1,4-diazine Ring Patents (Class 544/120)
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Publication number: 20090012062Abstract: The present invention concerns aryl and heteroaryl substituted pyrazinone derivatives having antagonistic melanin-concentrating hormone (MCH) activity, in particular MCH-1 activity according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of psychiatric disorders, including but not limited to anxiety, eating disorders, mood disorders, such as bipolar disorders and depression, psychoses, such as schizophrenia, and sleeping disorders; obesity; diabetes; sexual disorders and neurological disorders.Type: ApplicationFiled: December 18, 2006Publication date: January 8, 2009Inventors: Jose Ignacio Andres-Gil, Manuel Jesus Alcazar-Vaca, Rosa Maria Alvarez-Escobar, Julen Oyarzabal Santamarina, Frank Matthias Dautzenberg, Jacqueline Macritchie, Donald Simpson, Sonia Martinez Gonzalez
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Patent number: 7459554Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.Type: GrantFiled: October 14, 2004Date of Patent: December 2, 2008Assignee: OSI Pharmaceuticals, Inc.Inventors: Han-Qing Dong, Kenneth Foreman, Mark Joseph Mulvihill, Anthony Innocenzo Nigro, Arno G. Steinig, Douglas Werner, Robin Wilkes
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Publication number: 20080293708Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising themType: ApplicationFiled: August 26, 2005Publication date: November 27, 2008Inventors: Eiji Kawahara, Takahiro Miyake, Johannes Roesel
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Patent number: 7442699Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: August 24, 2005Date of Patent: October 28, 2008Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
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Publication number: 20080207613Abstract: A compound of the general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof, wherein A represents a variety of six membered nitrogen containing heterocyclic rings, Q is a bond, halogen, C1-4 alkyl, O, S, SO2, CO or CS and X1, X2, X3 and X4 are optionally substituted by 9 specific substituents or one can be nitrogen. Compositions comprising a carrier and at least one compound of formula (I) are also provided. Further provided are methods of treating tyrosine kinase-associated disease states by administering a compound of formula (I) and methods of suppressing the immune system of a subject by administering a compound of formula (I).Type: ApplicationFiled: January 12, 2005Publication date: August 28, 2008Applicant: CYTOPIA RESEARCH PTY LTDInventors: Michelle Leanne Styles, Jun Zeng, Herbert Rudolf Treutlein, Andrew Frederick Wilks, Marcel Robert Kling, Christopher John Burns, Xianyong Bu
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Publication number: 20080194583Abstract: Compounds of general formula (I), (II) (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: ApplicationFiled: December 3, 2004Publication date: August 14, 2008Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino, Collette Gloria Kewdale
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Publication number: 20080167305Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: March 18, 2008Publication date: July 10, 2008Inventors: Dean Wilson, Lev T.D. Fanning, Paul Krenitsky, Andreas Termin, Pramod Joshi, Urvi Sheth
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Publication number: 20080125410Abstract: The invention concerns compounds of general formula (I): Wherein n, X, Y, R1 and R2 are as defined herein. The invention also concerns a method for preparing the compounds and their therapeutic use.Type: ApplicationFiled: October 17, 2007Publication date: May 29, 2008Applicant: SANOFI-AVENTISInventors: Jacques Froissant, Frank Marguet, Anne Olivier-Bandini, Frederic Puech
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Patent number: 7317010Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and B are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.Type: GrantFiled: August 18, 2003Date of Patent: January 8, 2008Assignee: AstraZeneca ABInventor: Jean Claude Arnould
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Publication number: 20080004253Abstract: Certain TRPV1-modulating thiazolopyrimidine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: June 28, 2007Publication date: January 3, 2008Inventors: Bryan James Branstetter, James Guy Breitenbucher, Alec D. Lebsack, Wei Xiao
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Publication number: 20070270423Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases which are associated with the modulation of histamine 3 (H3) receptors.Type: ApplicationFiled: April 26, 2007Publication date: November 22, 2007Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Patent number: 7265108Abstract: Compounds represented by the following general formula: [wherein X1, X2, X3 and X4 each independently represent a single bond, C1-6 alkylene, etc.; A2 represents optionally substituted phenyl, etc.; A1 represents an optionally substituted 5- to 7-membered heterocyclic group containing —C(=Q1)- (wherein Q1 represents oxygen, sulfur or ?N—R11 (wherein R11 represents hydrogen or C1-6 alkyl)) and nitrogen, etc.; and Z1 represents piperidin-diyl, etc.], salts thereof and hydrates of the foregoing.Type: GrantFiled: July 1, 2005Date of Patent: September 4, 2007Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Mutsuko Ono, Koki Kawano, Yoshihiko Norimine, Tatsuhiro Onogi, Takashi Yoshinaga, Kiyoaki Kobayashi, Hiroyuki Suzuki, Hiroe Minami, Kohei Sawada
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Patent number: 7179807Abstract: Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula: The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.Type: GrantFiled: August 20, 2003Date of Patent: February 20, 2007Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Stéphane De Lombaert, Raymond F. Horvath, Dario Doller, Kevin J. Hodgetts, Lu Yan Zhang, Bernd Kaiser, Xuechun Zhang, Yasuchika Yamaguchi, Cunyu Zhang, Jim Darrow
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Patent number: 7122544Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: December 4, 2001Date of Patent: October 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
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Patent number: 7064201Abstract: Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1?, R1?, R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.Type: GrantFiled: August 1, 2003Date of Patent: June 20, 2006Assignee: Nereus Pharmaceuticals, Inc.Inventors: Yoshio Hayashi, Michael A. Palladino, Jr., Jennifer Grodberg
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Patent number: 7060822Abstract: Chemical compounds having structural formula I and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.Type: GrantFiled: July 24, 2000Date of Patent: June 13, 2006Assignee: Abbott GmbH & Co. KGInventors: Lee Arnold, Marina Moran Moset, Jose Maria Castellano Berlanga, Isabel Fernandez, David J. Calderwood, Paul Rafferty
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Patent number: 6995161Abstract: Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.Type: GrantFiled: February 16, 2001Date of Patent: February 7, 2006Assignee: Neurogen CorporationInventors: Taeyoung Yoon, Ping Ge, Raymond F. Horvath, Stephane DeLombaert, Kevin J. Hodgetts, Dario Doller, Cunyu Zhang
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Patent number: 6943196Abstract: An NF-?B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R4 is H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 19, 1999Date of Patent: September 13, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Yoichi Nunokawa, Kenji Suzuki, Masayuki Saitoh
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Patent number: 6908919Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: July 15, 2002Date of Patent: June 21, 2005Assignee: Pharmacia CorporationInventors: Michael S. South, Brenda L. Case, Thomas A. Dice, Ricky L. Fenton, Gary W. Franklin, Michael J. Hayes, Horng-Chih Huang, Wei Huang, Darin E. Jones, Carrie L. Kusturin, Richard J. Lindmark, Scott A. Long, William L. Neumann, David B. Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Matthew W. Mahoney, John J. Parlow, Melvin L. Rueppel
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6875764Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.Type: GrantFiled: October 27, 2000Date of Patent: April 5, 2005Assignee: New Pharma Research Sweden ABInventors: Sabrina Muzi, Shoaá Abdul Rahman
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6835832Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: December 28, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Publication number: 20040220403Abstract: A compound of the formula (I): wherein in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.Type: ApplicationFiled: June 30, 2003Publication date: November 4, 2004Inventors: Kazuhiko Take, Chiyoshi Kasahara, Shinji Shigenaga, Hidenori Azami, Yoshiteru Eikyu, Kazuo Nakai, Masataka Morita
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Patent number: 6774127Abstract: Novel pyridyl and pyrimidinyl substituted pyrazole and pyrazoline compounds and compositions for use in therapy.Type: GrantFiled: February 19, 2003Date of Patent: August 10, 2004Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Timothy Gallagher, Irennegbe Kelly Osifo
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Patent number: 6756377Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2 and R3 are as described in the specification, which compounds are ligands to the serotonin 5-HT2c receptor.Type: GrantFiled: November 19, 2001Date of Patent: June 29, 2004Assignee: Biovitrum ABInventors: Björn M. Nilsson, Martin Scobie
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Publication number: 20040110756Abstract: The invention relates to new anthracene derivatives of the general Formula 1 and to their synthesis and use as pharmaceutical preparations, especially for the treatment of a tumor.Type: ApplicationFiled: July 17, 2003Publication date: June 10, 2004Inventors: Peter Emig, Eckhard Gunther, Beate Aue, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt
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Publication number: 20040097730Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C 1-4 alkyl, 4) C 3-7 cycloalkyl, 5) CF3, 6) OCF3, 7) C 1-4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3.Type: ApplicationFiled: August 1, 2003Publication date: May 20, 2004Inventors: Mary Beth Young, Philippe G. Nantermet, Harold G. Selnick, Peter D. Williams
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Publication number: 20040082589Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 1Type: ApplicationFiled: October 23, 2003Publication date: April 29, 2004Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Marie Gerard
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Publication number: 20040077647Abstract: Disclosed are compounds of formula (I): 1Type: ApplicationFiled: August 1, 2003Publication date: April 22, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S. Riska, Christopher Pargellis
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Publication number: 20040072840Abstract: The invention relates to the compounds of formula: 1Type: ApplicationFiled: September 16, 2003Publication date: April 15, 2004Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
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Patent number: 6713472Abstract: A compound which is a chymase inhibitor and which is represented by a formula [I] and salts thereof. In the formula [I], X is R6—(A2)n—N, R1 and R2 are H, alkyl, cycloalkyl or aryl, R3 and R4 are H, alkyl, cycloalkyl, aryl or aromatic heterocycle, R5 is H, alkyl, cycloalkyl, aryl or —A3—A4—R7, R6 is H, alkyl, cycloalkyl, OH, alkoxy, aryl, aryloxy or an aromatic heterocycle, R7 is H, alkyl, OH, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle, A1 is alkylene, A2 is carbonyl or sulfonyl, A3 is alkylene, A4 is carbonyl or oxalyl and n is o or 1.Type: GrantFiled: January 18, 2002Date of Patent: March 30, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Eiko Matsumoto
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Patent number: 6710048Abstract: The present invention provides pyrazine derivatives that inhibit tyrosine kinase activity. Certain pyrazine derivatives are selective inhibitors of vascular endothelial growth factor (VEGF) receptor tyrosine kinase. The present invention also provides pharmaceutical formulations containing the pyrazine derivatives and methods of use of these formulations as anti-tumor agents and to treat solid-tumor cancers, angiogenesis, diabetic retinopathy, rheumatoid arthritis, endometriosis and psoriasis.Type: GrantFiled: September 19, 2001Date of Patent: March 23, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Gee-Hong Kuo, Peter J. Connolly, Catherine Prouty, Alan DeAngelis, Aihua Wang, Linda Jolliffe, Steve Middleton, Stuart Emanuel
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Patent number: 6706021Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: March 27, 2003Date of Patent: March 16, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6699856Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.Type: GrantFiled: July 25, 2002Date of Patent: March 2, 2004Assignee: Merck & Co., Inc.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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Publication number: 20040034219Abstract: This invention provides new benzothiophene derivatives of general formula (I) and a process for preparing them, the corresponding compositions and their use for manufacturing a medicine for the treatment of neurological disorders. These new compounds behave as serotonin reuptake inhibitors and show high affinity towards the 5-HT1A receptor.Type: ApplicationFiled: May 27, 2003Publication date: February 19, 2004Inventors: Marisabel Mourelle Mancini, Juan Carlos Del Castillo Nieto, Berta Esperanza Lasheras Aldaz, Antonio Monge Vega, Joaquin Del Rio Zambrana
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Publication number: 20040029876Abstract: This invention relates to novel acylamino cyclopropane derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as modulators of dopamine D3 receptors and for the treatment of anxiety, psychosis, substance abuse, Parkinson's disease, sexual dysfunction, and other central nervous system disorders.Type: ApplicationFiled: July 29, 2003Publication date: February 12, 2004Applicant: Pfizer IncInventors: Anton F. J. Fliri, Anthony R. Reinhold
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Publication number: 20040009970Abstract: Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: 1Type: ApplicationFiled: April 24, 2003Publication date: January 15, 2004Applicant: WyethInventor: P. Sivaramakrishnan Ramamoorthy
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Publication number: 20040002604Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: ApplicationFiled: June 17, 2003Publication date: January 1, 2004Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
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Publication number: 20030236402Abstract: Compounds represented by formula I: 1Type: ApplicationFiled: July 25, 2002Publication date: December 25, 2003Applicant: Merck Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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Publication number: 20030236403Abstract: Disclosed are compounds of formula I: 1Type: ApplicationFiled: November 25, 2002Publication date: December 25, 2003Applicant: Molecular Geriatrics CorporationInventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
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Publication number: 20030236247Abstract: Compounds having the formula 1Type: ApplicationFiled: March 21, 2003Publication date: December 25, 2003Inventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Publication number: 20030232807Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: ApplicationFiled: October 4, 2002Publication date: December 18, 2003Inventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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Publication number: 20030232788Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as 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: February 7, 2003Publication date: December 18, 2003Applicant: Idun Pharmaceuticals, Inc.Inventors: Donald S. Karanewsky, Vincent J. Kalish, Edward D. Robinson, Brett R. Ullman
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Patent number: 6664255Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: May 18, 2000Date of Patent: December 16, 2003Assignee: Pharmacia CorporationInventors: Michael South, John J. Parlow, Darin E. Jones, Brenda Case, Tom Dice, Richard Lindmark, Michael J. Hayes, Melvin L. Rueppel, Horng-Chih Huang, Wei Huang, Scott A. Long, Matthew Mahoney, William L. Neumann, David Reitz, John I. Trujillo, Ching-Cheng Wang, Rhonda Wood, Qingping Zeng, Rick Fenton, Gary W. Franklin, Carrie Kusturin
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Publication number: 20030225270Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: April 24, 2003Publication date: December 4, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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Publication number: 20030220323Abstract: The invention relates to new &agr;-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said &agr;-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 30, 2002Publication date: November 27, 2003Inventors: Francoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
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Publication number: 20030207882Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents, L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.Type: ApplicationFiled: May 2, 2003Publication date: November 6, 2003Applicant: ZENECA LIMITEDInventors: Andrew Stocker, John Preston, Michael James Smithers
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Publication number: 20030207877Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: December 19, 2002Publication date: November 6, 2003Inventors: Joseph Walter Strohbach, Steven P. Tanis, Malcolm Wilson Moon, James A. Nieman, Thomas J. Beauchamp, Jill M. Northuis, William D. McGhee
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Publication number: 20030195203Abstract: The invention relates to heterocyclic derivatives of formula (I)Type: ApplicationFiled: September 27, 2001Publication date: October 16, 2003Inventors: Andrew Stocker, John Preston, John Wall Rayner, Michael James Smithers, Paul Turner