Abstract

The invention relates to the use of a thienopyridone derivative of Formula (I), or its pharmaceutically acceptable salts and/or solvates, or a pharmaceutical composition comprising the same, in the treatment of diabetic nephropathy.

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

The invention relates to the use of a thienopyridone derivative, or a pharmaceutical composition comprising the same, in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

The invention relates to the use of a thienopyridone derivative, or a pharmaceutical composition comprising the same, in the treatment of genetic neurodegenerative diseases selected from adrenoleukodystrophy (ALD) and adrenomyeloneuropathy (AMN).

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

The invention relates to a process for preparing a monohydrate potassium salt of a 5 thienopyridone derivative. It also relates to a monohydrate potassium salt of a thienopyridone derivative and its use in medicine, in particular for treating or preventing metabolic disorders, such as NASH.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The invention relates to a pharmaceutical combination comprising a specific thienopyridone derivative, namely 2-chloro-4-hydroxy-3-(5-hydroxytetralin-6-yl)-5-phenyl-7H-thieno[2,3- b]pyridin-6-one or one of its pharmaceutically acceptable salts and/or solvates, and at least one THRβ agonist. This combination may be used for treating a liver disease such as NASH, including cirrhotic and non-cirrhotic NASH.

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The invention relates to a pharmaceutical combination comprising a specific thienopyridone derivative, namely 2-chloro-4-hydroxy-3-(5-hydroxytetralin-6-yl)-5-phenyl-7H-thieno[2,3- b]pyridin-6-one or one of its pharmaceutically acceptable salts and/or solvates, and at least one incretin agonist. This combination may be used for treating a liver disease such as NASH, including cirrhotic and non-cirrhotic NASH.

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 38/26 - Glucagons
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

Use of a thienopyridone derivative in the treatment of diabetic nephropathy The invention relates to the use of a thienopyridone derivative of Formula (I): or its pharmaceutically acceptable salts and/or solvates, or a pharmaceutical composition comprising the same, in the treatment of diabetic nephropathy.

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

The invention relates to the use of a thienopyridone derivative of Formula (I) or its pharmaceutically acceptable salts and/or solvates, or a pharmaceutical composition comprising the same, in the treatment of cardiovascular diseases selected from the group consisting of: heart failure with preserved ejection fraction, heart failure with reduced ejection fraction, chronic heart failure, diabetic cardiomyopathy, AL-amyloid cardiomyopathy, cardiac ischemia, myocardial ischemia, acute heart failure, acute myocardial infarction, angina, and doxorubicin-induced cardiotoxicity.

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The invention relates to the use of a thienopyridone derivative, or a pharmaceutical composition comprising the same, in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys

Abstract

The invention relates to the use of a thienopyridone derivative, or a pharmaceutical composition comprising the same, in the treatment of genetic neurodegenerative diseases selected from adrenoleukodystrophy (ALD) and adrenomyeloneuropathy (AMN).

IPC Classes  ?

• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
• A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

This invention pertains to a film-coated tablet comprising an inner core and an external coating, wherein the inner core comprises a high proportion of a specific triazine derivative, namely 2-amino-3,6-dihydro-4-dimethylamino-6-methyl-1,3,5-triazine and pharmaceutically acceptable salts thereof, and a specific binder. It is also directed to the use of these tablets in the treatment of diabetes and/or complications thereof. This invention is further directed to a specific process for the manufacture of these film-coated tablets, which involves a granulation step in a high-shear mixer.

IPC Classes  ?

• A61K 9/28 - DrageesCoated pills or tablets
• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine

Abstract

The invention relates to a pharmaceutical combination comprising a specific thienopyridone derivative, namely 2-chloro-4-hydroxy-3-(5-hydroxytetralin-6-yl)-5-phenyl-7H-thieno[2,3-b]pyridin-6-one or one of its pharmaceutically acceptable salts and/or solvates, and at least one farnesoid-X receptor (FXR) agonist. This combination may be used for treating a liver disease such as NASH, including cirrhotic and non-cirrhotic NASH.

IPC Classes  ?

• A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
• A61K 31/46 - 8-Azabicyclo [3.2.1] octaneDerivatives thereof, e.g. atropine, cocaine
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

Abstract

Monohydrate potassium salt of a thienopyridone derivative and its preparation process The invention relates to a process for preparing a monohydrate potassium salt of a 5 thienopyridone derivative. It also relates to a monohydrate potassium salt of a thienopyridone derivative and its use in medicine, in particular for treating or preventing metabolic disorders, such as NASH.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 3/06 - Antihyperlipidemics
• A61P 3/04 - AnorexiantsAntiobesity agents
• A61P 3/00 - Drugs for disorders of the metabolism
• A61P 9/00 - Drugs for disorders of the cardiovascular system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents
• A61P 9/12 - Antihypertensives
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

This invention pertains to a film-coated tablet comprising an inner core and an external coating, wherein the inner core comprises a high proportion of a specific triazine derivative, namely 2- amino-3,6-dihydro-4-dimethylamino-6-methyl-1,3,5-triazine and pharmaceutically acceptable salts thereof, and a specific binder. It is also directed to the use of these tablets in the treatment of diabetes and/or complications thereof. This invention is further directed to a specific process for the manufacture of these film-coated tablets, which involves a granulation step in a high- shear mixer.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention provides a method for treating or preventing heart failure with preserved ejection fraction (HFPEF), wherein the method comprises administering to a patient having or at risk of developing HFPEF a therapeutically effective amount of imeglimin.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 9/00 - Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

IPC Classes  ?

• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/42 - Oxazoles
• A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 38/21 - Interferons

Goods & Services

Pharmaceutical products and preparations. Development of pharmaceutical preparations, pharmaceutical products and medicines; evaluation of pharmaceutical products, namely research in the field of pharmaceutical products; pharmaceutical research and development; research and development for the pharmaceutical industry; provision of information concerning the results of clinical trials for pharmaceutical products.

Goods & Services

Pharmaceutical products for the treatment of diabetes, metabolic diseases, mitochondrial dysfunction; Pharmaceutical preparations for the treatment of metabolic diseases and disorders, diabetes, mitochondrial dysfunction Development of pharmaceutical preparations, pharmaceutical products and medicines; evaluation of pharmaceutical products, namely, research in the field of pharmaceutical products; pharmaceutical research and development; research and development for the pharmaceutical industry; provision of information concerning the results of clinical trials for pharmaceutical products

Goods & Services

Pharmaceutical products and preparations. Development of pharmaceutical preparations, pharmaceutical products and medicines; evaluation of pharmaceutical products; research in the field of pharmaceutical products; pharmaceutical research and development; research and development for the pharmaceutical industry; provision of information concerning the results of clinical trials for pharmaceutical products.

Goods & Services

Development of pharmaceutical preparations, pharmaceutical products and medicines; evaluation of pharmaceutical products; research in the field of pharmaceutical products; pharmaceutical research and development; research and development for the pharmaceutical industry; providing medical and scientific research information in the field of the results of clinical trials for pharmaceutical products [ Pharmaceutical preparations for metabolic diseases ]

Abstract

The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

IPC Classes  ?

• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• A61K 31/42 - Oxazoles
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/7072 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• A61K 38/21 - Interferons
• A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep

Abstract

Activators of AMPK and therapeutic uses thereof The invention relates to compounds that are direct activators of AMPK (AMP-activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, liver disease, hepatic steatosis, non alcoholic fatty liver disease (NAFLD), non alcoholic steato-hepatitis (NASH), liver fibrosis, dyslipidemia, hypertriglyceridemia, hypercholesterolemia, inflammation, cancer, cardiovascular diseases, atherosclerosis, high blood pressure, retinopathies or neuropathies.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems

Abstract

The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

IPC Classes  ?

• A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• A61P 31/20 - Antivirals for DNA viruses
• A61K 31/42 - Oxazoles
• A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
• A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

Goods & Services

Advertisement services, Management of business affairs, Business administration, Office functions; Cost price analysis services. Scientific and technological services and research and design relating thereto, namely evaluation; Engineering appraisals and research in the scientific and technological fields; Analysis, namely chemical analysis; Industrial research services, namely research and development of new products; Technical research; Design and development of computer hardware and software. Medical services; Veterinary services; Hygienic and beauty care for human beings and animals; medical analysis.

Goods & Services

Advertisement services, Business management, Business management, Office functions. Scientific and technological services and and research and design relating thereto, namely evaluations, assessments and research in the scientific and technological fields carried out by engineers, industrial analysis and research services, design and development of computer hardware and software. Medical services; Veterinary services; Hygienic and beauty care for human beings and animals.

Abstract

Activators of AMPK and therapeutic uses thereof The invention relates to compounds that are direct activators of AMPK (AMP-activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, liver disease, hepatic steatosis, non alcoholic fatty liver disease (NAFLD), non alcoholic steato- hepatitis (NASH), liver fibrosis, dyslipidemia, hypertriglyceridemia, hypercholesterolemia, inflammation, cancer, cardiovascular diseases, atherosclerosis, high blood pressure, retinopathies or neuropathies.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The present invention relates to a new process of separation of triazine derivatives enantiomers involving tartaric acid.

IPC Classes  ?

• C07D 251/24 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to three ring carbon atoms
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 3/04 - AnorexiantsAntiobesity agents

Abstract

The present invention relates to a new process of separation of triazine derivatives enantiomers involving tartaric acid.

IPC Classes  ?

• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• C07B 57/00 - Separation of optically-active organic compounds

Abstract

The invention relates to amino derivatives of dihydro-1,3,5-triazine, used for the treatment and/or prevention of diseases induced by ischemia and/or reperfusion, notably cardiac and renal complications.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

A new process for the enantiomeric separation of racemic 3,6-dihydro-1,3,5-triazine derivatives for the treatment of disorders associated with insulin-resistance syndrome, by preferential crystallization.

IPC Classes  ?

• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 3/04 - AnorexiantsAntiobesity agents

Abstract

The present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 9/20 - Pills, lozenges or tablets

Abstract

The present invention relates to triazine derivatives of Formule I for their use in the treatment of Type 2 diabetes, and to compositions comprising said triazine derivatives.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 9/20 - Pills, lozenges or tablets

Abstract

6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with the activity of AMP-activated protein kinase (AMPK). Another object of the invention concerns the use of said compounds for enhancing glucose homeostasis, improving podocytopathy and/or decreasing the production of reactive oxygen species (ROS). The invention also relates to a method for in-vitro diagnosing diabetic nephropathy and a method for screening compounds that reduce podocytopathy, in each case by applying synaptopodin as biomarker.

IPC Classes  ?

• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to compounds that are direct activators of AMPK (AMP- activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, inflammation, cancer and cardiovascular diseases.

IPC Classes  ?

• C07D 495/04 - Ortho-condensed systems
• A61K 31/33 - Heterocyclic compounds
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

The invention relates to amino derivatives of dihydro-1,3,5-triazine used in the treatment and/or prevention of ischemia and/or reperfusion related diseases, in particular heart and kidney complications.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention relates to amino derivatives of dihydro-1,3,5-triazine of formula (I), to be used for treating oxidative stress and diseases related thereto, in particular in persons suffering from hyperglycemia.

IPC Classes  ?

• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• A61P 35/00 - Antineoplastic agents

Abstract

A new process for the enantiomeric separation of racemic 3,6-dihydro-1,3,5-triazine derivatives for the treatment of disorders associated with insulin-resistance syndrome, by preferential crystallization.

IPC Classes  ?

• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine

Abstract

The invention relates to compounds of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with the activity of AMP-activated protein kinase (AMPK). Another object of the invention concerns the use of said compounds for enhancing glucose homeostasis, improving podocytopathy and/or decreasing the production of reactive oxygen species (ROS). The invention also relates to a method for in-vitro diagnosing diabetic nephropathy and a method for screening compounds that reduce podocytopathy, in each case by applying synaptopodin as biomarker.

IPC Classes  ?

• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

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Abstract

The present invention discloses a process for isolating enantiomer components from a mixture of enantiomers through particle-size-controlled crystallization, comprising the steps of: (a) forming a solution of a mixture of enantiomers (R) and (S) in a solvent in the absence of any further additives or agents; (b) seeding the solution of step (a) simultaneously or consecutively with seed crystals of enantiomer (R) and with seed crystals of enantiomer (S), wherein the seed crystals of enantiomer (R) differ in size and/or in quantity from the seed crystals of enantiomer (S) to allow separation of the crystals composed of a mixture enriched with enantiomer (R) from the crystals composed of a mixture enriched with enantiomer (S); (c) inducing simultaneous crystallization of enantiomer (R) and enantiomer (S); and (d) isolating crystals composed of a mixture enriched with enantiomer (R) from crystals composed of a mixture enriched with enantiomer (S) through size separation of the crystals, preferably through sieving, melting or sedimentation, in particular through sieving.

IPC Classes  ?

• C07C 33/26 - Polyhydroxylic alcohols containing only six-membered aromatic rings as cyclic part
• C07C 29/78 - SeparationPurificationStabilisationUse of additives by physical treatment by condensation or crystallisation
• C07D 251/10 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
• C07B 57/00 - Separation of optically-active organic compounds