Yaizu, Japan
Yaizu, Japan

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Patent
Bend Research Inc., Medivation Prostate Therapeutics Inc. and Astellas Pharma Inc. | Date: 2016-02-08

This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.


Patent
Astellas Pharma Inc. | Date: 2016-09-07

[Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an 7 nicotinic acetylcholine receptor (7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an 7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an 7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an 7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimers disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.


Patent
Astellas Pharma Inc. | Date: 2016-12-13

The present invention relates to a granular pharmaceutical composition obtained by coating a nucleus with: (1) a layer containing a material having a damp-proofing function, and (2) a drug layer containing linaclotide, a pharmaceutically acceptable salt, or a hydrate thereof, and (3) a layer containing a material having a damp-proofing function. Also, the present invention relates to a method for manufacturing the granular pharmaceutical composition obtained by coating the nucleus with (1) the layer containing the material having a damp-proofing function, (2) the drug layer containing the linaclotide, the pharmaceutically acceptable salt, or the hydrate thereof, and (3) the layer containing the material having a damp-proofing function.


Patent
Astellas Pharma Inc. | Date: 2017-01-04

[Problem] To provide a bispecific antibody for preventing or treating an immune inflammatory disease by acting on both human TLR2 and human TLR4 to inhibit human TLR2- and human TLR4-mediated immune inflammatory effects. [Means for Solution] Provided is a bispecific antibody for human TLR2 and human TLR4, including a heavy chain variable region of an anti-human TLR2 antibody consisting of the amino acid sequence of amino acid numbers 1 to 120 of SEQ ID NO: 4; a light chain variable region of an anti-human TLR2 antibody consisting of the amino acid sequence of amino acid numbers 1 to 113 of SEQ ID NO: 6; a heavy chain variable region of an anti-human TLR4 antibody consisting of the amino acid sequence of amino acid numbers 491 to 609 of SEQ ID NO: 4; and a light chain variable region of an anti-human TLR4 antibody consisting of the amino acid sequence of amino acid numbers 625 to 732 of SEQ ID NO: 4.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2017-04-05

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.


[Problem] Provided is a pharmaceutical composition for treating cancer in which one or more kinases of BTK, JAK3, and ITK is involved. [Means for Solution] The present inventors studied compounds having a BTK inhibiting effect, a JAK3 inhibiting effect and an ITK inhibiting effect, and confirmed that a specific pyrazine carboxamide compound has the BTK inhibiting effect, the JAK3 inhibiting effect, and the ITK inhibiting effect, and that a pharmaceutical composition comprising the compound as an active ingredient has a therapeutic effect on cancer in which one or more kinases of BTK, JAK3 and ITK is involved, in another aspect, cancer in which BTK is overexpressed or activated, in another aspect, cancer in which a B cell receptor signal is activated, in still another aspect, cancer in which JAK3 is activation-mutated or activated, and in still another aspect, cancer in which ITK is activated, thereby completing the present invention.


Patent
Astellas Pharma Inc. | Date: 2017-02-01

[Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition, e.g., a pharmaceutical composition for the treatment of chronic renal failure and/or diabetic nephropathy. [Solution] The inventors conducted in-depth studies of compounds having an EP4 receptor-antagonizing effect, discovered an amide compound or salt thereof having an EP4 receptor-antagonizing effect, and perfected the present invention. The amide compound or salt thereof has an EP4 receptor-antagonizing effect and can be used as an active ingredient of a pharmaceutical composition for the prevention and/or treatment of various diseases in which EP4 is involved, e.g., chronic renal failure and/or diabetic nephropathy.


Patent
Astellas Pharma Inc. | Date: 2017-04-12

To provide a compound useful as an active ingredient of a pharmacological composition for the treatment of urinary storage symptoms, dysuria, lower urinary tract diseases, and the like. [Solution] The inventors perfected the present invention after discovering that thiazole derivatives substituted at position 2 by pyrazinylcarbonylamino are exceptional muscarinic M_(3) receptor positive allosteric modulators and can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M_(3) receptors. The 2-acylaminothiazole derivatives or salts thereof of the present invention can be expected to serve as agents for the prevention or treatment of urinary bladder and urinary tract diseases involving bladder contraction mediated by muscarinic M_(3) receptors, e.g., underactive bladder and the like.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2016-04-20

Provided is the compound 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide or a salt thereof for use in a method for preventing and/or treating acute myelocytic leukemia or atypical chronic myelocytic leukemia.


Patent
Astellas Pharma Inc. | Date: 2016-09-14

The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.

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