The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Patent number: 6586423Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: February 1, 2002Date of Patent: July 1, 2003Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, George D. Hartman, Peter J. Manley, Randall W. Hungate, Leonard Rodman
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Publication number: 20030119817Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: January 17, 2002Publication date: June 26, 2003Inventors: Anita Mehta, Sudershan K. Arora, Biswajit Das, Abhijit Ray, Sonali Rudra, Ashok Rattan
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Publication number: 20030119849Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, -Z represents —C, ═C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy,and salts and prodrugs thereof. It has been found that these compounds have interesting pharmacological properties due to a combination of (partial) agonism towards the members of the dopamine D2-receptor subfamily and affinity for relevant serotonin and/or noradrenergic receptors.Type: ApplicationFiled: October 15, 2002Publication date: June 26, 2003Inventors: Roelof W. Feenstra, Johannes A.M. van der Heijden, Cornelis G. Kruse, Stephen K. Long, Gustaaf J.M. van Scharrenburg
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Patent number: 6583141Abstract: The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; —A1═A2—A3═A4— is a pyridinylidene, pyridazinylidene, pyrimidinylidene, pyrazinylidene or phenylidene; B represents an amide, ketone or oxadiazole; D represents Ar or Het; Q represents a covalent direct bond or a ketone, —N—, —O—, —CR5R6—, amide ethenyl, imine, sulfonyl, sulfinyl, 3-oxobutenyl, pyrazole, isoxazole or thiazole; L represents Ar or Het; R1 represents hydrogen, halo, hydroxy, C(2-6)alkenyl, C(2-6)alkynyl, C(3-6)cycloalkyl, C(3-6)cycloalkenyl, cyano, guanidine, nitro, NR17R18, an optionally substituted C(1-6)alkyl or C(1-6)alkyloxy; R2 and R3 each independently represent hydrogen, halo, C(1-6)alkyloxy or an optionally substituted C(1-6)alkyl; R5 and R6 each independently represent hydrogen, hydroxy, halo, an optionally substituted C(1-6)alkyl, C(2-6)alkenyl, C(2-6)alkynyl, C(3-Type: GrantFiled: April 6, 2001Date of Patent: June 24, 2003Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, José Ignacio Andrés-Gil, Frederik Dirk Deroose, Davy Petrus Franciscus Maria Petit, Maria Encarnacion Matesanz-Ballesteros, Rosa Maria Alvarez Escobar
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Patent number: 6579880Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of IL-8 and are thus useful as anti-inflammatory agents for a variety of diseases.Type: GrantFiled: June 6, 2001Date of Patent: June 17, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michele A. Weidner-Wells, Todd C. Henninger, Dennis J. Hlasta
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Patent number: 6576630Abstract: The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.Type: GrantFiled: March 15, 2000Date of Patent: June 10, 2003Assignee: AXYS Pharmaceuticals, Inc.Inventors: John O. Link, Arnold J. Martelli, Valeri Martichonok, John W. Patterson, Oliver L. Saunders, Sheila Zipfel
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Patent number: 6573262Abstract: The invention comprises substituted indoleoxoacetic piperazine derivatives of general Formula I, compositions thereof and their use as antiviral agents, and particularly for treating HIV infection.Type: GrantFiled: December 19, 2001Date of Patent: June 3, 2003Assignee: Bristol-Myers Sqibb CompanyInventors: Owen B. Wallace, Tao Wang, Kap-Sun Yeung, Bradley C. Pearce, Nicholas A. Meanwell, Zhilei Qiu, Haiquan Fang, Qiufen May Xue, Zhiwei Yin
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Publication number: 20030100567Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: ApplicationFiled: June 19, 2002Publication date: May 29, 2003Inventors: Mark T. Bilodeau, George D. Hartman
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Publication number: 20030073672Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.Type: ApplicationFiled: September 5, 2001Publication date: April 17, 2003Inventors: J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Yin Gu, Darin J. Gustin, Lars Karlsson, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Siquan Sun, Kevin L. Tays, Robin L. Thumond, Jianmei Wei
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Publication number: 20030069252Abstract: The use of CCR5 antagonists of the formula 1Type: ApplicationFiled: January 30, 2002Publication date: April 10, 2003Inventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
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Patent number: 6521621Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; p is 1 or 2; ═Q is ═O or ═NR3; X is a covalent bond or a bivalent radical of formula —O—, —S—, —NR3—; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl, wherein each C1-6alkyl group is optionally substituted with hydroxy, C1-4alkyloxy, oxo or a ketalized oxo substituent; R2 is Ar2, Ar2C1-6alkyl, Het1 or Het1C1-6alkyl; R3 is hydrogen or C1-6alkyl; L is hydrogen; Ar3; C1-6alkyl; C1-6alkyl substituted with 1 or 2 substituents selected from hydroxy, C1-6alkyloxy, Ar3, Ar3C1-6alkyloxy and Het2; C3-6alkenyl; Ar3C3-6alkenyl; di(Ar3)C3-6alkenyl or a radical of formula (a-1), (a-2), (a-3), (a-4) or (a-5); Ar1, Ar2 and Ar3 are each phenyl or substituted phenyl; Het1 and Het2 are each monocyclic or a bicyclic heterocycles; as substancType: GrantFiled: December 22, 2000Date of Patent: February 18, 2003Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: 6495549Abstract: Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.Type: GrantFiled: October 30, 2000Date of Patent: December 17, 2002Assignee: Pfizer IncInventors: Martin J. Wythes, Michael J. Palmer, Mark I. Kemp, Malcolm C. MacKenny, Robert J. Maguire, James F. Blake, Jr.
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Publication number: 20020177595Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: ApplicationFiled: March 27, 2002Publication date: November 28, 2002Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
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Patent number: 6465456Abstract: This invention describes isoxazolinone derivatives which possess antibacterial activity and are useful in the treatment of bacterial diseases. More particularly, new isoxazolinones are provided having the general formula I wherein R1, R2, R3, L and L1 are as described in the specification.Type: GrantFiled: June 28, 2001Date of Patent: October 15, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Dane M. Springer, Jason T. Goodrich, Zhaoxing Meng, Lawrence B. Snyder
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Patent number: 6458790Abstract: Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: March 20, 2001Date of Patent: October 1, 2002Assignee: Merck & Co., Inc.Inventors: Brenda L. Palucki, Khaled J. Barakat, Liangqin Guo, Yingjie Lai, Ravi P. Nargund, Min K. Park, Patrick G. Pollard, Iyassu K. Sebhat, Zhixiong Ye
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Patent number: 6455529Abstract: Compounds of the formula I in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.Type: GrantFiled: May 3, 1996Date of Patent: September 24, 2002Assignee: Merck Patent Gesellschaft mit beschraenkter HaftungInventors: Joachim Gante, Hörst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 6444677Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y1 is —(CH2)m—, C(O) or S(O); Y2 is N or CH; R1 and R2 are independently C1-4 alkyl; R3 is selected from the following: (a) optionally substituted —(CH2)p—C3-7 cycloalkyl; (b) optionally substituted —C5-7 alkyl; and (c) substituted —C1-4 alkyl; and (d) optionally substituted C7-9 bicycloalkyl; R4 is optionally substituted thiazolyl, imidazolyl or oxazolyl; X is S, —NH, —N—C1-4 alkyl or O; R5 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl or halo; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or S; and p is 0, 1, 2, 3, 4, 5 or 6. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.Type: GrantFiled: December 7, 2000Date of Patent: September 3, 2002Assignee: Pfizer Inc.Inventors: Takafumi Ikeda, Mitsuhiro Kawamura, Noriaki Murase, Seiji Nukui, Yuji Shishido, Makato Kawai, Yoshiyuki Okumura
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Publication number: 20020119983Abstract: The present invention relates to a novel isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptors represented by the following formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent, 1Type: ApplicationFiled: April 23, 2001Publication date: August 29, 2002Inventors: Hun Yeong Koh, Kyung II Choi, Yong Seo Cho, Ae Nim Pae, Kyung Ho Kang, Mi Young Cha, Jae Yang Kong, Dae Young Jeong, Hee-Yoon Lee
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Publication number: 20020103186Abstract: The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effec number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: ApplicationFiled: July 16, 2001Publication date: August 1, 2002Inventors: Anita Mehta, Sudershan K. Arora, Biswajit Das, Abhijit Ray, Sonali Rudra, Ashok Rattan
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Publication number: 20020065274Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: ApplicationFiled: November 28, 2001Publication date: May 30, 2002Inventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck,, David Lee Varie
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Publication number: 20020061890Abstract: This invention concerns compounds of formula 1Type: ApplicationFiled: November 19, 2001Publication date: May 23, 2002Inventors: Raymond Antoine Stokbroekx, Marc Andre Ceusters, Marcel Jozef Maria Van der Aa, Marcel Gerebernus Maria Luyckx, Marc Willems, Robert W. Tuman
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Patent number: 6391865Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.Type: GrantFiled: May 1, 2000Date of Patent: May 21, 2002Assignee: Schering CorporationInventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Eric Gilbert, Marc A. Labroli
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Publication number: 20020058666Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: August 29, 2001Publication date: May 16, 2002Applicant: Neurogen CorporationInventor: Xiao Shu He
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Patent number: 6384030Abstract: The present invention concerns novel compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein L represent a radical of formula wherein each Alk independently represents an optionally substituted C1-6alkanediyl; is 1, 2 or 3; Y is O, S or NR2; R1 represents hydrogen, aryl, Het1, or an optionally substituted C1-6alkyl; each R2 independently represents hydrogen or C1-6alkyl; or in case R1 and R2 are attached to the same nitrogen atom, they may be taken together to form a heterocyclic radical; or they may be taken together to form an azido radical; each R3 independently represents hydrogen, hydroxy or C1-4alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; Het1 represents an optionally substituted monocyclic or bicyclic heterocyclic radical; Het2 is the same as Het1 and may also be piperazinylType: GrantFiled: November 9, 2000Date of Patent: May 7, 2002Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Jan Heeres, Frank Christopher Odds
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Patent number: 6384035Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.Type: GrantFiled: October 9, 1998Date of Patent: May 7, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard H. Hutchings, Haripada Khatuya, Gee-Hong Kuo, Xiaobing Li, William V. Murray, Catherine Prouty, Frank Villani, Nelson C. F. Yim, Cynthia Maryanoff
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Publication number: 20020042421Abstract: This invention provides a compound of the formula (I): 1Type: ApplicationFiled: September 27, 2001Publication date: April 11, 2002Inventors: Yoshiyuki Okumura, Mitsuhiro Kawamura, Makato Kawai, Noriaki Murase, Takafumi Ikeda
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Patent number: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6355643Abstract: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.Type: GrantFiled: March 1, 2000Date of Patent: March 12, 2002Assignee: Merck & Co., Inc.Inventors: William C. Lumma, John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Christopher J. Dinsmore, Jeffrey M. Bergman
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Publication number: 20020013323Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of oxadiazole, thiadiazole and thiadiazole oxide derivatives of dihydropyridines of Formula I.Type: ApplicationFiled: July 2, 2001Publication date: January 31, 2002Inventors: Graham S. Poindexter, Mendi Higgins, James Guy Breitenbucher
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Publication number: 20010049370Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I.Type: ApplicationFiled: April 24, 2001Publication date: December 6, 2001Inventor: Sing-Yuen Sit
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Publication number: 20010047002Abstract: A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I).Type: ApplicationFiled: April 24, 2001Publication date: November 29, 2001Inventors: Sing-Yuen Sit, Graham S. Poindexter
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Publication number: 20010046993Abstract: This invention provides a compound of the formula (I): 1Type: ApplicationFiled: December 7, 2000Publication date: November 29, 2001Inventors: Takafumi Ikeda, Mitsuhiro Kawamura, Noriaki Murase, Seiji Nukui, Yuji Shishido, Makato Kawai, Yoshiyuki Okumura
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Patent number: 6284759Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substitutedamino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further defined herein, 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: September 30, 1999Date of Patent: September 4, 2001Assignee: Neurogen CorporationInventor: Xiao Shu He
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Patent number: 6239134Abstract: The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.Type: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: American Home Products Corp.Inventors: Annmarie L. Sabb, Robert L. Vogel, Michael G. Kelly, Yvette L. Palmer, Wayne E. Childers
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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: 6211183Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 3, 2001Assignee: COR Therapeutics, Inc.Inventors: Charles K. Marlowe, Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6204268Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: March 20, 2001Assignee: COR Therapeutics, INCInventors: Robert M. Scarborough, Bing-Yan Zhu, Ting Su
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Patent number: 6197772Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 3, 1998Date of Patent: March 6, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Frans Eduard Janssens, François Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux, Joseph Elisabeth Leenaerts, Yves Emiel Maria Van Roosbroeck
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Patent number: RE37886Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: August 23, 2001Date of Patent: October 15, 2002Assignee: Janssen Pharmaceuticals, N.V.Inventors: Frans E. Janssens, François M. Sommen, Dominique L. N. G. Surleraux, Joseph E. Leenaerts, Yves E. M. Van Roosbroeck