The present invention relates to 3-ethyl-3-phenylazepane derivatives having dual pharmacological activity towards both the sigma (σ) receptor and the μ- opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 223/04 - Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
2.
OXADIAZASPIRO COMPOUNDS FOR THE TREATMENT OF DRUG ABUSE AND ADDICTION
The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to oxadiazaspiro compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular against drug abuse and addiction.
The present invention relates to oxa-azaspiro compounds having pharmacological activity towards the sigma (σ) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
The present invention relates to oxa-diazaspiro compounds having pharmacological activity towards the sigma (σ) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
The present invention relates to substituted morpholine derivatives having pharmacological activity towards the sigma (σ) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 413/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to 1 -(4-(2-((1 -(3,4-difluorophenyl)-1 H-pyrazol-3-yl)methoxy)ethyl)piperazin-1 -yl)ethanone salts, specifically to the hydrochloride and to the maleate, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of sigma receptor associated diseases.
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
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The invention relates to compounds of general formula (I) having pharmacological activity towards the sigma receptor, for use in the treatment prevention of dyslipidemia.
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 amide derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
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 31/40 - 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 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 25/04 - Centrally acting analgesics, e.g. opioids
9.
SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to substituted amide derivatives of formula (I) having dual pharmacological activity towards both the sigma (σ) receptor, and the p-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 405/14 - 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 three or more hetero rings
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
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 405/04 - 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 directly linked by a ring-member-to-ring- member bond
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
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
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
C07D 295/125 - 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 with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
C07D 295/13 - 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 with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
C07D 295/135 - 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 with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61P 25/04 - Centrally acting analgesics, e.g. opioids
10.
ADENOASSOCIATED VIRUS VECTORS FOR THE TREATMENT OF MUCOPOLYSACCHARIDOSES
The present invention provides new Adeno-associated virus-derivedvectors and pharmaceutical compositions containing the same for the treatment of lysosomal storage disordersand specially, for the treatment of mucopolysaccharidoses Type II.
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to spiro-isoquinoline-4,4'-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to spiro-isoquinoline-3,4'-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
The invention relates to compounds of formula (I) or formula (II) having pharmacological activity towards the sigma receptor, for use in the treatment or prevention of osteoarthritis and pain due to osteoarthritis.
The present invention relates to 1-methylpyrazole-piperazine compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
15.
METHYL-1H-PYRAZOLE ALKYLAMINE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to methyl-1H-pyrazole alkylamine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 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
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to 1,9-diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
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 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 25/04 - Centrally acting analgesics, e.g. opioids
17.
SPIRO-ISOQUINOLINE-1,4'-PIPERIDINE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to spiro-isoquinoline-1,4'-piperidine compounds having dual pharmacological activity towards both the sigma (σ) receptor and the μ-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
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 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The present invention relates to new tricyclic triazolic compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
The present invention relates to compounds of general formula (I) having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
20.
AMIDE DERIVATIVES OF 1-OXA-4,9-DIAZASPIRO UNDECANE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. (formula 1) wherein Y is (formula 2) or (formula 3) • n is 1 or 2; • q is 1, 2, 3, 4, 5 or 6; • X is a bond, -C(O)O-, -C(0)NR 8-, -C(O)-, -0- or -C(R 4R 4.)-; • R 1is C(0)R 5or S(O) 2R 5.
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
21.
ALKYL DERIVATIVES OF 1-OXA-4,9-DIAZASPIRO UNDECANE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
22.
ADENOASSOCIATED VIRUS VECTORS FOR THE TREATMENT OF LYSOSOMAL STORAGE DISORDERS
The present invention provides new adenoassociated virus vectors and pharmaceutical compositions containing the same for the treatment of lysosomal storage disorders and specially, for the treatment of mucopolysaccharidoses Type IIIB.
The present invention relates to solid particles of a poorly soluble drug, pharmaceutical compositions comprising them and processes for their preparation. The compositions according to the present invention show an improved dissolution profile while being stable.
The invention refers to a synergistic combination comprising a Sigma ligand of general formula (I), and a Serotonin–Norepinephrine Reuptake Inhibitor (SNRI), a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and/or treatment of pain.
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to piperidene compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 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
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 25/04 - Centrally acting analgesics, e.g. opioids
The invention refers to a synergistic combination comprising a Sigma ligand of general formula (I), and a Gabapentinoid, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and/or treatment of pain.
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
The present invention relates to new fused imidazolyl derivatives having a high affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
The present invention relates to compounds having dual pharmacological activity towards both the sigma receptor and the mu-opioid receptor, and more particularly to piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - 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 three or more hetero rings
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
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 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 25/04 - Centrally acting analgesics, e.g. opioids
29.
PIPERAZINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to piperazine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/64 - 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 with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
The invention refers to a synergistic combination comprising a Sigma ligand, particularly a Sigma ligand of general formula (I), and NSAID compound, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and/or treatment of pain.
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
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The invention refers to compounds of general formula (I) wherein the variables take various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.
C07C 217/44 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and containing rings
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 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 295/096 - 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 with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic 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
A61P 25/00 - Drugs for disorders of the nervous system
32.
USE OF SIGMA RECEPTOR LIGANDS FOR THE PREVENTION AND TREATMENT OF PAIN ASSOCIATED TO INTERSTITIAL CYSTITIS/BLADDER PAIN SYNDROME (IC/BPS)
The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS).
The invention refers to compounds of general formula (I) wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
34.
PYRAZINO[1,2-a]INDOLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS
The invention refers to compounds of general formula (I) wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
35.
ALPHA-2 ADRENOCEPTOR AND SIGMA RECEPTOR LIGAND COMBINATIONS
The invention refers to a combination comprising a Sigma ligand of general formula (I) and alpha-2-adrenergic agonist compound, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and/or treatment of pain.
The present invention relates to new tricyclic triazolic compounds of formula (I) having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments for treating e.g. pain related diseases
The present invention relates to new 1,2,3-triazole-amine derivatives of formula (I), having affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments for the treatment of sigma receptor related diseases and disorders.
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 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
The present invention relates to new substituted pyrazolo[3,4- d]pyrimidine compounds of general formula (I) having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them and to their use as medicaments for the treatment of i.a. pain. n is selected from 1, 2, 3 or 4; R1 represents a carbon-linked optionally substituted aryl or heteroaryl radical; R2 and R3 independently represent a hydrogen atom, an optionally substituted aliphatic, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl radical, or R2 and R3 together with the bridging nitrogen form an optionally substituted heterocycloalkyl or heteroaryl radical.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Sánchez Palomino, Sonsoles
Álvarez Fernández, Carmen
Abstract
The present invention relates to the development of non-replicative virions comprising a human immunodeficiency virus (HIV) genome and vehiculized by the G protein of a vesicular stomatitis virus (VSV).Said virions areuseful in medicine, specifically for use in generating vaccines and more specifically for treating AIDS. The present invention further relates to a method for obtaining a customized vaccine.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Blanco Arbués, Julián Miguel
Carrillo Molina, Jorge
Abstract
The present invention relates to an in vitro method for determining HIV neutralizing antibodies in a sample. It further relates to a fusion protein to be used in said method and a nucleic acid encoding said fusion protein.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Joseph, Joan
Saubi Roca, Narcis
Abstract
The invention relates to polynucleotides and recombinant cell strains comprising said polynucleotides and the uses thereof for the delivery of the polypeptides encoded by said polynucleotides to a subject in need thereof. In particular, the invention refers to polynucleotides comprising a polypeptide of interest, auxotrophy-complementing genes and the use thereof in a mycobacterial double auxotrophic host cell to achieve the stable expression of the polypeptide of interest by using an antibiotic- free plasmid selection system.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Noguera I Julian, Marc
Paredes, Roger
Abstract
The invention relates to an enhanced method for rapid immunogen selection (RIS) based on the binding a library of recombinant viruses containing randomized variants of a surface polypeptide displayed to said neutralizing antibodies. The invention relates as well to the use of the immunogens isolated according to the RIS method of the invention in medicine for the treatment of diseases caused by a virus and in diagnosis for the identification of neutralizing antibodies in a patient.
The present invention relates to new indene derivatives having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
C07D 295/03 - 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 containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
C07D 213/36 - Radicals substituted by singly-bound nitrogen atoms
C07D 213/12 - Preparation by ring-closure involving the use of ammonia, amines, amine salts, or nitriles from unsaturated compounds
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 333/20 - Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/4465 - Non-condensed piperidines, e.g. piperocaine only substituted in position 4
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
44.
IMIDAZO[2,1-b]THIAZOLE DERIVATIVES, THEIR PREPARATION AND USE AS MEDICAMENTS
The present invention relates to new imidazo[2,1-b]thiazole derivatives (I) having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
The present invention relates to heterocyclyl-substituted-phenyl compounds of general formula (I), wherein A is a compound selected from the following group: n is selected from 0 or 1, for use in the treatment of erectile dysfunction and the pharmaceutical compositions comprising them.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
The present invention refers to a controlled release pharmaceutical formulation in solid form comprising Mesalamine. The invention also contemplates the preparation of the said formulation and its use for the treatment of patients suffering from inflammatory bowel disease (IBD).
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
Inventor
Ruiz Riol, Marta
Brander, Christian
Ibarrondo, Javier
Abstract
The invention relates to a method and a diagnostic kit for monitoring HIV specific T cell responses and identifying subjects capable of controlling HIV progression or preventing HIV infection altogether. The method is based on the combined use of boosted flow cytometry and toggle peptides and can cover a vastly larger set of effector functions than standard assays. The method is also suitable to detect T cell responses of any desirable cytokine or combination of cytokines to any pathogen.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
García Alcaide, Felipe
Gallart, Teresa
Climent Vidal, Núria
Gil Roda, Cristina
Gatell Artigas, Josep María
Abstract
The present invention relates to a process for obtaining an antigen- loaded dendritic cell showing higher viability and migratory capacity towards lymphatic nodes. The invention also relates to vaccines containing said dendritic cells as well as to the use thereof for the treatment of infectious diseases, especially AIDS.
Compositions comprising a mixture of at least two types of particles wherein a) the first type of particles comprise dabigatran etexilate in the form of the free base or in the form of pharmaceutically acceptable salts, polymorphs, solvates or hydrates thereof; and b) the second type of particles comprise at least one pharmaceutically acceptable organic acid, use of said compositions in the reduction of the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation and/or in the prevention of venous thromboembolic events in adult patients who have undergone elective total hip replacement surgery or total knee replacement surgery and processes for the preparation of said compositions.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
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
A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
51.
SUBSTITUTED PYRANO AND FURANOQUINOLINES, THEIR PREPARATION AND USE AS MEDICAMENTS
The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
A61K 31/436 - 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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
A61P 25/04 - Centrally acting analgesics, e.g. opioids
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
Inventor
Brander, Christian
Mothe Pujadas, Beatriz
Llano, Anuska
Abstract
The present invention relates to novel immunogens based on overlapping peptides (OLPs) and peptides derived therefrom useful for the prevention and treatment of AIDS and its related opportunistic diseases. The invention also relates to isolated nucleic acids, vectors and host cells expressing these immunogens as well as vaccines including said immunogens.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
Inventor
Buzón, Mª José
Martínez-Picado, Javier
Abstract
The present invention relates to a method for obtaining an antigen- loaded dendritic cell in vitro comprising contacting an immature dendritic cell with an immunogen, preferably a HIV immunogen, and simultaneously, during at least part of said step, placing said immature dendritic cell under conditions adequate for maturation. The invention relates also to HIV-1 immunogens lacking a functional integrase protein.
An assay for identifying ligands of the σι receptor based on a fusion protein comprising the σι receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive FRET when no ligand is bound to the σι receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist. Said fusion protein has been expressed in a cell, giving rise to a new cellular model useful for identifying σι receptor ligands, and additionally for discriminating between agonists and antagonists.
C12N 15/62 - DNA sequences coding for fusion proteins
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/74 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving hormones
G01N 33/542 - ImmunoassayBiospecific binding assayMaterials therefor with immune complex formed in liquid phase with steric inhibition or signal modification, e.g. fluorescent quenching
55.
INHIBITORS OF SIALOADHESIN FOR THE TREATMENT OF DISEASES CAUSED BY ENVELOPED VIRUSES
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
RUPRECHT-KARLS-UNIVERSITAET HEIDELBERG (Germany)
Inventor
Izquierdo Useros, Nuria
Kraüsslich, Hans-Georg
Lorizate, Maier
Martínez Picado, Javier
Abstract
The present invention refers to methods and compositions to prevent viral entry into cells expressing the CD169/sialoadhesin surface receptor by inhibiting the coupling of the sialyllactose molecule contained in the viral membrane gangliosides to the CD 169/ sialoadhesin receptor. The invention also pertains to vaccine compositions based on dendritic cells loaded with an antigen of interest whereby the vaccine is provided together with a composition capable of preventing viral entry into cells expressing the CD169/sialoadhesin. Moreover, the invention relates to diagnostic and therapeutic compositions that can be specifically delivered to enveloped virions wherein the diagnostic/therapeutic agent is coupled to CD169/sialoadhesin.
The present invention refers to oral solid pharmaceutical compositions comprising concentrate omeprazole pellets, processes for the preparation of the same and their use as medicaments, more particularly for the treatment and/or prophylaxis of a gastrointestinal disorder.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
C07D 209/08 - IndolesHydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
C07D 265/16 - 1,3-OxazinesHydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with only hydrogen or carbon atoms directly attached in positions 2 and 4
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
58.
METHOD FOR MONITORING CYTOTOXIC T LYMPHOCYTE (CTL) RESPONSES BY A DELAYED-TYPE HYPERSENSITIVITY REACTION USING DEFINED CTL VIRAL EPITOPES
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
Inventor
Brander, Christian
Ruiz Riol, Marta
Abstract
The present invention relates to an in vivo method for monitoring cytotoxic T lymphocyte (CTL) responses by inducing a delayed-type hypersensitivity (DTH) reaction using defined CTL epitopes. It further relates to the epitopes and the kits them.
The present invention relates to new pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA (Spain)
Inventor
Arnedo Valero, Mireia
Plana Prades, Montserrat
Gatell Artigas, Josep María
Abstract
The invention relates to methods for the identification of HIV-1infected subjects capable of controlling viral load based on the determination of the expression levels of several miRNAs. In addition, the invention also relates to methods for controlling HIV infection by using some of the differentially expressed miRNAs or polynucleotides encoding said miRNAs,as well as to compositions comprising a miRNA or a polynucleotide encoding said miRNA and an anti-HIV agent.
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
C12Q 1/70 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving virus or bacteriophage
61.
USE OF SIGMA LIGANDS IN DIABETES TYPE-2 ASSOCIATED PAIN
The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.
The invention refers to a new doxylamine resinate complex comprising doxylamine bound to a weakly acidic synthetic cation exchange resin, such as a copolymer of methacrylic acid and divinylbenzene The invention discloses a process for its preparation which comprises contacting a weakly acidic synthetic cation exchange resin with doxylamine or a pharmaceutically acceptable salt thereof and its use for the preparation of pharmaceutical compositions, such as chewable tablets or oral disintegrating tablets of immediate release. Further the invention refers to the doxylamine resinate complex for use as a medicament, preferably as a medicament for use in the treatment of occasional insomnia.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Yuste Herranz, María Eloísa
Sánchez Merino, Víctor
Ferreira, Carolina
Abstract
The invention relates to a method for rapid immunogen selection (RIS) based on the binding a library of recombinant viruses containing randomized HIV gp120 variants of a surface polypeptide displayed to said neutralizing antibodies. The invention relates as well to the use of the HIV gp120 immunogens isolated according to the RIS method of the invention in medicine for the treatment of diseases caused by a virus and in diagnosis for the identification of neutralizing antibodies in a patient.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA-CAIXA (Spain)
Inventor
Fabriàs Domingo, Gemma
Goñi Urcelay, Félix
Izquierdo Useros, Nuria
Llebaria Soldevila, Amadeu
Mañes Brotón, Santos
Martínez Picado, Javier
Abstract
The application relates to a method for the treatment of a disease caused by HIV infection by administering to a patient in need thereof of a specific inhibitor of the dehydroceramide desaturase. The invention relates as well to compositions comprising a Des-1inhibitor and one or more drugs suitable for the treatment of diseases caused by HIV infection as well as to methods for the identification of compounds suitable for the treatment of said diseases.
This invention relates to compressed solid oral dosage form able to contain a high load of active pharmaceutical ingredient, showing a controlled release profile, and consisting of individual particles wherein each individual particle comprises an active pharmaceutical ingredient and wherein each individual particle is coated with a layer comprising at least one plasticizer.
The invention relates to pyrazole derivatives of formula (I) having pharmacological activity and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of pain.
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to indazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and/or prophylaxis, in particular for the treatment of psychosis or pain.
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/00 - Drugs for disorders of the nervous system
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (Spain)
UNIVERSITY OF WASHINGTON (USA)
Inventor
Mothe Pujadas, Beatriz
Brander, Christian
Mullins, James, I.
Abstract
The invention relates to peptides comprising part or all of a conserved element within a Center-of-Tree (COT) sequence derived from a family of polypeptides encoded by naturally occurring variants of HIV. The invention also relates to immunogenic compositions and vaccines comprising said peptides. The invention also relates to methods for the identification of HIV controller patients based on the detection of the T cells of the patient to mount a cytotoxic T cell response against said peptides and to methods for the identification of immunogenic peptides within a family of variant polypeptides.
FUNDACIÓ PRIVADA INSTITUT DE RECERCA DE LA SIDA - CAIXA (Spain)
Inventor
Blanco Arbués, Julián Miguel
Carrillo Molina, Jorge
Curriu Martí, Marta
Abstract
The invention relates to human immunodeficiency virus (HIV) immunogens based on gp41 epitopes located in the membrane proximal extracellular region (MPER). The immunogens of the present invention are capable of inducing serum neutralizing activity. Various forms of these isolated immunogens are disclosed and exemplified. Isolated nucleic acid molecules expressing relevant portions of these immunogens, as well as the vectors and host cells utilized for their production, are also within the scope of the present invention.
The present invention relates to solid forms having a low degree of crystallinity or substantially amorphous of the hydrochloride salt of 4-[2-[[5-methyl-1-(2-naphthalenyl)-1H-pyrazol-3-yl]oxy]ethyl]morpholine (P027) and processes for their preparation.
The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat opioid-induced hyperalgesia (OIH) associated to opioid therapy.
The present invention provides new sequences, gene constructions, vectors and pharmaceutical compositions for the treatment of diseases and specially, for the treatment of mucopolysaccharidoses.
The present invention relates to oral pharmaceutical compositions comprising co-crystals of tramadol and celecoxib, processes for preparation of the same and their use as medicaments, more particularly for the treatment of pain.
The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - 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 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 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 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 25/00 - Drugs for disorders of the nervous system
77.
SIGMA LIGANDS FOR THE PREVENTION AND/OR TREATMENT OF EMESIS INDUCED BY CHEMOTHERAPY OR RADIOTHERAPY
The invention refers to the use of a sigma ligand, preferably a sigma ligand of formula (I), to prevent or treat emesis induced by a chemotherapeutic agent or radioactivity, especially emesis induced by taxanes, vinca alkaloids or platin chemotherapeutic drugs.
The present invention relates to polymorphs and solvates of the hydrochloride salt of 4- [2-[[5-methyl-1 -(2-naphthalenyl)-1 H-pyrazol-3-yl]oxy]ethyl]morpholine (P027), processes for their preparation, and to pharmaceutical compositions comprising them.
The invention refers to the use of a sigma ligand, particularly a sigma ligand of formulae (I), (II) or (III) to prevent and/or treat acute and chronic pain developed as a consequence of surgery, especially superficial and/or deep pain secondary to surgical tissue injury, and peripheral neuropathic pain, neuralgia, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuritis or neuropathy secondary to surgical procedure.
The invention refers to a combination comprising a sigma ligand of formula (I) and an opioid or opiate for use in the prevention and/or treatment of pain developed as a consequence of surgery, especially peripheral neuropathic pain, allodynia, causalgia, hyperalgesia, hyperesthesia, hyperpathia, neuralgia, neuritis or neuropathy. The invention also refers to the sigma ligands of formula (I) for use in potentiating the analgesic effect of an opioid or opiate and/or for decreasing the dependency induced thereby when said opioid or opiate is used in the prevention and/or treatment of pain developed as a consequence of surgery.
The present invention relates to a co-crystal of celecoxib and venlafaxine, processes for preparation of the same and its use as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain, including chronic pain; or of depression in patients which suffer from chronic pain and/or chronic inflammation or in patients with a chronic musculoskeletal inflammatory illness, with the inflammatory illness preferably being selected from osteoarthritis or rheumatoid arthritis.
The present invention relates to pharmaceutical compositions comprising venlafaxine and celecoxib and their uses as medicaments, more particularly for the treatment of pain, including chronic pain; or of depression in patients which suffer from pain or in patients with a chronic musculo-skeletal inflammatory illness, with the inflammatory illness preferably being selected from osteoarthritis or rheumatoid arthritis.
The present invention relates to 4-[-2-[[5-methyl-1 -(2-naphthalenyl)-1 H-pyrazol-3- yl]oxy]ethyl]morpholine salts, specifically to the hydrochloride, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of sigma receptor associated diseases.
The present invention relates to a pharmaceutical composition that comprises a compound of formula (I) as active pharmaceutical ingredient: or a pharmaceutically acceptable salt, isomer, prodrug or solvate thereof; and at least a pharmaceutically acceptable excipient, wherein the active pharmaceutical ingredient is present in an amount of at least 80% of the total dry weight of the composition.
The present invention relates to salts of duloxetine and NSAIDs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
The present invention is directed to a solid dosage form comprising (i) a core comprising a benzimidazole; (ii) a separating layer comprising a water soluble polymer and glyceryl monostearate; and (iii) an enteric coating.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain. In a preferred embodiment, the co-crystal is (rac) - tramadol. HcI - celecoxib (1:1).
The present invention relates to pharmaceutical compositions comprising tramadol and celecoxib and their uses as medicaments or analgesics, more particularly for the treatment of severe to moderate pain with an inflammation component.
The present invention relates to indane-amine derivatives, to processes for the preparation thereof, to medicaments comprising them as well as to their use for the preparation of a medicament for the treatment of 5HT7 receptor mediated diseases or conditions.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
The present invention relates to heterocyclyl-substituted alkylamino phenyl derιvatives (I) to processes for the preparation thereof, to medicaments comprising them as well as to their use for the preparation of a medicament for the treatment of 5HT7 receptor mediated diseases or conditions. In the compounds (I) x-y-z together form -N-N=CR1- or =C-NR2 -N=.
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.
The invention refers to the use of a sigma ligand of formula (I) to prevent or treatpain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum derivatives chemotherapeutic drugs.
The present invention relates to pharmaceutical compounds comprising O-desmethyl-Tramadol and at least one COX-inhibitor, especially NSAID, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain. The pharmaceutical compound may be a salt or a crystalline form of a salt or a co-crystal.
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
C07C 215/64 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
C07C 59/64 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
C07C 69/84 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 25/04 - Centrally acting analgesics, e.g. opioids
94.
SALTS OF TRAMADOL AND DIFLUNISAL AND THEIR CRYSTAL FORM IN THE TREATMENT OF PAIN
The present invention relates to tramadol-diflunisal salts, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
C07C 65/105 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
A61P 29/02 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
95.
DOMPERIDONE AT A LOW DAILY DOSE FOR USE IN THE TREATMENT OR PREVENTION OF A DISEASE ASSOCIATED WITH AN ALTERATION OF THE IMMUNE RESPONSE
The invention relates to the use of domperidone or a pharmaceutically acceptable salt thereof at low doses to prevent and/or treat a disease associated with an alteration of the immune response such as Leishmaniosis.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 33/02 - Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
The present invention relates to co-crystals of tramadol and paracetamol, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
C07C 233/25 - 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 six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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 25/00 - Drugs for disorders of the nervous system
97.
PROCESS FOR OBTAINING ENANTIOMERICALLY ENRICHED PYRAZOLE DERIVATIVES
The present invention is directed to a process for the enantioselective hydrolysis of an ester of formula (I), which comprises reacting a mixture of C4-enantiomers of esters of formula (I), or salts thereof, with an esterase enzyme in the presence of a solvent. The invention is further directed to the transformation of said esters of formula (I) into enantiomerically enriched pyrazoles.
The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain. In a preferred embodiment, the co-crystal is a co-crystal of (-) -tramadol and (S) -naproxen (1:2); (+) -tramadol and (R) -naproxen (1:2) or (rac) -tramadol-Hcl-celecoxib (1:1).
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61P 25/04 - Centrally acting analgesics, e.g. opioids
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
C07C 59/64 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
C07C 217/74 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
The present invention relates to pellets comprising a core with duloxetine, an intermediate non porous layer layer comprising one or more film forming water-soluble polymers, and an enteric layer comprising polyvinyl acetate phthalate as the enteric polymer, to a process for preparing the same, to the use of the pellets for manufacturing a pharmaceutical dosage form, and to a dosage form containing them.
The present invention relates to a pharmaceutical formulation comprising 5-(4-chlorophenyl)- 1-(2,4-dichlorophenyl)-N-(cis-2,6-dimethylpiperidin-1-yl)-4-methyl-4,5-dihydro-1 H-pyrazole-3- carboxamide as racemate or (S)-enantiomer or mixtures thereof in a solid solution and/or solid dispersion.
patents
