Abstract

The present application is directed compounds of general formula (I) which are active on the Hippo pathway and have antitumor activity. The application also discloses processes for the preparation of said compounds as well as their pharmaceutical compositions.

IPC Classes  ?

• A61P 35/00 - Antineoplastic agents
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/4245 - Oxadiazoles

Abstract

Pharmaceutical compositions in the form of dry powder for inhalation comprising a local anesthetic such as procaine, chloroprocaine, lidocaine, prilocaine, mepivacaine, bupivacaine, etidocaine, ropivacaine, and tetracaine or salts and/or solvates thereof and a hydrophilic biocompatible polymer, in particular hyaluronates, are described. The compositions of the invention are useful for the treatment of the cough.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• A61P 11/14 - Antitussive agents

Abstract

222 = H, alkyl, aryl, heteroaryl. and designed to act through a dual action: a) the inhibition of the metal enzyme Carbonic Anhydrase (AC; EC 4.2.1.1 ) specifically expressed by Malassezia pachydermatis; b) the function as a carrier of the element selenium in organic form which is known to very effectively interfere with the metabolism and biosynthesis of lipid components of the target fungal organisms.

IPC Classes  ?

• C07C 391/00 - Compounds containing selenium
• C07C 391/02 - Compounds containing selenium having selenium atoms bound to carbon atoms of six-membered aromatic rings
• C07D 201/00 - Preparation, separation, purification, or stabilisation of unsubstituted lactams
• C07D 277/52 - Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 33/00 - Antiparasitic agents
• A61K 31/00 - Medicinal preparations containing organic active ingredients

Abstract

Pharmacologically acceptable compound selected from a group consisting of histone deacetylases inhibitors, redox coenzymes and their precursors to restore the antiviral functions of depleted HBV-specific T lymphocytes. The invention also concerns a method to restore the antiviral functions of the latter through the administration of the compound as above.

IPC Classes  ?

• A61K 31/4406 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
• A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
• 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 31/7084 - Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
• A61P 31/12 - Antivirals

Abstract

A process for administering a predefined amount of a compound to a target, comprising the following steps: - providing a dosing chamber (2) having a predefined volume; - disposing the predefined amount of compound downstream of an outlet (2b) of the dosing chamber (2) and upstream of the target; - introducing a propellent into the dosing chamber (2); - discharging the propellent from the outlet (2b) of the dosing chamber (2) towards the predefined amount of compound so as to dispense the predefined amount of compound to the target.

IPC Classes  ?

• A61M 15/00 - Inhalators
• A61M 11/00 - Sprayers or atomisers specially adapted for therapeutic purposes
• A61M 11/02 - Sprayers or atomisers specially adapted for therapeutic purposes operated by air pressure applied to the liquid to be sprayed or atomised

Abstract

Surgical tool (100) for abdominal suture, comprising: an elongated body (101) comprising a distal end (102) and a proximal handle (105), and further comprising a lateral pair of notches (103) in between the distal end (102) and the proximal handle (105), the elongated body (101) having an oval or elliptical cross-section, wherein the pair of notches (103) are further transversally aligned on a major axis of the oval or elliptical cross-section; a pair of needles (106) housed in the distal end (102) having needle tips directed towards the proximal handle (105), the pair of needles (106) being configured to longitudinally slide and engage with the needle tips (115) the pair of notches (103); a suture thread (113) with respective terminations fixed to the pair of needles (106); a mover device (107) configured to proximally move the pair of needles (106) in engagement with the pair of notches (103), and further configured to further proximally move the pair of needles (106) beyond the pair of notches (103).

IPC Classes  ?

• A61B 17/04 - Surgical instruments, devices or methods for closing wounds or holding wounds closedAccessories for use therewith for suturing woundsHolders or packages for needles or suture materials
• A61B 17/06 - NeedlesHolders or packages for needles or suture materials

Abstract

The present invention relates to a process for preparing an extract with antimicrobial activity from by-products or waste products of the fruit and vegetable industry. The process comprises a step of mixing the by-products or waste products with at least one microorganism, preferably a bacterium of the genus Lactobacillus, a fermentation step and a subsequent extraction step.

IPC Classes  ?

• C12P 7/40 - Preparation of oxygen-containing organic compounds containing a carboxyl group
• C12P 7/22 - Preparation of oxygen-containing organic compounds containing a hydroxy group aromatic
• C12P 13/04 - Alpha- or beta-amino acids
• A23L 3/3508 - Organic compounds containing oxygen containing carboxyl groups

Abstract

Path planning method for computing optimal parking maneuvers for road vehicles including the steps of computing a set of value functions of a cost function of parking maneuvers reaching the target set of states as unique viscosity solution of a Hamilton Jacobi Bellman equation, supplying the set of value functions, together with a starting state of the vehicle, as input to the dynamic programming calculation procedure calculating at least the set of vehicle controls. The set of equations modeling the evolution of the state of said road vehicle is a switched system of equations between a first sub-system if the vehicle is in forward motion and a second sub-system if the vehicle is in reverse motion. The cost function takes into account the arrival time a number of direction changes of the road vehicle between forward motion and reverse motion.

IPC Classes  ?

• B60W 30/06 - Automatic manoeuvring for parking
• G05D 1/02 - Control of position or course in two dimensions
• B62D 15/02 - Steering position indicators
• B60W 50/14 - Means for informing the driver, warning the driver or prompting a driver intervention
• G01C 21/34 - Route searchingRoute guidance
• G05D 1/00 - Control of position, course, altitude or attitude of land, water, air or space vehicles, e.g. using automatic pilots
• B60W 50/00 - Details of control systems for road vehicle drive control not related to the control of a particular sub-unit

Abstract

A system (10) for the remote detection of substances, comprising a vehicle (20) that is mobile in space and remote-piloted using a control device (40) with a haptic interface suitable to return a force feedback to a user of the control device (40), wherein the vehicle (20) is equipped with a position sensor (22) and a sensor (21) for detecting a physical quantity whose intensity depends on the distance of at least one substance present in a detection point located in a vicinity of the position of the vehicle (20).

IPC Classes  ?

• G01T 1/169 - Exploration, location of contaminated surface areas
• G01T 7/00 - Details of radiation-measuring instruments
• G01V 5/02 - Prospecting or detecting by the use of ionising radiation, e.g. of natural or induced radioactivity specially adapted for surface logging, e.g. from aircraft
• G05D 1/00 - Control of position, course, altitude or attitude of land, water, air or space vehicles, e.g. using automatic pilots

Abstract

The invention provides a fluorescent nanovesicles with stability in an aqueous medium, and particularly a new fluorescent nanovesicle maintaining the fluorescence's property for a period of time in an aqueous medium. The invention is also directed to their uses as a fluorescent probe and to a method for preparing the stable fluorescent nanovesicles in an easy and feasibly way.

IPC Classes  ?

• A61K 49/22 - Echographic preparationsUltrasound imaging preparations

Abstract

The present invention relates to the use in the medical field of 2-oxo-2H-pyrrol- 1 (5)-carboxamide derivatives in the treatment of HIV infections, pharmaceutical compositions containing these derivatives as active ingredients, and a process for the preparation of such derivatives.

IPC Classes  ?

• A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
• A61K 31/402 - 1-aryl-substituted, e.g. piretanide
• A61P 31/18 - Antivirals for RNA viruses for HIV

Abstract

A system (10) for the remote detection of substances, comprising a vehicle (20) that is mobile in space and remote-piloted using a control device (40) with a haptic interface suitable to return a force feedback to a user of the con¬ trol device (40), wherein the vehicle (20) is equipped with a position sensor (22) and a sensor (21 ) for detecting a physical quantity whose intensity de¬ pends on the distance of at least one substance present in a detection point located in a vicinity of the position of the vehicle (20).

IPC Classes  ?

• G01T 7/00 - Details of radiation-measuring instruments
• G01V 5/02 - Prospecting or detecting by the use of ionising radiation, e.g. of natural or induced radioactivity specially adapted for surface logging, e.g. from aircraft

Abstract

New linear peptides are described with broad spectrum of action, high antimicrobial antiviral and antifungal activities, combined with other characteristics of non-toxicity and persistence of activity in unfavorable environmental conditions. The peptides of the invention have a length of 20 amino acids and the structure: A-B-C-D-E-F-G, in which: A represents a basic amino acid; B, D, F represent respectively 5, 3 and 3 amino acids, chosen from the group of hydrophobic amino acids; C, E represent 3 amino acids, where each C and E comprises at least one basic amino acid and at least 1 amino acid forming hydrogen bonds; G represents 2 amino acids, chosen from basic amino acids and/or hydrophobic amino acids, their salts and/or mixtures thereof.

IPC Classes  ?

• C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
• A61K 38/10 - Peptides having 12 to 20 amino acids
• C07K 14/46 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates

Abstract

Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.

IPC Classes  ?

• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
• A61K 31/365 - Lactones
• C07D 305/10 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having one or more double bonds between ring members or between ring members and non-ring members

Abstract

The present invention relates to an antibody capable of binding with high-affinity and high selectivity to the ectodomain of the transmembrane proteoglycan (PG) NG2/CSPG4, preferably to discrete isoforms of said PG, preferably isoforms that may be generated by alternative splicing, and/or coding single nucleotide polymorphisms, and/or post-transcriptional and/or post-translational modifications. The invention further relates to an anti-NG2/CSPG4 antibody possessing the ability to uniquely induce programmed cell death, exhibited as both canonical caspase-dependent apoptosis and authophagy, in NG2/CSPG4-expressing cancer cells. This action being manifested irrespectively of the coaction of other exogenously added factors. Moreover, the present invention refers to a composition comprising the antibody of the invention, in its naked, encapsulated or genetically engineered form, as pharmaceutical excipient. A further aspect of the present invention refers to the anti-NG2/CSPG4 molecule, or any of its isoforms and fragments, provided as proteolytically generated peptides or produced synthetically and/or recombinantly, for the treatment of apoptosis and/or autophagy-dependent diseases, including but not restricted to cancer.

IPC Classes  ?

• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

IPC Classes  ?

• C07D 205/085 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a nitrogen atom directly attached in position 3
• 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 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 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 413/12 - 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 chain containing hetero atoms as chain links

Abstract

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

IPC Classes  ?

• C07D 205/085 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a nitrogen atom directly attached in position 3

Abstract

New inhibitors of the activity of the multidrug resistance receptor 1 (MDR1), which are highly active to the MDR1 transporter, and showing a medium/ high selectivity to such transporter, described by the structural formula (I): where R is a C1-C4 alkylene, optionally substituted with a C1-C3 alkyl. Said inhibitors are useful in the treatment or prevention of multi-drug resistance.

IPC Classes  ?

• A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
• A61P 35/00 - Antineoplastic agents

Abstract

A formulation for extenders for the long-term conservation of animal semen, of both productive livestock and pets, intended for artificial insemination is described. More precisely, the invention concerns the composition for extenders without animal substances characterized by the presence of a polysaccharide and/or an oligosaccharide, particularly D-(+)-saccharose, and by the presence of a hydrolytic enzyme, particularly invertase, which catalyzes the hydrolysis of said polysaccharides and/or oligosaccharides to monosaccharides, which can be metabolized by the sperm cells.

IPC Classes  ?

• A01N 1/02 - Preservation of living parts

Abstract

The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.

IPC Classes  ?

• C07D 263/58 - BenzoxazolesHydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
• A61K 31/423 - Oxazoles condensed with carbocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.

IPC Classes  ?

• C07C 271/56 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 269/02 - Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups from isocyanates with formation of carbamate groups
• C07D 309/14 - Nitrogen atoms not forming part of a nitro radical

Abstract

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

IPC Classes  ?

• A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine

Abstract

The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine

Abstract

The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.

IPC Classes  ?

• C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
• C07D 239/557 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
• C07D 239/553 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
• C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms

Abstract

The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.

IPC Classes  ?

• C07D 305/12 - Beta-lactones
• A61K 31/585 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
• 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 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 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/365 - Lactones

Abstract

6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07C 233/00 - Carboxylic acid amides
• A61K 31/265 - Esters, e.g. nitroglycerine, selenocyanates of carbonic, thiocarbonic or thiocarboxylic acids, e.g. thioacetic acid, xanthogenic acid, trithiocarbonic acid
• A61K 31/16 - Amides, e.g. hydroxamic acids
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• C07C 271/56 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring

Abstract

The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.

IPC Classes  ?

• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 31/38 - Heterocyclic compounds having sulfur as a ring hetero atom
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 17/00 - Drugs for dermatological disorders

Abstract

The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.

IPC Classes  ?

• C07C 233/06 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• C07C 233/23 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
• C07D 309/14 - Nitrogen atoms not forming part of a nitro radical
• A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The present invention relates to calixarene derivatives functionalized at the upper and lower rim with arginine or guanidinylated amino acid units through proper variable spacers. The compounds of the invention interact with and non-covalently bind to nucleic acids, condense and transport them inside cells. These compounds can be used as non-viral vectors for cell transfection.

IPC Classes  ?

• C07C 279/14 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups

Abstract

A derivative of nicotinic acid N-oxide is described having formula (I): that acts as inhibitor of enzyme 3-hydroxyanthranilate-3,4-dioxygenase (3HAO), and is thus able to reduce QUIN biosynthesis in vivo under excitotoxic or pathological conditions, said compound being at the same time also chemically stable towards auto-oxidation.

IPC Classes  ?

• C07D 213/89 - 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 having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
• 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
• A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring

Abstract

Use for measuring temperatures of a coordination complex presenting formula I, wherein M1, M2, M3, M4, M5 are chosen, each independently of the others, in the group consisting of: CuI, AgI, AuI, PdII; n is equal to the sum of the oxidation states of M1, M2, M3, M4, M5 minus 3; II represents a respective portion of each tridentate ligand having the formula III in which R1 is chosen in the group consisting of: Ph, C1-C4 alkyl, halo-alkyl C1-C4 substituted phenyl; R2 is chosen in the group consisting of: Ph,C1-C4 alkyl, C1-C4 halo-alkyl-, substituted phenyl; R3 is chosen in the group consisting of: C3-C18 alkyl, benzyl, substituted benzyl, C1- C20 hydroxy-alkyl, C1-C20 alkoxy silane.

IPC Classes  ?

• C09K 11/06 - Luminescent, e.g. electroluminescent, chemiluminescent, materials containing organic luminescent materials
• G01K 11/20 - Measuring temperature based on physical or chemical changes not covered by group , , , or using thermoluminescent materials
• C09K 9/02 - Organic tenebrescent materials

Abstract

Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07C 271/56 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

The invention concerns a derivative of Formule (VII) wherein R27, R28 are, independently of each other, hydrogen, (C1-C6)alkyl, (CH2)n- COOR33, (CH2)n-CONR33R34, (CH2)n-NR33R34 or (CH2)n-morpholine; or NR27R28 is — N N-R27 selected from morpholine, piperidine and Formula (VIII), where R33, R34 are, independently, hydrogen or (C1-C6)alkyl; R29 is hydrogen or (C1-C6)alkyl; R30 is hydrogen or -OR35, where R35 is (C1-C6)alkyl, (CH2)n-NR33R34 or (CH2)n-piperidine or (CH2)n-morpholine, where R33, R34 are, independently, hydrogen or (C1-C6)alkyl; Y is a nitrogen atom or a carbon atom substituted by a cyano group; R31 and R32 are, independently of each other, hydrogen, bromine, chlorine, fluorine, ethinyl or methyl; X is hydrogen, bromine, chlorine, fluorine or -O(CH2)n-Q; Q is an aryl or heteroaryl group, optionally substituted by one or more substituents selected, independently of each other, from hydrogen, chlorine, fluorine, the CF3 radical or - NO2; n is a whole number selected from 0, 1, 2, 3, 4, 5, or 6. The derivatives of the invention are used as irreversible EGFR inhibitors with antiproliferative activity.

IPC Classes  ?

• C07D 239/94 - Nitrogen atoms
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61P 35/00 - Antineoplastic agents
• C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
• 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
• A61K 31/4706 - 4-Aminoquinolines8-Aminoquinolines, e.g. chloroquine, primaquine
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings

Abstract

A drug powder is described and a process for its preparation, which comprises drug particles in amounts equal to or higher than 90% w/w, wherein said drug particles are at least partially coated with an amount lower than or equal to 2.0% w/w of an adjuvant which consists of one or a mixture of C12-C18 saturated fatty acid or their salts. The invention relates particularly to powder of tobramycin.

IPC Classes  ?

• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/00 - Medicinal preparations containing organic active ingredients

Abstract

The described agglomeration of drug microparticles blended with excipient microparticles is a technique for the size enlargement of micronized products that could be damaged by granulation or compaction techniques. These agglomerates can be used as oral prompt or delayed-release dosage forms administered as they are or dispersed in a liquid. The composition and quantity of the excipient microparticles resulted to be the crucial factors for the agglomerate quality. Therefore, adjusting the content of surface-active agent between 8-20 %, of the excipient microparticles it is possible to agglomerate microparticles of drugs that could not be agglomerated per se. Increasing the surfactant concentration in the spray-dried excipient microparticles or increasing the fraction of these excipient microparticles in the blend, the agglomeration was improved. The spray drying technique concentrates the surface-active agent on the microparticle surface. By tumbling, the surface-active agent present on microparticles excipient surface was spread to fill the inter-particle interstices of drug particles giving rise to more resistant agglomerates. This phenomenon occurred also by vibration; the production in this case was quicker.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets

Abstract

Fatty acid amide hydrolase inhibitors of the Formula: 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

IPC Classes  ?

• A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine

Abstract

Device for the treatment of tinnitus, comprising generator means (12) able to generate an audio signal, and transducer means (16) connected to the generator means (12) in order to reproduce the audio signal. The device also comprises filter means (14) interposed between the generator means (12) and the transducer means (16) in order to filter and substantially suppress the audio signal at least in correspondence with an interval of frequencies around the dominant frequency (Ft) of tinnitus, so as to obtain a silent window (silent band) having a selected width or amplitude around said dominant frequency (Ft) of tinnitus.

IPC Classes  ?

• H04R 25/00 - Deaf-aid sets
• A61F 11/00 - Methods or devices for treatment of the ears or hearing sense Non-electric hearing aidsMethods or devices for enabling ear patients to achieve auditory perception through physiological senses other than hearing senseProtective devices for the ears, carried on the body or in the hand

Abstract

Gels of high cytocompatibility and stability are described, obtained from chitosan, specific sugars, alkaline or alkaline-earth metal phosphates and chlorides.

IPC Classes  ?

• C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
• C08L 5/08 - ChitinChondroitin sulfateHyaluronic acidDerivatives thereof
• A61K 47/38 - CelluloseDerivatives thereof

Abstract

A module which is destroyed in the presence of water solution, composed of a compressed powdery mixture, the said powdery mixture comprising a matrix building component, suitable to release an optionally included active substance into a surrounding aqueous liquid, and one or more tabletting aids chosen from the group consisting of lubricants, glidants, and anti-adherent agents, the said module being provided with particular male topological features allowing its connection to a corresponding female module, giving raise to an assembly that can be safely handled on industrial scale, wherein, in the composition of the male module, the percentage ratio between the tabletting aid and the matrix building component is comprised between 1:2.5 and 1:999. The module can be employed to convey pharmaceuticals, nutraceuticals, agrochemicals or other active principles to the intended site of action.

IPC Classes  ?

• A61J 3/10 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
• A61K 9/20 - Pills, lozenges or tablets

Abstract

A surgical instrument (20) for manipulating and inserting into an eye a lamina of cells (7), such as a thin stroma support with Descemet membrane and endothelial cells for corneal transplants, or other types of laminas, comprises a hollow tubular body (1) able to contain the lamina of cells (7) immersed in a maintenance solution. The hollow tubular body (1) comprises a distal part (5), tapered and open at the end, and the section of the distal part (5) diminishes towards the end of the hollow tubular body (1) so that, during use, the lamina of cells (7), emerging from the distal part (5), is able to be configured tubularly, adapting to the section of the end of the distal part (5).

IPC Classes  ?

• A61F 2/14 - Eye parts, e.g. lenses or corneal implantsArtificial eyes
• A61F 9/00 - Methods or devices for treatment of the eyesDevices for putting in contact-lensesDevices to correct squintingApparatus to guide the blindProtective devices for the eyes, carried on the body or in the hand
• A61F 9/007 - Methods or devices for eye surgery

Abstract

Novel melatonin ligands of Formula (I) or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8;Y is selected from the group consisting of hydrogen, aryl, heteroaryl, CrC6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, -OCF3, CF3, C1-C8 alkyl, C1C8 alkyloxy, C1C8 alkylthio, halogen and -Z-(CH2)P-A; R1 is selected from the group consisting of C1C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an -0-(CH2)v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R4 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R6 is selected from the group consisting of hydrogen and C1C6 alkyl; R7 is selected from the group consisting of hydrogen, C1C4 alkyl, C1C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; and R8 is selected from the group consisting of hydrogen and C1C4 alkyl.

IPC Classes  ?

• C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 25/24 - Antidepressants

Abstract

The invention describes novel dried powders of peptide therapeutic agent useful for producing highly respirable aerosols and the methods for their manufacture. Insulin is the peptide therapeutic agent in the preferred embodiment. The powders of insulin prepared for pulmonary administration are characterized by the peculiar structure and shape of the microparticles that allow the powder to flow and to be easy aerosolized. Typical dry powder of insulin described in this patent show corrugated, nonagglomerated microparticles with a low tapped density. The mean geometric diameter (particle size) ranges between 1.0 and 10.0 micron and the mass median aerodynamic diameter (MMAD) ranges between 1.0 and 4.0 micron. These insulin pulmonary powders exhibit in vitro a very high respirable fraction (>75%).

IPC Classes  ?

• A61K 38/28 - Insulins
• A61K 51/12 - Preparations containing radioactive substances for use in therapy or testing in vivo characterised by a special physical form, e.g. emulsion, microcapsules, liposomes

Abstract

It is described a polypeptide molecule able to selectively modulate uric acid conversion into S(+)-allantoin. A pharmaceutical composition for treating uric acid related disorders and a process to selectively modulate uric acid conversion into S(+)-allantoin are also disclosed.

IPC Classes  ?

• C12N 9/78 - Hydrolases (3.) acting on carbon to nitrogen bonds other than peptide bonds (3.5)
• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• C12N 9/88 - Lyases (4.)
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans