Abstract: A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.

Abstract: The present invention is directed to a regio- and stereoselective bioconversion of selected aliphatic dinitriles into corresponding cyanocarboxylic acids. More particularly, the present invention provides methods for the conversion of 2-isobutyl-succinonitrile into (S)-3 cyano-5-methylhexanoic acid, which is a useful intermediate in the synthesis of (S)-3(aminomethyl)-5-methylhexanoic acid (pregabalin). Pregabalin can be used for treating certain cerebral diseases, for example, in the treatment and prevention of seizure disorders, pain, and psychotic disorders.

Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.

Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 are as described herein; compositions thereof; and uses thereof.

Abstract: The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or “chiral tetralone.” The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).

Abstract: The present invention relates to microbial processes for carrying out the asymmetric reduction of a ketone to an alcohol, which comprises: contacting the ketone with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield more of the desired (R)-enantiomer of the corresponding alcohol than the undesired (S)-enantiomer. The chiral (R)-enantiomer can be used in the synthesis of certain &bgr;-adrenergic receptor agonists.

Abstract: The present invention provides novel processes for preparing 3(S)-[(5-chloro-1H-indole-2-carbonyl)-amino]-2(R)-hydroxy-4-phenyl-butyric acid. Also provided are novel intermediates used in those processes. Further, the 3(S)-[(5-chloro-1H-indole-2-carbonyl)-amino]-2(R)-hydroxy-4-phenyl-butyric acid prepared by the novel processes can be further reacted to yield known indole 2-carboxamides and derivatives thereof possessing glycogen phosphorylase inhibitory activity, which are useful in the treatment of mammals, especially human beings, having glycogen phosphorylase dependent diseases or conditions.

Abstract: The present invention relates to processes for the microbial oxidation of 2-methylquinoxaline to 2-quinoxalinecarboxylic acid which comprise contacting 2-methylquinoxaline with a microorganism, or a suitable mutant thereof, and incubating the resulting mixture under conditions sufficient to yield an amount of said 2-quinoxalinecarboxylic acid. The present processes optionally further comprise the isolation and purification of 2-quinoxalinecarboxylic acid.

Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

Abstract: The present invention relates to methods for treating congestive heart failure in a mammal by administering a congestive heart failure treating amount of a compound which inhibits phosphodiesterase type IV and the production of tumor necrosis factor, such as, for example, a substituted indazol derivative, e.g., of the formula or a pharmaceutically acceptable salt thereof, wherein R, R1 and R2 are as defined herein. The invention further relates to pharmaceutical compositions for the treatment of congestive heart failure comprising a congestive heart failure treating amount of a compound which inhibits phosphodiesterase type IV and the production of tumor necrosis factor, such as, for example, a substituted indazol derivative, e.g., of formula (I) herein, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable vehicle, diluent or carrier.

Abstract: This invention relates to suspensions for oral administration comprising novel trovafloxacin zwitterionic crystals, and processes for preparing such crystals. This invention further relates to other pharmaceutical compositions comprising these novel crystals, and to methods of using these suspensions, and these novel crystals in such other dosage forms, for treating bacterial infections in mammals.

Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and X are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

Abstract: The present invention relates to certain compounds of the formula (I), ##STR1## which are useful in the synthesis of certian .beta.-adrenergic receptor agonists. The invention also relates to a process for synthesizing the compounds of formula (I) and to compounds of the formula (II), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.4 are defined herein, which are useful in the synthesis of the compounds of formula (I). The invention also relates to a process for synthesizing a compound of formula (II). The invention further relates to processes for synthesizing compounds of formula (Z*), ##STR3## R.sup.1, R.sup.2 and Y.sup.2* are defined herein.

Abstract: The present invention relates to certain compounds of the formula (I), ##STR1## which are useful in the synthesis of certain .beta.-adrenergic receptor agonists. The invention also relates to a process for synthesizing the compounds of formula (I) and to compounds of the formula (II), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.4 are defined herein, which are useful in the synthesis of the compounds of formula (I). The invention also relates to a process for synthesizing a compound of formula (II). The invention further relates to processes for synthesizing compounds of formula (Z*), ##STR3## R.sup.1, R.sup.2 and Y.sup.2* are defined herein.

Abstract: Apparatus for spectrophotometric analysis of material in vials 16 in which material in each vial is subjected to a beam 4 at a scanning station 20. An array of the vials 16 is carried by a carousel 60 for each vial 16 automatically and sequentially to be delivered to the scanning station and thereafter removed following scanning by the beam 4. Rotation of the carousel 60 to feed the vials to the scanning station and to remove them from that station is controlled by a computer 3 which also controls spectrophotometric measurement of the material in the respective vials whilst at the scanning station.

Abstract: There are described devices for creating artistic designs which are simple in approach and execution, and which enable the user to create a unique work of art without the user coming into direct contact with the medium used to create the design.The subject devices comprise a first sheet and a second sheet, the sheets being in superposed relation, sealed around their periphery and defining a first area and a second area, a plurality of rupturable containers containing a spreadable medium, arranged in the first area and adapted to discharge the spreadable medium into the second area, provided that at least one of the sheets permits the viewing of the discharged spreadable medium.A kit is also provided which includes the subject device and additional materials, such as, for example, decorative materials for application to the device and materials with which to attach the device to various surfaces.

Abstract: This invention relates to a method for reducing morbidity and/or mortality in a mammal with congestive heart failure due to non-ischemic etiology comprising administering amlodipine or a pharmaceutically acceptable amlodipine acid addition salt, and, optionally, a diuretic and/or digoxin. The invention further relates to methods for treating patients with congestive heart failure due to non-ischemic etiology, comprising administering a non-ischemic congestive heart failure treating amount of amlodipine or a pharmaceutically acceptable amlodipine salt and, optionally, a diuretic and/or digoxin. The invention also provides a kit which comprises a container means and a) amlodipine and a diuretic, b) amlodipine and digoxin, or c) amlodipine, digoxin and a diuretic; and a kit which comprises a container means and a) amlodipine, an angiotensin converting enzyme (ACE) inhibitor and a diuretic, b) amlodipine, an ACE inhibitor and digoxin, or c) amlodipine, an ACE inhibitor, digoxin and a diuretic.

Abstract: There is described a novel process of polymerizing 4-vinyl pyridine monomer in an aqueous polymerization system which comprises preparing an aqueous solution of polyvinyl alcohol, and contacting said aqueous solution of a polyvinyl alcohol with less than about 10% by weight of 4-vinyl pyridine monomer and a water-soluble initiator capable of decomposing to give free radicals.The resultant dispersion of the novel polymerization process comprises a homogeneous, i.e., weight average molecular weight and particle size, poly-4-vinylpyridine, with no appreciable residual 4-vinyl pyridine monomer.The resultant dispersion may be used to coat image- and ink-receiving layers of image-recording materials and ink jet recording sheets, respectively.

Abstract: The present invention relates to an apparatus for spectrophotometric analysis of a material in a container by reflectance of a beam applied to the material through an aperture in a primary mask. A restricted beam resulting from the primary mask is applied through a port in an opaque secondary mask to the material. The restricted beam is wholly within the port and radiation reflected from the material passes through the port to detectors for analysis. The secondary mask defines by its port an area on the base of the container through which the restricted beam is applied to the material and is not subjected to spurious reflections and refractions otherwise created by the container between its base and side wall. The container may be spaced from the secondary mask and inclined relative thereto so that the secondary mask shields the top and bottom ends of the container.

Abstract: There are described diffusion transfer photosensitive film units which include a novel antihalation layer comprising an antihalation material, titanium dioxide and a binder. Diffusion transfer film units prepared according to the invention provide silver images of enhanced resolution, film speed and sharpness.