Abstract: Compounds of Formula I: I (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.

Abstract: The present invention relates to spiroindoline modulators of muscarinic receptors. The present invention also provides compositions comprising such spiroindoline modulators, and methods therewith for treating muscarinic receptor mediated diseases.

Abstract: The invention relates to a method for relieving or ameliorating symptoms of gastroesophageal reflux disease by administering a medicament that includes the cholecystokin-2 (CCK-2) receptor antagonist itriglumide and a proton pump inhibitor (PPI).

Abstract: A method of treating a disorder such as rheumatoid arthritis or multiple sclerosis in a subject is carried out by administering to the subject a composition comprising a modulator compound of Th1 differentiation or Th17 expansion.

Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, m, A, R1 and R2 have the significance given in the description. The compounds are useful as HSL inhibitors and may be used in the treatment or prophylaxis of diabetes, dyslipidemia, atherosclerosis or obesity.

Abstract: The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal insufficiency, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.

Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

Abstract: The present invention generally relates to compounds and pharmaceutical compositions containing the compounds. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

Abstract: The invention is related to compounds of formula (I) that can be used as antagonists of the TGF? family type I receptors, Alk5 and/or Alk4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGF? family signaling activity is desirable.

Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention provides a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention provides a compound represented by the formula (I): wherein each symbol is as in the specification, or a salt thereof.

Abstract: The present invention is directed to compounds of Formula I: Formula I: Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention relates to certain pharmaceutical compositions containing at least one vasopressin receptor antagonist and at least one angiotensin receptor blocker (ARB) and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of vasopressin and/or angiotensin-mediated disorders.

Abstract: The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: The invention is directed to nonpeptide substituted benzazepines of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension, among others disclosed. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.

Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the ? opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other ? opioid receptor-mediated conditions.

Abstract: Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X? is pharmaceutical acceptable organic or inorganic anion.

Abstract: The invention relates to organic compounds which have interesting pharmaceutical properties. In particular, the compounds are useful in the treatment and/or prevention of infections such as those caused by Plasmodium falciparum, Plasmodium vivax, Plasmodium malariae, Plasmodium ovale, Trypanosoma cruzi and parasites of the Leishmania genus such as, for example, Leishmania donovani. The invention also relates to pharmaceutical compositions containing the compounds, as well as processes for their preparation.

Abstract: Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: The invention relates to compounds of formula (I): along with pharmaceutical compositions containing the same and methods of use thereof.

Abstract: The present invention provides an enantiomerically pure compound of Formula I: along with pharmaceutical formulations containing the same and methods of use thereof.

Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.

Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.

Abstract: Disclosed are chemical entities including compounds of Formula I and pharmaceutically acceptable salts thereof, wherein X is chosen from CN, CF3, CF2H, S(O)nR8, and S(O)2N(R9)R10; Y is chosen from CR11 and N; Z is chosen from O and NH; R3 is chosen from —C(O)R12 and —C(O)N(R9)R10; and n, R1, R2 and R4-R12 are defined herein; compositions comprising one or more such chemical entities; and methods of using one or more such chemical entities for modulating the activity of certain receptors (e.g., farnesoid X) or for the treatment or prevention of one or more symptoms of disease or disorder related to the activity of those receptors.

Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract: Described herein are compounds that have a spiro structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent diseases or conditions associated with the activity of steroid hormone nuclear receptors.

Abstract: The present invention relates to certain pharmaceutical compositions containing at least one vasopressin receptor antagonist and at least one angiotensin converting enzyme (ACE) inhibitor and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of vasopressin and/or angiotensin converting enzyme mediated disorders.

Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.

Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).

Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.

Abstract: Pharmaceutical compositions containing substituted aminoalcohols, the use of preparations containing substituted aminoalcohols for treatment of conditions such as pain, emesis, neurotropic conditions, cardiovascular diseases, urinary incontinence, diarrhea, pruritus, alcohol or drug dependency, inflammation, depression, decreased vigilance, or depressed libido, as well as 2-(aminomethyl)cycloalkane-1-ol compounds and a process for their preparation.

Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract: The present invention relates to the use of a 2-cyanopyrimidine compound of the formula wherein R1, R2, R3 and X are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in tautomeric form, as an inhibitor of the activity of cathepsin S.

Abstract: The present invention provides new substituted prolinamides of the general formula (I) in which D, L, E, G, J, M, R3, R4, R5, and R13 are defined as in claim 1, their tautomers, their enantiomers, their diastereomers, their mixtures and their salts, more particularly their physiologically tolerated salts with organic or inorganic acids or bases, which exhibit valuable properties.

Abstract: The use of a compound of formula I, wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; R?, R2, R3, R4, R8 and Ra are specified organic groups and p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; provided that when p is 2 then q is not 2; p+q is 1, 2, 3, 4, 5 or 6; or salts or N-oxides thereof or compositions containing them and their using in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.

Abstract: The present invention is directed to a compound of Formula (I) or a form thereof: wherein U, V, W and Ring A are as defined herein, useful as vasopressin receptor antagonists.

Abstract: The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.

Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3, R4 and R5 are as described herein. The compounds exhibit anticancer activity.

Abstract: Substituted azaspiro derivatives of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).