- AMINOALKYLPYRIMIDINE DERIVATIVES AS HISTAMINE H4 RECEPTOR ANTAGONISTS
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Aminoalkyipyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 52
(2011/07/09)
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- 2H-PYRAZOLO [4,3-D]PYRIMIDIN-5-AMINE DERIVATIVES AS H4 HISTAMINE RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ALLERGIC, IMMUNOLOGICAL AND INFLAMMATORY DISEASES
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Pyrazolopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 91-92
(2010/04/30)
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- PIPERIDIN-PYRIMIDINE DERIVATIVES AS ANTAGONISTS OF HISTAMINE H4 RECEPTOR
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Piperidin-pyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 68
(2010/09/17)
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- 4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS
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The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
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Page/Page column 179
(2010/07/09)
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- FURO[3,2-D]PYRIMIDINE DERIVATIVES
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Furo[3,2-d]pyrimidine derivatives of formula I, wherein the meanings for the various substituents are as defined in the description. These compounds are useful as H4 receptor antagonists.
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Page/Page column 54
(2009/06/27)
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- 2 -AMINOPYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS
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2-Amino-pyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine receptor H4antagonists.
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Page/Page column 101-102
(2009/07/18)
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- 4-AMINO-PYRIMIDINE DERIVATIVES
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4-Amino-pyrimidine derivatives of Formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 72
(2009/07/25)
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- 2 -AMINO-PYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS
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2-Aminopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 54
(2009/07/03)
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- FURO [3, 2-D] PYRIMIDINE DERIVATIVES AS H4 RECEPTOR ANTAGONISTS
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Furo[3,2-d]pypnnidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 78-79
(2009/10/22)
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- Macrocyclic Spiro Pyrimidine Derivatives
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Macrocyclic spiro pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.
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Page/Page column 78
(2009/09/28)
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- SUBSTITUTED PYRIMIDINE DERIVATIVES
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The present application describes substituted pyrimidine compounds of formula (I) wherein X, A1, R1, R2, R3, R4, R5, R6, R7, R8, R9, p, q, r, v,
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Page/Page column 27
(2009/10/31)
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- MACROCYCLIC BENZOFUSED PYRIMIDINE DERIVATIVES
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Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.
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Page/Page column 121
(2008/12/05)
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- Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: A new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models
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A new structural class of histamine H4 receptor antagonists (6-14) was designed based on rotationally restricted 2,4-diaminopyrimidines. Series compounds showed potent and selective in vitro H4 antagonism across multiple species, goo
- Cowart, Marlon D.,Altenbach, Robert J.,Liu, Huaqing,Hsieh, Gin C.,Drizin, Irene,Milicic, Ivan,Miller, Thomas R.,Witte, David G.,Wishart, Neil,Fix-Stenzel, Shannon R.,McPherson, Michael J.,Adair, Ronald M.,Wetter, Jill M.,Bettencourt, Brian M.,Marsh, Kennan C.,Sullivan, James P.,Honore, Prisca,Esbenshade, Timothy A.,Brioni, Jorge D.
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experimental part
p. 6547 - 6557
(2009/10/09)
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- 2-AMINOPYRIMIDINE DERIVATIVES AS MODULATORS OF THE HISTAMINE H4 RECEPTOR ACTIVITY
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2-Aminopyrimidine derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as modulators of the H4 receptor.
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Page/Page column 24
(2008/06/13)
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- Pyrimidine derivatives
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A compound of Formula (I): or a pharmaceutically and/or veterinarily acceptable derivative thereof, wherein R1, R2, R3, R4, R5, and R8 are as defined above.
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Page/Page column 23-24
(2010/11/28)
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- Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1
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The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited potent binding affinity and functional activity at MCH-R1, and good oral bioavailability in rat.
- Rowbottom, Martin W.,Vickers, Troy D.,Dyck, Brian,Grey, Jonathan,Tamiya, Junko,Zhang, Mingzhu,Kiankarimi, Mehrak,Wu, Dongpei,Dwight, Wesley,Wade, Warren S.,Schwarz, David,Heise, Christopher E.,Madan, Ajay,Fisher, Andrew,Petroski, Robert,Goodfellow, Val S.
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p. 4450 - 4457
(2007/10/03)
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- MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISTS AND COMPOSITIONS AND METHODS RELATED THERETO
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Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure: including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, X, R1, R2, R3, R4, and R5 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
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- Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
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The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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- BENZOFUSED HETEROARYL AMIDE DERIVATIVES OF THIENOPYRIDINES USEFUL AS THERAPEUTIC AGENTS, PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME, AND METHODS FOR THEIR USE
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The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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