PATENTSCOPE: EN_ALL:nmr AND PA:takeda

HETEROCYCLIC COMPOUND AND USE THEREOF (Fri, 08 Feb 2019)
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I) : wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis treatment of narcolepsy.
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HETEROCYCLIC COMPOUND (Fri, 08 Feb 2019)
The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of central nervous system diseases including neurodegenerative disease, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
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TETRAHYDROPYRIDOPYRAZINE MODULATORS OF GPR6 (Fri, 21 Dec 2018)
Disclosed is a compound of Formula 1 as described in the specification and a pharmaceutically acceptable salt thereof. This disclosure also relates to materials and methods for preparing the compound of Formula 1, to pharmaceutical compositions which contain it, and to its use for treating diseases, disorders, and conditions associated with GPR6.
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HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS (Fri, 26 Oct 2018)
The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I) : wherein each symbol is as described in the specification, salt thereof.
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PIPERIDINYL- AND PIPERAZINYL-SUBSTITUTED HETEROAROMATIC CARBOXAMIDES AS MODULATORS OF GPR6 (Fri, 05 Oct 2018)
Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R4, R5, R8, R10, R11, X1, X2, X3, X9, X12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.
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SUBSTITUTED CYCLYL-ACETIC ACID DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS (Fri, 05 Oct 2018)
Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I) : wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
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IP6K INHIBITORS (Fri, 05 Oct 2018)
The present invention aims to provide a heterocyclic compound having an IP6K inhibitory action and expected to be useful as a prophylactic or therapeutic agent for- diseases such as cardiac failure, diabetes and the like. A compound represented by the formula (I) : wherein each symbol is as defined in the SPECIFICATION, or a salt thereof has an IP6K inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for diseases such as cardiac failure, diabetes and the like.
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METHOD OF PREDICTING EFFECTS OF CDC7 INHIBITOR (Sat, 08 Sep 2018)
The present invention relates to a method of predicting the likelihood that a patient will respond therapeutically to a pancreatic cancer treatment comprising the administration of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one (Compound 1) and/or tautomers thereof or a pharmaceutically acceptable salt or hydrate thereof, comprising the steps of: STEP (1): determining a KRAS gene mutation status of a sample from a patient, and STEP (2): predicting an increased likelihood that the patient will respond therapeutically to the pancreatic cancer treatment if the patient has the presence of KRAS gene mutation(s), and to methods of treating pancreatic cancer.
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CYCLIC PURINE DINUCLEOTIDES AS STING (STIMULATOR OF INTEFERON GENES) AGONISTS (Fri, 08 Jun 2018)
The present disclosure provides a compound having a STING (stimulator of interferon genes) agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases, such as cancer. The present disclosure relates to a compound represented by the formula (I) wherein each symbol is as defined in the description, or a salt thereof.
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MGLUR7 AGONIST COMPOUNDS FOR TREATING MGLUR7- REGULATED DISEASES, DISORDERS, OR CONDITIONS (Fri, 25 May 2018)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof wherein Z, R1, R2, R3, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. The present invention further provides methods of treating at least one disease, disorder, or condition associated with the glutamatergic and GABAergic signalling pathways regulated in full or in part by metabotropic glutamate receptor 7 (mGluR7) by administering a compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject. The compound may be a selective agonist of mGluR7, which modulates the release of at least one neurotransmitter in the subject.
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MGLUR7 MODULATORS (Fri, 04 May 2018)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2, R3 and n are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy as metabotropic glutamate receptor 7 (mGluR7) modulators.
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TETRAHYDROFURO[3,4-C]ISOQUINOLINES AS INHIBITORS OF PDE4 (Fri, 20 Apr 2018)
The compounds of a certain formula 1, in which R1, R2 and R3 have the meanings as given in the description, are novel effective inhibitors of phosphodiesterase type 4.
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THERAPEUTIC COMPOUNDS (Fri, 13 Apr 2018)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof : in which n, X, R1, R2, R3 and R4 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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TREATMENT OF PROSTATE CANCER (Fri, 06 Apr 2018)
Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethyiamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
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INDANE DERIVATIVES USEFUL AS MODULATORS OF MGLUR7 (Fri, 16 Mar 2018)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, X, Y, Z, D, R1, R2, R3, R4, R12, R15nd R16 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use as modulators of mGluR7.
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HETEROCYCLIC COMPOUNDS WITH AN ROR(GAMMA)T MODULATING ACTIVITY (Fri, 16 Feb 2018)
The present invention relates to a compound that may have an ROR(gamma)t modulating activity and can thus be useful in the treatment of cancer.
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ETHYL 6-[(2-CHLORO-4-FLUOROPHENYL)METHANESULFONYL]-3-METHYLCYCLOHEX-1-ENE-1-CARBOXYLATE AS TLR4 ANTAGONIST (Fri, 26 Jan 2018)
The invention provides a compound of ethyl 6- [ (2-chloro- 4-fluorophenyl)methanesulfonyl] -3-methylcyclohex-1-ene-1- carboxylate. The compound possesses an advantageous combination of TLR4 antagonist properties and brain permeability, and therefore, the compound would be expected to be useful in the treatment of central nervous system diseases mediated at least in part by TLR4.
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NOVEL COMPOUNDS (Fri, 29 Dec 2017)
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, X1, X2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12and R13 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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HETEROCYCLIC COMPOUND (Fri, 06 Oct 2017)
The present invention provides a compound having an MAGL inhibitory action, and useful as an agent for the prophylaxis or treatment of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, traumatic brain injury, glaucoma, multiple sclerosis etc.), anxiety disorder, pains (e.g., inflammatory pain, cancerous pain, neurogenic pain etc.), epilepsy, depression and the like. The present invention relates to a compound represented by the formula (I) : wherein each symbol is as defined in the specification, or a salt thereof.
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CRYSTALLINE FORMS OF 2-[(2S)-1-AZABICYCLO[2.2.2]OCT-2-YL]-6-(3-METHYL-1H- PYRAZOL-4-YL)THIENO[3,2-D]PYRIMIDIN-4(3H)-ONE HEMIHYDRATE (Fri, 06 Oct 2017)
The present disclosure relates to crystalline forms of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one hemihydrate (Compound 1) and/or tautomers thereof, wherein Compound 1 has the structure: (I) ⋅ 0.5 H2O; processes for preparing crystalline forms of Compound 1 and/or tautomers thereof; pharmaceutical compositions comprising the crystalline forms; methods of inhibiting a cell division cycle 7 in a mammal comprising administering the crystalline forms; and methods of treating a cell division cycle 7 mediated cancer in a mammal comprising administering the crystalline forms or a pharmaceutical composition comprising the crystalline forms.
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