Abstract: Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, ?-aminooxylations, ?-hydroxyaminations, ?-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5- or 6-membered rings, having one or more chiral centers. Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention provides an isoquinuclidine derivative which can be used to easily synthesize oseltamivir or an analog thereof. In particular, the present invention provides an isoquinuclidine derivative represented by the following formula (1) or an enantiomer thereof: wherein in the formula (1), A represents a protective group for the nitrogen atom; R1 to R1 each independently represent an alkyl group which may have a substituent, an aryl group which may have a substituent, or a hydrogen atom; and X represents a halogen atom.

Abstract: The invention provides an improved process for the preparation and purification of Varenicline and intermediates for the preparation of Varenicline.

Abstract: The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.

Abstract: Disclosed are a photosensitive compound containing oxime group which is directly decomposed by exposure to light, which is a molecular resist whose size is smaller than conventional polymer for photoresist, and a photoresist composition including the same. The photosensitive molecular compound has a structure represented by a following formula. In Formula, R1 is hydrogen atom or methyl group (CH3); Ra and Rb each is independently alkyl group of 1-6 carbon atoms, alkylcarbonyl group of 2-7 carbon atoms, aryl group of 6-10 carbon atoms or arylcarbonyl group of 7-11 carbon atoms, and Ra and Rb form one group as an united body, alkyl or cycloalkyl group of 1-20 carbon atoms or arylalkyl group of 7-20 carbon atoms which are doubly bonded to nitrogen atom.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: A compound of Formula I, a pharmaceutically-acceptable salt or a hydrate thereof, wherein R1 is H, or C1-4 alkyl; R2 is H, halogen, or C1, alkyl; R3 is H, halogen, or C1-4 alkyl, and R4 is C1-6 alkyl, aryl; or ?CR3R4 is cyclopentylidene, cyclohexylidene, 1-methylpiperidin-4-ylidene, or inden-1-ylidene; R5 is independently at each occurrence F, Cl, Br, CF3, R9, OR9, NR9R10, NO2, CN, COOR9, O2CR9, CONR9R10, NR9C(O)R10, heterocyclic group, aryl, or a group of Formula II; R6 is H, halogen, or C1-4 alkyl; R7 is H, halogen, or C1-4 alkyl; R8 is H, C1, alkyl group; R9 is H, or C1-6 alkyl; R10 is H, or C1-6 alkyl; R11 is H, or C1-4 alkyl; R12 is H, or C1-4 alkyl; m is 0, 1, or 2; when R5 is F, Cl, Br, CF3, R9, OR9, NR9R10, NO2, CN, COOR9, O2CR9, CONR9R10, NR9C(O)R10, heterocyclic group, or aryl, n is 1, 2, 3, or 4; when R5 is the group of Formula II, n is 0, 1, 2, 3, or 4; x is 0, 1, 2, 3, or 4.

Abstract: The present invention provides methods of ameliorating or reducing the extent of ischemic injury, reperfusion injury, and myocardial infarction, by administering an inhibitor of histone deacetylase enzyme (HDAC) or an inhibitor of DNA methyltransferase enzyme (DNMT).

Abstract: Provided are crystalline forms of dolasetron trifluoroacetate, methods for their preparation, and their use in preparing dolasetron mesylate.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2OH, —CH2NH2, —NHSO2CH3, Q is O or S and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

Abstract: Substituted tricyclic piperidone derivatives corresponding to Formula I: a method for producing such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds to treat pain, depression, urinary incontinence, diarrhea, pruritus, alcohol and drug abuse, drug dependency, lethargy and/or anxiety.

Abstract: The invention relates to compounds that are substituted azaadamantane ester and carbamate derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a benzazocine moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein B, J, K, Z, R, Ra, Rb, Rc, Rd, Rq, Rw, m and n are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two hydrogen atoms on a nitrogen atom, and carbon dioxide.

Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.

Abstract: The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and/or norepinephrine reuptake. Also provided herein are pharmaceutical compositions comprising novel tropane analogs and a pharmaceutically acceptable carrier, and methods for treating conditions in which inhibition of reuptake of monoamines is desired. The inventive compositions as described herein are also useful for medical therapy and diagnosis.

Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.

Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases

Abstract: Pharmaceutical compositions comprising compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, in combination with another therapeutic agent and methods of using such combinations in the treatment of neurological and psychological disorders.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.

Abstract: This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine and related compounds, in which an opioid compound is linked via the nitrogen at position 17 to a spacer group, which in turn is linked to a charged group, or a pharmaceutically acceptable salt thereof. In particularly preferred embodiments the opioid compound is morphine, codeine, or buprenorphine.

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, 1

Abstract: The present invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3 -benzazocin-10-ols of general formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as set forth herein, processes for preparing them, pharmaceutical compositions thereof and their use in treating or preventing a disease or disorder by blocking the voltage-dependent sodium channel.

Abstract: The present invention relates to novel fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula 1

Abstract: This invention is directed to compounds of the formula (I): 1

Abstract: The present invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ols of general formula 1 1

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts

Abstract: Compounds of the formula 1

Abstract: Compounds of the formula 1

Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.

Abstract: Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.

Abstract: Compounds of the formula 1

Abstract: Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: 1

Abstract: Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which are identical or different, are each hydrogen, C1-C6-alkyl, C1--C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4 and R5, which are identical or different, are each hydrogen, methyl, or ethyl; R6 is hydrogen; X is NH2, NH—(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which are identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH2—, —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—,

Abstract: Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which may be identical or different, are each hydrogen, C1-C6-alkyl, C1-C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4, R5, and R6, which may be identical or different, are each hydrogen, methyl, or ethyl; X is NH2, NH-(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which may be identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH213 , —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—,  the

Abstract: Intermediates useful for the synthesis of huperzine A represented by the structures below, and methods for their synthesis, wherein: R1 is lower alkyl, benzyl, or substituted benzyl; X is a suitable leaving group; Y is an electron withdrawing group that can subsequently be converted into an amino group; one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.

Abstract: The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is or R″ and Y together form ═CH; R is (C1-C5) alkyl, wherein n is 0 or 1, X is H, (C1-C5) alkyl; (C1-C5) alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis-(C1-C5) alkyl; —(CH2)m COOZ, wherein m=0-5, Z is H or (C1-C5) alkyl; —CH═CH—G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl substituted by (C1-C5) alkyl at the nitrogen atom; R′ is H, (C1-C5) alkyl, pyridoyl, benzoyl substituted by (C1-C5) alkyloxy; R″ is H or (C1-C5) alkyl; processes for their use as acetylcholinesterase inhibitor.