Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.

Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.

Abstract: It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.

Abstract: The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R1, R2, R3, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

Abstract: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.

Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.

Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, Ar2, Hy, L, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses thereof, processes for making the compounds, as well as methods for the medical treatment of mGluR5-mediated disorders.

Abstract: A medication delivery system is disclosed to mitigate or reverse the pharmacologic effect of a medication beyond the desired therapeutic window. The system provides sequential delivery of medications including a first agent which induces a physiologic change, a second agent for reversing the physiologic change, and a medication release delaying agent for delaying the release of the second agent so that, upon receipt of the medication delivery system into the body the first agent is released before the second agent so that the physiologic effect of the first agent is mitigated by the second agent. The system can be a pill with the first agent comprising an outer medication and the second agent an inner medication with the medication release delaying agent intermediate the outer medication and the inner medication. In an example, the first agent can comprise a sleep aid and the second agent an arousal agent.

Abstract: A Compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M1, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5, and R5a are as defined herein for the treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.

Abstract: Disclosed are compounds having Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, A, and B are as defined herein, for use in methods for treating, preventing or ameliorating hyperproliferative disorders, such as cancer and other diseases and conditions. The invention also relates to pharmaceutical compositions and formulations comprising a compound having Formula I, and in combination with one or more other active agents and/or treatments.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.

Abstract: This invention relates to compounds of formula (I).

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where G, J, L, M, x, y, W, V, R2, R3, R4, R5, R6, R7, R8, R8a, R9, R9a, R10, R10a, R11 and R11a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: A compound of formula (I) P—W—C(?X)-L-Q ??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.

Abstract: This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated with the Ras/Raf/MEK signaling cascade in a mammal, such as neoplasms, strokes, osteoporosis, cancer, rheumatoid arthritis, inflammatory disease, polycystic kidney disease, and colonic polyps, and methods of making the compounds of formula 1 and intermediates.

Abstract: A compound of Formulae (1), (2) or (3), A1-Ph (1) or A1-Ar-A2 (2) or A1-(A2)A?-A3 (3) wherein A1, A2 and A3 are selected from Formulae (4), (5) and (6), or a salt whereof; wherein Ar is selected from the group consisting of 1,2-phenyl, 1,3-phenyl and 1,4-phenyl optionally substituted with one or more methyl groups; m and n are independently integers from 0 to 1; Ph is phenyl, optionally substituted with one or more methyl groups; Ar1 is trisubstituted phenyl optionally substituted with one or more phenyl groups; and R1, R2 and R3 are independently selected from the group consisting of H, Me and linear chain C2-C4 alkyl.

Abstract: 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.

Abstract: The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: Provided herein are methods for diagnosis and prognosis using polymorphic variants of sirtuins. Such polymorphic may be used, for example, to identify subjects that would be responsive to treatment with a sirtuin modulating compound and/or subjects that are suffering from or susceptible to a disease mediated by a sirtuin. Also provided are methods for determining the predictive value of a sirtuin polymorphic variant, methods for evaluating sirtuin modulating compounds, and methods for determining appropriate dosage and/or treatment regimens for subjects having one or more sirtuin polymorphic variants. Screening methods for identifying sirtuin modulating compounds using polymorphic variants of a sirtuin are also provided.

Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.

Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.

Abstract: The present invention relates to Compound S of Formula (I).

Abstract: The invention relates to novel piperazine derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, especially malaria.

Abstract: Compounds of formula (I) wherein R1, R2, R3, and HET-1 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.

Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof, a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.

Abstract: Provided herein are methods for treatment of a liver disease by administering a matrix metalloproteinase inhibitor. Also provided are methods for reducing liver damage associated with a liver disease by administering the matrix metalloproteinase inhibitor described herein. Further provided are methods for lowering an elevated level of liver enzymes by administering the matrix metalloproteinase inhibitor.

Abstract: The invention relates to compounds of formula (I), Chemical formula should be inserted here.

Abstract: Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: The present invention relates to pyrazine derivatives according to the general formula (I) and pharmaceutically acceptable salts thereof and their use as pharmaceutical compounds as well as the use of these compounds for the preparation of a pharmaceutical composition for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases, stroke and especially for the treatment of herpesviral induced infections, including opportunistic infections as well as infections and diseases caused by human cytomegalovirus (HCMV).

Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS.

Abstract: This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine diamide derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.

Abstract: Compounds of formula (I) wherein A and B are amine-substituted sidechains, Y1 and Y2 form various tricyclic cores, Xa and Xb are C, CH, or N, as defined herein, and Rx is an optional substituent. Compounds and compositions of formula (I) are contemplated as well as methods for treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands that encompass compounds of formula (I) and other tricyclic derivatives. Methods of using amino-substituted tricyclic derivatives also are described herein.

Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

Abstract: The invention pertains to inhibitors of various kinases (e.g. S/T kinases, Tyr kinases, etc.), which inhibitors are previously known as cyclin dependent kinase inhibitors (CDKs). As described herein, the inhibitors of this invention are capable of inhibiting various wild-type and mutant form kinases, including drug resistant forms of mutant kinases. Thus the subject kinase inhibitors are useful in treating a wide range of diseases/conditions associated with abnormal functions/excessive activities of the target kinases, including mutant kinases. The invention further provides methods for treating cancers, tumors and patients which are resistant or refractory to other therapeutic agents. Pharmaceutical compositions and packaged pharmaceuticals with instructions of these inhibitors, and methods of using these inhibitors are also provided.

Abstract: The present invention relates to the use of agonists of 5-HT2C receptors for the treatment of urinary incontinence, preferably mixed incontinence or stress urinary incontinence. The invention also relates to the use of antagonists of 5-HT2C receptors for the treatment of urine retention. The present invention also relates to a method of treatment of incontinence, to assays to screen for compounds useful in the treatment of incontinence, and to methods of preparing compositions for the treatment of urinary incontinence.

Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.

Abstract: treatment of a variety of disorders, including the treatment of pathological conditions associated with tumor necrosis factor alpha. The inhibitors of tumor necrosis factor alpha have the following structures: including stereoisomers, pharmaceutically acceptable salts, and solvates thereof, wherein substituents are as defined herein. Compositions containing an inhibitor of tumor necrosis factor alpha in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2, W, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.

Abstract: A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3?, E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed

Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.

Abstract: This invention concerns the use of compounds of formula (I) wherein ?a1=a2?a3=a4—is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.

Abstract: This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

Abstract: The present invention provides sodium channel blockers represented by formula (I): where the structural variables are defined herein. The compounds of the present invention may be used for treating a variety of conditions as described herein.

Abstract: The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptabl

Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.