Abstract: The present invention describes a process for preparing N-substituted phthalimides of Formula I which are widely useful as intermediates in the preparation of organic compounds such as pharmaceuticals

Abstract: The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, ?-aminoacids, ?-aminoacids and derivatives thereof of Formula I: P-M-M1I or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Disclosed herein are novel spiro beta-lactone/gamma lactams for use in treating bacterial infections and cancer. The compounds are characterized by a terminal electron-withdrawing group such as a nitro group. Screening data shows antimicrobial activity against various bacterial cell lines, particularly gram-positive bacteria, and anti-cancer activity.

Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, M and L have the definitions as described herein.

Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein.

Abstract: The present invention provides a method for producing an optically active ?-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

Abstract: Selectively BRS-3-agonistic compounds of formula I wherein A1, A2, A3, R1, R2, R3, Ar1, Ar2, Ar3, m and n have the meanings given in the description, and also pharmaceutical compositions containing these compounds and a process for the preparation of compounds of Formula I are described.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: The present invention provides a process for preparing thiazole derivatives of formula (XI), that activate the delta subtype of the human Peroxisome Proliferator Activated Receptor (hPPAR?), and also provides processes for compounds of formula (VI), (VII), (VIII) and (IX), intermediate compounds for preparation of the above compounds of formula (XI).

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity.

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R5, R7, X, Y and U are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

Abstract: In one aspect, the invention provides a process for the preparation of compounds of Formula I wherein R1 is —CN, —OP, alkyl, aryl or heteroaryl; wherein P represents any suitable protecting group; and R2 is alkyl or aryl; by reacting a compound of Formula II wherein R1 is —CN, —OP, alkyl, aryl or heteroaryl; wherein P represents any suitable protecting group; and R2 is alkyl or aryl; with a reducing agent (e.g. sodium borohydride) in the presence of a metal halid (e.g. CeCl3) or a metal alkoxid (e.g. Ti(OiPr)4).

Abstract: The present invention relates to substituted Azetidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

Abstract: In one aspect, the invention provides a process for the preparation of an amorphous HMG-CoA reductase inhibitor and hydrates thereof of desired particle size, which comprises: dissolving the HMG-CoA reductase inhibitor in a hydroxylic solvent, and removing the solvent by freeze-drying.

Abstract: The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same.

Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.

Abstract: A compound having Formula I R1—Z—R2Formula I wherein R1 is an optionally substituted phenyl ring; R2 is or comprises an optionally substituted aromatic ring; and Z is —X—Y—L— or —Y—X—L— wherein either X is selected from —S(?O)(?O)— and —C(?O)—; and Y is —NR3—; or X is selected from —S(?O)(?O)— and —S—, and Y is —C(R4)(R5)—; L is an optional linker; and R3, R4 and R5 are each independently selected from H and hydrocarbyl; and wherein when R2 comprises the following structural moiety wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R1—C(?O)—NR3—L—R2; R1—S(?O)(?O)—C(R4)(R5)—L—R2; R1—S—C(R4)(R5)—L—R2; R1—NR3—S(?O)(?O)—L—R2; R1—NR3—C(?O)—L—R2; R1—C(R4)(R5)—S(?O)(?O)—L—R2; and R1—C(R4)(R5)—S—L—R2.