There is disclosed a dispersion of amorphous uridine triacetate in Hypromellose Acetate Succinate-MG and optionally also Copovidone. The amorphous dispersion compositions allow high loading of uridine. They also have good stability and oral bioavailability. They can be used to deliver exogenous uridine to a mammalian subject in need thereof, for example a subject who has an energy failure disorder or certain other conditions.
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 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
Compounds and compositions that deliver both uridine and ketoleucine are useful in treating disorders characterized by diminished muscle strength or diminished muscle lean mass. One such a compound is 5 ' -O-ketoleucyl-2',3 ' -di-O-acetyluridine.
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 31/7064 - 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
A61K 31/706 - 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
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
There is disclosed a dispersion of amorphous uridine triacetate in Hypromellose Acetate Succinate-MG and optionally also Copovidone. The amorphous dispersion compositions allow high loading of uridine. They also have good stability and oral bioavailability.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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
4.
IMIDAZOQUINOLINE COMPOUND HAVING ANTI-INFLAMMATORY, ANTIFUNGAL, ANTIPARASITIC, AND ANTICANCER ACTIVITY
ABSTRACT OF THE DISCLOSURE An imidazoquinoline compound having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer is described.
A61K 31/437 - 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 containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
5' -O-Phenylacetyluridine effectively delivers both phenylacetate and uridine to a subject. It can be used to treat hepatic encephalopathy and genetic disorders of the hepatic nitrogen cycle.
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 25/00 - Drugs for disorders of the nervous system
5'-O-(Acetoacetyl)-2',3'-di-O-acetyluridine is useful in the treatment or prevention of disorders characterized by cerebral metabolic energy failure or diminished mitochondrial energy reserve capacity.
A61K 31/7064 - 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
A61K 31/7068 - 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
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
C07H 1/00 - Processes for the preparation of sugar derivatives
C07H 3/00 - Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
This invention provides a solution comprising uridine triacetate dissolved in a solvent, wherein the solvent comprises triacetin. Diacetin can be added if the solution contains water or will be used in an aqueous environment. The solution of this invention and formulations comprising that solution are useful for administering uridine triacetate to a patient.
A61K 31/7064 - 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
A61K 31/7068 - 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
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
8.
COMPOSITIONS AND DEVICES FOR SYSTEMIC DELIVERY OF URIDINE
A solution of uridine in saline, and optionally also containing beta-hydroxybutyrate, can be administered subcutaneously. A reservoir capable of holding a uridine solution in saline is described, the reservoir being fluidically linked to one or more infusion needles, and a pump configured to move the solution from the reservoir through the one or more infusion needles into a subject.
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
A61P 25/00 - Drugs for disorders of the nervous system
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations for treatment in the areas of oncology, hematology, neurology, dermatology, metabolic disorders, neurometabolic disorders and mitochondrial disorders, all of the foregoing goods excluding pharmaceutical preparations and substances for the treatment of depression; biological agents for treatment in the areas of oncology, anti-virals, infectious diseases and mitochondrial disorders. Pharmaceutical and biological research and development services.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations for treatment in the areas of oncology, hematology, neurology, dermatology, metabolic disorders, neurometabolic disorders and mitochondrial disorders, all of the foregoing goods excluding pharmaceutical preparations and substances for the treatment of depression; Biological agents for treatment in the areas of oncology, anti-virals, infectious diseases and mitochondrial disorders; Pharmaceuticals, medical and veterinary preparations, all of the foregoing goods excluding pharmaceutical preparations and substances for the treatment of depression; Sanitary preparations for medical purposes; Dietetic food and substances adapted for medical or veterinary use, food for babies; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides, herbicides. Pharmaceutical and biological research and development services; Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Design and development of computer hardware and software.
Uridine triacetate or other uridine prodrugs are used to treat genetic glycosylation disorders by administering them in an amount sufficient to raise plasma uridine in the to a level greater than 30 micromolar. They can be administered alone or in combination with a sugar whose transfer is defective in the glycosylation disorder being treated.
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
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical products, namely, uridine triacetate, other uridine prodrugs and preparations for use in the fields of mitochondrial diseases, and neurodegenerative diseases, namely, Huntington's Disease, Down Syndrome dementia, Parkinson's Disease and Alzheimer's Disease.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical products and preparations; Pharmaceutical products and preparations for use in the fields of hematology, metabolic disorders, uric acid disorders, oncology, mitochondrial diseases, neurodegenerative diseases and antidotes; Veterinary preparations; Sanitary preparations for medical purposes; Dietetic food and substances adapted for medical or veterinary use, food for babies; Dietary supplements for humans and animals; Plasters, materials for dressings; Material for stopping teeth, dental wax; Disinfectants; Preparations for destroying vermin; Fungicides, herbicides. Development of pharmaceutical products and preparations; Pharmaceutical drug development services; Research and development of pharmaceuticals and biologicals; Providing medical and scientific research information in the field of pharmaceuticals and clinical trials; Pharmaceutical product evaluation; Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Design and development of computer hardware and software. Medical and pharmaceutical consultation; Providing information regarding the properties and efficacy of pharmaceuticals; Dispensing of pharmaceuticals; Medical services; Veterinary services; Hygienic and beauty care for human beings or animals; Agriculture, horticulture and forestry services.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical products and preparations for use in the fields of oncology, mitochondrial disease, neurodegenerative disease and antidotes. Development of pharmaceutical products and preparations; Pharmaceutical drug development services; Research and development of pharmaceuticals and biologicals; Providing medical and scientific research information in the field of pharmaceuticals and clinical trials; Pharmaceutical product evaluation; Scientific and technological services and research and design relating thereto; Industrial analysis and research services; Design and development of computer hardware and software. Medical and pharmaceutical consultation; Providing information regarding the properties and efficacy of pharmaceuticals; Dispensing of pharmaceuticals; Medical services; Veterinary services; Hygienic and beauty care for human beings or animals; Agriculture, horticulture and forestry services.
16.
AMINE COMPOUNDS HAVING ANTI-INFLAMMATORY, ANTIFUNGAL, ANTIPARASITIC AND ANTICANCER ACTIVITY
Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Pharmaceutical preparations for treatment in the areas of oncology, hematology, neurology, namely mitochondrial disorders, Lesch-Nyhan syndrome, renal tubular acidosis, traumatic brain injury, hypoxic-ischemic encephalopathy, Huntington's Disease, Down Syndrome dementia, Parkinson's Disease and Alzheimer's Disease, metabolic disorders, namely diabetes, dyslipidemia, hyperuricemia, tumor lysis syndrome, gout, hypoglycemia and neurometabolic disorders, namely genetic mitochondrial diseases, glycosylation disorders, impaired cerebral fuel availability and Glut1 deficiency; biological agents for treatment in the areas of oncology and non-viral infectious diseases, namely antibacterial vaccines and antifungal vaccines. (1) Pharmaceuticals and biologicals research and development.
18.
STEM CELL MOBILIZATION AND TISSUE REPAIR AND REGENERATION
Stem cells are mobilized from bone marrow by administering an amount of Phe-Pro-His-Phe-Asp-Leu-Ser-His-Gly-Ser-Ala-Gln-Val-Ser-Asp-Lys-Pro (SEQ ID NO: 2) or Phe-Ala- His-Phe-Asp-Leu-Ser-His-Gly-Ser-Ala-Gln-Val-Ser-Asp-Lys-Pro (SEQ ID NO: 3) effective to mobilize the stem cells. This is useful for promoting bodily tissue regeneration in a patient in need of tissue regeneration treatment. Alternatively, the mobilized stem cells can be collected for transplant.
Stem cells are mobilized from bone marrow by administering an amount of Phe-Pro-His- Phe-Asp-Leu-Ser-His-Gly-Ser- Ala-Gin- Val (SEQ ID NO: 1) effective to mobilize the stem cells. This method is useful for promoting preservation, repair, or regeneration of bodily tissue, or revascularization, in a patient in need of such treatment. Alternatively, the mobilized stem cells can be collected for transplant.
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or its pharmaceutically acceptable salts. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. R1 is hydrogen or alkyl having from 1 to 3 carbon atoms. R2 is alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, hydroxy, nitro, halo, thio, alkylthio, or cyano. R3 and R4 are each independently hydrogen, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, perfluoromethoxy, halo, hydroxy, nitro, or amino.
A01N 35/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having two bonds to hetero atoms with at the most one bond to halogen, e.g. aldehyde radical
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I). The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium Jalciparum-induced inflammation. In Formula I, t, q, r, R6, R7, X and A are as defined herein.
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula 1. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation.
A severity score for 5-fluorouracil (5FU) toxicity is calculated by taking the square root of the sum of: (a) the square of the logarithm of the dose of 5-fluorouracil administered to the patient; and (b) the square of the logarithm of the administration rate of the 5-fluorouracil to the patient. Severity Score = [(log Dose)2 + (log Rate)2]1/2.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
A method for synthesizing (phenylalkyloxy)phenyl-oxobutanoic acid compounds is described. The corresponding (phenylalkyloxy)acylphenyl compound is halogenated, giving the alpha haloketone. The halide is displaced by the anion of a dialkyl malonate to give a substituted malonic ester. Hydrolysis of the ester and decarboxylation of the diacid gives the desired product.
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. In Formula (I) m is 0, 1, 2, 3 or 4; n is 0 or 1; m + n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are -CH2CH2-. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of Formula (I) by a ring carbon; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently monosubstituted by methyl or ethyl. The uric acid-lowering effects of the Compounds of Formula (I) are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, and cognitive impairment.
A01N 43/08 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom five-membered rings with oxygen as the ring hetero atom
26.
SYNTHESIS OF 4-[3-(2,6-DIMETHYLBENZYLOXY)PHENYL]-4-OXOBUTANOIC ACID
The compound 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobutanoic acid (DPA) is synthesized from 1-[3-(2,6-Dimethylbenzyloxy)-phenγl]-ethanone (DPE) via the intermediate 4-[3-(2,6-Dimethylbenzyloxy)phenyl]-4-oxobulanoic acid ethyl ester (DPAE).
C07D 213/00 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation. In Formula 1, x is 1 or 2: y is O, 1, 2 or 3; and R1 is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms, hydroxy, alkoxy having 1 or 2 carbon atoms, fluoro. chloro, bromo, and amino. A is phenyl unsubstituted or substituted by one, two or three groups selected from the group consisting of halo, alkyl having 1 or 2 carbon atoms. perfluoromethyL alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring atoms wherein the cycloalky! is unsubstituted or one one two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heleraromatic ring having 1 or 2 ring heteroatoms selected from N. S and O and the heteroaromatic ring is covalently bound to the remainder of the compound by a ring carbon.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A01N 43/64 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
28.
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. The agent is a compound of Formula (I): wherein m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; R1 is hydrogen or alkyl having from 1 to 3 carbon atoms; and R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono- substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a compound selected from an incretin mimetic and a dipeptidyl peptidase IV inhibitor in combination with a Compound of Formula,I or a pharmaceutically acceptable salt thereof, Formula (I) Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is -OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is -NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is -NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.
3-(2,4-Bis(trifluoromethyl)benzyloxy)phenylacetic acid, 4-(2,6-Dimethylbenzyloxy)- phenylacetic acid, and their pharmaceutically acceptable salts are useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis.
A01N 57/10 - Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds having phosphorus-to-oxygen bonds or phosphorus-to-sulfur bonds
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R 5 is hydrogen or alkyl having from one to six carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or A is cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or A is a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
Various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis can be treated with a combination of a direct PPAR-gamma agonist and a Compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) Three of R1, R2, R3, R4 and R5 are hydrogen and the remainder are independently selected from the group consisting of hydrogen, halo, hydroxy, methyl, ethyl, perfiuoromethyl, methoxy, ethoxy, and perfluoromethoxy; and m is 0, 2 or 4. R6 is hydrogen, O or hydroxy, and X is -OR7, wherein R7 is hydrogen or alkyl having from 1 to 3 carbon atoms; or R6 is hydrogen, and X is -NR8R9, wherein R8 is hydrogen or hydroxy and R9 is hydrogen, methyl or ethyl. When X is -NR8R9, hydroxy none of R1, R2, R3, R4 and R5 is hydroxy.
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/435 - 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
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R and R is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are =0. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, hydroxy, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of formula (I).
A61K 31/055 - Phenols the aromatic ring being substituted by halogen
C07C 59/01 - Saturated compounds having only one carboxyl group and containing hydroxy or O-metal groups
C07C 39/21 - Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic, containing only six-membered aromatic rings as cyclic part, with unsaturation outside the rings with at least one hydroxy group on a non-condensed ring
C07C 39/27 - Halogenated derivatives monocyclic monohydroxylic containing halogen bound to ring carbon atoms all halogen atoms being attached to the ring
35.
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; tis 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R3 and R4 is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are =O; R5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (I) by a ring carbon. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of formula (I).
A01N 35/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having two bonds to hetero atoms with at the most one bond to halogen, e.g. aldehyde radical
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I), wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; t is 0 or 1; R1 is hydrogen, halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; R2 is alkyl having from 1 to 3 carbon atoms; R3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R4 and R5 is hydrogen or hydroxy and the other is hydrogen; or R4 and R5 together arc =O; R6 is hydrogen or alkyl having one, two, three, four or five carbon atoms; or a pharmaceutically acceptable salt of the compound. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
A01N 35/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having two bonds to hetero atoms with at the most one bond to halogen, e.g. aldehyde radical
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1 ; t is 0 or 1 ; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R3 and R4 is hydrogen or hydroxy and the other is hydrogen; or R3 and R4 together are =O; R5 is hydrogen or alkyl having one, two, three, four or five carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon. Alternatively, the. agent can be a pharmaceutically acceptable salt of the compound of Formula I.
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed as Formula (I).
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations for treatment in the areas of oncology, hematology, neurology, dermatology, metabolic disorders and neurometabolic disorders[; biological agents for treatment in the areas of oncology, anti-virals and infectious diseases; biological preparations for medical purposes] PHARMACEUTICAL AND BIOLOGICAL RESEARCH AND DEVELOPMENT SERVICES
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Pharmaceutical preparations for treatment in the areas of oncology, hematology, namely, disorders of the blood and blood-forming organs, neurology, namely Alzheimer's, epilepsy, dementia, Parkinson's Disease, and Huntington's Disease, dermatology, namely, actinic keratosis and wound healing, metabolic disorders namely, diabetes, metabolic syndrome, cardiovascular disease, liver disease, and obesity, and neurometabolic disorders, namely mitochrondrial disease; biological agents for treatment in the areas of oncology, anti-virals and infectious diseases, namely hepatitis and influenza. (1) Pharmaceuticals and biologicals research and development.
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
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Pharmaceuticals and biological products; pharmaceuticals and biologicals in the fields of oncology and biologicals in the fields of oncology, hematology and others. Pharmaceuticals and biologicals research and development.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for treatment in the areas of oncology, [ hematology, ] neurology, [ dermatology, metabolic disorders ] and neurometabolic disorders [ ; biological agents for treatment in the areas of oncology, anti-virals and infectious diseases ]
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
PHARMACEUTICAL PREPARATIONS FOR TREATMENT IN THE AREAS OF ONCOLOGY, HEMATOLOGY, NEUROLOGY, DERMATOLOGY, METABOLIC DISORDERS AND NEUROMETABOLIC DISORDERS; BIOLOGICAL AGENTS FOR TREATMENT IN THE AREAS OF ONCOLOGY, ANTI-VIRALS AND INFECTIOUS DISEASES
