharbia, Meier E Freed as- signed to American Home Products Corpora- tion
This invention concerns tetra- hydropyridoindoles of the formula: See Patent for Chemical Structure I wherein Q represents See Patent for Chemical Structure in which R3 is hydrogen, C1-4 alkyl, C1-4 alkoxy, or - COO(C1-2) alkyl, and n is an integer from 1 to 7; R I is hydrogen, halogen, hydroxy, or CI-3 alkyl; and R2 is hydrogen, CI-4 alkyl or -(CH2)m-A where A is -N(CH3)2,-N(C2H5)2, See Patent for Chemical Structure in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from I-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit anti- hypertensive properties. Four of the disclosed compounds also exhibit antipsychotic pro- perties. Also disclosed are compounds of For- mula XX in which Q of Formula I is replaced by Q1, wherein QI is 2- or 3-pyridinyl, and R2 of Formula I is restricted to hydrogen. The com- pounds of Formula XX exhibit antipsychotic properties.
T H E R A P E U T I C A G E N T FOR M E M O R Y D I S T U R B A N C E
Masayoshi Goto, Nobutaka Demura, Takash Sakaguchi, Tokyo, Japan assigned to Hoechst Aktiengesellschaft
A therapeutic agent for memory disturbance containing 1,2,3, 6-tetrahydro-3-methyl-1-(5- oxohexyl)-7-propyl-purine-2,6-dione as its ac- tive ingredient and a method for treating a patient suffering from memory disturbance with such a therapeutic agent.
A N T I - C A N C E R C O M P O S I T I O N FOR DELIVERING 5-
Setsuro Fujii, Norio Unemi, Setsuo Takeda, Toyonaka, Japan assigned to Taiho Pharma- ceutical Company Limited
An anti-cancer composition for delivering a 5- fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil. The composition comprises uracil or a pharmaceutically acceptable salt thereof, and a 5-fluorouracil pro drug selected
296 PATENT ABSTRACTS
from the group consisting of I, 3-bis (2- tetrahydrofuryl)-5-fluorouracil and 3-(2- tetrahydrofuryl)-5-fluorouracil in a small amount of about 0.1 to less than 0.1 mole per mole of uracil or salt thereof.
Q U A T E R N A R Y D E R I V A T I V E S O F N O R O X Y M O R P H O N E W H I C H
R E L I E V E N A U S E A A N D E M E S I S
Leon I Goldberg assigned to University of Chicago
Quaternary derivatives of noroxymorphone are used to prevent or relieve nausea and emesis as- sociated with the use of narcotic analgesics without interfering with the analgesic activity of the drugs. A particularly preferred compound is methylnaltrexone. The compound is ad- ministered in a concentration between 0.25 mg/kg and 1.0 mg/kg prior to or concurrently with the administration of the narcotic analgesic.
H E X A H Y D R O P Y R R O L O ( 2 , 1 - A)ISOQUINOLINE D E R I V A T I V E S
AS A N T I D E P R E S S A N T S
Bruce E Maryanoff assigned to McNeilab lnc
Novel compounds are disclosed, which are derivatives of 1,2,3,5,6, 10b- hexahydropyrrolo(2,1 -a)-isoquinolines, represented by general formula (I): See Patent for Chemical Structure (I) as well as pharma- ceutical compositions and methods for the treat- ment of depression in warm-blooded animals, e.g., man. Novel intermediates are also part of the invention.
Compounds of formula (1) or a pharma- ceutically acceptable salt thereof: See Patent for Chemical Structure (I) wherein: R 1 is C 1-6 alkyl; R2 is amino or C1-7 acylamino; R3 is halo or C1- 6 alkythio; R4 and R5 are independently selected from hydrogen, C 1-6 alkyl, phenyl or phenyl C 1- 4 alkyl any of which phenyl moieties may be substituted by one or two of halo, CF3, C1-6 alkoxy or CI-6 alkyl; R6 is C1-7 alkyl, - (CH2)sR7, s being 0 to 2 and R7 being C3-8 cycloalky, -(CH2)tR8, t being 1 or 2 and R8 being thienyl or phenyl optionally substituted by one or two substituents selected from C1-4 alkoxy, trifluoromethyl, halogen, nitro, car- boxy, esterified carboxy and C1-4 alkyl op- tionally substituted by hydroxy, C1-4 alkoxy, carboxy, esterified carboxy or in vivo hydro- lysable acyloxy; and n is 0 to 3; having gastric motility enhancing activity and anti-emetic ac- tivity, a process for their preparation and their use as pharmaceuticals.
P Y R R O L O ( 1 , 2 - A ) I M I D A Z O L E A N D P Y R R O L O ( 1 , 2 - A ) P Y R I D I N E
D E R I V A T I V E S A N D T H E I R U S E AS 5 - L I P O X Y G E N A S E P A T H W A Y
I N H I B I T O R
Paul E Bender, Nabil Hanna assigned to Smith- Kline Beckman Corporation
A method of inhibiting the production of 5- lipoxygenase products in an animal in need thereof which comprises administering an effec- tive, 5-1ipoxygenase pathway inhibiting amount of a 2(3)-(pyridyl)-3-(2)-substituted phenyl)-6,7- dihydro-(5H)-pyrrolo-(1, 2-a)imidazole, a 2(3)- (pyridyl)-3(2)-(substit uted phenyl)-5,6,7, 8- tetrahydro-imidazo(1,2,-a)pyridine, or a pharmaceutically acceptable salt thereof, to such animal.
C E R T A I N N - A Z A B I C Y C L O A L K Y L - B E N Z A M I D E S U S E F U L I N T H E
T R E A T M E N T O F I M P A I R E D G A S T R O - I N T E S T I N A L M O T I L I T Y
O R E M E S I S
Francis D King, Michael S Hadley, Bishop's Stortford, United Kingdom assigned to Beecham Group p 1 c
P H A R M A C E U T I C A L C O M P O S I T I O N S A N D A N T I -
T H R O M B O T I C M E T H O D S O F U S E T H E R E O F
Stevan W Djuric, Robert B Garland assigned to G D Searle & Co