Abstract: The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections 4 erected on one support sheet, each microprojection 4 having a drug layer 5 soluble in vivo at its top part and having an intermediate layer 6 under the drug layer 5, the intermediate layer 6 containing a polymeric substance for adhesion of the drug layer 5 to the support sheet, the drug layer 5 at the top part of the microprojection 4 containing a single drug, the microprojections 4 holding difference types of drugs being arranged together on the support sheet 2.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: The present invention provides a microneedle patch which can solve the problem that microneedle production is difficult and requires high accuracy, the problem that time and mental burdens on a health professional and a patient are large, and the problem caused by compounding a plurality of drugs. The microneedle patch comprises a large number of drug-carrying microprojections 4 erected on one support sheet, each microprojection 4 having a drug layer 5 soluble in vivo at its top part and having an intermediate layer 6 under the drug layer 5, the intermediate layer 6 containing a polymeric substance for adhesion of the drug layer 5 to the support sheet, the drug layer 5 at the top part of the microprojection 4 containing a single drug, the microprojections 4 holding difference types of drugs being arranged together on the support sheet 2.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: A combination agent containing an LHRH receptor agonist or antagonist and an androgen receptor agonist, which is useful as an agent for the prophylaxis or treatment of hormone-dependent diseases and the like, is provided.

Abstract: The present invention provides a novel variant androgen receptor (ARaiv) lacking ligand binding domain, a nucleic acid encoding the same and use thereof. That is, the present invention provides a method of screening for a substance for the prophylaxis or treatment of cancer, which includes contacting an ARaiv protein or ARaiv-producing cell with a test compound, measuring the activity of ARaiv (e.g., transcription regulating action of androgen responsive gene) or expression level thereof, and selecting a compound that suppresses the activity or expression level.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.

Abstract: The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3? (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3? represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5? (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5? represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively.

Abstract: The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.

Abstract: The present invention provides a premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process, which contains a nonpeptidic compound having a gonadotropin releasing hormone antagonistic action. The premature ovulation inhibitor for use in in vitro fertilization or embryo transfer process of the present invention is low toxic, permits oral administration, and has a superior inhibitory effect on premature ovulation in in vitro fertilization or embryo transfer process.

Abstract: A combination agent containing an LHRH receptor agonist or antagonist and an androgen receptor agonist, which is useful as an agent for the prophylaxis or treatment of hormone-dependent diseases and the like, is provided.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4alkyl and (4?) a C1-4alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4alkoxy-C1-4alkyl, (3?) a mono-C1-4alkyl-carbamoyl-C1-4alkyl, (4?) a C1-4alkoxy and (5?) a mono-C1-4alkylcarbamoyl-C1-4alkoxy, or the like; R3 is a C1-4alkyl; R4 is a C1-4alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

Abstract: In the field of pharmaceuticals, it is intended to provide drugs whereby the preventive and therapeutic effects of a GnRH agonist on various diseases can be enhanced and QOL can be improved. More specifically, combination of drugs characterized in that the GnRH agonist is combined with a chemical selected from among SERM, SARM, sex hormone synthesis inhibitors, receptor-type tyrosine kinase inhibitors, bone metabolism regulators, drugs for immunotherapy, cytokine/chemokine inhibitors and endothelin receptor antagonists. Owing to these combinations, excellent effects of enhancing the preventive and therapeutic effects of the GnRH agonist on various diseases and relieving side effects can be established. Furthermore, QOL can be improved thereby.

Abstract: There are provided a fused pyrimidine compound having antagonistic activity against luteinizing hormone releasing hormone, and a medicine containing the compound. A luteinizing hormone releasing hormone antagonist containing a compound represented by the formula: wherein R1a is a hydrocarbon group which may be substituted or a hydrogen atom, ring Aa is a 6-membered aromatic ring which may be further substituted, ring Ba is a homocyclic or heterocyclic ring which may be further substituted, Wa is an oxygen atom or a sulfur atom, Xa1 and Xa2, which may be identical or different, are each a hydrogen atom, a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted, or Xa1 and Xa2 together may form an oxygen atom, a sulfur atom or NR3a (wherein R3a is a hydrocarbon group which may be substituted or a hydrogen atom), and Ya is C1-6 alkylene which may be substituted or a bond, or a salt or prodrug thereof.

Abstract: The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.

Abstract: A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and are useful for preventing and treating a mammal suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.