Three Or More Hetero Atoms In The Polycyclo Ring System Patents (Class 540/578)
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Patent number: 7329653Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.Type: GrantFiled: April 11, 2006Date of Patent: February 12, 2008Assignee: WyethInventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
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Patent number: 7297790Abstract: Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours, comprising drying crystals of mirtazapine hydrate; a crystal of a mirtazapine hydrate represented by the formula (I): wherein n is an integer of 1 to 5; and a process for preparing crystals of a mirtazapine hydrate, comprising crystallizing a crude mirtazapine using a water-soluble organic solvent and water. The anhydrous mirtazapine crystals can be suitably used, for instance, as an antidepressant.Type: GrantFiled: December 24, 2003Date of Patent: November 20, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Eiichi Iishi, Yoshiyuki Imamiya
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Publication number: 20070260057Abstract: The present invention is directed to novel processes for the preparation of fused pyrazole compounds, useful for the treatment of disorders and conditions mediated by serotonin receptor activity.Type: ApplicationFiled: May 4, 2007Publication date: November 8, 2007Inventors: Xiaohu Deng, Jimmy T. Liang, Neelakandha Mani
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Patent number: 7262302Abstract: The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: August 28, 2007Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb, D.O.O.Inventors: Mladen Mercep, Milan Mesic, Marina Modric, Dijana Pesic, Davor Kidemet
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Patent number: 7262190Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.Type: GrantFiled: December 8, 2005Date of Patent: August 28, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage, Laurence Danober
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Patent number: 7262189Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts Medicaments.Type: GrantFiled: December 20, 2002Date of Patent: August 28, 2007Assignee: Les Laboratoires ServerInventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Patent number: 7253163Abstract: Compounds of formula (I): wherein: R1 represents a heterocycle, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, their isomers, and also addition salts thereof.Type: GrantFiled: June 10, 2004Date of Patent: August 7, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alex Cordi, Pierre Lestagé
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Patent number: 7253161Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts. Medicaments.Type: GrantFiled: December 20, 2002Date of Patent: August 7, 2007Assignee: Les Laboratoires ServierInventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Patent number: 7211574Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: August 27, 2003Date of Patent: May 1, 2007Assignee: Schering CorporationInventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee, Thavalakulamgara K. Sasikumar
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Patent number: 7176195Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists.Type: GrantFiled: June 21, 2001Date of Patent: February 13, 2007Assignee: Ferring BVInventors: Doreen Ashworth, Gary R. W. Pitt, Peter Hudson, Christopher Yea, Richard J. Franklin, Graeme Semple, David Paul Jenkins
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Patent number: 7122545Abstract: The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R?, R?, X, R?? and n are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compound of formula I are adenosine receptor ligands with good affinity to the A1 and A3 receptors. These compounds have useful pharmaceutical activities.Type: GrantFiled: May 11, 2004Date of Patent: October 17, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 7105506Abstract: Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: May 2, 2002Date of Patent: September 12, 2006Assignee: Lilly Icos LLCInventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
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Patent number: 7105667Abstract: Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein which are useful in treating leukocyte activation-associated disorders.Type: GrantFiled: November 6, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb Co.Inventors: William J. Pitts, Joseph Barbosa, Junqing Guo
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Patent number: 7056910Abstract: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 27, 2001Date of Patent: June 6, 2006Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Koshio, Akio Kakefuda, Ippei Sato, Ryutaro Wakayama, Masanao Sanagi
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Patent number: 6951850Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: February 21, 2003Date of Patent: October 4, 2005Assignee: Pfizer, Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6916925Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.Type: GrantFiled: July 22, 2003Date of Patent: July 12, 2005Assignee: 3M Innovative Properties Co.Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
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Patent number: 6908926Abstract: Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.Type: GrantFiled: April 12, 2000Date of Patent: June 21, 2005Assignee: Novo Nordisk A/SInventors: Florencio Zaragoza Dörwald, Knud Erik Andersen, Tine Krogh Jørgensen, Bernd Peschke, Birgitte Schjellerup Wulff, Ingrid Pettersson, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Müller, Bernd Krist
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Patent number: 6852855Abstract: A novel process for preparing a compound of the formula I: wherein R1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R2 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R3 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy is disclosed. These compounds are useful in the synthesis of the antidepressant mirtazapine and other tetracyclic compounds.Type: GrantFiled: August 24, 2001Date of Patent: February 8, 2005Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Ben-Zion Dolitzky
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Publication number: 20040229862Abstract: The invention relates to 2-imidazo-benzothiazoles of general formula 1Type: ApplicationFiled: May 11, 2004Publication date: November 18, 2004Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6815440Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 3, 2003Date of Patent: November 9, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Publication number: 20040192670Abstract: The present invention relates to cyclic urea derivatives, their synthesis, and their use as &agr;v integrinreceptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;15 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, tumor growth and metastasis.Type: ApplicationFiled: March 11, 2003Publication date: September 30, 2004Inventors: John H Hutchinson, Aiwen Li
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Patent number: 6774230Abstract: The preparation of 1-(3-carboxypyridyl-2)-4-methyl-2-phenylpiperazine dihydrate and other mirtazapine intermediates are described. These compounds are particularly useful in the preparation of mirtazapine.Type: GrantFiled: February 14, 2002Date of Patent: August 10, 2004Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Leonid Metzger, Shlomit Wizel
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Patent number: 6770647Abstract: The present application describes to novel bicyclic hydroxamates derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, B1, B2, R1, and C are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: August 15, 2002Date of Patent: August 3, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan
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Publication number: 20040092503Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.Type: ApplicationFiled: August 19, 2003Publication date: May 13, 2004Inventors: Thomas Arrhenius, Jie Fei Cheng, Mark E Wilson, Rossy Serafimov
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Patent number: 6723845Abstract: Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours, comprising drying crystals of mirtazapine hydrate; a crystal of a mirtazapine hydrate represented by the formula (I): wherein n is an integer of 1 to 5; and a process for preparing crystals of a mirtazapine hydrate, comprising crystallizing a crude mirtazapine using a water-soluble organic solvent and water. The anhydrous mirtazapine crystals can be suitably used, for instance, as an antidepressant.Type: GrantFiled: January 7, 2003Date of Patent: April 20, 2004Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Eiichi Iishi, Yoshiyuki Imamiya
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Patent number: 6720316Abstract: The present invention provides compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.Type: GrantFiled: August 2, 2002Date of Patent: April 13, 2004Assignee: Pharmacia & Upjohn CompanyInventor: William W. McWhorter, Jr.
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Publication number: 20040048912Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: 1Type: ApplicationFiled: June 9, 2003Publication date: March 11, 2004Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
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Publication number: 20040034012Abstract: To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 27, 2003Publication date: February 19, 2004Inventors: Hiroyuki Koshio, Akio Kakefuda, Ippei Sato, Ryutaro Wakayama, Masanao Sanagi
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Patent number: 6686352Abstract: The present invention is a compound of formula wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl; R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2; m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A &agr;5 receptor binding sites.Type: GrantFiled: April 9, 2002Date of Patent: February 3, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
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Patent number: 6660730Abstract: Methods for producing anhydrous mirtazapine crystals that are either (1) substantially free of lower alcohol insolubles or (2) substantially free of residual solvent and have an average particle diameter of from 10 to 50 &mgr;m, are provided, and the resulting anhydrous mirtazapine crystals produced thereby, which are useful in pharmaceuticals.Type: GrantFiled: April 27, 2001Date of Patent: December 9, 2003Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Chiharu Maeda, Sadanobu Yoshikawa, Eiichi Iishi
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Patent number: 6653471Abstract: Disclosed are heterocyclic compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptor.Type: GrantFiled: August 6, 2001Date of Patent: November 25, 2003Assignee: Neurogen CorporationInventors: Daniel Yohannes, George Maynard, Jun Yuan, Linghong Xie, Kyungae Lee, Manuka Ghosh, George Luke, Xiaojun Liu, Arthur Nagal, Lawrence Vincent, Kevin Currie, Zhe-Quing Wang
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Publication number: 20030216378Abstract: The invention provides a compound of formula (I): 1Type: ApplicationFiled: January 6, 2003Publication date: November 20, 2003Inventor: Jian-min Fu
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Patent number: 6649604Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 23, 2002Date of Patent: November 18, 2003Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffrey A. Zablocki
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Patent number: 6642222Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.Type: GrantFiled: May 3, 2000Date of Patent: November 4, 2003Assignee: Abbott LaboratoriesInventors: William A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Patent number: 6638934Abstract: The present invention is directed to novel compounds represented by structural Formulas (I) and (I-a): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R4b, R5, R6, R7, R8, R9, n, and X are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep and sexual disorders, migraine and other conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: October 28, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, Ian S. Mitchell, Taekyu Lee, Wenting Chen
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Patent number: 6632809Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: December 12, 2001Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20030171357Abstract: Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.Type: ApplicationFiled: February 10, 2003Publication date: September 11, 2003Inventors: Deniele Fancelli, Valeria Pittala, Mario Varasi
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Patent number: 6603003Abstract: A novel method for the synthesis of piperazine and its derivatives of formula 1, wherein R is selected from hydrogen, or a lower alkyl group having 1 to 6 carbon atoms or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; R1 is selected from hydrogen, a methyl group, a phenyl group optionally substituted with an alkyl group having 1 to 6 carbon atoms, or a phenylalkyl group the alkyl of which has 1 to 4 carbon atoms; and R2 is selected from hydrogen, or a methyl group, or a fluoromethyl group; comprising the steps: a. reacting an ester of formula 11 with substituted or unsubstituted ethylenediamine of formula 7 to give 3,4-dehydropiperazine-2-one and its derivatives of formula 12, wherein R, R1, R2 are as defined above and R6 is a C1 to C4 linear or branched alkyl group; and b. reacting the 3,4-dehydro-piperazine-2-one and its derivatives of formula 12 with a reducing agent to yield the piperazine and its derivatives of formula 1.Type: GrantFiled: October 25, 2001Date of Patent: August 5, 2003Assignee: Sun Pharmaceutical Industries LTDInventors: Sonny Sebastian, Hetal Virendra Patel, Rajamannar Thennati
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Publication number: 20030087895Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: July 2, 2002Publication date: May 8, 2003Inventors: Frans Eduard Janssens, Joseph Elisabeth Leenaerts, Francois Maria Sommen, Dominique Louis Nestor Ghislaine Surleraux
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Publication number: 20030088094Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C.Type: ApplicationFiled: October 30, 2002Publication date: May 8, 2003Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
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Publication number: 20030078255Abstract: The present application describes 6-5, 6-6, or 6-7 heterobicycles of Formula I or pharmaceutically acceptable salt forms thereof: 1Type: ApplicationFiled: March 22, 2002Publication date: April 24, 2003Inventor: Donald Joseph Phillip Pinto
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Patent number: 6552189Abstract: Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours, comprising drying crystals of mirtazapine hydrate; a crystal of a mirtazapine hydrate represented by the formula (I): wherein n is an integer of 1 to 5; and a process for preparing crystals of a mirtazapine hydrate, comprising crystallizing a crude mirtazapine using a water-soluble organic solvent and water. The anhydrous mirtazapine crystals can be suitably used, for instance, as an antidepressant.Type: GrantFiled: January 10, 2002Date of Patent: April 22, 2003Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Eiichi Iishi, Yoshiyuki Imamiya
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Patent number: 6544979Abstract: This invention concerns the use of compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X—is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CHType: GrantFiled: March 15, 2000Date of Patent: April 8, 2003Assignee: Janssen Pharmaceuticals, N.V.Inventor: Henricus Johannes Matheus Snoeck
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Publication number: 20030055035Abstract: 1Type: ApplicationFiled: May 3, 2000Publication date: March 20, 2003Inventors: Willilam A. Carroll, Konstantinos A. Agrios, Robert J. Altenbach, Irene Drizin, Michael E. Kort
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Publication number: 20030055042Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: April 9, 2002Publication date: March 20, 2003Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
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Patent number: 6503899Abstract: The invention provides a compound of formula (I): wherein: R1-R5, m, n, p, and the bonds a and b represented by - - - have any of the values, specific values, or preferred values described in the specification; or a salt or solvate thereof. The invention also provides pharmaceutical compositions comprising such a compound, as well as intermediates and processes useful for preparing such a compound, and therapeutic methods including the administration of such a compound.Type: GrantFiled: July 6, 2001Date of Patent: January 7, 2003Assignee: Pharmacia & Upjohn CompanyInventor: Jian-min Fu
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Publication number: 20020198190Abstract: The present invention provides compounds of formula I: 1Type: ApplicationFiled: June 17, 2002Publication date: December 26, 2002Applicant: PHARMACIA & UPJOHN COMPANYInventors: Jackson B. Hester, Bruce N. Rogers, Eric Jon Jacobsen, Michael D. Ennis, Brad A. Acker, Susan L. Vander Velde, Kristine E. Frank
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Publication number: 20020198189Abstract: A method of treatment or prophylaxis of SSAO-mediated complications in mammals including humans, comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of Formula (I): 1Type: ApplicationFiled: November 9, 2001Publication date: December 26, 2002Inventors: Olivier Besencon, Rolf Olsson, Johan Ohman, Patrizia Caldirola
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Patent number: 6489323Abstract: The current invention relates to compounds of Formula I pharmaceutical compositions and methods of use as nitric oxide synthase inhibitors, wherein the substituents are defined in the application.Type: GrantFiled: June 10, 1999Date of Patent: December 3, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., R. Keith Webber, E. Ann Hallinan, Mihaly V. Toth, Barnett S. Pitzele, Alok K. Awasthi, Alan E. Moormann, Suzanne Metz, Jeffery S. Snyder, William M. Moore, Jeffrey A. Scholten
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Patent number: 6448270Abstract: Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as cerebral ischemia, central nervous system trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headaches, convulsions, aminoglycoside antibiotics-induced hearing loss, chronic pain, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, urinary incontinence and neurodegenerative disorders such as lathyrism, Alzheimers' Disease, Parkinsonism, and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.Type: GrantFiled: June 13, 2000Date of Patent: September 10, 2002Assignees: Warner-Lambert Company, Cocensys, IncorporatedInventors: Christopher F. Bigge, Jonathan Wright, Sui Xiong Cai, Eckard Weber, Richard Woodward, Nancy C. Lan, Zhang-Lin Zhou, John F.W. Keana