UREA DERIVATIVES EFFECTIVE AS MUSCARINREZEPTOR ANTAGONISTS

RAS FARNESYL TRANSFERASE INHIBITORS

Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

Substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds

This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.

CARBAMAT DERIVATIVES AS MUSCARIN RECEPTOR ANTONISTEN

IMIDAZOÄ4,5-CÜPYRIDINVERBINDUNGEN AND PROCEDURE FOR THE ANTIVIRAL TREATMENT

ANTAGONISTE FOR THE TREATMENT OF CD11/CD18 ADHESION-RECEPTOR-CONCILIATORY DISEASES

RECEPTOR SPECIFIC ATRIAL NATRIURETIC PEPTIDES

Human receptor selective atrial natriuretic factor variants containing various substitutions, especially G16R, show equal potency and binding affinity for the human A-receptor but have decreased affinity for the human clearance or C-receptor. These ANF variants have natriuretic, diuretic and vasorelaxant activity but have increased metabolic stability, making them suitable for treating congestive heart failure, acute kidney failure and renal hypertension.

LFA-1 ANTAGONIST COMPOUNDS

The invention relates to novel compounds having formula (I), wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation. © KIPO & WIPO 2007 ...

RECEPTOR SPECIFIC ATRIO NATRIURETI PEPTIDE

ANTIVIRAL PHOSPHONATE SIMILAR ONE

Receptor specific atrial natriuretic peptides

IMIDAZOA4,5-CUPYRIDINVERBINDUNG AND PROCEDURE FOR THE ANTIVIRAL TREATMENT

INTERMEDIATE PRODUCTS FOR THE PRODUCTION OF UREA DERIVATIVES WITH MUSCARINE RECEPTOR OF ANTAGONISTIC ACTIVITY

Urea compounds having muscarinic receptor antagonist activity

LFA-1 antagonist compounds

The invention relates to novel compounds having formula (I)wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.

HARNSTOFFDERIVATE WIRKSAM ALS MUSCARINREZEPTOR-ANTAGONISTEN

Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole

Anti-cancer phosphonate analogs

LFA-1 antagonist compounds

HARNSTOFFDERIVATE WIRKSAM ALS MUSCARINREZEPTOR-ANTAGONISTEN

Antiviral phosphonate analogs

Anti-inflammatory phosphonate compounds

UREA COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY

The invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds. © KIPO & WIPO 2007 ...

Inhibitors of hiv reverse transcriptase

Antagonists for treatment of CD/11CD18 adhesion receptor mediated disorders

Compounds of the general structure D-L-B-(AA), for example (A), that are useful for treating Mac-1 or LFA-1-mediated disorders such as inflammatory disorders, allergies, and autoimmune diseases are provided.

ANTAGONISTE ZUR BEHANDLUNG VON CD11/CD18 ADHÄSIONSREZEPTOR-VERMITTELTEN KRANKHEITEN

REZEPTOR SPEZIFISCHE ATRIO-NATRIURETISCHE PEPTIDE

Carbamate derivatives having muscarinic receptor antagonist activity

MUSCARINIC RECEPTOR ANTAGONISTS

Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

INHIBITORS OF HIV REVERSE TRANSCRIPTASE

Disclosed are multibinding compounds which inhibit the enzyme HIV reverse transcriptase, an enzyme which catalyzes the conversion of viral RNA to single stranded DNA. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each multibinding compound comprises at least one nucleoside reverse transcriptase inhibitor and at least one non-nucleoside reverse transcriptase inhibitor. The multibinding compounds of this invention are useful to inhibit HIV reverse transcriptase in vivo, and accordingly to inhibit HIV replication in vivo.

ANTIVIRALE PHOSPHONATE ANALOGE

Antiviral phosphonate analogs

Muscarinic receptor antagonists

Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

LFA-1 antagonist compounds

Carbamate derivatives having muscarinic receptor antagonist activity

Antagonists for treatment of CD11/CD18 adhesion receptor mediated disorders

RECEPTOR SPECIFIC ATRIAL NATRIURETIC PEPTIDES

Human receptor selective atrial natriuretic factor variants containing various substitutions, especially G16R, show equal potency and binding affinity for the human A-receptor but have decreased affinity for the human clearance or C-receptor. These ANF variants have natriuretic, diuretic and vasorelaxant activity but have increased metabolic stability, making them suitable for treating congestive heart failure, acute kidney failure and renal hypertension.

Urea compounds having muscarinic receptor antagonist activity

Muscarinic receptor antagonists

ANTAGONISTEN ZUR BEHANDLUNG VON CD11/CD18 ADHÄSIONSREZEPTOR-VERMITTELTEN KRANKHEITEN

Novel therapeutic agents for macromolecular structures

Zwischenprodukte für die Herstellung von Harnstoffderivaten mit Muskarinrezeptor-antagonistischer Aktivität

Therapeutic carbamates

This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Muscarinic receptor antagonists

LFA-1 antagonist compounds

Substituted 4-amino-benzylpiperidine compounds

This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

ANTIVIRAL PHOSPHONATE ANALOGS

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. © KIPO & WIPO 2007 ...

LFA-1 antagonist compounds

The invention relates to novel compounds having formula (I)wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.

CARBAMAT-DERIVATE ALS MUSCARIN-REZEPTOR ANTONISTEN

ANTI-INFLAMMATORY PHOSPHONATE COMPOUNDS

The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. © KIPO & WIPO 2007 ...

ANTIVIRAL PHOSPHONATE ANALOGUE

PROBLEM TO BE SOLVED: To provide a therapeutic antiviral preparation having improved pharmacological characteristics, a dosing regimen for a new antiviral compound not more troublesome than the conventional regimen, or an assay method determining the presence or absence of, or the amount of virus-inhibition. SOLUTION: The invention relates not only to a phosphorus-substituted compound having antiviral activity, a composition containing such compound and a therapeutic method including a process for dosing such compound, but also to a useful process and an intermediate for preparing such compound. The invention provides new phosphonate-containing analogues of the antiviral compounds. These analogues have all of usefulness of these parent compounds, and provide accumulation of them in cells described below, at need. The compounds of the invention can inhibit RNA-dependent RNA polymerase of retro virus or reverse transcriptase, and therefore, can inhibit duplication of virus. COPYRIGHT: (C) ...

REZEPTOR SPEZIFISCHE ATRIO-NATRIURETISCHE PEPTIDE

ANTI-CANCER PHOSPHONATE ANALOGS

The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. © KIPO & WIPO 2007 ...

ANTIVIRAL PHOSPHONATE ANALOGS

OF THE DISCLOSUREANTIVIRAL PHOSPHONATE ANALOGSThe invention is related to phosphorus substituted compounds with antiviral activity,compositions containing such compounds, and therapeutic methods that include theadministration of such compounds, as well as to processes and intermediates useful for preparingsuch compounds.(NO FIGURE) ...

Muscarinic receptor antagonists

Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

CARBAMAT-DERIVATE ALS MUSCARIN-REZEPTOR ANTONISTEN

ANTAGONISTS FOR TREATMENT OF CD11/CD18 ADHESION RECEPTOR MEDIATED DISORDERS

Compounds of the general structure D-L-B-(AA), for example (A), that are useful for treating Mac-1 or LFA-1-mediated disorders such as inflammatory disorders, allergies, and autoimmune diseases are provided. © KIPO & WIPO 2007 ...

Substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds

This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.

ANTIVIRAL PHOSPHONATE ANALOGS

Therapeutic ureas

This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

ANTI-CANCER PHOSPHONATE ANALOGUE

【課題】抗癌治療薬（すなわち、抗癌性および薬物動態学的性質（増強された癌発症活性が含まれる）が改良され、経口生物学的利用能が改良され、有効性が増大し、ｉｎ ｖｉｖｏでの有効な半減期が延長された薬物）が必要である。このような抗癌化合物は、種々の癌に活性であり、異なる耐性プロフィールを有し、副作用がより少なく、投与計画の複雑さが軽減され、経口で活性である。複雑さが軽減された投薬計画に必要である（例えば、１日１回の丸薬１錠）。 【解決手段】本明細書中に記載の抗癌結合体。 【選択図】なし

LFA-1 antagonist compounds

The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R_1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.

Substituted 4-amino-1-benzylpiperidine compounds

This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

Muscarinic receptor antagonists

Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

Receptor specific atrial natriuretic peptides

Human receptor selective atrial natriuretic factor variants containing various substitutions, especially G16R, show equal potency and binding affinity for the human A-receptor but have decreased affinity for the human clearance or C-receptor. These ANF variants have natriuretic, diuretic and vasorelaxant activity but have increased metabolic stability, making them suitable for treating congestive heart failure, acute kidney failure and renal hypertension.

ANTI-INFLAMMATORY PHOSPHONATE COMPOUND

PROBLEM TO BE SOLVED: To provide a new anti-inflammation agent such as a drug having improved anti-inflammatory property, improved pharmacological property, improved activity, improved bioavailability and improved effective half-life period in vivo. SOLUTION: The invention provides a conjugated material containing an anti-inflammatory compound linked to one or more phosphonate groups and its pharmacologically allowable salt or solvate. In one embodiment, the compound of the conjugated material is either one compound substituted with one or more A0 groups and expressed by formulas 500-611. COPYRIGHT: (C)2007,JPO&INPIT ...

ANTAGONIST FOR TREATING CD11/CD18 ADHESION RECEPTOR-MEDIATED DISEASE

PROBLEM TO BE SOLVED: To provide a compound useful for treating Mac-1 or LFA-1-mediated diseases such as inflammatory diseases, allergy, autoimmune diseases and the like. SOLUTION: The compound has a general structure of D-L-B(AA), wherein D expresses an aromatic group; L expresses an alkylene group; B(AA) expresses a benzene ring having an amino acid-containing substituent. As a concrete example, a compound expressed by structural formula (I) is cited. COPYRIGHT: (C)2007,JPO&INPIT ...

VIRAL INHIBITORS

Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A),

ANTIVIRAL PHOSPHONATE ANALOGS

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. 2. The conjugate of wherein C-Csubstituted alkyl claim 1 , C-Csubstituted alkenyl claim 1 , C-Csubstituted alkynyl claim 1 , C-Csubstituted aryl claim 1 , and C-Csubstituted heterocycle are independently substituted with one or more substituents selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , OH claim 1 , —NH claim 1 , —NH claim 1 , —NHR claim 1 , —NR claim 1 , —NR claim 1 , C-Calkylhalide claim 1 , carboxylate claim 1 , sulfate claim 1 , sulfamate claim 1 , sulfonate claim 1 , 5-7 membered ring sultam claim 1 , C-Calkylsulfonate claim 1 , C-Calkylamino claim 1 , 4-dialkylaminopyridinium claim 1 , C-Calkylhydroxyl claim 1 , C-Calkylthiol claim 1 , —SOR claim 1 , —SOAr claim 1 , —SOAr claim 1 , —SAr claim 1 , —SONR claim 1 , —SOR claim 1 , —COR claim 1 , —C(═O)NR claim 1 , 5-7 membered ring lactam claim 1 , 5-7 membered ring lactone claim 1 , —CN claim 1 , —N claim 1 , —NO claim 1 , C-Calkoxy claim 1 , C-Ctrifluoroalkyl claim 1 , C-Calkyl claim 1 , C-Ccarbocycle claim 1 , C-Caryl claim 1 , C-Cheterocycle claim 1 , polyethyleneoxy claim 1 , phosphonate claim 1 , phosphate claim 1 , and a prodrug moiety.3. The conjugate of wherein protecting group is selected from a carboxyl ester claim 1 , a carboxamide claim 1 , an aryl ether claim 1 , an alkyl ether claim 1 , a trialkylsilyl ether claim 1 , a sulfonic acid ester claim 1 , a carbonate claim 1 , and a carbamate.5. The conjugate of wherein X is O and each Ris H.14. The conjugate of wherein Z is H.15. The conjugate of wherein B is adenine.18. The conjugate of wherein Yis O.19. The conjugate of wherein Yis N(CH).21. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a conjugate as described in ...

ANTIVIRAL PHOSPHONATE ANALOGS

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. 123-. (canceled)32. The method of claim 31 , wherein the viral infection is an HIV infection. This application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application Ser. Nos. 60/465,630, 60/465,400, 60/465,587, 60/465,463, 60/465,602, 60/465,598, 60/465,633, 60/465,550, 60/465,610, 60/465,720, 60/465,634, 60/465,537, 60/465,698, 60/465,667, 60/465,554, 60/465,553, 60/465,561, 60/465,548, 60/465,696, 60/465,347, 60/465,289, 60/465,478, 60/465,600, 60/465,591, 60/465,684, 60/465,821, 60/465,647, 60/465,742, 60/465,649, 60/465,690, 60/465,469, 60/465,408, 60/465,608, 60/465,584, 60/465,687, 60/465,759, 60/465,559, 60/465,322, 60/465,377, 60/465,844, and 60/465,544, all filed Apr. 25, 2003; and to U.S. Provisional Patent Application Ser. No. 60/490,799, filed Jul. 29, 2003; and to U.S. Provisional Patent Application Ser. Nos. 60/495,687, 60/495,490, 60/495,805, 60/495,684, 60/495,600, 60/495,342, 60/495,564, 60/495,772, 60/495,592, 60/495,453, 60/495,491, 60/495,964, 60/495,317, 60/495,696, 60/495,760, 60/495,334, 60/495,671, 60/495,349, 60/495,273, 60/495,763, 60/495,345, 60/495,602, 60/495,343, 60/495,344, 60/495,278, 60/495,277, 60/495,275, 60/495,630, 60/495,485, 60/495,430, 60/495,388, 60/495,341, 60/495,631, 60/495,633, 60/495,632, 60/495,539, 60/495,387, 60/495,392, 60/495,425, 60/495,393, and 60/495,616, all filed Aug. 15, 2003; and to U.S. Provisional Patent Application Ser. No. 60/510,245, filed Oct. 10, 2003; and to U.S. Provisional Patent Application Ser. Nos. 60/514,202, 60/513,948, and 60/514,258, all filed Oct. 24, 2003; and to U.S. Provisional Patent Application Ser. No. 60/515,266, filed Oct. 29, 2003; and to U.S. Provisional Patent ...

VIRAL INHIBITORS

Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), 2. The compound according to claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein Y is a single bond claim 1 , and Ris phenyl substituted with 1 to 3 R.4. The compound according to claim 1 , wherein X is C1-C3 alkyl and Ris heterocycle independently substituted with 1 or 2 R.5. The compound of wherein Rindependently is substituted with 1 or 2 R.6. The compound of wherein Y is a bond.7. The compound of wherein Ris aryl independently substituted with 1 or 2 R.8. The compound of wherein R claim 5 , Rand Rare hydrogen.9. The compound of wherein X is methylene.10. The compound of wherein Ris a five membered heteroaryl containing 1 to 3 N claim 5 , O and/or S ring atoms.11. The compound of wherein Ris isoxazolyl or pyridizinyl.12. The compound of wherein Rindependently is aryl.13. The compound of wherein aryl is phenyl.14. The compound of wherein Ris independently substituted with 1 or 2 R.15. The compound of wherein Ris independently halo or C1-C6 haloalkyl.16. The compound of wherein Ris substituted with 2 R.17. The compound of wherein X is methylene and Ris isoxazolyl substituted with 1 R.18. The compound of wherein Ris substituted with 1 R.19. The compound of wherein Ris substituted with 1 or 2 R.20. The compound of wherein Ris C3-C6 cycloalkyl.21. A composition comprising a compound of and a pharmaceutically acceptable excipient or carrier.23. The method of claim 22 , wherein said viral infection is an infection of a virus belonging to the family of the Flaviviridae.24. The method of claim 22 , wherein said viral infection is an infection of a hepatitis-C virus. This non-provisional application is a divisional of U.S. application Ser. No. 11/957,017, filed Dec. 14, 2007, which claims the benefit of Provisional Application No. 60/874,797, filed Dec. 14, 2006, both of which are incorporated herein by reference.The present invention relates to a series of novel ...

Imidazo[4,5-d]pyrimidines, their uses and methods of preparation

The present invention relates to pharmaceutical compositions for the treatment of prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyrimidine having the general formula (A), wherein the substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.

Antiviral phosphonate analogs

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Anti-cancer phosphonate analogs

The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Therapeutic phosphonate compounds

The invention is related to phosphorus substituted therapeutic agents, compositions containing such phosphorus substituted agents, and therapeutic methods that include the administration of such phosphorus substituted agents, as well as to processes and intermediates useful for preparing such agents.

Antiviral phosphinate compounds

A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administation of such compounds.

Imidazo 4,5-c pyridine compounds and methods of antiviral treatment

The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening ofcompounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

Imiadazo[4,5-c] pyridine compound and method of antiviral treatment

The compound 5-((3-(2,4-trifluoromethyphenyl)isoxazol-5-yl)methyl)-2 -(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine, together with the salts and solvates thereof. Also provided are compositions comprising this compound and pharmaceutically acceptable carriers, as well as the use of such compositions in the treatment or prophylaxis of viral infections.

Pyridazine compound and use thereof

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.

Imidazo[4,5-d]pyrimidines, their uses and methods of preparation

The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula (A): wherein U is N or C; X is selected from C 1 -C 10 alkylene, C 2-10 alkenylene or C 2-10 alkynylene, where each may include one or more intrachain heteroatoms selected from O, S, or NR 11 , provided any such heteroatom is not adjacent to the N in the ring; R 3 is selected from aryl, aryloxy, arylthio, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl-N(R 10 )—, or heterocycle, where each said substituent is optionally substituted with at least one R 17 , provided that for cycloalkenyl the double bond is not adjacent to a nitrogen; and the other substituents are described in the specification. The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula, their pharmaceutically acceptable formulations and their use as a medicine or to treat or prevent viral infections.

Urea compounds having muscarinic receptor antagonist activity

The invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Lfa-1 antagonist compounds

The invention relates to novel compounds having formula (I), wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation

Antagonists for treatment of cd11/cd18 adhesion receptor mediated disorders

Compounds of the general structure D-L-B-(AA), for example (A), that are useful for treating Mac-1 or LFA-1-mediated disorders such as inflammatory disorders, allergies, and autoimmune diseases are provided.

Antagonists for the treatment of cd11 / cd18 adhesion receptor-mediated disorders and method for treating or ameliorating an immune or inflammatory response or disorder in a mammal mediated through the cd11 / cd18 family in cell adhesion molecules

"ANTAGONISTAS PARA O TRATAMENTO DE DISTúRBIOS MEDIADOS POR RECEPTOR DE ADERêNCIA CD11/CD18 E MéTODO PARA TRATAR OU MELHORAR UMA RESPOSTA OU DISTúRBIO IMUNOLóGICO OU INFLAMATóRIO EM UM MAMìFERO MEDIADA ATRAVéS DA FAMìLIA CD11/CD18 DE MOLéCULAS DE ADERêNCIA CELULAR" A presente invenção refere-se a compostos de estrutura geral D-L-B-(A-A), por exemplo (A), que são úteis para o tratamento de distúrbios mediados por Mac-1 e LFA-1 tais como distúrbios inflamatórios, alergias e doenças autoimunológicas.

Urea compounds having muscarinic receptor antagonist activity

The invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Therapeutic carbamates

This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Therapeutic ureas

This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Urea compounds having a muscarinic receptor antagonist activity

Muscarinic receptor antagonists

Novel therapeutic agents for macromolecular structures

Disclosed are novel multibinding compounds (agents) which bind macromolecular structures including cellular, extracellular, and microbial components derived from vectors, viruses, fungi, yeasts, bacteria, and the like. The compounds of this invention comprise a plurality of ligands each of which can bind to such macromolecular structures thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of cell as compared to the aggregate of the individual units of the ligand.

Antiviral phosphonate analogue, its pharmaceutical composition, its use in the treatment of virus infections in an animal, and a method of promoting an anti-viral effect in vitro

Antiviral phosphonate analogs

ANTIVIRAL PHOSPHONATE ANALOGS.

El compuesto **Fórmula** o su sal o solvato farmacéuticamente aceptable. The compound ** Formula ** or its pharmaceutically acceptable salt or solvate.

Carbamate derivatives having muscarinic receptor antagonist activity

This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists and antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Novel therapeutic agents for macromolecular structures

Disclosed are novel multibinding compounds (agents) which bind macromolecular structures including cellular, extracellular, and microbial components derived from vectors, viruses, fungi, yeasts, bacteria, and the like. The compounds of this invention comprise a plurality of ligands each of which can bind to such macromolecular structures thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of cell as compared to the aggregate of the individual units of the ligand.

Imidazo[4,5-C]Pyridine Compounds And Methods Of Antiviral Treatment

Viral inhibitors

Imidazo[4,5-c]pyridine compound and method of antiviral treatment

Antiviral phosphonate analogs

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Antiviral phosphonate analogs

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Novel therapeutic agents for macromolecular structures

Urea compounds having muscarinic receptor antagonist activity

The invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Fused pyridine compounds useful in the prophylaxis or treatment of viral infections

Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.

Imidazo[4,5-c]pyridine compound and method of antiviral treatment

The compound 5-((3-(2, 4-trifluoromethyphenyl)isoxazol-5-yl)methyl)-2-(2~5 fluorophenyl)-5H-imidazo[4,5-c]pyridine, together with the salts and solvates thereof. Also provided are compositions comprising this compound and pharmaceutically acceptable carriers, as well as the use of such compositions in the treatment or prophylaxis of viral infections.

Muscarinic receptor antagonists.

Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment

The present invention relates to pharmaceutical compositions for the treatment or prevention of vital infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general formula (A): wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general formula and their use in the treatment or prophylaxis of viral infections.

IMIDAZOE4,5-CYPYRIDINE COMPOUND AND METHOD FOR ANTIVIRAL TREATMENT

Antagonists for treatment of CD11/CD18 adhesion receptor mediated disorders.

Ras farnesyl transferase inhibitors

Benzodiazepine derivatives represented by the structure below are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases foe which inhibition of the ras farnesyl:protein transferase as indicated. ##STR1##

Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment

Novel pyridazine compound and use thereof

Novel pyridazine compound and use thereof

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.

Imidazo[4,5-c]pyridine compounds and methods of antiviral treatment

The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

Novel pyridazine compound and use thereof

(1) Spoj formule (1) i njegove soli i solvati su za tretman ili profilaksu infekcija virusom hepatitisa C. Prikazane su metode priprave spoja (1). (1) The compound of formula (1) and its salts and solvates are for the treatment or prophylaxis of hepatitis C virus infections. Methods for preparing compound (1) are shown.

Receptor specific atrial natriuretic peptides

Human receptor selective atrial natriuretic factor variants containing various substitutions, especially G16R, show equal potency and binding affinity for the human A-receptor but have decreased affinity for the human clearance or C-receptor. These ANF variants have natriuretic, diuretic and vasorelaxant activity but have increased metabolic stability, making them suitable for treating congestive heart failure, acute kidney failure and renal hypertension.

Substituted 4-amino-1-benzylpiperidine compounds

This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

Antiviral phosphonate analogs

The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

IMIDAZO[4,5-c]PYRIDINE COMPOUNDS AND METHODS OF ANTIVIRAL TREATMENT

The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general Formula (A) wherein the substituents are described in the specification. The invention also relates to processes for the preparation and screening of compounds according to the invention having above mentioned general Formula and their use in the treatment or prophylaxis of viral infections.

CARBAMATE DERIVATIVES WITH MUSCARINIC RECEIVER ANTAGONIST ACTIVITY.

Un compuesto de **fórmula** en la que A es fenilo o piridilo; Rx es alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, acilo, acilamino, aminoaciloxi, arilo, carboxialquilo, cicloalquilo, cicloalquilo sustituido, cicloalquenilo, cicloalquenilo sustituido, heteroarilo, heteroaralquilo, alquilsulfonilo, o alquilsulfinilo; R2 es pirrolilo, piridinilo, imidazolilo o fenilo; K es un enlace o un grupo metileno; B es pirrolidina, piperidina o hexahidroazepina; R46 es alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, o heterociclo; R47 es alquilo, alquilo sustituido, arilo, acilo, heterociclo, o ¿COOR50 en la que R50 es alquilo; o R46 y R47 junto con el átomo de nitrógeno al que están unidos forman un heterociclo, que está opcionalmente sustituido con 1 a 5 sustituyentes seleccionados independientemente entre el grupo constituido por alcoxi, alcoxi sustituido, cicloalquilo, cicloalquilo sustituido, cicloalquenilo, cicloalquenilo sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminoacilo, aminoaciloxi, oxiaminoacilo, azido, ciano, halógeno, hidroxilo, ceto, tioceto, carboxilo, carboxilalquilo, tioariloxi, tioheteroariloxi, tioheterociclooxi, tiol, tioalcoxi, tioalcoxi sustituido, arilo, ariloxi, heteroarilo, heteroariloxi, heterociclilo, heterociclooxi, hidroxiamino, alcoxiamino, nitro, -SO-alquilo, -SO-alquilo sustituido, -SO-arilo, -SO-heteroarilo, -SO2-alquilo, -SO2- alquilo sustituido, -SO2-arilo, -SO2-heteroarilo, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, y alquinilo sustituido; o una sal farmacéuticamente aceptable del mismo. A compound of ** formula ** in which A is phenyl or pyridyl; Rx is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, acyl, acylamino, aminoacyloxy, aryl, carboxyalkyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heteroaryl, heteroaralkyl, alkylsulphonyl; R2 is pyrrolyl, ...

Fused pyridine compounds useful in the prophylaxis or treatment of viral infections

Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.

NEW PYRIDAZIN COMPOUND AND ITS USE

Imidazo 4,5-C Pyridine Compounds and Methods of Antiviral Treatment

The present invention relates to a pharmaceutical composition for the treatment or prevention of viral infections comprising as an active principle at least one imidazo[4,5-c]pyridine prodrug having the general formula (Z): The invention also relates to processes for the preparation of compounds according to the invention having above mentioned general formula and their use as a medicine or to treat or prevent viral infections.

Novel pyridazine compound and use thereof

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.

Novel pyridazine compound and use thereof

Imidazo[4,5-c]pyridine compound and method of antiviral treatment

Anti-cancer phosphonate analogs

The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Novel pyridazine compound and use thereof

A compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections. Methods of making and formulating compound (1) are provided.

Novel pyridazine compound and use thereof

Urea compounds having muscarinic receptor antagonist activity

Pronalazak se odnosi na jedinjenja karbamida koja imaju antagonističku aktivnost na muskarinske receptore, farmaceutske kompozicije koje sadrže takva jedinjenja, i postupke za dobijanje ovih jedinjenja.[The invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Urea compounds having muscarinic receptor antagonist activity.

Compounds of formula <CHEM> are useful as intermediates in the preparation of certain urea compounds having muscarinic receptor antagonist activity.

Carbamate derivatives having muscarinic receptor antagonist activity

This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists and antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Viral inhibitors

Zwischenprodukte für die herstellung von harnstoffderivaten mit muskarinrezeptor- antagonistischer aktivität

Rezeptor spezifische atrio-natriuretische peptide

Neue pyridazinverbindung und ihre verwendung

Antagoniste zur behandlung von cd11/cd18 adhäsionsrezeptor-vermittelten krankheiten

Imidazoä4,5-cüpyridinverbindungen und verfahren zur antiviralen behandlung

Antivirale phosphonate analoge

Carbamat-derivate als muscarin-rezeptor antonisten

Harnstoffderivate wirksam als muscarinrezeptor- antagonisten

Imidazole[4,5-c]pyridine copmounds and methods of antiviral treatment

THE PRESENT INVENTION RELATES TO PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF PREVENTION OF VIRAL INFECTIONS COMPRISING AS AN ACTIVE PRINCIPLE AT LEAST ONE IMIDAZO[4,5-C]PYRIDINE PRODRUG HAVING THE GENERAL FORMULA (A) WHEREIN THE SUBSTITUENTS ARE DESCRIBED IN THE SPECIFICATION. THE INVENTION ALSO RELATES TO PROCESSES FOR THE PREPARATION AND SCREENING OF COMPOUNDS ACCORDING TO THE INVENTION HAVING ABOVE MENTIONED GENERAL FORMULA AND THEIR USE IN THE TREATMENT OR PROPHYLAXIS OF VIRAL INFECTIONS.

Imidazoa4,5-cupyridinverbindung und verfahren zur antiviralen behandlung

Anti-inflammatory phosphonate compounds