Astellas Pharma Inc.

Yaizu, Japan

Astellas Pharma Inc.

Yaizu, Japan
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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. | 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.


[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. 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.


Patent
Astellas Pharma Inc. and Cytokinetics Inc. | Date: 2017-07-19

The problem to be solved by the present invention is to provide a novel pharmaceutical composition for prevention and/or treatment of urinary incontinence, which differs from conventional drugs. The present invention provides a therapeutic agent for prevention and/or treatment of urinary incontinence having 1-[2-({[trans-3-fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methyl}amino)pyrimidin-5-yl]-1 H-pyrrole-3-carboxamide or a salt thereof, as an active ingredient.


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. | 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: 2017-04-12

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. | Date: 2017-09-27

[Problem] Provided is a bispecific antibody with a novel format that retains high binding affinity to both antigens, and can be efficiently produced in a commercial production process. [Means for Solution] A bispecific antibody comprising two heavy chains, two first light chains, and two second light chains, in which the heavy chains each comprise a first heavy chain variable region, a CH1 region, a first linker, a second heavy chain variable region, and a heavy chain constant region in order from the amino terminus side; the first light chains comprise a first light chain variable region and a first light chain constant region; the second light chains comprise a second light chain variable region and a second light chain constant region; the first heavy chain variable region and the first light chain variable region form a first antigen binding site; the second heavy chain variable region and the second light chain variable region form a second antigen binding site; and the first antigen binding site and the second antigen binding site recognize different antigens each other.

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