Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 544/400)
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Publication number: 20030045478Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.Type: ApplicationFiled: December 14, 2001Publication date: March 6, 2003Inventors: Yongxin Han, Renee Aspiotis, Andre Giroux, Erich L. Grimm, Christophe Mellon, Robert Zamboni, Christopher I. Bayly
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Patent number: 6525036Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.Type: GrantFiled: January 5, 2001Date of Patent: February 25, 2003Assignee: Merck & Co., Inc.Inventors: Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
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Patent number: 6515024Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 11, 2001Date of Patent: February 4, 2003Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Publication number: 20020198378Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: ApplicationFiled: December 11, 2001Publication date: December 26, 2002Applicant: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6498162Abstract: 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 in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: November 1, 2000Date of Patent: December 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Kurt Schromm, Horst Dollinger, Birgit Jung, Georg Speck
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Patent number: 6495681Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.Type: GrantFiled: October 17, 2000Date of Patent: December 17, 2002Assignee: Theravance Inc.Inventors: Sabine M. Axt, Timothy J. Church, Witold Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
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Publication number: 20020183260Abstract: Compounds of the formula 1Type: ApplicationFiled: May 9, 2002Publication date: December 5, 2002Inventor: Cynthia Anne Fink
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Publication number: 20020137743Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: October 31, 2001Publication date: September 26, 2002Inventors: Jing Wu, Eugene D. Thorsett, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Varghese John, Lawrence Y. Fang, James E. Audia
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Patent number: 6451798Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: February 22, 2001Date of Patent: September 17, 2002Assignee: CV Therapeutics, Inc.Inventors: Vaibhav Varkhedkar, Venkata P. Palle, Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn
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Publication number: 20020123493Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: September 5, 2002Inventors: Michael Mullican, David Lauffer
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Publication number: 20020107241Abstract: The present invention relates N-heterocyclic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 8, 2002Inventors: David Lauffer, Brian Ledford, Michael Mullican
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Publication number: 20020103190Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 1, 2002Inventors: David Lauffer, Michael Mullican
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Publication number: 20020103205Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) 1Type: ApplicationFiled: July 11, 2001Publication date: August 1, 2002Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
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Patent number: 6403585Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 8, 2000Date of Patent: June 11, 2002Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6395737Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.Type: GrantFiled: December 28, 1999Date of Patent: May 28, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
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Patent number: 6380358Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.Type: GrantFiled: December 1, 1999Date of Patent: April 30, 2002Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Konrad Feichtinger, Todd T. Romoff
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Publication number: 20020045626Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: October 11, 2001Publication date: April 18, 2002Applicant: Neurogen CorporationInventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Publication number: 20020042376Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: January 16, 2001Publication date: April 11, 2002Inventors: Donald S. Karanewsky, Robert J. Ternansky, Steven D. Linton, Thang Dinh
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020025934Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: ApplicationFiled: December 4, 2000Publication date: February 28, 2002Applicant: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 6339087Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonist, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 20, 1998Date of Patent: January 15, 2002Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6337398Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 13, 1995Date of Patent: January 8, 2002Assignee: G.D. Searle & Co.Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6335444Abstract: A process for preparing a 2-acylamino alcohol derivative which comprises (A) reacting an aminopropanol derivative represented by the following formula (1): Y—CH2—C*H (NHP1)—C*H(OH)—R1 (1) with an amine represented by R2H to synthesize an amino alcohol derivative represented by the following formula (2): R2—CH2—C*H(NHP1)—C*H(OH)—R1 (2) (B) leaving P1 from said amino alcohol derivative represented by formula (2) to synthesize an amino alcohol derivative represented by the following formula (3): R2—CH2—C*H(NH2)—C*H(OH)—R1 (3) (C) reacting said amino alcohol derivative represented by formula (3) with a carboxylic acid represented by R11COOH or a reactive derivative thereof to prepare a 2-acylamino alcohol derivative represented by the following formula (4): R2—CH2—C*H(NHCOR11)—C*H(OH)—R1 (4 ) wherein * represents an asymmetric carbon atom, and P1, R1, R2 and RType: GrantFiled: February 23, 1999Date of Patent: January 1, 2002Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Masayuki Jinbo, Hidekazu Oyamada, Jinichi Inokuchi
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Publication number: 20010047001Abstract: Novel compounds of the general formula: 1Type: ApplicationFiled: February 22, 2001Publication date: November 29, 2001Inventors: Vaibhav Varkhedkar, Venkata P. Palle, Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn
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Publication number: 20010041704Abstract: Novel compounds of the general formula: 1Type: ApplicationFiled: February 22, 2001Publication date: November 15, 2001Inventors: Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn, Tim Marquart, Prabha N. Ibrahim, Venkata P. Palle
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Patent number: 6291423Abstract: The invention concerns a complex comprising at least a lipid and at least a therapeutically active substance useful for transferring said substance into a target cell, characterised in that said lipid is of formula (I): in which: n1, n2, identical or different are whole numbers between 0 and 1; R1, R2, identical or different are: a) selected among the group consisting of a hydrogen atom and alkyl radicals with 1 to 6 carbon atoms optionally substituted, independently of one another, by a hydroxyl radical; or b) in one particular case for which n1=n2=1, R1 and R2 can form together a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); R3, R4, identical or different are alkyl radicals of 1 to 6 carbon atoms or can together form a divalent alkylene chain of 2 to 3 carbon atoms (C2-C3); m, p, identical or different are whole numbers between 1 and 10; R5, R6, identical or different are selected in the group consisting of radicals of formula: 1) R7 C(═O)—X— in which: X=NH, OType: GrantFiled: February 12, 1999Date of Patent: September 18, 2001Assignee: Transgene S.A.Inventors: Rainer Bischoff, Danis Heissler, Abdesslame Nazih
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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: 6274584Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (1): wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.Type: GrantFiled: July 19, 2000Date of Patent: August 14, 2001Assignee: Novo Nordisk A/SInventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Thøgersen
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Patent number: 6258851Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.Type: GrantFiled: October 8, 1999Date of Patent: July 10, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
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Patent number: 6255120Abstract: A combinatorial chemical library comprising a plurality of members of the Formula [S]—C(O)—L′-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L′-Z is a linker/compound residue. In this library, Z is and Y is —NR3R4 or —OR9. R3 and R4 are independently selected from the group consisting of H, alkyl, aralkyl, heteroarylalkyl, heterocycloalkyl, —CH(R5)CH(R6)OH, —CH(R5)C(O)NHR6 and —CH(R5)C(O)NHCH(R6)C(O)NHR7. R3 and R4 together are wherein X=O or NR8 and R9 is aryl, aralkyl or R7CH═CH(CH2){overscore (n)}. The combinatorial library can be optionally encoded with identifiers T′-L, which are covalently attached to the solid support. The methods of synthesizing such a library are described. The use of such library in assays to discover biologically active compounds is also disclosed.Type: GrantFiled: May 15, 1998Date of Patent: July 3, 2001Assignee: Pharmacopeia, Inc.Inventors: Roland Ellwood Dolle, III, Cullen Lee Cavallaro, Timothee Felix Herpin
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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: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6221898Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
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Patent number: 6211176Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 1, 1999Date of Patent: April 3, 2001Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6174887Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.Type: GrantFiled: February 20, 1998Date of Patent: January 16, 2001Assignee: Japan Tobacco Inc.Inventors: Junichi Haruta, Kazuhiko Sakuma, Yoshihiro Watanabe
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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: 6159979Abstract: Novel bicyclic aryl/bicyclic heterocyclic ring containing compounds having a combined 5HT.sub.1A, 5HT.sub.1B and 5HT.sub.1D receptor antagonistic activity are provided.Type: GrantFiled: October 15, 1999Date of Patent: December 12, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 6140501Abstract: Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds.The present invention related to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula ##STR1## in which R.sub.1 represents a --CONH.sub.2, --CN, --COOH, --COOM or --COOR.sub.3 group, M being an alkali metal and R.sub.3 being an alkyl radical having from 1 to 4 carbon atoms; andR.sub.2 represents a hydrogen atom or a group --COR.sub.4 or --R.sub.5, where R.sub.4 is chosen from the groups --OR.sub.6 or --R.sub.7, in whichR.sub.5 represents an allyl or alkylaryl radical,R.sub.6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, andR.sub.Type: GrantFiled: October 9, 1998Date of Patent: October 31, 2000Assignee: UCB, S.A.Inventors: Guy Duchene, Michel Deleers, Guy Bodson, Genevieve Motte, Francoise Lurquin
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Patent number: 6124296Abstract: The invention relates to new arylglycinamide derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1 and R.sup.2 together with the N to which they are bound form a ring of the formula ##STR2## wherein p is 2 or 3 andX denotes oxygen, N(CH.sub.2).sub.n R.sup.6 or CR.sup.7 R.sup.8,and R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, 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: October 29, 1997Date of Patent: September 26, 2000Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Horst Dollinger, Franz Esser, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6114325Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.Type: GrantFiled: October 22, 1998Date of Patent: September 5, 2000Assignee: Shiseido Co., Ltd.Inventors: Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima, Koji Kobayashi
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Patent number: 6103719Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: May 27, 1999Date of Patent: August 15, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
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Patent number: 6084098Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH;R.sub.1, R.sub.2 and R.sub.3 independently represent organic or inorganic substituents;R.sub.4 and R.sub.4 ' independently represent hydrogen, alkyl or form a ring with the atom to which they are attached;R.sub.5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R.sub.6 represents hydrogen or alkyl; or R.sub.5 and R.sub.6 form a ring together with the atoms to which they are attached; andR.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 independently represent hydrogen or alkyl,which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.Type: GrantFiled: February 26, 1999Date of Patent: July 4, 2000Assignee: Neurogen CorporationInventors: Renata Xavier Kover, Silva Terdjanian, Jennifer Tran, Andrew Thurkauf
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Patent number: 6072075Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.Type: GrantFiled: May 22, 1997Date of Patent: June 6, 2000Assignee: The Regents of the University of CaliforniaInventors: Murray Goodman, Konrad Feichtinger, Todd T. Romoff
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Patent number: 6057322Abstract: Compounds of the formula I ##STR1## and the pharmaceutically tolerated salts thereof, are described. A process for their preparation and their use as medicaments in cardiovascular diseases are also described.Type: GrantFiled: July 30, 1997Date of Patent: May 2, 2000Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6002002Abstract: The present invention provides novel hydroxylamine derivatives represented by the general formula: wherein:X is O, --NH, or a group of formula NR', wherein R and R' are independently selected from alkyl, cycloalkyl, phenylalkyl, phenyl optionally substituted with halo, haloalkyl,alkyl, alkoxy or nitro; and a N-containing heterocyclic ring;R.sup.1 is H or alkanoyl,R.sup.2 is H or hydroxy optionally acylated with alkanoyl, andR.sup.3 is a group of the formula --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected fromH, alkyl, and a group of the formula --CO--NH--R wherein R is as defined above, orwherein R.sup.4 and R.sup.5 when taken together form a 5- to 7-membered heterocyclic ring which may optionally contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl or phenylalkyl.Type: GrantFiled: May 13, 1998Date of Patent: December 14, 1999Assignee: Biorex Research & Development Co.Inventors: Laszlo Urogdi, Ede Marvanyos, Mihaly Barabas, Laszlo Jaszlits, Katalin Biro, Andrea Jednakovits, Erzsebet Radvanyne, Maria Kurthy, Istvanne Udvardy Nagy
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Patent number: 5981531Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --Gand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: May 29, 1998Date of Patent: November 9, 1999Assignee: Zeneca LimitedInventors: Andrew George Brewster, Peter William Rodney Caulkett, Alan Wellington Faull, Robert James Pearce, Richard Eden Shute
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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: 5962507Abstract: Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl having up to 17 carbon atoms.Type: GrantFiled: December 5, 1997Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5935958Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetyl-cholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.Type: GrantFiled: June 26, 1997Date of Patent: August 10, 1999Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Derek B. Lowe, Wei K. Chang, Sundeep Dugar