The Tricyclo Ring System Consists Of A Five-membered Carbocyclic Ring Ortho Fused To Both A Six-membered Carbocyclic Ring And The Six-membered Hetero Ring (e.g., Indenopyridines, Etc.) Patents (Class 546/111)
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Patent number: 6958328Abstract: This invention provides novel arylindenopyridines of the formula: , and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing PDE activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: GrantFiled: April 16, 2002Date of Patent: October 25, 2005Assignee: Ortho-McNeil Pharmaceutical, IncInventors: Geoffrey R. Heintzelman, Kristin M. Averill, John H. Dodd
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Patent number: 6903109Abstract: This invention provides novel arylindenopyridines of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing Adensine A2a receptors or reducing PDE activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: GrantFiled: September 27, 2002Date of Patent: June 7, 2005Assignee: Ortho-Muniel Pharmaceutical, Inc.Inventors: Geoffrey R. Heintzelman, Kristin M. Averill, John H. Dodd, Keith T. Demarest, Yuting Tang, Paul F. Jackson
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Patent number: 6620821Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholesterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis and pharmaceutically acceptable salts thereof, n is 0 or 1; x is 0, 1, 2, 3 or 4; y is 0, 1, 2, 3 or 4, provided that at least one of x and y is other than 0; and optionally one or more carbons of (CH2)x and/or (CH2)y together with additional carbons form a 3 to 7 membered spirocyclic ring; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; R3 is H or lower alkyl; R4 and R7 are as defined herein.Type: GrantFiled: December 4, 2001Date of Patent: September 16, 2003Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 6515011Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.Type: GrantFiled: December 18, 2001Date of Patent: February 4, 2003Assignee: Merck & Co., Inc.Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
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Patent number: 6462044Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: August 30, 2001Date of Patent: October 8, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Patent number: 6331543Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: September 1, 1999Date of Patent: December 18, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Patent number: 6323227Abstract: This invention relates to compounds of formula which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: February 26, 1999Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada, Heinz W. Pauls, Yong Gong, Daniel G. McGarry
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Patent number: 6248884Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.Type: GrantFiled: June 3, 1999Date of Patent: June 19, 2001Assignee: The Perkin-Elmer CorporationInventors: Joe Y. L. Lam, Scott C. Benson, Steven M. Menchen
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Patent number: 6080767Abstract: The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: June 27, 1997Date of Patent: June 27, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
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Patent number: 6063788Abstract: Bicyclic-fused pyridines are prepared by introducing the appropriate side chain by reaction of the corresponding aldehydes with the aid of Wittig or Grignard reagents. The bicyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of arteriosclerosi.Type: GrantFiled: June 27, 1997Date of Patent: May 16, 2000Assignee: Bayer AktiengesellschaftInventors: Arndt Brandes, Michael Logers, Gunter Schmidt, Rolf Angerbauer, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher
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Patent number: 6034098Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.Type: GrantFiled: July 21, 1997Date of Patent: March 7, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, R. Michael Lawrence, David R. Magnin, Michael A. Poss, Richard B. Sulsky, Joseph A. Tino, John E. Lawson, Henry M. Holava, Richard A. Partyka
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Patent number: 5965582Abstract: The N-benzylindole- and benzopyrazole derivatives of the general formula 1 ##STR1## possess anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulating effect and are suitable for the preparation of medicaments.Type: GrantFiled: May 12, 1997Date of Patent: October 12, 1999Assignee: ASTA Medica AktiengesellschaftInventors: Guillaume Lebaut, Fabienne Fouchard, Bernhard Kutscher, Peter Emig, Ilona Fleischhauer, Jurgen Schmidt, Stefan Szelenyi
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Patent number: 5958972Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: May 20, 1997Date of Patent: September 28, 1999Assignee: Warner-Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Joseph Armand Picard, Andrew David White, Qi-Zhuang Ye
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Patent number: 5952336Abstract: Hexahydroindenopyridine compounds having the following formula and relative stereochemistry ##STR1## where R.sup.1 is C.sub.1-6 alkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; R.sup.3 is carboxyl or a group which is metabolized to a carboxyl group under mammalian physiological conditions; R.sup.4 is halogen; mixtures of said compound and acid addition salts thereof exhibit potent antispermatogenic activity and are useful in a method of inhibiting spermatogenesis in mammals.Type: GrantFiled: January 31, 1997Date of Patent: September 14, 1999Assignee: Research Triangle InstituteInventors: C. Edgar Cook, Joseph M. Jump, Pingsheng Zhang, John R. Stephens, Patricia A. Fail, Yue-Wei Lee, Mansukh C. Wani
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Patent number: 5885983Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.Type: GrantFiled: April 23, 1997Date of Patent: March 23, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Scott A. Biller, John K. Dickson, Jr.
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Patent number: 5854274Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.Type: GrantFiled: December 5, 1996Date of Patent: December 29, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
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Patent number: 5808015Abstract: Dyestuffs of the formula ##STR1## wherein D is the radical of a carbo- or heterocyclic diazo component,X represents O, NH, NT, NCOT, NCCH.sub.2 T or NSO.sub.2 T,are preferably suitable, if m=n=l=o, for dyeing and printing hydrophobic synthetic fiber materials and mixtures thereof with naturally occurring fiber materials.Type: GrantFiled: September 18, 1996Date of Patent: September 15, 1998Assignee: Bayer AktiengesellschaftInventor: Rainer Hamprecht
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Patent number: 5773618Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, or cycloalkyloxy; R.sup.2 represents hydrogen or halogen; R.sup.3 represents hydrogen, alkyl, or cycloalkyl; and the dotted line represents a single or double carbon--carbon bond!; and salts thereof have valuable fungicidal activities which make them of considerable value in agriculture and horticulture.Type: GrantFiled: May 14, 1997Date of Patent: June 30, 1998Assignee: Sankyo Company, LimitedInventors: Hideo Takeshiba, Chiaki Imai, Hiroshi Ohta, Shigehiro Kato, Hiroyuki Itoh
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Patent number: 5663344Abstract: The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A. The compounds are capable of inhibiting cholinesterase enzymes and, therefore, are useful as pharmaceutical agents for treatment of disorders involving cholinesterase enzymes. Examples of such disorders include myasthenia gravis, Alzheimer's dementia and the improvement of senile memory loss.Type: GrantFiled: July 22, 1994Date of Patent: September 2, 1997Assignee: Mayo Foundation for Medical Education and ResearchInventors: Alan Paul Kozikowski, Yan Xia
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Patent number: 5637554Abstract: A method for controlling undesired plant growth and for regulating plant growth by allowing 4-methyl-5H-indeno[3,2-b]pyridines and 1-methyl-9H-indeno[2,3-c]pyridines of the general formula I ##STR1## where X, Y, Z and the radicals R.sup.1 to R.sup.5 have the meanings as described in the specification,to act on the plants, and novel 4-methyl-5H-indeno- [3,2-b]pyridines and herbicides and plant growth regulators containing these.Type: GrantFiled: May 12, 1995Date of Patent: June 10, 1997Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Norbert Meyer, Juergen Kast, Peter Plath, Hartmann Koenig, Albrecht Harreus, Uwe Kardorff, Matthias Gerber, Helmut Walter, Andreas Landes, Karl-Otto Westphalen
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Patent number: 5594001Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.Type: GrantFiled: March 28, 1994Date of Patent: January 14, 1997Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Christopher A. Teleha, Wendell W. Wilkerson, Richard A. Earl
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Patent number: 5438056Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.Type: GrantFiled: October 5, 1993Date of Patent: August 1, 1995Assignee: American Home Products CorporationInventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
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Patent number: 5424430Abstract: Polycyclic cognition enhancers having the general formula (1a), (1b) or (1c) are provided: ##STR1## wherein: R.sub.1 is a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;R.sub.2 and R.sub.3 are independently H, F, Cl, Br, NO.sub.2, CONH.sub.2, CON(R.sub.4)(R.sub.4 '), S(O).sub.m R.sub.4, CF.sub.3, or N(R.sub.4)(R.sub.4 ');R.sub.4 and R.sub.4 ' are independently H, alkyl having from 1 to 4 carbon atoms, CH.sub.2 Phe--W, or Phe--W;Phe is a phenyl group;R.sub.5 is --(CH.sub.2).sub.n --Y or --OCOR.sub.4 ;Y is H, OH, NH.sub.2, NHR.sub.4, N(R.sub.4)(R.sub.4 '), NHCOR.sub.4, NHCO.sub.2 R.sub.4, NHS(O).sub.2 R.sub.4, F, Cl, Br, OR.sub.4, S(O).sub.m R.sub.4, CO.sub.2 H, CO.sub.2 R.sub.4, CN, CON(R.sub.4)(R.sub.4 '), CONHR.sub.4, CONH.sub.2, COR.sub.4, Phe, Phe--W, --C.tbd.CCO.sub.2 R.sub.4, --CH.dbd.CHR.sub.4, --C.tbd.CR.sub.4, or a heterocyclic aromatic moiety such as a 4-pyridyl, 2-pyridyl, 4-pyrimidyl, or pyrazinyl group;W is F, Cl, Br, R.sub.4, OR.sub.4, NO.sub.2, NH.Type: GrantFiled: September 10, 1993Date of Patent: June 13, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: James H. Jensen, Timothy D. Costello, Leon De Brabander, Jr., Matthew E. Voss
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Patent number: 5319084Abstract: Hexahydroindenopyridine compounds having the following formula and relative stereochemistry ##STR1## where R.sup.1 is C.sub.1-6 alkyl, R.sup.2 is hydrogen or C.sub.1-6 alkyl and R.sup.3 is carboxyl or a group which is metabolized to a carboxyl group under mammalian physiological conditions exhibit potent antispermatogenic activity and are useful in a method of inhibiting spermatogenesis in mammals.Type: GrantFiled: August 16, 1993Date of Patent: June 7, 1994Assignee: Research Triangle InstituteInventors: C. Edgar Cook, Yue-Wei Lee, Mansukh C. Wani, Patricia A. Fail, Joseph M. Jump
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Patent number: 5278316Abstract: Novel unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.Type: GrantFiled: December 19, 1990Date of Patent: January 11, 1994Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, Julian Aranda
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Patent number: 5276053Abstract: 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: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
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Patent number: 5254561Abstract: A class of 2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridine and 2,3,4,4a,5,6,7,11b-octahydro-1H-benzo[3,4]cyclohepta[1,2-c]pyridine derivatives are selective ligands at sigma recognition sites and are therefore useful in the treatment and/or prevention of psychiatric and/or gastrointestinal disorders.Type: GrantFiled: June 18, 1991Date of Patent: October 19, 1993Assignee: Merck Sharp & Dohme LimitedInventors: David C. Billington, Michael G. N. Russell
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Patent number: 5248681Type: GrantFiled: September 19, 1991Date of Patent: September 28, 1993Assignee: Pfizer Inc.Inventor: Kelvin Cooper
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Patent number: 5198462Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.Type: GrantFiled: October 16, 1991Date of Patent: March 30, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Hiroyuki Tawada, Hitoshi Ikeda
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Patent number: 5185447Abstract: Ketones having formulas (1)-(3) are provided by improved methods which involve the treatment of compounds having formulas (9)-(11) with aqueous base. ##STR1## wherein R.sub.x is NO.sub.2.Type: GrantFiled: January 29, 1992Date of Patent: February 9, 1993Assignee: Du Pont Merck Pharmaceutical CompanyInventor: Edward C. Crapps
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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: 5162335Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.Type: GrantFiled: November 27, 1989Date of Patent: November 10, 1992Assignee: Duphar International Research B.V.Inventors: Maurits E. A. Vandewalle, Johan T. A. Van der Eycken, Ineke van Wijngaarden, Roelof van Hes, Antonius Hulkenberg, Christophorus M. J. F. Keet
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Patent number: 5086179Abstract: This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.Type: GrantFiled: September 24, 1990Date of Patent: February 4, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Matthew R. Powers, Raymond D. Youssefyeh, William L. Studt, Frederick A. Golec
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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: 5049564Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno-[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.Type: GrantFiled: November 17, 1989Date of Patent: September 17, 1991Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
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Patent number: 5030631Abstract: Novel tricyclic arylsulfonamides useful for treating hypertension and bronchoconstiction, as well as to their pharmaceutical compositions and methods for using the same.Type: GrantFiled: November 27, 1989Date of Patent: July 9, 1991Assignee: Schering CorporationInventor: Barr E. Bauer
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Patent number: 4954509Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.Type: GrantFiled: February 17, 1989Date of Patent: September 4, 1990Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
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Patent number: 4873250Abstract: The use of the naturally occurring and readily synthesized alkaloid compound onychine as an antimicrobial agent and particularly against Candida albicans organism.Type: GrantFiled: July 14, 1988Date of Patent: October 10, 1989Assignee: The University of MississippiInventors: Charles D. Hufford, Alice M. Clark
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Patent number: 4824852Abstract: New indole derivatives of the general formula I ##STR1## in which Ind is a 3-indolyl radical which can be substituted by a hydroxymethyl, methylenedioxy, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, CN or COW group and/or can be substituted once or twice by alkyl, O-alkyl, OH, F, Cl or Br,is H, OH, O-alkyl, NH.sub.2, NH-alkyl or N(alkyl).sub.2,is --(CH.sub.2).sub.n --, --CH.sub.2 --S--CH.sub.2 CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 CH.sub.2 --or --CH.sub.2 --SO.sub.2 --CH.sub.2 CH.sub.2 --,Z is --(CH.sub.2).sub.m --, --CH.dbd.CH--, --CHOH--, --CO--, S, SO, SO.sub.2 or O,is 2, 3, 4 or 5 andis 1, 2 or 3, in which the alkyl groups each have 1-4 C atoms, and their salts,have effects on the central nervous system.Type: GrantFiled: February 8, 1988Date of Patent: April 25, 1989Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Henning Bottcher, Hans-Heinrich Hausberg, Christoph Seyfried, Klaus-Otto Minck
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Patent number: 4808718Abstract: Novel fused polycyclic and bridged compounds are disclosed which are useful as calcium entry blockers.Type: GrantFiled: May 6, 1986Date of Patent: February 28, 1989Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko, Brian T. Phillips
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Patent number: 4778894Abstract: Tautomeric mixtures of trans-(.+-.)-3,5-dialkyloctahydropyrazolo[3,4-g]quinoline, of trans-(.+-.)-6-alkyloctahydropyrazolo[4,3-f]quinoline, and of trans-(.+-.)-1,6-dialkyloctahydropyrazolo[4,3-f]quinoline, individual enantiomer thereof, pharmaceutically-acceptable acid addition salts thereof, and intermediates useful in the preparation thereof, useful as hypotensive agents.Type: GrantFiled: April 23, 1986Date of Patent: October 18, 1988Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Diane L. Huser, Richard N. Booher
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Patent number: 4740602Abstract: New indole derivatives of the general formula I ##STR1## in which Ind is a 3-indolyl radical which can be substituted by a hydroxymethyl, methylenedioxy, S-alkyl, SO-alkyl, SO.sub.2 -alkyl, CN or COW group and/or can be substituted once or twice by alkyl, O-alkyl, OH, F, Cl or Br,W is H, OH, O-alkyl, NH.sub.2, NH-alkyl or N(alkyl).sub.2,A is --(CH.sub.2).sub.n --, --CH.sub.2 --S--CH.sub.2 CH.sub.2 --, --CH.sub.2 --SO--CH.sub.2 CH.sub.2 -- or --CH.sub.2 --SO.sub.2 --CH.sub.2 CH.sub.2 --,is --(CH.sub.2).sub.m --, --CH.dbd.CH--, --CHOH--, --CO--, S, SO, SO.sub.2 or O,n is 2, 3, 4 or 5 andm is 1, 2 or 3,in which the alkyl groups each have 1-4 C atoms, and their salts, have effects on the central nervous system.Type: GrantFiled: June 26, 1986Date of Patent: April 26, 1988Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Henning Bottcher, Hans-Heinrich Hausberg, Christoph Seyfried, Klaus-Otto Minck
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Patent number: 4652567Abstract: There are disclosed novel compounds of the formula ##STR1## where X is H, halogen, loweralkyl, loweralkoxy, --CF.sub.3, or --OH; R is H, loweralkyl, arylloweralkyl, diarylloweralkyl, loweralkanoyl, arylloweralkanoyl or diarylloweralkanoyl; and R.sub.1 is H.sub.2, O or --NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being independently H or loweralkyl, or taken together with the nitrogen atom to which they are attached constitute ##STR2## R.sub.4 in turn being H, loweralkyl, hydroxyloweralkyl, aryl, arylloweralkyl or diarylloweralkyl or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory.Type: GrantFiled: March 13, 1985Date of Patent: March 24, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak, Susan J. Scott
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Patent number: 4605660Abstract: Indeno[2,1-c]pyridine compounds, particularly cyano substituted tetrahydroindeno[2,1-c]pyridine dicarboxylic acid ester compounds, their preparation and their use as calcium entry blockers are disclosed.Type: GrantFiled: June 3, 1985Date of Patent: August 12, 1986Assignee: Merck & Co., Inc.Inventor: David C. Remy
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Patent number: 4593033Abstract: Novel substituted indeno[2,1-c] pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.Type: GrantFiled: April 24, 1985Date of Patent: June 3, 1986Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko, Steven D. Young
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Patent number: 4535085Abstract: A perfluorotricyclic amine compound which is usable as an oxygen carrier in an artificial blood, represented by the general formula ##STR1## wherein R denotes a perfluoroalkyl group having 1-4 carbon atoms; the ring A denotes a five- or six-membered ring, the ring B denotes a five-, six- or seven-membered ring, the ring C denotes a five- or six-membered ring any one of the rings A, B and C optionary being substituted by one or more lower perfluoroalkyl group in addition to the above-mentioned substituent R; and further f, g, h, i, j and k denote integers appropriately selected to construct the above-mentioned size of rings A, B, and C; is prepared by reacting the corresponding perhydrotricyclic amine with fluorine.Type: GrantFiled: March 29, 1983Date of Patent: August 13, 1985Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4529798Abstract: Fused carbocyclic ring derivatives of pyridine which contain a nitrile or thioamide group on the carbocyclic ring e.g. 8-cyano or thiocarboxamido-5,6,7,8-tetrahydroquinolines are prepared by a process in which a sodium, potassium, lithium or magnesium halide derivative of the pyridine compound is treated with a compound RaRbNCN wherein Ra and Rb are the same or different and represent alkyl, cycloalkyl, or aralkyl, or Ra and Rb are joined to form a heterocyclic ring with the nitrogen, and the product is treated with a proton source to obtain the nitrile which is optionally treated with a sulphurizing agent to form the thioamide. The nitriles or thioamides may be isolated as their acid addition salts.Type: GrantFiled: December 2, 1981Date of Patent: July 16, 1985Assignee: John Wyeth & Brother LimitedInventor: Robin G. Shephard
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Patent number: 4511569Abstract: Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.Type: GrantFiled: August 26, 1982Date of Patent: April 16, 1985Assignee: Schering CorporationInventors: Elizabeth M. Smith, Ronald J. Doll, Bernard R. Neustadt
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Patent number: 4487778Abstract: Certain benzocycloalkaneheteroaromaticmethyl, e.g., benzocycloalkanethiophenemethyl, esters and insecticidal compositions containing these esters are useful for the control of a broad range of insects and acarids.Type: GrantFiled: January 27, 1983Date of Patent: December 11, 1984Assignee: FMC CorporationInventor: Ernest L. Plummer
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Patent number: 4482714Abstract: Herein is disclosed pyrazino[2',3'-3,4]pyrido[1,2-a]indole derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.Type: GrantFiled: January 26, 1983Date of Patent: November 13, 1984Assignee: American Home Products CorporationInventors: George Santroch, Ivo Jirkovsky