A61K31/4439

PRODUCTION METHOD OF THIAZOLE DERIVATIVE

Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A.sub.2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like:

##STR00001##

(wherein R.sup.1 represents furyl, R.sup.4, R.sup.5 and R.sup.6 are the same or different and each represents lower alkyl or aryl, R.sup.2 represents pyridyl or tetrahydropyranyl, and X.sup.1 represents halogen).

AGENT FOR PREVENTING AND/OR TREATING AMYOTROPHIC LATERAL SCLEROSIS
20180000771 · 2018-01-04 · ·

The present invention provides a prophylactic and/or therapeutic agent for amyotrophic lateral sclerosis (ALS), which contains one or more kinase inhibitors selected from the group consisting of an epithelial cell growth factor receptor (EGFR) inhibitor, a fibroblast growth factor receptor (FGFR) inhibitor, an Aurorakinase inhibitor, a protein kinase A (PKA) inhibitor, a protein kinase C (PKC) inhibitor, an MEK inhibitor, an Met inhibitor, a JNK inhibitor, a Syk inhibitor and a JAK inhibitor, a prostaglandin analogue and an estrogen receptor antagonist, or one or more kinase inhibitors selected from the group consisting of Tivozanib and an analog thereof, SB 216763, Cdk2 Inhibitor II, BUDESONIDE, RIBOFLAVIN, alpha-TOCHOPHEROL, AMODIAQUINE, SU9516, Sunitinib and an analog thereof, GSK-3 Inhibitor XIII, Bisindolylmaleimide I, HYDROQUINONE, FLUNISOLIDE, MGCD-265, Indirubin-3′-monoxime, HYDRASTINE (1R,9S), PIPERINE, BUTAMBEN, Axitinib and an analog thereof, APOMORPHINE, FENBUFEN, Bosutinib (SKI-606) and an analog thereof, a Wee1 Inhibitor, Cdk2 Inhibitor IV, NU6140, 3-hydroxybutyric acid, AT9283, Imatinib, Nilotinib, Rebastinib, and Bafetinib for the prophylaxis and/or treatment of ALS. Particularly, using a compound already on the market as a pharmaceutical product, a pharmaceutical product for the prophylaxis or treatment of ALS can be developed rapidly at a low cost.

Pesticidal Active Mixtures Comprising Isoxazoline Compounds I
20180007904 · 2018-01-11 ·

The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I)

##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.

The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant propagation material as like seeds.

Pesticidal Active Mixtures Comprising Isoxazoline Compounds I
20180007904 · 2018-01-11 ·

The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I)

##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts.

The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant propagation material as like seeds.

Piperidinyl-Indole Derivatives Complement Factor B Inhibitors and Uses Thereof

The present invention provides a compound of formula I:

##STR00001##

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Piperidinyl-Indole Derivatives Complement Factor B Inhibitors and Uses Thereof

The present invention provides a compound of formula I:

##STR00001##

a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Pharmaceutical composition containing dabigatran etexilate and preparation method thereof

Disclosed is a pharmaceutical composition containing dabigatran etexilate and a preparation method thereof. The pharmaceutical composition comprises a pharmaceutically active ingredient, dabigatran etexilate and/or dabigatran etexilate mesylate, and a amphiphilic polymer of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. The mass ratio of the two is 1:0.23 to 1:3. The pharmaceutical composition not only increases the bioavailability of the pharmaceutically active ingredient, but also reduces absorption variability, and provides a more stable concentration of dabigatran in plasma, thereby reducing adverse side effects.

Pharmaceutical composition containing dabigatran etexilate and preparation method thereof

Disclosed is a pharmaceutical composition containing dabigatran etexilate and a preparation method thereof. The pharmaceutical composition comprises a pharmaceutically active ingredient, dabigatran etexilate and/or dabigatran etexilate mesylate, and a amphiphilic polymer of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. The mass ratio of the two is 1:0.23 to 1:3. The pharmaceutical composition not only increases the bioavailability of the pharmaceutically active ingredient, but also reduces absorption variability, and provides a more stable concentration of dabigatran in plasma, thereby reducing adverse side effects.

PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CHRONIC MYELOID LEUKEMIA AND METHOD USING THE SAME
20180008579 · 2018-01-11 · ·

Provided are a pharmaceutical composition for preventing or treating chronic myeloid leukemia and a method of preventing or treating chronic myeloid leukemia using the same, thereby being effectively applied to the prevention or treatment of chronic myeloid leukemia.

PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CHRONIC MYELOID LEUKEMIA AND METHOD USING THE SAME
20180008579 · 2018-01-11 · ·

Provided are a pharmaceutical composition for preventing or treating chronic myeloid leukemia and a method of preventing or treating chronic myeloid leukemia using the same, thereby being effectively applied to the prevention or treatment of chronic myeloid leukemia.