The present invention relates to homogeneous formulations comprising omega-3 polyunsaturated fatty acids (n-3 PUFA) and resveratrol for oral administration, in which the resveratrol is solubilized in a solvent system consisting of omega-3 polyunsaturated fatty acids (n-3 PUFA), or their alkyl esters, and a ionic emulsifier. The composition according to the present invention can be formulated as food or nutritional supplement or medicament in the prevention or treatment of cardiovascular diseases due to lipid metabolism disorders and increased platelets aggregation, as well as damages due to free radicals and/or viral diseases.
A61K 47/12 - Carboxylic acids; Salts or anhydrides thereof
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
The present application relates to invention a solid composition comprising omega-3 polyunsaturated fatty acids (n-3 PUFA), or their alkyl esters, and resveratrol, adsorbed on an inert substrate and wherein the recovery of omega-3 is at least 96% after 6 months at 25°C. The composition according to the present invention can be formulated as food supplement or medicament for preventing or treating cardiovascular diseases due to lipid metabolism disorders and increased platelets aggregation; damages due to free radicals selected from the group consisting of atherosclerosis, cancer, inflammatory joint disease, asthma, diabetes, senile dementia and degenerative eye disease; and/or viral diseases.
The present application relates to compositions comprising simvastatin, omega-3 polyunsaturated fatty acids (n-3 PUFA), or their alkyl esters, and a ionic solvent selected between sodium docusate and a phosphatidylcholine-enriched lechitin, wherein the recovery of simvastatin is at least 95% after 6 months at 40°C. The pharmaceutical composition according to the present invention can be used in the prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and all the pathologies related.
Here is described a synergystic composition for promoting female fertility, comprising as active ingredients L-carnitine, acetyl L-carnitine; N-acetyl cysteine, and several specific vitamins, aminoacids, antioxidants and micro elements.
The present invention relates to 7-azaindole derivatives of Formula (I), pharmaceutical compositions containing such derivatives. The invention further relates to said pharmaceutical compositions for use in medicine, and more particularly in the treatment of cancer diseases where an inhibition of PARP is responsive.
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
The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
C07D 205/08 - 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
C07D 207/277 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 211/78 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
The present application relates to a composition comprising a statin totally solubilized in a solvent system consisting of omega-3 polyunsaturated fatty acids (n- 3 PUFA), or their alkyl esters, and a ionic emulsifier selected between sodium docusate and a phosphatidylcholine enriched lecithin. The pharmaceutical composition according to the present invention can be used in the prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and all the pathologies related.
The present invention relates to hyaluronic acid derivative of Formula I, their synthesis and use thereof as cosmetics or as medicaments in a subject in need.
The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
C07D 205/08 - 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
C07D 207/277 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 211/78 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
The present invention describes oxidized avidin, suitable for inhalation, for conditioning the lung affected by inoperable/diffuse diseases, enabling the targeted delivery of biotinylated therapeutic agents to it.
The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
The present invention relates to a composition useful for the treatment of lipid metabolism disorders, comprising one or more of the following active ingredients: (a) extract of rice fermented with Monascus purpureus, (b) at least one omega-3 fatty acid, (c) L-carnitine or a salt thereof; and one or more of the following active ingredients: (d) at least one policosanol or a natural extract containing policosanols; (e) resveratrol or a natural extract containing resveratrol; (f) Coenzyme Q10; and (g) at least one vitamin.
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
It is described a composition, topically administrable, comprising as active ingredients L- carnitine o a derivative thereof, biotin, and at least one or more of the following active ingredients: vitamin B 12; vitamin E; bisabolol; and panthenol; useful for treating skin disorders.
It is described the use of L-carnitine and/ or one or more alkanoyl L- carnitines, or mixture thereof, or one of their pharmaceutically acceptable salts, for the preparation of a medicament or a nutritional supplement useful for preventing or treating the Leber optic neuropathy.
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
C07C 211/31 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the six-membered aromatic ring being part of a condensed ring system formed by at least three rings
C07C 251/34 - Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 251/54 - Oximes having oxygen atoms of oxyimino groups bound to carbon atoms of substituted hydrocarbon radicals of hydrocarbon radicals substituted by singly-bound oxygen atoms
A engineered bacteriophage is herein described, displaying at its surface multiple copies of a polypeptide, which comprises a domain of the bacterial adhesion protein FimH fused with the coat protein pVIII.The domain is preferably the region 45- 159aa of the mature protein FimH. The polypeptide beingantigenic, raises a desired immunological response, in particular against urinary tract infections (UTI) in a human or animal. The engineered bacteriophage is therefore suitable for the preparation of vaccinesfor therapy, diagnosis and/or prevention of urinary tract infections (UTI) in a human or animal.
The invention described herein is directed to the use of acetyl L- carnitine, or propionyl L-carnitine, or a salt thereof, for preparing a medicament for increasing neurogenesis in neural tissue; in which said increased neurogenesis is useful for preventing central nervous system disorders due to ageing or genetic predisposition.
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
22.
COMPOSITION COMPRISING AS ACTIVE INGREDIENT L-CARNITINE IN COMBINATION WITH HYDROXYKYNURENNINE-0-BETA-DL-GLUCOSIDE, FOR THE PREVENTION AND/OR TREATMENT OF PATHOLOGIES OF THE EYE DUE TO ULTRAVIOLET RADIATION
It is described a composition in the form of eye drops or ointment, comprising as active ingredients L-carnitine or a physiologically acceptable salt thereof; and 3-Hydroxykynurenine O-β -DL-glucoside, useful for preventing or treating pathologies of the eyes due to ultraviolet radiation.
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
COMBINATION COMPOSITION, COMPRISING AS ACTIVE INGREDIENT L-CARNITINE OR PROPIONYL L-CARNITINE, FOR THE PREVENTION OR TREATMENT OF CHRONIC VENOUS INSUFFICIENCY
It is described a combination composition comprising as active ingredients L-carnitine or propionyl L-carnitine, troxerutine, diosmine and hesperidine, useful for the prevention and /or treatment of chronic venous diseases.
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
A61K 31/335 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.
This invention relates to a process for preparing a crystalline form of (4S)-11(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing from methanol.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
27.
5-β, 14-β-ANDROSTANE DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEINURIA, GLOMERULOSCLEROSIS AND RENAL FAILURE
Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure.
The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
C07D 307/56 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
C07D 333/26 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom 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 to ring carbon atoms
A61K 31/341 - 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 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/40 - 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
A61K 31/095 - Sulfur, selenium or tellurium compounds, e.g. thiols
A pharmaceutical composition containing as active ingredient a therapeutically effective amount of a derivative of the retinoids having general Formula (I) wherein : R represents H or adamantyl; R' represents OR"'; R" represents, COOH, COO RIV CONHOH, CONH, CONH RIV; R"' represents H or alkyl,; RVI represents H or alkyl; its optically active forms such as enantiomers, diastereoisomers and its racemate forms, as well as pharmaceutically acceptable salts, and the proteasome inhibitor bortezomib, for the treatment of ovarian carcinoma, drug-resistant forms included. The compounds according to the present invention can be administrated in a co-ordinated or combined manner. The combination is also used for the preparation of a medicament for the treatment of ovarian carcinoma.
The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
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
The present invention relates to new retinoid derivatives of Formula (I), and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.
C07C 59/64 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
C07C 69/24 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with monohydroxylic compounds
C07C 69/587 - Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
C07C 69/74 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
C07C 69/96 - Esters of carbonic or haloformic acids
C07C 229/08 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to hydrogen atoms
C07C 229/32 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
C07C 233/05 - 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 atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 255/54 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
C07C 271/42 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 271/52 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 271/54 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07D 295/02 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
33.
USE OF ALKANOYL L-CARNITINE IN COMBINATION WITH CHEMOTHERAPEUTIC AGENTS FOR THE TREATMENT OF NEOPLASMS
The present invention relates to the use of an alkanoyl L-carnitine selected from the group consisting of acetyl, propionyl, valeryl, isovaleryl and butirryl L-carnitine; in combination with one or more chemotherapeutic agent selected from the group consisting of: a camptothecin derivative; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; toxins; and imides; for the treatment of neoplasms.
A61K 31/475 - Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
The present invention relates to the use of acetyl L-carnitine for the preparation of a medicament for the prevention and/or treatment of cancer. Methods of preventing and/or treatment of cancer by administering an effective amount of acetyl L-carnitine to subject in need thereof are also disclosed.
A61K 31/475 - Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
It is described a composition comprising as active ingredients green tea extract and pomegranate extract for the prevention or reduction of the progression of prostate cancer.
It is described the use of L-carnitine, in combination with antioxidants such as vitamin E and inorganic elements such as manganese, zinc, sodium and potassium, for the preparation of a physiological supplement or medicament for opthalmic use, for the prevention or treatment of accomodative asthenopia.
It is described here the use of a compound (ST1926) belonging to the class of atypical retinoids for the preparation of a medicament for treating pathological states, which arise from a complex series of cellular responses to vascular injury, for example after some surgery procedures, such as angioplasty, bypass grafting, endartherectomy and stent implantation
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
The present invention relates to dual-targeting cytotoxic compounds of formula (I) and to their preparation. The described compounds are endowed with tumour specific action, incorporating three functional units: a tumour recognition moiety and a tumour selective enzymatic substrate sequence connected together by means of a spacer. These conjugates are designed to guarantee serum stability and, at the same time, the desired action inside the tumour cells as a result of enzymatic cleavability. [(L-D)nE]m-F-D-PI-SI-CT Formula (I).
The present invention relates to new oxime carbamoyl derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
C07C 271/60 - Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups having oxygen atoms of carbamate groups bound to nitrogen atoms
C07D 295/20 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
C07D 333/22 - Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 25/00 - Drugs for disorders of the nervous system
41.
ENOL CARBAMATE DERIVATIVES AS MODULATORS OF FATTY ACID AMIDE HYDROLASE
The invention provides novel enol carbamate derivatives of formula (I) for inhibiting Fatty Acid Amide Hydrolase (FAAH), compositions that include such compounds as well as methods of treating diseases of energy metabolism, central nervous system disorders, cardiovascular and respiratory disorders, retinopathy, cancer, gastrointestinal and liver disorders and/or musculoskeletal disorders. The compounds of the present invention proved particularly efficacious in animal models of anxiety and pain.
C07C 271/12 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms 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 271/28 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
42.
9-SUBSTITUTED CAMPTOTHECIN DERIVATIVES AS ANTITUMOR COMPOUNDS
ISTITUTO NAZIONALE PER LO STUDIO E LA CURA DEI TUMORI (Italy)
Inventor
Dallavalle, Sabrina
Merlini, Lucio
Zunino, Franco
Giannini, Giuseppe
Abstract
Compounds are described with the general formula (I) in which the groups are as defined in the description and characterized by the presence of substituents in position 9. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicines for the treatment of tumours and viral and parasite infections.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
New aminooxime derivatives at position 3 of 2-and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described,where the radicals have the meanings described in detail in the application.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
The present invention relates to a new crystalline form of R-4- trimethylammonium-3-(tetradecylcarbamoyl)-amino butyrate (also named crystalline Form I of ST 1326 or teglicar), a process for its preparation and pharmaceutical compositions containing same.
C07C 275/14 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
C07C 275/16 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/00 - Drugs for disorders of the cardiovascular system
45.
CRYSTALLINE FORM II OF 7-(DIMETHOXY-METHYL) CAMPTOTHECIN, ITS USE AS INTERMEDIATE AND PRODUCTS OBTAINED THEREFROM
This invention relates to a process for preparing a crystalline form of (4S)-11-(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]qui-no line-3,14(4H,12H)-dione (also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing it from methanol.
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of pediatric tumors such as for examplerhabdomyosarcoma, primitive neuroectodermal tumors (PNET) and neuroblastoma.
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
The present invention describes chemically modified avidins that have higher permanence in treated tissues compared to wild type avidin. Avidin oxidation is performed by periodate incubation in the presence of the low affinity ligand HABA which, occupying the biotin binding sites, prevents protein denaturation during the oxidation step. Periodate oxidation generates CHO groups from avidin mannose ring opening that, once injected, react with tissue NH2 residues to form stable Schiff's bases. The anchored avidins maintain the ability to bind biotinylated agents endowed of therapeutic activity, like radiolabeled biotins, stem cells and somatic cells, useful for brachytherapies like Intraoperative Avidination Radionuclide Therapy (IARTꡞ) or degenerative or genetic diseases.
New heparin derivatives having low molecular weight are described as well as their use for the treatment of neurovegetative disorders related to the amyloidogenesis, such as Alzheimer's disease or diseases brought about by prions.
Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/ or treatment of obstructive vascular lesions following vascular surgery and for the prevention and/or treatment of diseases due to organ fibrosis.
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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
50.
COMPOSITION USEFUL FOR THE PREVENTION OF ADVERSE EFFECT DUE TO THE USE OF PPAR-GAMMA AGONISTS
The present invention relates to the use of acetyl L-carnitine, or a pharmaceutically acceptable salt thereof, for the prevention of theadverse effects,such as steoporosis, weight gain and edema, due to the use ofPPAR-gamma agonists selected from the group consisting of spirolaxine or a glitazonederivative selected fromthe group consisting ofroglitazone, pioglitazone androsiglitazone.
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
51.
GEL USEFUL FOR THE DELIVERY OF COSMETIC ACTIVE INGREDIENTS
It is described a gel, for cosmetic use, composed of a mixture of a polymer which forms a gel, a surfactant, and propionyl L-carnitine glycinate hydrochloride, useful for treating disturbances of the skin such as cellulite and wrinkles.
A61K 8/44 - Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts, esters or N-acylated derivatives thereof
A61K 8/81 - Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
A61Q 19/06 - Preparations for care of the skin for countering cellulitis
An anti-EpCAM antibody, designated ST3232/10, of murine origin exhibits properties suitable for both therapeutic and diagnostic applications. It shows high affinity for the native antigen and good tumour selectivity.
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
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
53.
COMPOSITION USEFUL FOR THE PREVENTION OF TYPE 2 DIABETES AND ITS COMPLICATIONS IN PRE-DIABETIC PATIENTS WITH INSULIN RESISTANCE
The present invention relates to the use of acetyl L-carnitine in combination with an anti hypertensive drug, and a statin, for the preparation of a medicament for the prevention or delay of onset of type 2 diabetes and its complications, in pre-diabetic patients with insulin resistance.
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
A61K 31/366 - Lactones having six-membered rings, e.g. delta-lactones
A61K 31/405 - Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 and CF3 for the preparation of a medicament, in particular for for selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells, for inducing differentiation of tumor cells in a tumor, for inhibiting the activity of histone deacetylase and for the treatment of primary cancer or secondary cancer.
C07D 273/02 - Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups having two nitrogen atoms and only one oxygen atom
C07D 273/01 - Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups having one nitrogen atom
55.
COMPOSITION USEFUL FOR THE TREATMENT OF TYPE 2 DIABETES
It is described the use of L-camitine and/or an alkanoyl L-camitine, or a pharmaceutically acceptable salt thereof, in combination with a statin, for the preparation of a medicament for the treatment of type 2 diabetes.
ISTITUTO NAZIONALE PER LO STUDIO E LA CURA DEI TUMORI (Italy)
Inventor
Pisano, Claudio
Vesci, Loredana
Zunino, Franco
Abstract
A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of a cancer or tumor pathology selected from the group consisting of head and neck carcinoma, pancreas carcinoma, melanoma, bladder carcinoma, mesothelioma and epidermoid skin carcinoma.
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
The invention described herein relates to a method for identifying the antigenic regions of HCMV proteins involved in the human B-cell response to HCMV infection, for combining such antigenic regions in the form of chimeric fusion products, and their use as diagnostic and immunogenic agents.
The present invention relates to pharmaceutical compositions comprising a topoisomerase I inhibitor including, but not limited to, a camptothecin derivative.
A61K 31/4741 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
59.
COMBINATION OF A RETINOID AND A PLATINUM ANTICANCER AGENT
A combination comprising an atypical retinoid compound, preferably E-4- (3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid and an anticancer drug of the platinum family, preferably cisplatin, together witha pharmaceutical composition comprising it and a kit for its administration in unitary or in coordinated sequential form.The kit preferably comprises a first formulation of E-4-(3-(1-adamantyl)-4-hydroxyphenyl)cinnamic acid dissolved in a mixture of ethanol and cremophor, and suspended in a saline solution, and a second formulation of cisplatin in saline solution.The combination is used for the preparation of a medicament to inhibit tumor growth and tumor migration,in particular for the treatment of ovarian tumor and/or carcinoma.
It is described a gel composed of a mixture of a polymer which forms a gel, a buffer; a saccharide and one or more active ingredients useful for treating diseases of the eyes.
Use of L-carnitine or a pharmaceutically acceptable salt thereof, for the preparation of an opthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal oedema.
USE OF L-CARNITINE OR OF ALKANOYL L-CARNITINES FOR THE PREPARATION OF A PHYSIOLOGICAL SUPPLEMENT OR MEDICAMENT FOR OPHTHALMIC USE IN THE FORM OF EYE DROPS
Use of L-carnitine and/or of one or more alkanoyl L-carnitines or one of their pharmaceutically acceptable salts for the preparation of an opthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal diseases.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
The invention concerns the use of thymosin alpha 1 for the preparation of a medicament for the prevention and treatment of autoimmune diseases such as multiple sclerosis, and inflammatory bowel diseases such as Crohn's disease or ulcerative colitis.
The invention provides a new class of compounds capable of inhibiting carnitine palmitoyl transferase (CPT) having formula (I). The invention also relates to pharmaceutical compositions, which comprise at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, such as for example congestive heart failure and obesity.
C07C 275/34 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
C07C 275/24 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
C07C 275/16 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
C07C 235/20 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
New aminoalkoxyimino derivatives at position 3 of substituted B- homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
C07J 3/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by one carbon atom
C07J 63/00 - Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/566 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol having an oxo group in position 17, e.g. oestrone
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
It is described the use of thymosin alpha in combination with dacarbazine and optionally with Interferon alpha, for preparing a medicament for the treatment of malignant melanoma on stage IV characterized by distant unresectable metastases.
It is described the use of thymosin alpha 1 for preparing a medicament useful for the prevention or treatment of graft-versus-host disease or graft rejection reactions in organ transplantation, in a mammal subject, in which the cells, tissues or organs for transplant is selected from the group comprising: stem cells, hematopoietic stem cells, bone marrow, heart, liver, kidney, lung, pancreas, small intestine, cornea or skin.
It is described the use of thymosin alpha 1 in combination with long pentraxin PTX3 or Ganciclovir, for the preparation of a medicament for the prevention or treatment of viral diseases and/or for inhibiting virus activation.
Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+,K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
71.
AMINO DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS
Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
C07J 41/00 - Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
Antimalarial agents having a novel pharmacophore of formula (I) are herein described. These polycyclic compounds are able to inhibit chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum (Pf). Furthermore, the synthesis of these compounds involves few steps from commercial products with low cost of production.
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 233/54 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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
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
C07C 211/27 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
C07D 235/06 - Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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 409/06 - 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 carbon chain containing only aliphatic carbon atoms
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 417/06 - 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 carbon chain containing only aliphatic carbon atoms
73.
QUINOLIN-4-YLHYDRAZINE DERIVATIVES AS ANTIMALARIAL AGENT
Novel quinolyl and acridinylhydrazone compounds of formula (I), which present remarkable biological activity especially against the choloroquine-resistant Plasmodium falciparum strains, useful for the treatment and prevention of malaria infection are described herein.
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 413/12 - 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
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 215/42 - Nitrogen atoms attached in position 4
The invention relates to a new class of compounds with inhibitory action on carnitine palmitoyl transferase (CPT) in the central nervous system (SNC), derived from trimetazidine and perhexiline, preferentially selective for the hepatic form of CPT1 (CPT1L), pharmaceutical compounds which contain at least one new compound according to the invention, and their therapeutic use in the treatment and/or in the prevention of obesity, hyperglycaemia, diabetes and disorders associated with them, such as, for example, diabetic retinopathy, diabetic neuropathy and cardiovascular disorders. The compounds of the present invention are also used in the prevention and/or treatment of heart disorders such as CHF (congestive heart failure).
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 295/08 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
C07D 295/12 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
A61K 31/455 - Nicotinic acid, i.e. niacin; Derivatives thereof, e.g. esters, amides
It is described a vector suitable for efficient selection and/or maturation of a recombinant antibody characterized in that it contains at least one element able to reduce the expression level and/or has an improved efficiency of display of said recombinant antibody.
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
C40B 40/08 - Libraries containing RNA or DNA which encodes proteins, e.g. gene libraries
C40B 50/06 - Biochemical methods, e.g. using enzymes or whole viable microorganisms
The present invention relates to the use of a compound belonging to the class of atypical retinoids for the preparation of a medicament for treating pathological states, which arise from a complex series of cellular responses to vascular injury, for example after some surgery procedures, such as angioplasty, bypass grafting, endartherectomy and stent implantation.
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 43/00 - Drugs for specific purposes, not provided for in groups
A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I.
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
New crystalline forms of 17β-(3-Furyl)-5-βandrostane-3β,14β,17α-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.
C07J 17/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
Compounds useful in the treatment of disorders characterised by deposits of amyloid aggregates are herein described together with pharmaceutical compounds containing the same. In particular the compounds of the present invention are those having the Formula (I) as reported below. where the radicals have the meaning indicated in the description.
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
C07C 215/84 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings being part of condensed ring systems
C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
C07C 227/16 - Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
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
80.
DIETARY SUPPLEMENT ENERGY-PROVIDING TO SKELETAL MUSCLES AND PROTECTING THE CARDIO VASCULAR TRACT
Dietary supplements - providing energy and strengthening skeletal muscles and facilitating skeletal muscles ability to sustain prolonged periods of physical activity - containing propionyl-L-carnitine or one of its salts, coenzyme Q10, nicotinamide, riboflavin, pantothenic acid and optionally other components such as amino acids and creatines.
Is described the use of propionyl L-carnitine, or a pharmaceutical salt thereof, for preparing a medicament for the prevention and/or treatment of left ventricular hypertrophy in ESRD or dialysed patients.
Formula (I) compounds are described: Formula (I) where the radicals are as defined in the description, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
83.
IMMEDIATE RELEASE THERAPEUTIC SYSTEMS FOR IMPROVED ORAL ABSORPTION OF 7- [ (E) -TERT-BUTYLOXYIMINOMETHYL] CAMPTOTHECIN
A pharmaceutical composition comprising a camptothecin as active ingredient is herein described. In particular immediate-release therapeutic systems are described for the improved oral absorption of 7-[(E)-t-butyloxyminomethyl] camptothecin, comprising a matrix consisting of liquid amphiphilic substances or having a melting point lower than 60°C, in which the active principle is at least partially dissolved and/or dispersed and/or inglobated.
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/44 - Oils, fats or waxes according to two or more groups of ; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
84.
USE OF A COMBINATION COMPRISING L-CARNITINE OR ALKANOYL L-CARNITINE, LIPID SOLUBL BENZOQUINONE AND OMEGA-3-POLYUNSATURATED FATTY ACID FOR THE PREPARATION OF A DIETARY SUPPLEMENT OR MEDICAMENT FOR THE TREATMENT OF CORNEAL DISEASES
Use of L-carnitine and/or one or more alkanoyl L-carnitines or one of their pharmaceutically acceptable salts for the preparation of a dietary supplement or medicament for the treatment of corneal diseases.
A61K 31/122 - Ketones having the oxygen atom directly attached to a ring, e.g. quinones, vitamin K1, anthralin
A61K 31/202 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having three or more double bonds, e.g. linolenic acid
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
A process for the synthesis of deoxybiotinyl hexamethylenediamine-DOTA is herein described. Said process comprises reacting biotinyl hexamethylenediamine with tri-t-butyl-DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as the base.
USE OF L-CARNITINE OR OF ALKANOYL L-CARNITINES FOR THE PREPARATION OF A PHYSIOLOGICAL SUPPLEMENT OR MEDICAMENT FOR OPHTHALMIC USE IN THE FORM OF EYE-DROPS
Use of L-carnitine and/or of one or more alkanoyl L-carnitines or one of their pharmaceutically acceptable salts for the preparation of an opthalmic physiological supplement or medicament in the form of eye-drops, for the treatment of corneal diseases.
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
A61K 31/205 - Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
A61K 9/00 - Medicinal preparations characterised by special physical form
Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumour, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumours.
C07C 259/06 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
A61K 31/185 - Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
Cinnamic and phenylpropiolic acid derivatives of Formula (I) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
C07C 251/48 - Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
C07C 251/80 - Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
C07D 209/08 - Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
Indole derivatives of Formula (I+A) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/405 - Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
The use of a substance belonging to the class of atypical retinoids for the topical treatment of acne is described. In particular the effects on an animal model for this skin disease of a pharmaceutical or cosmetic compound for topical use containing adamantyl methoxydiphenyl propenoic acid formulated in a gel are demonstrated.
The use of acetyl L-carnitine, or of one of its pharmaceutically acceptable salts, is described for the preparation of a medicament useful for the prevention of painful peripheral neuropathy in patients suffering from type 2 diabetes, in which said symptoms are selected from the group consisting of pain, paraesthesia and hyperaesthesia, in which the acetyl L-carnitine is administered orally at a dose of at least 3 grams/day.
A61K 31/221 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
92.
CARNITINE-CONTAINING PERITONEAL DIALYSIS SOLUTION HAVING IMPROVED BIOCOMPATIBILITY
The protective effect on peritoneum of L-carnitine and its lower alkanoyl derivatives, both in the form of inner or pharmaceutically acceptable salts is disclosed. Concentrations of carnitine from about 0.02 to 0.5% w/v are suitable for preparing a solution for peritoneal dialysis having higher biocompatibility and protecting peritoneum from toxic effects of continuous use of solutions for peritoneal dialysis, in particular ones containing glucose as osmotic agent. A particularly preferred embodiment is a solution for peritoneal dialysis containing carnitine, glucose and xylitol.
A61K 31/195 - Carboxylic acids, e.g. valproic acid having an amino group
A61K 31/35 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
A61P 13/00 - Drugs for disorders of the urinary system
The invention relates to a new class of compounds with action inhibiting carnitine palmitoyl transferase (CPT), pharmaceutical compounds which contain at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, congestive heart failure and obesity.
C07C 275/16 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
C07D 211/90 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
