Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blocker such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.

Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.

Abstract: The present invention provides a pharmaceutical composition which prevents from decreasing the blood exposure of the third generation coxib-drugs, a process for preparing the said pharmaceutical composition and its use. It has been founded in this invention that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can afford a pharmaceutical composition which can prevent from decreasing the blood exposure, AUC and bioavailability. The pharmaceutical composition of the present invention has also good stability, which is useful for drugs. Namely, the technological thought that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can prevent from decreasing the blood exposure, AUC and bioavailability has been established in this invention.

Abstract: An adsorption carrier-packed column includes a central pipe, adsorption carrier, plate A, and plate B, wherein an insertion material C is inserted between the adsorption carrier and the plate A; an insertion material D is inserted between the adsorption carrier and the plate B; the ratio of the deformation rate of the insertion material C (C1) to the deformation rate of the adsorption carrier (E0) is 1<C1/E0<10, and the ratio of the deformation rate of the insertion material D (D1) to the deformation rate of the adsorption carrier (E0) is 1<D1/E0<10; and the ratio of the thickness of the insertion material C (TC) to the distance of a gap between the adsorption carrier and the plate A (LA) is 1.1<TC/LA<4, and the ratio of the thickness of the insertion material D (TD) to the distance of a gap between the adsorption carrier and the plate B (LB) is 1.1<TD/LB<4.

Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.

Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blocker such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.

Abstract: The present invention provides a pharmaceutical composition which prevents from decreasing the blood exposure of the third generation coxib-drugs, a process for preparing the said pharmaceutical composition and its use. It has been founded in this invention that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can afford a pharmaceutical composition which can prevent from decreasing the blood exposure, AUC and bioavailability. The pharmaceutical composition of the present invention has also good stability, which is useful for drugs. Namely, the technological thought that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can prevent from decreasing the blood exposure, AUC and bioavailability has been established in this invention.

Abstract: The present invention relates to use of a compound of the present invention or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, for the manufacture of a medicament for the treatment of cachexia. The invention also relates to a method for the treatment of cachexia, comprising administering the compound of the present invention or a pharmaceutical composition comprising the same to a human or an animal. The invention further relates to use of said compound, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt, in combination with one or more second active agents. Moreover, the invention relates to a pharmaceutical composition and a kit comprising the compound of the present invention or a pharmaceutically acceptable salt thereof, for the treatment of said disease.

Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.

Abstract: It was found that an antibody containing the amino acid sequences described in the sequence listing as SEQ ID NOS: 1 to 6 was an antibody having reactivity also to ovarian cancer, as well as the cancer species known so far such as gastric cancer, colon cancer and breast cancer, and was useful as an ovarian cancer tissue-specific diagnostic and/or therapeutic agent.

Abstract: There is provided a novel evaluation method for predicting the pharmacokinetics of PM using PM liver cells of drug metabolizing enzyme cytochrome P450 having a genetic polymorphism. According to the present invention, the pharmacokinetics (metabolism) of PM can be predicted by using PM liver cells of CYP2D6among drug metabolizing enzyme cytochrome P450 known to have a genetic polymorphism.

Abstract: This invention provides a method for predicting pharmacokinetic properties of molecules comprising the steps of:

Abstract: Compounds of the formula wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: This invention relates to a method for evaluating the susceptibility of pharmaceutical drugs to metabolism by a specific cytochrome P-450 isozyme, which comprises contacting the sample compound with a reagent composition prepared by adding the specific cytochrome P-450 isozyme to liver microsomes lacking said specific cytochrome P-450 isozyme in a carrier material. More particularly, this invention relates to a useful in vitro quantitative assay for drug metabolism by P-450 isozymes such as CYP2D6, CYP2C19, and CYP2A6. This invention also relates to a reagent composition which is useful for said in vitro assay.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: This invention relates to the quinuclidine derivative (2S, 3S)-N-(5-n-propyl-2-methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo?2.2 .2!octan-3-amine and its pharmaceutically acceptable salts. These compounds are substance P antagonists and are useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.