Abstract: The present invention relates to novel crystalline forms of (R)—N—((S)-1-(4-(3,3-dimethyl-2-oxoindolin-1-yl)piperidin-1-yl)-1-oxo-4-phenylbutan-2-yl)piperidine-3-carboxamide hydrochloride (HCl-salt), and to pharmaceutical compositions thereof, process for preparation or isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of various diseases or disorders which are mediated by motilin receptor activity.

Abstract: The present invention relates to heterocyclic derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which 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 voltage gated sodium channels are involved.

Abstract: The present invention relates to 3-hydroxyoxindole derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 is 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 CRHR2 is involved.

Abstract: The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is 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 CRHR1 and/or CRHR2 is involved.

Abstract: This invention relates to pyrimidin-4(3H)-one derivatives that act as modulators of the TRPV4 receptor. The present invention also relates to processes for the preparation of novel pyrimidin-4(3H)-one derivatives and to their use in the treatment of a wide range of diseases, syndromes, and disorders, in particular for the treatment of inflammatory, pain, and urological diseases or disorders.

Abstract: The present invention provides a method for selecting a cancer patient for whom a combination therapy with a retinoid and a cancer treatment agent is effective, which comprises a step of selecting a cancer patient having a malignant tumor with the infiltration of cancer-associated fibroblasts in the stroma. In addition, the present invention provides a medicament which comprises a cancer patient having a malignant tumor with the infiltration of cancer-associated fibroblasts in the stroma is a subject and is administered in combination of a retinoid and a cancer therapeutic agent.

Abstract: The present invention relates to a use of compounds having TRPV4 inhibitory activity or pharmaceutically acceptable salts thereof, or pharmaceutical compositions containing them for the manufacture of a medicament for preventing or treating a retinal disease accompanied with blood flow disorder or cell disorder. It also relates to a method for preventing or treating the disease, wherein the method comprises administering the compounds or the pharmaceutical compositions containing them to humans or animals. The compounds, the pharmaceutically acceptable salts thereof, or the pharmaceutical compositions containing them may be used in combination with one or more second active agents. The present invention relates to a pharmaceutical composition and a kit containing a compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof, which is used for preventing or treating the disease.

Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

Abstract: The present invention relates to heterocyclic derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which 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 voltage gated sodium channels are involved.

Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which 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 voltage gated sodium channels are involved.

Abstract: A medicament for preventing or treating heart failure containing an antagonist of the corticotropin releasing hormone receptor 2 as an active ingredient.

Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

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 biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is 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 voltage gated sodium channels are involved.

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 tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

Abstract: The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is 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 CRHR1 and/or CRHR2 is involved.

Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

Abstract: The present invention relates to biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is 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 voltage gated sodium channels are involved.

Abstract: The present invention relates to a use of benzimidazole derivative compounds for improvement and treatment of nocturnal acid breakthrough (NAB). The benzimidazole derivative compounds can more effectively prevent and treat gastric acid-related diseases by effectively improving and treating nocturnal nocturnal acid breakthrough symptoms.