Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 544/393)
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Patent number: 6316617Abstract: This invention encompasses compounds of the formula where X1, X2, and X3, independently represent substituents of formula and the pharmaceutically acceptable salts thereof wherein the remaining variables are as defined herein and wherein said compounds are useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: August 8, 2000Date of Patent: November 13, 2001Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6313297Abstract: A process for preparing a 1-aryl-4-(arylethyl)piperazine of the formula (I) by reacting a 1-arylpiperazine of the formula (II) with an aromatic olefin of the formula (III) Ar′CR1═CHR2 (III) in an inert solvent in the presence of at least one basic catalyst, where in the formulae (I) to (III) Ar and Ar′ independently of one another are an aryl radical, selected from the group of the fused and unfused C6-C22-aromatics and the fused or unfused C5-C22-heteroaromatics which have at least one nitrogen, oxygen or sulfur atom in the ring; and R1 and R2 independently of one another are a hydrogen atom, a C1-C8-alkyl radical or an aryl radical Ar.Type: GrantFiled: July 13, 2000Date of Patent: November 6, 2001Assignees: Aventis Research & Technologies, GmbH & Co. KGInventors: Jürgen Herwig, Matthias Beller, Claudia Breindl
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Patent number: 6306859Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.Type: GrantFiled: March 1, 2000Date of Patent: October 23, 2001Assignee: American Home Products CorporationInventors: Wayne E. Childers, Michael G. Kelly, Gan Zhang, Yvette L. Palmer, Edward J. Podlesny
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Patent number: 6294549Abstract: A method for eliciting an &agr;v&bgr;5 or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonizing effect in a mammal which comprises administering to the mammal a therapeutically effective amount of a compound of the formula which are useful for inhibiting restenosis, angiogenesis, atherosclerosis, diabetic retinopathy, macular degeneration, inflammation or tumor growth.Type: GrantFiled: July 23, 1998Date of Patent: September 25, 2001Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan
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Patent number: 6291465Abstract: The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.Type: GrantFiled: February 25, 2000Date of Patent: September 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
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Patent number: 6281215Abstract: New 4-(1-piperazinyl)benzoic acid derivatives of the formula (I) are described. Also described is methods for making these compounds and their use as therapeutic agents. In particular, the compounds find use in the treatment of diabetes.Type: GrantFiled: October 20, 1999Date of Patent: August 28, 2001Assignee: Merck Patent GmbHInventors: Gérard Moinet, Gérard Botton, Liliane Doare, Micheline Kergoat, Didier Messangeau
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Patent number: 6277989Abstract: The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.Type: GrantFiled: March 14, 2000Date of Patent: August 21, 2001Assignee: Scios, Inc.Inventors: Sarvajit Chakravarty, Sundeep Dugar, John J. Perumattam, George F. Schreiner, David Y. Liu, John A. Lewicki
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Patent number: 6274583Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: June 30, 1999Date of Patent: August 14, 2001Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Mark G. Bock, Randall C. Newton
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Patent number: 6251909Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula wherein p is 2 or 3 and X denotes oxygen, N(CH2)nR6 or CR7R8, and R3, R4, R5, R6, R7, R8, Ar and n have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin)-antagonists.Type: GrantFiled: February 18, 2000Date of Patent: June 26, 2001Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6218394Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkylType: GrantFiled: December 9, 1996Date of Patent: April 17, 2001Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Patent number: 6172057Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: February 19, 1998Date of Patent: January 9, 2001Assignee: American Cyanamid CompanyInventors: Aranapakam Mudumbai Venkatesan, George Theodore Grosu, Jamie Marie Davis, Baihua Hu, Derek Cecil Cole, Jannie Lea Baker, Marcy Pamela Jacobson, Matthew Robin O'Dell
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Patent number: 6153612Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.Type: GrantFiled: October 5, 1999Date of Patent: November 28, 2000Assignee: Warner-Lambert CompanyInventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
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Patent number: 6133265Abstract: Amido, amino and sulfonamide substituted benzylamine derivatives useful in treating eating disorders have the formula ##STR1## where X.sub.1, X.sub.2, and X.sub.3, independently represent substituents of formula ##STR2## D=H, lower straight or branched chain alkyl having 1-6 carbon atoms, a methylene unit incorporated into a ring connected with G as in the cases of pyrrolidine, pyrrolidone, piperidine, and piperidone;E=O or H.sub.2 ;O=0 or 1;G=straight or branched chain lower alkyl having 1-6 carbon atoms, aryl, aryl substituted with halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, heteroaryl--selected from the group consisting of 2-, 3-, or 4-pyridyl, 2-pyrazyl, 2-, or 3-thienyl, 2-pyrazinyl, 2-, 3-, or 4-quinolyl, 1-, 3-, or 4-isoquinolyl, 2-quinoxalyl, 3-, or 4-cinnolyl, said heteroaryl substituted with halogen, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms;and A, T and R.sub.1 -R.sub.Type: GrantFiled: July 18, 1997Date of Patent: October 17, 2000Assignee: Neurogen CorporationInventors: Charles A. Blum, Robert DeSimone, Alan Hutchison, John M. Peterson
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Patent number: 6114335Abstract: The present invention relates to novel benzoylguanidine derivatives, processes for preparing them and their use in the preparation of pharmaceutical compositions.The novel benzoylguanidine derivatives correspond to general formula (I) ##STR1## which benzoylguanidine derivatives are useful in the treatment of ischemia.Type: GrantFiled: September 25, 1998Date of Patent: September 5, 2000Assignee: Boehringer Ingelheim KGInventors: Erich Buerger, Christian Eickmeier, Otto Roos
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Patent number: 6069143Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: January 11, 1996Date of Patent: May 30, 2000Assignee: SmithKline Beecham CorporationInventors: Fadia El-Fehail Ali, William Edward Bondinell, Raul Rolando Calvo, Thomas Wen-Fu Ku, William Henry Miller, James Samanen, Joseph Walter Venslavsky, Tobias Oregon Yellin
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Patent number: 5977141Abstract: Sulfonamide compounds are described which are inhibitors of matrix metalloproteinases, particularly stromelysin-1 and gelatinase A (72 kD gelatinase). Also described are methods for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes using the compounds.Type: GrantFiled: May 13, 1998Date of Patent: November 2, 1999Assignee: Warner-Lambert CompanyInventors: Daniel F. Ortwine, Claude F. Purchase, Jr., Andrew D. White
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Patent number: 5977115Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: December 4, 1997Date of Patent: November 2, 1999Assignee: Merck & Co., Inc.Inventors: Michael A. Patane, Mark G. Bock, Roger M. Freidinger, Rose Ann Ponticello, Randall C. Newton
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Patent number: 5962455Abstract: This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.Type: GrantFiled: July 18, 1997Date of Patent: October 5, 1999Assignee: Neurogen CorporationInventors: Charles A. Blum, Alan Hutchison, John M. Peterson
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Patent number: 5952306Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2## which are useful for inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: January 14, 1997Date of Patent: September 14, 1999Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Mark E. Duggan, James J. Perkins, Cecilia A. Hunt, Amy E. Krause, John H. Hutchinson, Benny C. Askew, Karen M. Brashear, Nathan C. Ihle
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Patent number: 5932582Abstract: Fibrinogen receptor antagonist alcohol prodrugs having the structure, for example, ofX--W--Y--Z--A--Bmore particularly, ##STR1##Type: GrantFiled: June 26, 1997Date of Patent: August 3, 1999Assignee: Merck & Co., Inc.Inventors: Steven D. Young, George D. Hartman, Laura A. Libby, Melissa S. Egbertson, Donald E. Slaughter
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Patent number: 5917037Abstract: The present invention relates to a process for the preparation of N-carboxyalkyl-3-fluoro-4-dialkylaminoanilines, which comprises reacting, in a first step, an orthonitrochlorobenzene of the formula (1) ##STR1## in which X is Cl or F, with a secondary amine of the formula (2) HNR.sup.1 R.sup.2, in which R.sub.1 and R.sup.2, independently of one another, are identical or different and are an alkyl radical having from 1 to 10 carbon atoms or, together with the N atom to which they are bonded, form a ring having from 3 to 7 members, in the presence of a base in the presence or absence of a solvent at from -10 to 120.degree. C., reacting, in a second step, the 2-chloro-4-dialkylamino-5-fluoronitrobenzene with hydrogen at from 30 to 150.degree. C.Type: GrantFiled: March 5, 1998Date of Patent: June 29, 1999Assignee: Clariant GmbHInventors: Thomas Schach, Theodor Papenfuhs
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Patent number: 5905080Abstract: Novel amide and urea derivatives, processes for their preparation, pharmaceutical compositions containing hem and their use as medicaments are disclosed.Type: GrantFiled: February 15, 1996Date of Patent: May 18, 1999Assignee: SmithKline Beecham, p.l.c.Inventors: David Malcolm Duckworth, Laramie Mary Gaster, Sarah Maragaret Jenkins, Andrew John Jennings, Keith Raymond Mulholland
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Patent number: 5900415Abstract: This invention encompasses compounds of formula (I) and the pharmaceutically ##STR1## acceptable salts thereof, wherein W,X,Y,A,T,R.sub.1 -R.sub.4,B,Ar,n and m are described herein and are useful in treating feeding disorders and certain cardiovascular diseases due to the binding of these compounds to human Neuropeptide Y1 receptors.Type: GrantFiled: April 29, 1997Date of Patent: May 4, 1999Assignee: Pfizer Inc.Inventors: John Matthew Peterson, Charles Albert Blum, Guolin Cai, Alan Jeffrey Hutchison
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Patent number: 5900485Abstract: Process for the manufacture of triazolone compounds and in particular nefazodone and intermediates useful in the manufacture thereof.Type: GrantFiled: October 15, 1997Date of Patent: May 4, 1999Assignee: Apotex, Inc.Inventors: Bo Lei, Tim Fat Tam, Khashayar Karimian, Rudolf Kubela
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Patent number: 5872119Abstract: The invention related to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z--Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sup.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.Type: GrantFiled: December 10, 1996Date of Patent: February 16, 1999Assignees: Institut National De La Sante et De La Recherche Medicale--INSERM, Societe Civile BrioprojetInventors: Camille-Georges Wermuth, Andre Mann, Fabrice Garrido, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Pierre Sokoloff
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Patent number: 5854245Abstract: Fibrinogen receptor antagonists having the structureX--Y--Z--A--Band pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g.Type: GrantFiled: June 26, 1997Date of Patent: December 29, 1998Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, George D. Hartman, Steven D. Young, Nathan C. Ihle
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Patent number: 5834471Abstract: Novel amide derivatives, processes for their preparation, and pharmaceutical compositions containing them are disclosed.Type: GrantFiled: February 2, 1996Date of Patent: November 10, 1998Assignee: SmithKline Beecham p.l.c.Inventors: David Malcolm Duckworth, Sarah Margaret Jenkins, Andrew John Jennings
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Patent number: 5807860Abstract: A compound represented by formula (I) and a salt thereof, and a hydrate and solvate thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent independently, for example, hydrogen atom, hydroxyl group, or C.sub.1-3 alkoxy group; R.sub.4 represents, for example, C.sub.1-7 alkyl group or C.sub.3-7 cycloalkyl group; R.sub.5 and R.sub.6 represent independently, for example, hydrogen atom or C.sub.1-3 alkyl group; Y represents C.sub.1-3 alkyl group, a heterocyclic group containing 1 to 4 nitrogen atoms and 5 or 6 ring-membered atoms, or C.sub.6-10 aryl group; k represents an integer of 1 to 3; and l represents an integer of 2 to 4. These urea compounds have excellent inhibitory activities against ACAT and are useful as active ingredients of medicines for preventive and/or therapeutic treatment of hyperlipemia and atherosclerosis.Type: GrantFiled: November 13, 1996Date of Patent: September 15, 1998Assignee: Mitsubishi Chemical CorporationInventors: Shinya Inoue, Masao Taniguchi, Yoshihiro Tarao, Kazuo Suzuki, Chizuko Takahashi, Mizue Kawai, Masayuki Mitsuka
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Patent number: 5807856Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.Type: GrantFiled: November 12, 1996Date of Patent: September 15, 1998Assignee: Merck & Co., Inc.Inventors: Marg G. Bock, Michael A. Patane
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Patent number: 5795890Abstract: A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.Type: GrantFiled: September 24, 1996Date of Patent: August 18, 1998Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Takahiko Nakae, Masashi Kato, Takehito Fujita, Kazuhito Kawabata, Hiroyuki Ohno
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Patent number: 5723475Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.Type: GrantFiled: October 28, 1996Date of Patent: March 3, 1998Assignee: Suntory LimitedInventors: Hirokazu Annoura, Mayumi Uesugi, Atsuko Fukunaga, Shigeki Tamura
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Patent number: 5710155Abstract: The invention relates to new arylglycinamide derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokin (tachykinin) antagonists.Type: GrantFiled: July 30, 1996Date of Patent: January 20, 1998Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5707994Abstract: The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.Type: GrantFiled: April 19, 1996Date of Patent: January 13, 1998Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yoshihara Ikeda, Yasuyuki Ueki, Hisakazu Kishimoto, Toshio Nishihara, Yumiko Kamikawa
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Patent number: 5688795Abstract: The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1;t is 0, 1 or 2;X is O, S or NR.sup.6 (in which R.sup.6 is hydro or (C.sub.1-6)alkyl);Y and Z are independently CH or N;R.sup.1 is hydro, hydroxy, halo, nitro, amino, cyano, (C.sub.1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C.sub.1-6)alkyl, (C.sub.3-6)cycloalkyl, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C.sub.1-4)alkyl, heteroaryl (C.sub.1-4)alkyl, (C.sub.1-6)alkyloxy, (C.sub.3-6)cycloalkyloxy, (C.sub.3-6)cycloalkyl (C.sub.1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C.sub.1-4)alkyloxy or heteroaryl (C.sub.1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano);R.sup.2 is hydro, hydroxy, halo, cyano, (C.sub.1-6)alkyl or (C.sub.Type: GrantFiled: November 8, 1994Date of Patent: November 18, 1997Assignee: Syntex (U.S.A.) Inc.Inventors: Jurg Roland Pfister, David Ernest Clarke, Todd Richard Elworthy, David John Morgans, Jr., David Bruce Repke, Eric Brian Sjorgren, Helen Yen-hui Wu
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Patent number: 5681954Abstract: A compound represented by formula (I): ##STR1## wherein Q represents an aryl group, a heterocyclic group, a diarylmethyl group, an aralkyl group composed of an aryl group and an alkylene group, an alkyl group or a cycloalkyl group, in which the aryl group, heterocyclic group, and the aryl moiety of the diarylmethyl group and aralkyl group may be substituted with one or more substituents; R represents a bicyclic, substituted, nitrogen-containing heterocyclic group or a substituted phenyl group, in which the nitrogen-containing heterocyclic group is composed of a 5-membered, substituted, aromatic or saturated ring containing one or two nitrogen atoms and a 6-membered ring; and Z represents an alkylene group, an alkenylene group, an alkylene group, a carbonyl group, an alkylene group containing a carbonyl group or an oxalyl group, or a salt thereof.Type: GrantFiled: April 4, 1995Date of Patent: October 28, 1997Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Kenjiro Yamamoto, Atsushi Hasegawa, Hideki Kubota, Masahiro Ando, deceased, Hitoshi Yamaguchi
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Patent number: 5672602Abstract: The present invention relates to substituted piperazine derivatives (herein referred to as compounds or compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.Type: GrantFiled: April 30, 1996Date of Patent: September 30, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Timothy P. Burkholder, Tieu-Binh Le, Elizabeth M. Kudlacz
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Patent number: 5637701Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.Type: GrantFiled: April 11, 1995Date of Patent: June 10, 1997Assignee: John Wyeth & Brother, LimitedInventor: Mark A. Ashwell
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Patent number: 5607953Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: November 23, 1994Date of Patent: March 4, 1997Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5607936Abstract: Disclosed are substituted aryl piperazines of Formula I ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.Type: GrantFiled: September 30, 1994Date of Patent: March 4, 1997Assignee: Merck & Co., Inc.Inventors: Yuan-Ching P. Chiang, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Daniel J. Miller, Sander G. Mills, Albert J. Robichaud, Shrenik K. Shah
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Patent number: 5541326Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.Type: GrantFiled: November 14, 1994Date of Patent: July 30, 1996Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5532242Type: GrantFiled: July 7, 1994Date of Patent: July 2, 1996Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5476850Abstract: There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.Type: GrantFiled: December 5, 1994Date of Patent: December 19, 1995Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz Gogelein, Joachim Kaiser
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Patent number: 5451584Abstract: The compounds ##STR1## where: R and R.sup.6 are members independently selected from the group consisting of H, CN, OR.sup.2, NO.sub.2, NR.sup.2 R.sup.3, NR.sup.2 COR.sup.3, NR.sup.2 COOR.sup.3, COR.sup.2, COOR.sup.2, CONR.sup.2 R.sup.3, SR.sup.2, SOR.sup.2, SO.sub.2 R.sup.2, SO.sub.2 NR.sup.2 R.sup.3, alkyl, alkenyl, alkynyl, perhaloalkyl, and a halogen;in which R.sup.2 and R.sup.3 are alkyl, alkenyl, alkynyl, phenyl, or benzyl;R.sup.4 is a member selected from the group consisting of H, alkyl, heteroalkyl, in which the hetero atom is oxygen, sulfur or nitrogen, alkenyl and alkynyl;R.sup.5 is alkynyl of 2 to 8 carbon atoms or 1-alkynylcycloalkyl in which the alkynyl group contains 2 to 6 carbon atoms and the cycloalkyl group contains 3 to 10 carbon atoms;or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents.Type: GrantFiled: November 10, 1994Date of Patent: September 19, 1995Assignee: American Home Products CorporationInventors: Reinhardt B. Baudy, Scott C. Berta
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Patent number: 5436244Abstract: Novel indanes in all possible stereoisomer forms of the formula ##STR1## wherein the substituents are as defined in the specification and their non-toxic, pharmaceutically acceptable acid addition salts and their hydrates having central analgesic properties as well as antiarrhythmic and diuretic activities.Type: GrantFiled: July 22, 1993Date of Patent: July 25, 1995Assignee: Roussel UclafInventors: Francois Clemence, Michel Fortin, Gilles Hamon, Odile Le Martret, Anne M. Moura
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Patent number: 5420278Abstract: Piperazine derivatives of formula ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula n is 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is an aryl or nitrogen containing heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is aryl, C.sub.4-8 alkyl or aryl(lower)alkyl and X is a functionalized group of specified meaning. The compounds exhibit activity as 5-HT.sub.1A antagonists and can be used, into alia, for the treatment of CNS disorders, such as anxiety.Type: GrantFiled: May 24, 1994Date of Patent: May 30, 1995Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5416212Abstract: An anilide compound represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represent an alkyl group having 1 to 4 carbon atoms; n represents 0, 1 or 2; A represents an alkylene group having 1 to 14 carbon atoms or a group represented by --CH.sub.2 CO--; and Ar represents a phenyl group, a phenyl group substituted with a halogen atom, a nitro group, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an alkanoyl group having 2 to 5 carbon atoms or a trifluoromethyl group, a benzyl group, a pyridyl group, a pyridyl group substituted with a halogen atom or a trifluoromethyl group, or a pyrimidyl group, or a salt thereof. The disclosed anilide compounds have potent ACAT inhibitory activity.Type: GrantFiled: June 20, 1994Date of Patent: May 16, 1995Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Masahiro Kawase, Akira Manaka, Yutaka Kawashima, Katsuo Hatayama
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Patent number: 5395835Abstract: Naphthalamides are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic agents and as agents for the treatment of disorders which respond to dopaminergic blockade including psychotic depression, substance abuse, and compulsive disorders.Type: GrantFiled: March 24, 1994Date of Patent: March 7, 1995Assignee: Warner-Lambert CompanyInventors: Shelly A. Glase, Suzanne R. Kesten, Lawrence D. Wise, Jonathan Wright
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Patent number: 5382583Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.Type: GrantFiled: December 29, 1992Date of Patent: January 17, 1995Assignee: John Wyeth & Brother, LimitedInventor: Ian A. Cliffe
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Patent number: 5356893Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.Type: GrantFiled: September 17, 1992Date of Patent: October 18, 1994Assignee: Glaxo Group LimitedInventors: John Bradshaw, John W. Clitherow, Ian B. Campbell
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Patent number: 5352677Abstract: Cinnamamide derivatives and the salts thereof are provided. An antihyperlipidemic composition is also provided. The composition comprises an active ingredient which is at least one selected from the group consisting of the above-mentioned cinnamamide derivative and the pharmaceutically acceptable salt thereof.Type: GrantFiled: July 15, 1992Date of Patent: October 4, 1994Assignee: Kanegafuchi Kagaku Kogyo Kabushiki KaishaInventors: Yoshihide Fuse, Kenji Fujii, Keiji Kameyama, Taizo Kawabe, Toshiaki Miwa, Ikuo Katsumi