Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which the

Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which th

Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.

Abstract: One aspect of the present invention relates to ionic liquids comprising a pendant Bronsted-acidic group, e.g., a sulfonic acid group. Another aspect of the present invention relates to the use of an ionic liquid comprising a pendant Bronsted-acidic group to catalyze a Bronsted-acid-catalyzed chemical reaction. A third aspect of the present invention relates to ionic liquids comprising a pendant nucleophilic group, e.g., an amine. Still another aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to catalyze a nucleophile-assisted chemical reaction. A fifth aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to remove a gaseous impurity, e.g., carbon dioxide, from a gas, e.g., sour natural gas.

Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.

Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.

Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.

Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.

Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.

Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which the

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: This invention relates to an improved method for crystallizing 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, the present invention provides an industrial process for crystallization of Compound A by evaporating methanol and water from the mother liquor after an initial crystallization of Compound A following the acetylation reaction. Specifically, the mother liquor is maintained at more than about 75% (v/v) of water and less than about 25% (v/v) of alcoholic solvent.

Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

Abstract: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: This invention relates to active pharmaceutical ingredients (APIs) with specific water surface areas, to pharmaceutical compositions comprising said APIs, to processes for preparing such compositions, and to methods for determining the water surface areas of substances such as APIs and other particles.

Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.

Abstract: A process for the preparation of N-[3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl]-N-ethyl acetamide of formula II, comprising reacting a compound N-[3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl]acetamide of formula III, with an ethylating agent in the presence of a strong alkali metal hydroxide and a phase transfer catalyst in a polar-aprotic solvent, and a process for preparation of Zaleplon, which is substantially free of impurities using the said compound of formula II.

Abstract: Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined 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: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: This invention provides compounds of formula I where X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. The invention also provides pharmaceutical compositions comprising compounds of formula I. Such compounds are potassium channel modulators.

Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: A medicament containing, separately or together, (A) formoterol or a pharmaceutically acceptable salt thereof or a solvate of formoterol or said salt and (B) a tiotropium salt of a pharmaceutically acceptable acid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.

Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.

Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.

Abstract: The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.

Abstract: A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-&agr;-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.

Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.

Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.

Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.

Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.

Abstract: A purified acid addition salt of a (2S, 3S, 5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane, e.g., (2S, 3S, 5S)-2-tert-butoxycarbonylamino-3-hydroxy-5-amino-1,6-diphenylhexane, is obtained from its mixture, in an arbitrary ratio, with its (2S, 3S, 5R) stereoisomer in the presence of an inorganic or organic acid. The desired (2S, 3S, 5S) acid addition salt may be recovered from the mixture by, for example, recrystallization. These purified acid addition salts are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.