Disclosed herein are compounds for use in lightening skin, treating uneven skin pigmentation and/or improving the appearance of aging skin, as well as methods utilizing the compounds, and anti-aging compositions comprising the compounds and a pharmaceutically acceptable carrier. The compounds have the general Formula I:
3 are as defined herein.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Industrial chemicals; Chemicals used in science; Chemical preparations for use in photography; Chemicals used in forestry; Chemicals for use in agriculture; Chemicals used in horticulture; Unprocessed artificial resins for processing industries; Unprocessed plastics; Fertilizers for soil; Fire extinguishing compositions; Metal tempering preparations; Soldering chemicals; Chemical substances absorbed on carriers for use as food preservatives; Tan; Commercial adhesives [other than for stationery or household use]; Contact cements; Degreasing preparations for use in manufacturing processes. Bleaching preparations and other substances for laundry use; Scouring solutions; Shining preparations [polish]; Degreasers, other than for use in manufacturing processes; Abrasive paste; Soap; Perfumes; Perfumery, essential oils; Cosmetics; Hair liquids; Dentifrices. Advertising; Business management; Business assistance, management and administrative services; Business administration; Clerical services. Science and technology services; Scientific and industrial research; Industrial analysis and research services; Design and development of computer hardware; Software design and development. Medical services; Animal healthcare services; Human hygiene and beauty care; Agriculture, horticulture and forestry services; Animal beautician services.
3.
USE OF HETEROCYCLIC COMPOUNDS IN THE TREATMENT OF PIGMENTED SKIN
Disclosed herein are compounds for use in lightening skin, treating uneven skin pigmentation and/or improving the appearance of aging skin, as well as methods utilizing the compounds, and anti-aging compositions comprising the compounds and a pharmaceutically acceptable carrier. The compounds have the general Formula (I): or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1-R3 are as defined herein.
Compositions are disclosed herein, as well as methods and uses utilizing the compositions for improving the appearance of aging skin, lightening skin, treating uneven skin pigmentation and/or treating a sexual disorder. The compositions comprise a compound of the general Formula (I): or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1- R5 are as defined herein, and a carrier suitable for topical administration on skin, being in a form of a water-in-oil emulsion, the emulsion comprising: propylene glycol, phosphatidyl choline, lauroyl macrogolglycerides, macrogolglycerol stearate, ethanol, caprylocaproyl macrogolglycerides, propylene glycol monolaurate and water, in proportions described herein.
Compositions are disclosed herein, as well as methods and uses utilizing the compositions for improving the appearance of aging skin, lightening skin, treating uneven skin pigmentation and/or treating a sexual disorder. The compositions comprise a compound of the general Formula (I): or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1- R5 are as defined herein, and a carrier suitable for topical administration on skin, being in a form of a water-in-oil emulsion, the emulsion comprising: propylene glycol, phosphatidyl choline, lauroyl macrogolglycerides, macrogolglycerol stearate, ethanol, caprylocaproyl macrogolglycerides, propylene glycol monolaurate and water, in proportions described herein.
Disclosed herein are compounds for use in lightening skin, treating uneven skin pigmentation and/or improving the appearance of aging skin, as well as methods utilizing the compounds, and anti-aging compositions comprising the compounds and a pharmaceutically acceptable carrier. The compounds have the general Formula (I): or a pharmaceutically acceptable salt thereof, wherein the dashed line, X, Y, Z, Ra-Rd, and R1-R3 are as defined herein.
Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
8.
Heterocyclic compounds and uses thereof in the treatment of sexual disorders
Novel heterocyclic compounds having the Formula I:
wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
C07D 401/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 473/06 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
C07D 473/30 - Oxygen atom attached in position 6, e.g. hypoxanthine
C07D 401/14 - 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 three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
Novel heterocyclic compounds having the Formula I:
wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
11.
Piperazine, piperidine and tetrahydropyridine derivatives and their pharmaceutical use
Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
12.
PIPERAZINE, PIPERIDINE AND TETRAHYDROPYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
Novel piperazine, piperidine and tetrahydropyridine derivatives of the formula I comprising a dibenzofurane moiety are privided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof to treat disorders such as central nervous disorders.
C07D 407/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 25/00 - Drugs for disorders of the nervous system
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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
13.
Heterotricyclic compounds as serotonergic and/or dopaminergic agents and uses thereof
A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III:
B is a moiety selected from the group consisting of:
D is a moiety selected from the group consisting of:
A1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
C07D 401/00 - 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
Novel heterocyclic compounds having the formula:
or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as described in the specification, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, are disclosed, as well as processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
15.
HETEROTRI CYCIII C COMPOUNDS AS SEROTONERGIC AND/OR DOPAMINERGIC AGENTS AND USES THEREOF
Novel heterocyclic compounds of formula I: A-B-D Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: Formula II Formula III B is a moiety selected from the group consisting of: O D is a moiety selected from the group consisting of: N and which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTAi agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.
Novel heterocyclic compounds, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
C07D 473/06 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
C07D 401/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
C07D 473/30 - Oxygen atom attached in position 6, e.g. hypoxanthine
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
17.
PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF SEXUAL DISORDERS
Novel heterocyclic compounds are disclosed herein, having the general formula: (see formula) which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity. Processes of preparing the compounds, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are also disclosed.
Novel heterocyclic compounds are disclosed herein, having the general formula:(see above formula)which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity. Processes of preparing the compounds, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are also disclosed.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 15/10 - Drugs for genital or sexual disordersContraceptives for impotence
C07D 239/90 - Oxygen atoms with acyclic radicals attached in position 2 or 3
C07D 311/22 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
C07D 401/06 - 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 linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 473/06 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
C07D 473/30 - Oxygen atom attached in position 6, e.g. hypoxanthine
