PATENTSCOPE: EN_ALL:nmr AND PA:astellas pharma

TETRAHYDROISOQUINOLINE DERIVATIVES (Fri, 18 Aug 2017)
Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.
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FORMULATIONS OF ENZALUTAMIDE (Fri, 21 Mar 2014)
This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
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TREATMENT OF NEUROINFLAMMATORY DISEASE WITH SELECTIVE COX1 INHIBITORS (Fri, 14 Dec 2012)
Highly selective COX1 inhibitors can be used to treat a neuroinflammatory disease.
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OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF (Fri, 27 Apr 2012)
The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.
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BRADYKININ RECEPTOR AGONISTS AND USES THEREOF TO TREAT OCULAR HYPERTENSION AND GLAUCOMA (Fri, 24 Feb 2012)
The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds arc bradykinin agonists, of formula (I).
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NOVEL SALT OF 1,3,5-TRIAZINE-2,4,6-TRIAMINE DERIVATIVE (Fri, 08 Oct 2010)
Anytime obtained is uniform crystal of N- (4-f luorophenyl) -N' -phenyl-N' ' - (pyrimidin-2-ylmethyl) -1, 3, 5-triazine-2, 4, 6-triamine (compound A) and/or N, N' -bis (4-f luorophenyl) -N' ' - (pyrimidin-2-ylmethyl) - 1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.
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COMPOSITIONS COMPRISING 2, 4, 6-TRIAMINO-1, 3, 5-TRIAZINE DERIVATIVES FOR TREATMENT OF SCHIZOPHRENIA (Fri, 08 Oct 2010)
The present invention is useful for providing an excellent pharmaceutical composition for prevention and/or treatment of schizophrenia, containing a BEC1 potassium channel inhibitor or a pharmaceutically acceptable salt thereof as an active ingredient, and is particularly useful for providing a pharmaceutical composition for prevention and/or treatment of the positive symptoms, negative symptoms, cognitive impairments and the like of schizophrenia.
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PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF (Fri, 01 Oct 2010)
Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
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PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF (Fri, 16 Apr 2010)
Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
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HETEROCYCLIC CARBOXAMIDE COMPOUNDS (Fri, 26 Mar 2010)
This invention relates to novel heterocyclic carboxamide derivatives and salts thereof. More particularly, it relates to novel heterocyclic carboxamide derivatives and salts thereof which act as a ROCK inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of ROCK-related disease.
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SORDARIN DERIVATIVES FOR PREVENTING OR TREATING INFECTIOUS DISEASES CAUSED BY PATHOGENIC MICROORGANISMS (Fri, 30 Oct 2009)
This invention relates to a new sordarin derivative or a pharmaceutically acceptable salt thereof, which has antimicrobial activities (especially, antifungal activities), to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases in a human being or an animal.
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PYRIDONE DERIVATIVES AS P38A MAPK INHIBITORS (Fri, 21 Nov 2008)
A compound represented by the formula (I): wherein R1 is lower alkyl, cycloalkyl or aromatic hydrocarbon ring, each of which is optionally substituted with one or more substituents; R2 is hydrogen atom, halogen atom, lower alkyl, halo(lower)alkyl or lower alkoxy; and R3 is (1) a group represented by the formula: wherein R4 is lower alkyl, etc.; (2) a group represented by the formula: wherein R5 is lower alkyl, etc.; (3) a group represented by the formula: wherein R6 is lower alkyl, etc.; or (4) a group selected from halogen atom, carboxy, hydroxy and lower alkoxy, or a salt thereof.
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NEW CYCLIC PEPTIDE COMPOUNDS (Fri, 21 Nov 2008)
The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.
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N-HYDROXYACRYLAMIDE COMPOUNDS (Fri, 27 Jun 2008)
A compound having the following formula (I) : wherein - R1 is hydrogen, optionally substituted lower alkyl, cyclo (lower) alkyl, cyclo (higher) alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo (lower) alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with -OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.
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POLYCYCLIC ACID COMPOUNDS USEFUL AS CRTH2 ANTAGONISTS AND ANTIALLERGIC AGENTS (Fri, 20 Jun 2008)
The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.
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CEPHEM COMPOUNDS AND USE AS ANTIMICROBIAL AGENTS (Fri, 26 Oct 2007)
The present invention provides a compound of the formula [I]: wherein R1 is lower alkyl, etc. and R2 is hydrogen, etc., or R1 and R2 are bonded together to form lower alkylene; R3 is a group represented by wherein R6 and R7 are independently optionally protected amino, etc.; m and n are independently an integer of 0 to 6; R8 and R9 are independently optionally protected amino, etc., and q and r are independently an integer of 0 to 6, or R8 and R9, together with the adjacent alkylene(s) and the nitrogen atom, form saturated nitrogen-containing heterocycle optionally having substituent(s); R4 is lower alkyl, etc.; and R5 is amino, etc., or a pharmaceutically acceptable salt thereof.
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N-HYDROXYACRYLAMIDE COMPOUNDS (Fri, 17 Aug 2007)
This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof . More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC- related disease.
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HETEROCYCLIC JANUS KINASE 3 INHIBITORS (Fri, 13 Jul 2007)
The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).
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NEW CYCLIC PEPTIDE COMPOUNDS (Fri, 04 May 2007)
The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, to a process for preparation thereof comprising a rearrangement reaction under a mild acidic condition and the following amino acid changing reactions etc., to a pharmaceutical composition comprising, the same, and to a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.
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PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF CANCER (Fri, 20 Apr 2007)
The invention provides compounds which are pyrimidines of formula (I): wherein -XR3 is bonded at ring position 2 and -YR4 is bonded at ring position 5 or 6; R1 and R2 form, together with the N atom to which they are attached, a morphorine ring which is unsubstituted or substituted; X is a direct bond; R3 is is selected from (i) a group of the following formula (1): wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from -OR, CH2ORand -NRS(O) mR , wherein each R is independently selected from H, C1- C6 alkyl, C3 - C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the group being unsubstituted or substituted, and m is 2; and (ii) an indazole group which is unsubstituted or substituted; and Y is selected from -O-(CH2)n-, -NH-(CH2)n,-, -NHC(O)-(CH2)n- and -C(O)NH-(CH2)n- wherein n is 0 or an integer of 1 to 3, and R4 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group -NR5R6 wherein R5 and R6, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3 - C10 cycloalkyl which is unsubstituted or substituted, -C(O)R, -C(O)N(R)2 and -S(O)mR wherein R and m are as defined above, or R5 and R6 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
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