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: 2017-05-03

Provided is a pharmaceutical composition for oral administration enabling improved solubility, improved dissolution properties, and improved oral absorbability of (2R)-N-({5-[3-(2,5-difluorophenyl)-2-(1,3-dihydro-2H-benzimidazole-2-ylidene)-3-oxopropanoyl]-2-fluorophenyl}sulfonyl)-2-hydroxypropane imide amide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, as well as size reduction. The pharmaceutical composition for oral administration contains an amorphous form of compound A or its pharmaceutically acceptable salt, and a polymer.


Patent
Astellas Pharma Inc. | Date: 2017-05-24

[Problem] To provide an anti-human Tie2 antibody which prevents or treats diabetic macular edema, diabetic retinopathy, or critical limb ischaemia by binding to human Tie2 and activating human Tie2. [Solution] The inventors of the present invention studied anti-human Tie2 antibodies and have provided an anti-human Tie2 antibody including four heavy chain variable regions and four light chain variable regions. The heavy chain variable regions comprise an amino acid sequence from amino acid no. 1 to 122 of SEQ ID NO:2, and the light chain variable regions comprise an amino acid sequence from amino acid no. 1 to 113 of SEQ ID NO:4. One of the heavy chain variable regions and one of the light chain variable regions constitute one antigen-binding site, and the antibody includes four antigen-binding sites.


Patent
Astellas Pharma Inc. | Date: 2017-06-14

[Problem] To provide an anti-human Ig antibody in which BCR and FcRIIb are crosslinked and which has a more enhanced immunosuppressive function compared to conventional antibodies. [Solution] An anti-human Ig antibody including: a heavy-chain variable region that includes a CDR 1 comprising an amino acid sequence from amino acid numbers 31-35 of SEQ ID NO: 2, a CDR 2 comprising an amino acid sequence from amino acid numbers 50-65 of SEQ ID NO: 2, and a CDR 3 comprising an amino acid sequence from amino acid numbers 98-108 of SEQ ID NO: 2; a light-chain variable region that includes a CDR 1 comprising an amino acid sequence from amino acid numbers 24-38 of SEQ ID NO: 4, a CDR 2 comprising an amino acid sequence from amino acid numbers 54-60 of SEQ ID NO: 4, and a CDR 3 comprising an animo acid sequence from amino acid numbers 93-101 of SEQ ID NO: 4; and a heavy-chain constant region, said region being a human Ig1 constant region having S239D, H268D, and L328W amino acid variations.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2016-09-27

As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

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