C07D217/24

Piperazine derivatives as FASN inhibitors

Compounds of the formula I ##STR00001##
in which R, X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2 and q have the meanings indicated in Claim 1,
are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

Piperazine derivatives as FASN inhibitors

Compounds of the formula I ##STR00001##
in which R, X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2 and q have the meanings indicated in Claim 1,
are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

Anti-inflammatory agents

Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.

Amine compound for inhibiting SSAO/VAP-1 and use thereof

An amine compound serving as a semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, and an application thereof in medicines that can be used for treating inflammation and/or inflammation related diseases, diabetes and/or a disease related diabetes, psychiatric disorder, ischemic disease, vascular disease, fibrosis, or tissue transplant rejection.

Amine compound for inhibiting SSAO/VAP-1 and use thereof

An amine compound serving as a semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, and an application thereof in medicines that can be used for treating inflammation and/or inflammation related diseases, diabetes and/or a disease related diabetes, psychiatric disorder, ischemic disease, vascular disease, fibrosis, or tissue transplant rejection.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

NAPHTHALIMIDE DERIVATIVES AS ANTI-PARASITIC AGENTS FOR THE TREATMENT OF LEISHMANIASIS AS WELL AS VIRAL, BACTERIAL AND NEOPLASTIC DISEASES

Disclosed are naphthalimide derivatives and in particular e.g. N-aryl-substituted naphthalimidopropylamine derivatives (i.e. 2-[3-(amino)propyl]-1H-benz[de]isoquinoline-1,3(2H)-dione derivatives) such as e.g. such as e.g. (Formula I) or (Formula III) as anti-parasitic agents for the treatment of Leishmaniasis. The compounds could also be useful to treat viral, bacterial and/or neoplastic diseases. The description discloses exemplary synthesis as well as biological tests against Leishmania infantum parasites (e.g. pages 54 to 58; examples 1 to 7). Exemplary compounds are: (example 3)(example 4) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1, 3(2H)-dione (example 5) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (example 6).

NAPHTHALIMIDE DERIVATIVES AS ANTI-PARASITIC AGENTS FOR THE TREATMENT OF LEISHMANIASIS AS WELL AS VIRAL, BACTERIAL AND NEOPLASTIC DISEASES

Disclosed are naphthalimide derivatives and in particular e.g. N-aryl-substituted naphthalimidopropylamine derivatives (i.e. 2-[3-(amino)propyl]-1H-benz[de]isoquinoline-1,3(2H)-dione derivatives) such as e.g. such as e.g. (Formula I) or (Formula III) as anti-parasitic agents for the treatment of Leishmaniasis. The compounds could also be useful to treat viral, bacterial and/or neoplastic diseases. The description discloses exemplary synthesis as well as biological tests against Leishmania infantum parasites (e.g. pages 54 to 58; examples 1 to 7). Exemplary compounds are: (example 3)(example 4) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1, 3(2H)-dione (example 5) 2-(3-((5-amino naphthalene-1-yl)amino)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione (example 6).

Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9

The present invention encompasses compounds of general formula (I) wherein the groups R.sup.1 to R.sup.9, X.sub.1 and X.sub.2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament. ##STR00001##