The Polycyclo Ring System Is Tricyclo-carbocyclic Patents (Class 546/203)
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Patent number: 5189065Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.Type: GrantFiled: October 17, 1991Date of Patent: February 23, 1993Assignee: Roussel UclafInventors: Jorg Czech, Hans H. Sedlacek, Lucien Nedelec, Jacques Guillaume, Christian Marchandeau
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Patent number: 5180736Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: May 17, 1991Date of Patent: January 19, 1993Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5164499Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.Type: GrantFiled: January 2, 1990Date of Patent: November 17, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thaliyil V. Rajanbabu
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Cyclophanes, pharmaceutical compositions containing these compounds and processes for preparing them
Patent number: 5147882Abstract: Cyclophanes of the general formula ##STR1## wherein X.sub.1, X.sub.2, A, R and R.sub.1 to R.sub.4 are as defined herein, the enantiomers, diastereomers and addition salts thereof and, more particularly, for pharmaceutical use, the physiologically acceptable addition salts thereof, which have pharmacological properties such as lowering blood pressure, dilating the coronary blood vessels and a mild heart rate lowering activity, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: March 28, 1991Date of Patent: September 15, 1992Assignee: Karl Thomae GmbHInventors: Manfred Psiorz, Volker Trach -
Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 5132313Abstract: The present invention relates to novel NMDA receptor antagonists and methods for their use. The present invention also provided pharmaceutical compositions comprising such NMDA receptor antagonists.Type: GrantFiled: October 26, 1989Date of Patent: July 21, 1992Assignee: University of PittsburghInventors: Alan P. Kozikowski, Yuan-Ping Pang
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Patent number: 5120732Abstract: Substituted 3-aminosydnone imines of the formula I ##STR1## and their pharmacologically acceptable acid addition salts, in which A denotes, for example, --CH.sub.2 --,R.sup.1 denotes hydrogen or the radical --COR.sup.5,R.sup.2, R.sup.3 denote alkyl having 1 to 4 C atoms,R.sup.5 denotes, for example, an aliphatic radical having 1 to 4 C atoms,and methods for preparing such compounds by cyclization of a compound of the formula II ##STR2## and if desired subsequent acylation. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the control and prophylaxis of cardiovascular disorders.Type: GrantFiled: August 29, 1990Date of Patent: June 9, 1992Assignee: Cassella AktiengesellschaftInventors: Karl Schonafinger, Rudi Beyerle, Helmut Bohn, Melitta Just
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Patent number: 5114919Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.Type: GrantFiled: February 11, 1991Date of Patent: May 19, 1992Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David C. Remy
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Patent number: 5100901Abstract: A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22) r--, R22 being H or methyl, --CO-- (CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.Type: GrantFiled: October 18, 1989Date of Patent: March 31, 1992Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Yutaka Tsuchiya, Kunizou Higurashi, Norio Karibe, Youichi Iimura, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Takashi Kosasa, Atsuhiko Kubota, Michiko Kosasa, Kiyomi Yamatsu
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5095022Abstract: A piperidine derivative represented by the following general formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group; X represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or --CH.sub.2 O--; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represented an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), a method for preparation of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).Type: GrantFiled: June 13, 1990Date of Patent: March 10, 1992Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Ito, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Hiroyuki Nishino, Jun Sakaguchi
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Patent number: 5089506Abstract: Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl wherein each of R.sup.12 and R.sup.Type: GrantFiled: April 30, 1990Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5071853Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: February 27, 1990Date of Patent: December 10, 1991Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine
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Patent number: 5071860Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.Type: GrantFiled: March 7, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
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Patent number: 5015678Abstract: The Michael addition products of N-hydroxy hindered amines with alpha,beta-unsaturated carbonyl compounds including derivatives of esters, amids, imides and anhydrides are effective stabilizers for protecting organic polymers from the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: May 14, 1991Assignee: Ciba-Geigy CorporationInventors: Raymond Seltzer, James P. Galbo, Ramanathan Ravichandran
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Patent number: 5011853Abstract: This invention discloses the use of muscarinic anti-cholinergic agents for reducing or preventing the toxic or lethal effects (such as seizures and brain damage) caused by cholinergic neurotoxins. The parent application disclosed that certain muscarinic anti-cholinergics classified as aryl-cycloalkyl-alkanolamines are effective in reducing or preventing the neurotoxicity of soman, a powerful nerve gas. This invention extends that discovery and identifies other muscarinic anti-cholinergic agents, including scopolamine, benactyzine, and benztropine, as highly effective and useful agents to protect against two major classes of cholinergic neurotoxins (acetylcholine receptor agonists, and cholinesterase inhibitors). Analogs of those compounds may also be effective in protecting against cholinergic neurotoxicity, as can be determined through routine screening tests using rats.Type: GrantFiled: January 26, 1990Date of Patent: April 30, 1991Assignee: Washington UniversityInventor: John W. Olney
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Patent number: 5004813Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: August 24, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4996321Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.Type: GrantFiled: February 26, 1990Date of Patent: February 26, 1991Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David C. Remy
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Patent number: 4996215Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.Type: GrantFiled: September 15, 1989Date of Patent: February 26, 1991Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
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Patent number: 4994463Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: December 8, 1988Date of Patent: February 19, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 4977151Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.Type: GrantFiled: March 29, 1990Date of Patent: December 11, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
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Patent number: 4942261Abstract: An allyl type amine is prepared by reacting an allyl type alcohol represented by the following formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently stand for a hydrogen atom, an aliphatic hydrocarbon group or alicyclic hydrocarbon having 1 to 8 carbon atoms, or an aromatic hydrocarbon group,with at least one member selected from the group consisting of ammonia, a primary amine and a secondary amine in the presence of a palladium compound and a multidentate phosphorus compound.Type: GrantFiled: December 9, 1988Date of Patent: July 17, 1990Assignee: Showa Denko Kabushiki KaishaInventors: Yoshimasa Ishimura, Takami Oe, Yuseki Suyama, Nobuyuki Nagato
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Patent number: 4933344Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.Type: GrantFiled: August 31, 1988Date of Patent: June 12, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
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Patent number: 4912222Abstract: 4-Dibenzocycloheptenyl, 4-dibenzocycloheptyl, and 4-dibenzoxepinylpiperidine compounds possessing antihistaminic activity.Type: GrantFiled: June 17, 1988Date of Patent: March 27, 1990Assignee: Fisons CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 4904688Abstract: The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin- and dibenzocyclo-octenamine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.Type: GrantFiled: March 8, 1989Date of Patent: February 27, 1990Assignee: Akzo N.V.Inventors: Duncan R. Rae, James Cairns
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Patent number: 4898607Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.Type: GrantFiled: August 18, 1988Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Henry Szczepanski, Lourens Wals
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Patent number: 4891376Abstract: A compound which is a pyrimidinylamino derivative of piperidine of formula (I) ##STR1## in which: X is a (CH.sub.2).sub.2, CH.dbd.CH or CH.sub.2 --CO group;Y is a CH.dbd.CH gruop or sulphur;n is 2, 3 or 4;R.sub.1 is hydrogen or a halogen;R.sub.2 is hydrogen or a (C.sub.1-4) alkyl group; andR.sub.3 is hydrogen or a hydroxy group;or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 8, 1988Date of Patent: January 2, 1990Assignee: SynthelaboInventors: Philippe Manoury, Alfred Saarmets
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Patent number: 4876357Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.Type: GrantFiled: October 26, 1987Date of Patent: October 24, 1989Assignee: Ciba-Geigy CorporationInventors: Rox Phaff, Davor Bedekovic
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Patent number: 4855316Abstract: Certain 1,2-diamino-4,5-dimethoxycyclohexane amide derivatives have analgesic activity, and bind selectively to the kappa opioid receptor site. Pharmaceutical compositions containing these compounds, and a method of alleviating pain in mammals are also disclosed.Type: GrantFiled: February 18, 1988Date of Patent: August 8, 1989Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Stephen J. Johnson
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Patent number: 4835313Abstract: The invention relates to novel [5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a -tetrahydrofluoren-7-yl)]alkanoic acids and alkanimidamides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.Type: GrantFiled: December 10, 1987Date of Patent: May 30, 1989Assignee: Merck & Co., Inc.Inventors: Adolph M. Pietruszkiewicz, Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
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Patent number: 4804684Abstract: Drugs with high anticonvulsant and analgesic activities constituted by symmetrical .beta.-dialkoxyiminocycloalklene derivatives in which the imine double bonds are conjugated with the cyclic double bond or bonds belonging to one or more fused benzene rings.Type: GrantFiled: January 20, 1987Date of Patent: February 14, 1989Assignee: Panmedica S.A.Inventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4798894Abstract: Compounds containing at least one N,N-dialkylatable amino or amido group (e.g., aniline, dodecylamine, acetamide) are converted in a highly efficient manner into gem cyclodialkylated compounds by reaction with an unstrained cyclic ether (e.g., tetrahydrofuran) or a polyol (e.g., 1,4-butane diol) cyclizable to an unstrained ether using titanium dioxide catalysts that have prior to use:(1) a surface area of at least 70 square meters per gram (as determined by the BET method), and(2) the capability of chemically adsorbing at 100.degree. C. at least 35.times.10.sup.4 millimoles of gaseous ammonia per square meter of surface area.Type: GrantFiled: May 11, 1987Date of Patent: January 17, 1989Assignee: Ethyl CorporationInventor: Duane C. Hargis
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Patent number: 4772615Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: October 14, 1987Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4758577Abstract: Novel 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle.Type: GrantFiled: April 5, 1984Date of Patent: July 19, 1988Assignee: Merck & Co., Inc.Inventor: Steven D. Young
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Patent number: 4731447Abstract: A process for the preparation of piperidylidene-dihydro-dibenzo[a,d]cycloheptene or aza-derivatives thereof and intermediates in such process are disclosed.Type: GrantFiled: March 12, 1986Date of Patent: March 15, 1988Assignee: Schering CorporationInventors: Doris P. Schumacher, Bruce L. Murphy, Jon E. Clark
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Patent number: 4727072Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.Type: GrantFiled: February 12, 1986Date of Patent: February 23, 1988Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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Patent number: 4683330Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: July 28, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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10,11-dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives in a method for treating cardiac arrhythmia
Patent number: 4670435Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The novel substances are useful for the treatment of disorders.Type: GrantFiled: December 2, 1985Date of Patent: June 2, 1987Assignee: BASF AktiengesellschaftInventors: Albrecht Franke, deceased, Claus D. Mueller, Dieter Lenke -
Patent number: 4668814Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.Type: GrantFiled: January 11, 1985Date of Patent: May 26, 1987Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4658061Abstract: Fluorenes bearing a 9-aminoalkyl substituent are useful antiarrhythmic agents. Pharmaceutical formulations containing such compounds are provided, as well as a method of treatment.Type: GrantFiled: December 24, 1984Date of Patent: April 14, 1987Assignee: Eli Lilly and CompanyInventors: William B. Lacefield, Richard L. Simon
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Patent number: 4656282Abstract: Piperidines substituted in the 3- and/or 4-position are prepared by reacting a glutardialdehyde substituted in the 2- and/or 3-position with ammonia or a primary amine and hydrogen at elevated temperature and under superatmospheric pressure in the presence of a hydrogenation catalyst.Type: GrantFiled: November 4, 1985Date of Patent: April 7, 1987Assignee: BASF AktiengesellschaftInventors: Walter Himmele, Walter-Wielant Wiersdorff, Marco Thyes
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Patent number: 4654431Abstract: A novel photocurable monomer having the formula: ##STR1## wherein: Ar is arylene;R.sup.1 is H, alkyl, alkoxy, amino, halogen, sulfide, sulfoxide, sulfonate, aryl or heterocyclic;R.sup.2 is H, alkyl, aryl or aralkyl; andR.sup.3 is H or methyl,is useful in preparing a polymer having a high refractive index. The polymer is useful in optical components, such as lenses.Type: GrantFiled: September 10, 1982Date of Patent: March 31, 1987Assignee: Eastman Kodak CompanyInventor: Charles D. DeBoer
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Patent number: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4647557Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.Type: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
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Patent number: 4645758Abstract: The invention concerns:Novel dibenz/b,e/oxepin and dibenz/b,e/thiepin compounds having the general formula: ##STR1## wherein X is O or S,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are each selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulponyl, halogen, trifluoromethyl, trifluoromethylthio, lower dialkylsulphonamido, nitro, hydroxy, cyano, carbamyl, carboxy, lower alkoxycarbonyl, amino, N-lower alkylamino, N,N-diloweralkylamino, lower acylamido, lower alkanesulfonamido and lower acyl and, when on adjacent carbon atoms at the positions 2 and 3 and/or 8 and 9, two of the substituents R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 taken together may form a methylenedioxy group;R.sup.5 and R.sup.Type: GrantFiled: January 17, 1986Date of Patent: February 24, 1987Inventors: Nils-Erik Willman, Bengt C. H. Sjogren, Lennart G. Nordh, Gustav L. Persson, Goran H. Sjoholm
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Patent number: 4626542Abstract: Pharmaceutical compositions comprising 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds and the use of 4-(5H-dibenzo[a,d]cyclohepten-5-yl)piperidine compounds for treatment of certain cardiovascular disorders are disclosed.Type: GrantFiled: April 5, 1984Date of Patent: December 2, 1986Assignee: Merck & Co., Inc.Inventors: Stella W. King, David C. Remy
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Patent number: 4609664Abstract: Piperidylidene derivatives of formula ##STR1## wherein n is 2 or 3, R.sub.1 comprises a tricyclic nucleus and R.sub.2 is hydrogen or an acid residue, useful in the treatment and prophylaxis of asthmatic conditions.Type: GrantFiled: July 16, 1984Date of Patent: September 2, 1986Assignee: Sandoz Ltd.Inventor: Klaus Hasspacher
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Patent number: 4599409Abstract: The present invention relates to new bisamidine derivatives of polycyclic compounds such as 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrene-6(5H)-phenanthridone and 5,10-dioxo-4,5,9,10-tetrahydro-4,9-dioxapyrenephenanthridine and to a process for their preparation. The polycyclic bisamidines according to the invention are distinguished by valuable chemotherapeutic properties, such as, for example, an action against amoebas and trichomonads.Type: GrantFiled: February 15, 1984Date of Patent: July 8, 1986Assignee: Hoechst AktiengesellschaftInventors: Balbir S. Bajwa, deceased, Dipak K. Chatterjee, Bimal N. Ganguli, Jurgen Reden, Noel J. de Souza
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Patent number: 4568743Abstract: The invention concerns 1,8-dihydroxy-9-anthrones substituted in the 10-position of the formula: ##STR1## in which: R.sub.1 represents a group taken from the set constituted by: wherein R.sub.2 represents H, C.sub.1-8 alkyl, C.sub.1-3 mono- or poly-hydroxyalkyl, carbamoly or phenyl,R.sub.3, R.sub.4, and R.sub.5 represent H, C.sub.1-8 alkyl, C.sub.3-8 mono- or poly-hydroxyalkyl, possibly interrupted by an oxygen, C.sub.3-6 cycloalkyl, or R.sub.3 and R.sub.4 form a divalent group: --(CH.sub.2).sub.(4 or 5) --, --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --, or --(CH.sub.2).sub.2 --N(R.sub.8)--(CH.sub.2).sub.2 --, R.sub.8 being H, --CH.sub.3, or --CH.sub.2 CH.sub.2 OH,R.sub.6 represents 13 CO.sub.2 R.sub.5, --CN, --CHO, --CONH.sub.2, or --CONH--CH.sub.2 OH,and R.sub.7 and R'.sub.7 are H or --CH.sub.3, and their optical isomers.Utilization of the compounds (I) in human or veterinary medicine, in particular in the treatment of psoriasis and of warts, and in cosmetics.Type: GrantFiled: June 29, 1982Date of Patent: February 4, 1986Assignee: Groupement d'Interet Economique dit Centre International de Recherches Dermatolgiques C.I.R.D.Inventors: Braham Shroot, Jean Maignan, Gerard Lang
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Patent number: 4548973Abstract: A 2,2,6,6-tetramethyl-4-piperidinyl derivative having a formula comprising: ##STR1## wherein R.sub.1 is hydrogen, an alkyl or alkylene group having 1 to about 8 carbon atoms, or cycloalkyl or aryl groups having about 5 or 6 ring carbon atoms; R.sub.2 and R.sub.3 are individually selected from hydrogen, alkyl groups having 1 to about 8 carbon atoms, and cycloalkyl and aryl groups having about 5 or 6 ring carbon atoms; R.sub.4 is selected from hydrogen and alkyl groups having 1 to about 8 carbon atoms; and n is either 1 or 2.These compounds are useful as UV light stabilizers in plastics and cosmetics (e.g. sunscreens).Type: GrantFiled: August 27, 1984Date of Patent: October 22, 1985Assignee: Olin CorporationInventor: Robert J. Raynor