Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.

Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial 3 to 6 days of treatment the daily dosage is raised so that in total the R-fold (R being the accumulation factor) standard daily dosage is administered and thereafter continued at the standard daily dosage or at a daily dosage lower than the standard daily dosage.

Abstract: Immune-modulators of formula (I) below are prepared: A pharmaceutical composition contains the immune-modulators. The pharmaceutical composition is used as a drug, especially as an immune-modulating drug. The compound can be used in treatment of immune disorders and for immune suppression. Thus, for example, the compound can be used in treating hypo-immunity, rejection after organ transplantation and auto-immune disease.

Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.

Abstract: Disclosed are pharmaceutical combinations comprising at least one S1P receptor agonist, as well as a method for treating demyelinating diseases, e.g. multiple sclerosis or disorders associated therewith or Guillain-Barré syndrome, comprising co-administration, e.g. concomitantly or in sequence, of a therapeutically effective amount of a) an S1P receptor agonist, and b) at least one co-agent shown to have clinical activity against at least one symptom of a demyelinating disease.

Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.

Abstract: The present application provide processes for the preparation of fingolimod and its pharmaceutically acceptable salts, process for the purification of fingolimod hydrochloride and process for the preparation of amorphous fingolimod hydrochloride.

Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.

Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage

Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.

Abstract: The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+)benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol.

Abstract: The invention relates to compounds which are agonists of at least one receptor selected from S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5 receptors, for use in methods for treating HIV infections in humans or animals.

Abstract: Disclosed are compounds of formula I wherein R1, R2, R5 and R6 are as defined in the claims; such compounds have interesting pharmacological properties.

Abstract: Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical composition thereof.

Abstract: The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof. The application provides processes for preparation of crystalline polymorphic forms-?, ? and ? substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which are useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment or prevention of autoimmune related disorder including multiple sclerosis.

Abstract: Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).

Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.

Abstract: The present invention relates to pharmaceutical compositions comprising a 2-amino-2-[2-(4-C2-20-alkyl-phenypethyl]propane-1,3-diol compound or a pharmaceutically acceptable salt thereof, and to the use thereof for treating, preventing or delaying the progression of multiple sclerosis in a paediatric patient or a patient suffering from a specific condition.

Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.

Abstract: S1P receptor modulators are administered following a dosage regimen providing a positive benefit-risk profile.

Abstract: There are provided new iodo- and bromo-compounds, and their use as diagnostic agents and imaging agents for diseases and disorders wherein S1P receptor expression is altered.

Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.

Abstract: Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical compositions thereof.

Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.

Abstract: The present invention provides a convenient and efficient process for the preparation of O-desmethylvenlafaxine (ODV), comprising the reaction of venlafaxine, or a salt thereof, with a thiol reagent such as a dithiol, an aminothiol or an inorganic thiol. The present invention also provides a process for purifying ODV base, said process comprising the steps of mixing crude ODV base with an alcohol to form a suspension and adding acid followed by base to generate ODV base with high purity.

Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.

Abstract: The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.

Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

Abstract: Therapeutic compounds based on synthetic sphingolipid analogs are provided, particularly alkylthiophenyl substituted ceramide analogs, suitable for treating degenerative, infectious, and other diseases.

Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

Abstract: To provide a medicament which efficiently expresses an immunosuppressive agent or an anti-inflammatory agent and reduces expression of side effect. A medicament includes diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, in combination with an immunosuppressive agent and/or an anti-inflammatory agent.

Abstract: A medicine which effectively functions as an immunosuppressant or anti-inflammatory agent and is effective in diminishing the occurrence of side effects. The medicine comprises a combination of: a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure and having the function of diminishing lymphocytes circulating through the periphery; and an immunosuppressant and/or an anti-inflammatory agent.

Abstract: The present invention relates to process for the preparation of novel crystalline Desmethylvenlafaxine succinate polymorphic Forms-A, B. The present invention also relates to novel processes for the preparation of 0-Desmethylvenlafaxine succinate polymorphic Forms-(I), (II), (III) and amorphous.

Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .

Abstract: Drug discovery is a complex undertaking facing many challenges, not the least of which is a high attrition rate as many promising candidates prove ineffective or toxic in the clinic owing to a poor understanding of the diseases, and thus the biological systems, they target. Therefore, it is broadly agreed that to increase the productivity of drug discovery one needs a far deeper understanding of the molecular mechanisms of diseases, taking into account the full biological context of the drug target and moving beyond individual genes and proteins. The present methods rely on the use of label-free cellular assays, particularly the DMR index, to systematically display the mode of actions, the toxicity, and the target(s) and pathway(s) of any molecules.

Abstract: The present invention relates to a novel process for the preparation of O-desmethyl venlafaxine (ODV).

Abstract: A method for inhibiting therapeutic drug resistance within a cell over-expressing a membrane protein is provided. The method comprises synthesizing a dimeric prodrug inhibitor of a monomeric therapeutic agent; administering the dimeric prodrug inhibitor to the membrane protein together with the monomeric therapeutic agent; and occupying at least one substrate binding site of the membrane protein with the synthesized dimeric prodrug to allow the monomeric therapeutic agent to accumulate within the cell. The dimeric prodrug inhibitor contains a crosslinking agent that is adapted to breakdown under reducing conditions within the cytosol of the cell to cause the dimeric prodrug to revert back to a form equivalent to the monomeric therapeutic agent.

Abstract: The present invention relates to crystalline forms of O-desmethyl venlafaxine (ODV) succinate monohydrate, namely Forms I and II, in pure form and to novel processes for their preparation. The present invention provides a process for the preparation of Form II free of Form I and a process for the preparation of Form I free of Form II. The present invention provides direct methods for the preparation of ODV succinate Form II from ODV free base and for the preparation of ODV succinate Form I from ODV free base.

Abstract: This invention provides pharmaceutically active enantiomers of the venlafaxine metabolite O-Desmethyl venlafaxine, R(?)-4-[2-(Dimethylamino-1-(1-hydroxycyclo-hexyl)ethyl]phenol or R(?)1-[2-(dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclo-hexanol, and S(+)-1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol or S(+)-4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol, or one or more pharmaceutically acceptable salts or salt hydrates thereof, as well as pharmaceutical compositions utilizing these enantiomers and methods of using the enantiomers to treat, inhibit or control central nervous system disorders.

Abstract: This invention relates to compounds with the formula (I) given below or one of their pharmaceutically acceptable salts, as a medicine; Formula (I) of pharmaceutical compositions comprising one or more compounds with Formula (I) as active constituent, use of compounds with Formula (I) for the preparation of compositions designed to prevent or treat at least one illness involving an abnormal cellular proliferation, pro-apoptotic compositions and/or anti-proliferative compositions comprising at least one compound with Formula (I)/and the use of compounds with formula (I) as pro-apoptotic and/or anti-proliferative agents.

Abstract: A process for preparing venlafaxine in a high yield as well as processes for producing venlafaxine hydrochloride of form I having a very hight polymorphic purity are described.

Abstract: The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a ?-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and/or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and/or growth in a mammal by administering a composition comprising a ?2-selective antagonist or agonist.

Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.

Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

Abstract: The present invention describes processes for the preparation of O-desmethylvenlafaxine and tridesmethylvenlafaxine, which may be used as an intermediate in preparing O-desmethylvenlafaxine.

Abstract: The present invention relates to a method for the prophylaxis or treatment of pain using compounds of formula I, in which R, R2, R3, R4 and R5 have the meanings indicated in the specification.

Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:

Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.