C07C271/12

MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: Pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack, angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: Pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack, angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

Compositions comprising (R)-2-amino-3-phenylpropyl carbamate and uses thereof
20230183172 · 2023-06-15 ·

The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.

Compositions comprising (R)-2-amino-3-phenylpropyl carbamate and uses thereof
20230183172 · 2023-06-15 ·

The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.

Compositions comprising (R)-2-amino-3-phenylpropyl carbamate and uses thereof
20230183172 · 2023-06-15 ·

The present invention relates to a newly identified solvate form of (R)-2-amino-3-phenylpropyl carbamate (APC) hydrochloride, a method of preparing APC hydrochloride, and methods of using the same to treat disorders. The invention further relates to methods of producing APC hydrochloride with increased purity.

1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

1,3-Di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.

MONOFUNCTIONAL OR MULTIFUNCTIONAL URETHANE ACRYLATE OLIGOMERS WITHOUT ISOCYANATES
20170342024 · 2017-11-30 · ·

The present invention relates to an acrylated and/or methacrylated urethane oligomer obtained by reaction of a specific polyamine a) with a cyclic carbonate compound b) carrying m cyclic carbonate groups, giving an intermediate product c) carrying m formed urethane groups which carry residual reactive amine —NH— groups, and subsequently an addition reaction of each of the said residual reactive amine groups of the said product c) with an acrylate group of a compound d) carrying, in addition to the said acrylate group, p additional acrylate and/or methacrylate groups, with each residual reactive amine —NH— group of the said product c) being thus converted into a carbon-nitrogen bond carrying the said acrylate and/or methacrylate groups, and thus production of the said urethane oligomer, with each carbon-nitrogen bond formed carrying p acrylate and/or methacrylate groups and the said urethane oligomer carrying m urethane groups and m hydroxyl groups in the alpha or beta position with respect to the said urethane and having a functionality in acrylates and/or methacrylates ranging from m*p(n−1) to m*p(2n−2).

The invention also relates to a process for the preparation of the said oligomer in two stages, to the intermediate product c) and to the use of the said urethane oligomer in crosslinkable compositions, in particular in coating compositions, adhesive compositions, compositions for systems for the layer-by-layer manufacture of 3D objects, compositions for 3D printing systems, moulding compositions, leaktightness agent compositions, chemical sealing compositions, concrete compositions or composite compositions.

MONOFUNCTIONAL OR MULTIFUNCTIONAL URETHANE ACRYLATE OLIGOMERS WITHOUT ISOCYANATES
20170342024 · 2017-11-30 · ·

The present invention relates to an acrylated and/or methacrylated urethane oligomer obtained by reaction of a specific polyamine a) with a cyclic carbonate compound b) carrying m cyclic carbonate groups, giving an intermediate product c) carrying m formed urethane groups which carry residual reactive amine —NH— groups, and subsequently an addition reaction of each of the said residual reactive amine groups of the said product c) with an acrylate group of a compound d) carrying, in addition to the said acrylate group, p additional acrylate and/or methacrylate groups, with each residual reactive amine —NH— group of the said product c) being thus converted into a carbon-nitrogen bond carrying the said acrylate and/or methacrylate groups, and thus production of the said urethane oligomer, with each carbon-nitrogen bond formed carrying p acrylate and/or methacrylate groups and the said urethane oligomer carrying m urethane groups and m hydroxyl groups in the alpha or beta position with respect to the said urethane and having a functionality in acrylates and/or methacrylates ranging from m*p(n−1) to m*p(2n−2).

The invention also relates to a process for the preparation of the said oligomer in two stages, to the intermediate product c) and to the use of the said urethane oligomer in crosslinkable compositions, in particular in coating compositions, adhesive compositions, compositions for systems for the layer-by-layer manufacture of 3D objects, compositions for 3D printing systems, moulding compositions, leaktightness agent compositions, chemical sealing compositions, concrete compositions or composite compositions.

CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
20170342230 · 2017-11-30 ·

A chemical blowing agent is described that includes at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can, for example, be incorporated into thermally expandable baffle and/or reinforcement elements, which can be used in automotive manufacturing and building insulation.