Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/375)
  • Patent number: 5104985
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: April 14, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 5093336
    Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: March 3, 1992
    Assignee: Hoechat-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5093331
    Abstract: The present invention relates to polyoxygenated labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive inotropic effect, an effect of lowering intraocular pressure and lowering blood pressure.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: March 3, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bansi Lal, Ashok K. Gangopadbya, Alihussein N. Dohadwalla, Ramanujam Rajgopalan, Richard H. Rupp
  • Patent number: 5026846
    Abstract: Diaryl sulphides and diaryl selenides of formula:Ar--X--Arwhere X=S or Se and Ar=aryl are made by the action of sulphur and sulphur dioxide or selenium and selenium dioxide on a compound of formula:Ar--HThe process is especially useful for the preparation of phenothiazines of formula ##STR1## in which X=S or Se and Z and Z.sub.1, which may be identical or different, are each hydrogen, halogen, alkyl or alkoxy.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: June 25, 1991
    Assignee: Rhone-Poulenc Sante
    Inventor: Jean-Pierre Duchesne
  • Patent number: 5013734
    Abstract: The esters of phenylalkanoic acid of the formula: ##STR1## wherein R.sup.1 is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen,(ii) two or three of nitrogen and sulfur in total, or(iii) one or two sulfur;R.sup.2 is hydrogen; orR.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen, or(ii) two or three of nitrogen and oxygen in total,the aforementioned hetero rings, represented by R.sup.1 or formed by R.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl;R.sup.3 each, independently, is hydrogen or C1-4 alkyl;R.sup.4 is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, cyano, nitro or nitroxy;R.sup.5 each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R.sup.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: May 7, 1991
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Sadahiko Iguchi, Masanori Kawamura, Tsumoru Miyamoto
  • Patent number: 4997836
    Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: March 5, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa
  • Patent number: 4994463
    Abstract: 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: Grant
    Filed: December 8, 1988
    Date of Patent: February 19, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 4948796
    Abstract: A piperazine derivative represented by the following formula or a salt thereof: ##STR1## which is useful for curing cerebro-vascular disease and post-cerebro-vascular disease.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: August 14, 1990
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Toru Hiraiwa, Kenji Takeda, Joji Nakano, Mineichi Sudani, Kunikazu Furuhata, Makoto Takata, Hiroyo Kawafuchi, Isao Watanabe
  • Patent number: 4943571
    Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: July 24, 1990
    Assignee: Hoechst-Roussel Phamraceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4942184
    Abstract: Antineoplastic, water soluble, taxol derivatives and methods for preparing the same are described.
    Type: Grant
    Filed: March 7, 1988
    Date of Patent: July 17, 1990
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Rudiger D. Haugwitz, Leon Zalkow, Jan Glinski, Mathew Suffness, Howard M. Deutsch, Venkatachala Narayanan
  • Patent number: 4937259
    Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Ta Jyh Lee
  • Patent number: 4935059
    Abstract: Basic rhodamine dyes suitable for use in recording fluids for the ink jet process and for coloring paper stock have the formula ##STR1## where L is C.sub.2 -C.sub.10 -alkylene,R.sup.1, R.sup.2 and R.sup.3 are each independently of the others hydrogen, substituted or unsubstituted C.sub.1 -C.sub.10 -alkyl or C.sub.5 -C.sub.7 -cycloalkyl or R.sup.1 and R.sup.2 together with the nitrogen atom linking them together are a hetero cyclic radical,An.sup..crclbar. is one equivalent of an anion and m and n are each independently of the other 0 or 1.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: June 19, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Udo Mayer, Andreas Oberlinner
  • Patent number: 4898876
    Abstract: A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: February 6, 1990
    Assignee: Kowa Co., Ltd.
    Inventors: Setsuro Fujii, Eizou Hattori, Mitsuteru Hirata, Koichiro Watanabe, Kazuhiro Onogi, Masahiko Nagakura
  • Patent number: 4892878
    Abstract: The present invention relates to pharmaceutical compositions of novel oleic acid esters of wellknown neuroleptics and tranquillizers of the phenothiazine, thioxanthene and butyrophenone type containing an aliphatic hydroxy group, and which may be represented by the following general formula: ##STR1## wherein R represents the residue of a hydroxy group containing neuroleptic selected from phenothiazines, thioxanthenes and butyrophenones, as well as pharmaceutically acceptable acid additions salts thereof, which compositions take the form of injectable solutions or suspensions in propylene glycol dioleate (TS-RD-9), methyl oleate or ethyl oleate.None of the esters of Formula I have been specifically described before but have only been broadly disclosed in the patent literature, and the esters as such, as well as a method of preparation of said esters, fall within the scope of the present invention.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: January 9, 1990
    Assignee: H. Lundbeck A/S
    Inventors: Klaus G. Jensen, Peter Bregnedal
  • Patent number: 4889858
    Abstract: The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof.
    Type: Grant
    Filed: February 17, 1988
    Date of Patent: December 26, 1989
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Uno, Mikio Kurokawa, Fuminori Sato, Shunsuke Naruto, Yoshinobu Masuda
  • Patent number: 4873237
    Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: October 10, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4837210
    Abstract: The invention relates to novel fluoran compounds of the general formula ##STR1## wherein R.sub.1 and R.sub.2, each independently of the other, are lower alkyl;A is ##STR2## or a pyrrolidinyl, piperidino, morpholino or piperazino radical; and R.sub.3 and R.sub.4, each independently of the other, are C.sub.1 -C.sub.12 alkyl, cycloalkyl, phenyl or phenyl substituted by lower alkyl or lower alkoxy.These compounds are particularly suitable for use as color formers in pressure-sensitive or heat-sensitive recording materials.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: June 6, 1989
    Assignee: Appleton Papers Inc.
    Inventors: Patricia Dwyer-Hallquist, William J. Becker, Robert E. Miller, Kenneth D. Glanz
  • Patent number: 4837227
    Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: June 6, 1989
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4775672
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4775663
    Abstract: A benzofuran derivative which is a compound of formula (I): ##STR1## wherein a to d each are 0 to 1, with a+b+c+d.gtoreq.2; R.sub.1 to R.sub.6 are each H or C.sub.1 -C.sub.6 alkyl; R.sub.7 is --CH.sub.2 OR.sub.8 (R.sub.8 =H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl), --COR.sub.9 (R.sub.9 =H, C.sub.1 -C.sub.6 alkyl, ##STR2## which is an amino acid or amino sugar residue or where R' and R" are H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl, C.sub.3 -C.sub.6 alkenyl or form a heterocycle) or OR.sub.10 (where R.sub.10 is H, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.6 mono- or polyhydroxyalkyl or --OR.sub.10 is derived from a sugar) has retinoid type action and can be used in cosmetics (body and hair hygiene) and in medicine (treatment of dermatological conditions; atopy; degenerative diseases of connective tissue; or corneopathies).
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: October 4, 1988
    Assignee: L'Oreal
    Inventors: Serge Forestier, Alain Lagrange, Gerard Lang, Braham Shroot
  • Patent number: 4771049
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: March 16, 1987
    Date of Patent: September 13, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4771069
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: February 11, 1987
    Date of Patent: September 13, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4751238
    Abstract: This invention relates to substituted alkyl amine derivatives of 6,11-dihydro-11-oxodibenz[b,e]oxepins of the formula: ##STR1## where X is hydrogen, halogen, lower alkoxy, lower alkyl, nitro, hydroxyl and CF.sub.3 ; R is H, and lower alkyl, R.sub.1 is CH.sub.3 SO.sub.3 and ##STR2## where R.sub.2 and R.sub.3 are the same of different and are hydrogen, lower alkyl, mesyl (CH.sub.3 SO.sub.2 --), and cycloalkyl loweralkyl; ##STR3## and the pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: June 18, 1986
    Date of Patent: June 14, 1988
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4734500
    Abstract: A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: March 11, 1986
    Date of Patent: March 29, 1988
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Akihiro Tobe, Shinichiro Fujimori, Tomoshi Yamazaki, Mamoru Sugano, Ryoji Kikumoto, Issei Nitta
  • Patent number: 4719224
    Abstract: Novel optically active isomers or racemic mixtures of thiophene acetic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, Y is selected from the group consisting of --OR.sub.2 and ##STR2## R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and ##STR3## n is an integer from 2 to 5, X' and X" are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken together with the nitrogen atom form an optionally unsaturated heterocycle of 5 to 6 ring members, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids and bases having a good analgesic and anti-inflammatory activity and inhibition of 5-lipoxygenase and cyclooxygenase, a process and intermediates for their preparation.
    Type: Grant
    Filed: March 6, 1986
    Date of Patent: January 12, 1988
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
  • Patent number: 4713453
    Abstract: The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: December 15, 1987
    Assignee: Suntori Limited
    Inventors: Toshio Tatsuoka, Kenji Suzuki, Kayoko Imao, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
  • Patent number: 4685934
    Abstract: Monoazo compounds of formula ##STR1## wherein R.sub.1 is a coupling component radical,R.sub.1 is C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted by 1 or 2 substituents selected from chloro, cyano, hydroxy, C.sub.1-4 alkoxy, phenyl and phenyl substituted by 1 or 2 substituents selected from chloro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, sulfo, sulfamoyl and acetamido; C.sub.5-7 cycloalkyl; C.sub.5-7 cycloalkyl substituted by 1 to 3 C.sub.1-4 alkyl groups; phenyl; phenyl substituted by 1 to 3 substituents selected from chloro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acetamido (maximum of 1), carboxy (maximum of 1), sulfo (maximum of 1) and --SO.sub.2 NR.sub.7 R.sub.8 (maximum of 1); 1- or 2-naphthyl or 1- or 2-naphthyl substituted by sulfo,whereineach of R.sub.7 and R.sub.8 is independently hydrogen; C.sub.1-4 alkyl; C.sub.1-4 alkyl monosubstituted by hydroxy or phenyl; cyclohexyl; phenyl or phenyl monosubstituted by chloro, methyl or methoxy, or--NR.sub.7 R.sub.
    Type: Grant
    Filed: July 12, 1985
    Date of Patent: August 11, 1987
    Assignee: Sandoz Ltd.
    Inventors: Francois Benguerel, Roland Mislin
  • Patent number: 4684664
    Abstract: Disclosed herein are derivatives of .beta.-(4-isocyano-1,2,3,4-diepoxycyclopentyl)acrylic acid, the derivatives showing an antibacterial activity, an antifungal activity and an antimycoplasmal activity.
    Type: Grant
    Filed: January 16, 1985
    Date of Patent: August 4, 1987
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Katsuhisa Osugi, Isao Ichinose, Eisaku Takahashi, Masato Arahira
  • Patent number: 4678788
    Abstract: N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepins are disclosed of the general formula I, ##STR1## in which R represents an aminocarbonyl, amino-oximinomethyl, 1,3-dioxolan-2-yl or 1,3-dioxan-2-yl, group and their addition salts with convenient organic and inorganic acids. These compounds are highly potent antidopaminergic, non-cataleptic neuroleptics of use in the treatment of schizophrenia. According to recent pharmacological assay results, the subject compounds are expected to be substantially free of the usual undesired extrapyramidal side effects. They can be obtained by common preparative methods from the respective starting compounds of formula III, IV or V, or also by appropriate interconversion reactions of other compounds of formula I.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: July 7, 1987
    Assignee: SPOFA, Spojene Podniky Pro Zdravotnickou Vyrobu
    Inventors: Miroslav Protiva, Jiri Jilek, Irena Cervena, Antonin Dlabac, Martin Valchar, Josef Pomykacek
  • Patent number: 4673752
    Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: June 16, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4672115
    Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: June 9, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4668695
    Abstract: Novel aminoalkylthiodibenzothiepins and related compounds, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as antidepressant, analgetic, and anticonvulsant agents.
    Type: Grant
    Filed: October 28, 1983
    Date of Patent: May 26, 1987
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
  • Patent number: 4668690
    Abstract: This invention relates to 1,2,3,4,4a,9b-hexahydro-4a-aminoalkyldibenzofurans of the formula ##STR1## where X is hydrogen, loweralkyl, F and Cl; R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkoxyloweralkyl, aryloxyloweralkyl, cycloalkylloweralkyl and heteroarylloweralkyl: R.sub.2 is hydrogen, lower alkyl or R.sub.1 and R.sub.2 taken together with the N ring atom constitute a saturated or unsaturated heterocyclic ring having 5 or 6 members; R.sub.3 is hydrogen, lower alkyl; n is an interger of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the stereo, optical and geometrical isomers of the foregoing.
    Type: Grant
    Filed: December 30, 1985
    Date of Patent: May 26, 1987
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventor: Gregory M. Shutske
  • Patent number: 4663456
    Abstract: The .beta.-carbolines N-substituted in 2-position with a piperidinyl alkyl group are antipsychotic agents and anxiolytic agents with minimal extrapyramidal side effects, useful in the treatment of psychological disorders such as paranoia and schizophrania as well as general states of anxiety.
    Type: Grant
    Filed: September 16, 1985
    Date of Patent: May 5, 1987
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4647675
    Abstract: Novel compounds of the general formula I ##STR1## where A.sup..crclbar. is an anion, R is hydrogen or unsubstituted or substituted alkyl or cycloalkyl, R.sup.1 and R.sup.2 independently of one another are each hydrogen or unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be aryl, or R.sup.1 and R.sup.2, together with the nitrogen atom, form a saturated heterocyclic structure, the radicals R.sup.3 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.4 and R.sup.5 independently of one another are each unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be hydrogen, aryl or hetaryl, R.sup.4 and R.sup.5, together with the nitrogen atom, form a saturated heterocyclic structure, n is 1, 2 or 3, X is hydrogen, chlorine, bromine, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or nitro and Y is hydrogen or chlorine, are particularly useful for dyeing paper stocks.
    Type: Grant
    Filed: July 11, 1985
    Date of Patent: March 3, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Udo Mayer, Andreas Oberlinner
  • Patent number: 4645758
    Abstract: 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: Grant
    Filed: January 17, 1986
    Date of Patent: February 24, 1987
    Inventors: Nils-Erik Willman, Bengt C. H. Sjogren, Lennart G. Nordh, Gustav L. Persson, Goran H. Sjoholm
  • Patent number: 4639446
    Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: January 27, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4624949
    Abstract: The invention relates to compounds having the general formula (I) ##STR1## wherein R.sub.1 is carboxy, esterified carboxy or an amide of formula ##STR2## in which R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl, A is C.sub.2 -C.sub.6 alkylene and R.sub.a and R.sub.b are hydrogen or C.sub.1 -C.sub.6 alkyl or R.sub.a and R.sub.b taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;each of R.sub.3 to R.sub.8 is independently hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.4 alkenyloxy or C.sub.1 -C.sub.6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.
    Type: Grant
    Filed: March 4, 1986
    Date of Patent: November 25, 1986
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
  • Patent number: 4569994
    Abstract: Dibenzopyran derivatives which possess antihypoxia activity are 7,8,9,10-tetrahydro-6H-dibenzo[b,d]pyranyloxyaminopropanols having the formula: ##STR1## Where X is oxygen or dialkyl in which each alkyl group contains one to seven carbons (C.sub.1 -C.sub.7); R is hydrogen or alkyl containing one to seven carbons (C.sub.1 -C.sub.7); and A is --NR.sub.1 R.sub.2 where R.sub.1 and R.sub.2 may independently be hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, C.sub.7 -C.sub.10 phenylalkyl, C.sub.7 -C.sub.10 phenoxyalkyl, C.sub.2 -C.sub.6 alkanol, 6-oxo-6H-dibenzo[b,d]pyran-3-yl, 2-hydroxy-3-(7,8,9,10-tetrahydro-6-oxo-6H-dibenzo[b,d]pyranyl-3-oxy)-propy l; or A is a heterocyclic ring of structure: ##STR2## where n=2 or 3; or A is a substituted heterocyclic ring of structure: ##STR3## where Y and Z may be independently hydrogen or methyl and B represents a single bond, methylene, ethylene, propylene, CH-phenyl, CHCH.sub.2 -phenyl, oxygen, sulfur, or N--R.sub.4 where R.sub.4 is hydrogen, C.sub.
    Type: Grant
    Filed: June 27, 1985
    Date of Patent: February 11, 1986
    Assignee: Pennwalt Corporation
    Inventor: Ronald C. Griffith
  • Patent number: 4539412
    Abstract: 7-Hydroxylucanthone and 7-hydroxyhycanthone derivatives have been found to have significant antitumor effect. The derivatives are of the general formula: ##STR1## wherein the radicals R.sup.1 and R.sup.2 are lower alkyl groups or other simple groups and R.sup.3 is OH where X.dbd.O, and H or OH where X.dbd.S.
    Type: Grant
    Filed: February 1, 1984
    Date of Patent: September 3, 1985
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Sydney Archer
  • Patent number: 4526891
    Abstract: This invention relates to compounds of the formula: ##STR1## where X is hydrogen, halogen, lower alkoxy, lower alkyl, nitro, hydroxyl and CF.sub.3 ; R is H, and lower alkyl, R.sub.1 is CH.sub.3 SO.sub.3 and ##STR2## where R.sub.2 and R.sub.3 are the same or different and are hydrogen, lower alkyl, mesyl (CH.sub.3 SO.sub.
    Type: Grant
    Filed: March 10, 1983
    Date of Patent: July 2, 1985
    Assignee: Hoechst Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Linda L. Setescak
  • Patent number: 4515793
    Abstract: A compound of the formula ##STR1## in which A is ##STR2## n is 1, 2 or 3, and R is phenyl optionally substituted with halogen, alkyl, phenyl, cyano, hydroxy, alkoxy, mercapto, sulfinyl, sulfonyl, amino, nitro, trifluoromethyl and/or naphthyl radicals; or a furan, thiophene, pyridine, benzofuran, dibenzothiophene or thianthrene radical,or a pharmacologically acceptable salt thereof, for treating schistosomiasis.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: May 7, 1985
    Assignee: Edna McConnell Clark Foundation
    Inventors: Leslie M. Werbel, Norman Colbry, William Turner, Donald F. Worth
  • Patent number: 4496557
    Abstract: Compounds corresponding to the general formula: ##STR1## in which X and Y identical or different, represent a hydrogen or a halogen atom, a lower alkyl, a lower alkoxy or a trifluormethyl group,A represents a methylene group, a direct bond or an imino--NR.sub.3 -- group in which R.sub.3 is a hydrogen atom or a lower alkyl or lower alkanoyl groupR.sub.1 and R.sub.2 identical or different, each represents a hydrogen atom or a lower alkyl group, or together with the nitrogen atom to which they are attached they form a pyrrolidino, piperidino or methyl-4 piperazine group, andn represents an integer from 1 to 3, in their racemic or optical isomeric forms, as well as their salts of addition with a therapeutically compatible mineral or organic acid.These compounds are useful as antidepressants.
    Type: Grant
    Filed: August 16, 1982
    Date of Patent: January 29, 1985
    Assignee: Adir
    Inventors: Charles Malen, Jean-Claude Poignant
  • Patent number: 4463001
    Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.
    Type: Grant
    Filed: October 1, 1981
    Date of Patent: July 31, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
  • Patent number: 4459306
    Abstract: This invention relates to novel tricyclic ethers, pharmaceutically acceptable addition salts and optical isomers therefrom. The compounds described herein are useful as psychotropic agents in the treatment of depression and anxiety. Also included herein are methods of preparing said compounds, pharmaceutical compositions including them and methods of treating human or animal beings by administering these pharmaceutical compositions.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 10, 1984
    Assignee: Science Union et Cie
    Inventors: Charles Malen, Jean-Claude Poignant
  • Patent number: 4436921
    Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
    Type: Grant
    Filed: July 16, 1980
    Date of Patent: March 13, 1984
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
  • Patent number: 4424213
    Abstract: Novel heterobicyclic compounds of Formula I, processes for preparing same and pesticidal compositions and methods are described.
    Type: Grant
    Filed: November 2, 1981
    Date of Patent: January 3, 1984
    Assignee: SDS Biotech Corporation
    Inventors: Thomas A. Magee, Robert D. Battershell, Lawrence E. Limpel, Andrew W. Ho, Arthur W. Friedman, H. Glenn Corkins, William W. Brand, Russell Buchman, Louis Storace, Edmond R. Osgood
  • Patent number: 4409221
    Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are identical or different and represent hydrogen, halogen, lower alkyl or alkoxy or trifluoromethyl; R.sub.5 represents hydrogen or lower alkyl, X represents hydrogen and Y represents hydroxy, or X and Y together represent oxygen and Ar represents an optionally substituted aromatic moiety, having potent anti-bronchoconstrictor properties.
    Type: Grant
    Filed: June 9, 1982
    Date of Patent: October 11, 1983
    Assignee: Riom Laboratories - Cerm S.A.
    Inventors: Michel Combourieu, Jean-Claude Laigle, Norbert Busch
  • Patent number: 4356186
    Abstract: Novel acetic acid derivatives of the formula: ##STR1## wherein X is oxygen or sulfur; R.sub.1 is hydrogen or a lower alkyl; R.sub.2 is hydroxy, an alkoxy, an alkenyloxy, a cycloalkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-disubstituted amino-lower alkoxy, a lower alkoxycrbonyl-lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group ##STR2## wherein R.sub.3 is hydrogen, hydroxy, a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy-lower alkyl, R.sub.4 is hydrogen, a lower alkyl or a hydroxy-lower alkyl, or the R.sub.3 and R.sub.4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group --CH(R.sub.1)COR.sub.
    Type: Grant
    Filed: March 20, 1981
    Date of Patent: October 26, 1982
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Hitoshi Uno, Mikio Kurokawa, Hideo Nakamura
  • Patent number: 4329461
    Abstract: Novel polyhalothyronines or immunogenic mimetic analogs are provided conjugated to a fluorescer compound with the resulting conjugate being highly fluorescent. Specifically, the compounds have at least one of the following characteristics: bromine(s) at the 3',5'-positions of the thyronine or mimetic analog; or a rigid linking group between the thyronine and the fluorescer, so as to inhibit heavy atom catalyzed decay of fluorescence. The subject conjugates find a wide variety of uses in detecting for thyroid hormones as well as proteins which specifically bind to thyroid hormones.
    Type: Grant
    Filed: January 11, 1980
    Date of Patent: May 11, 1982
    Assignee: Syva Company
    Inventors: Pyare L. Khanna, Edwin F. Ullman