Methods for providing a carboxamide compound and intermediates used in the preparation of the carboxamide compound are provided. The methods include reacting 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanenitrile benzoate with a reagent and hydrochloric acid to form the carboxamide compound including 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide hydrochloride.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
2.
FILLING HEAD FOR POWERED LAYERING OF A DRY POWDER INHALER
A filling head (20) for filling a container (22) includes a receptacle (24). The receptacle (24) includes an interior surface (26) configured to receive a powder (28) and having a plurality of openings (34) disposed therein to allow passage of the powder (28); and an exterior surface (52). The exterior surface (52) of the receptacle (24) has a plurality of raised surfaces (54), each of the plurality of raised surfaces having a plurality of openings (56) aligned with at least one of the plurality of openings (34) of the interior surface (26) to allow passage of the powder (28) from the receptacle (24) to the container (22). Methods of filling a container (22) are also provided.
A filling head (20) for filling a container (22) includes a receptacle (24). The receptacle (24) includes an interior surface (26) configured to receive a powder (28) and having a plurality of openings (34) disposed therein to allow passage of the powder (28); and an exterior surface (52). The exterior surface (52) of the receptacle (24) has a plurality of raised surfaces (54), each of the plurality of raised surfaces having a plurality of openings (56) aligned with at least one of the plurality of openings (34) of the interior surface (26) to allow passage of the powder (28) from the receptacle (24) to the container (22). Methods of filling a container (22) are also provided.
Methods for providing a carboxamide compound and intermediates used in the preparation of the carboxamide compound are provided. The methods include reacting 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanenitrile benzoate with a reagent and hydrochloric acid to form the carboxamide compound including 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide hydrochloride.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations used for stimulating white blood cell production for the treatment of neutropenia and neutropenia-related clinical conditions, for the treatment of hematopoietic syndrome, and for patients undergoing autologous peripheral blood progenitor cell collection and therapy
6.
4-(biphen-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I) as GABA receptor modulators for use in the treatment of epilepsy and pain
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the prevention and treatment of cranial and facial nerve disorders, connective tissue injuries, diseases and disorders, bone and cartilage injuries, diseases and disorders; Pharmaceutical preparations for the prevention and treatment of neuromuscular and neurological diseases and disorders, namely, central nervous system diseases and disorders, namely central nervous system infections, brain diseases, central nervous system movement disorders, muscle diseases and disorders, namely inflammatory muscle diseases and disorders and muscular dystrophy, ocular motility and spinal cord infections, injuries and diseases, and seizure disorders; Pharmaceutical preparations for the prevention and treatment of genitourinary diseases, namely, inflammatory pelvic, urological and reproductive system diseases, disorders and infections, sexually transmitted diseases, erectile and sexual dysfunction, infertility and incontinence; Pharmaceutical preparations for the prevention and treatment of auto-immune, cardiovascular, gastrointestinal, blood, oncological, ophthalmological and respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of allergies, hypertension, menopause, diabetic neuropathy, arthritis, and pain; Antibiotics, anti-infectives, anti-inflammatories, anti-fungals, anti-virals, oral and injectable pharmaceutical contraceptives, human vaccines; Pharmaceutical preparations for the prevention and treatment of smoking habits and addictions; Pharmaceutical preparations for the prevention and treatment of renal disease and disorders; Pharmaceutical preparations for the prevention and treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; Pharmaceutical preparations for the prevention and treatment of muscular atrophy; Pharmaceutical preparations for the prevention and treatment of inflammatory diseases, namely inflammatory bowel diseases, inflammatory joint diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; Pharmaceutical preparations for the prevention and treatment of metabolic diseases and disorders, namely diabetes, hypoglycemia, muscular dystrophy, sickle cell disease, and anemia
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the prevention and treatment of cranial and facial nerve disorders, connective tissue injuries, diseases and disorders, bone and cartilage injuries, diseases and disorders; Pharmaceutical preparations for the prevention and treatment of neuromuscular and neurological diseases and disorders, namely, central nervous system diseases and disorders, namely central nervous system infections, brain diseases, central nervous system movement disorders, muscle diseases and disorders, namely inflammatory muscle diseases and disorders and muscular dystrophy, ocular motility and spinal cord infections, injuries and diseases, and seizure disorders; Pharmaceutical preparations for the prevention and treatment of genitourinary diseases, namely, inflammatory pelvic, urological and reproductive system diseases, disorders and infections, sexually transmitted diseases, erectile and sexual dysfunction, infertility and incontinence; Pharmaceutical preparations for the prevention and treatment of auto-immune, cardiovascular, gastrointestinal, blood, oncological, ophthalmological and respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of allergies, hypertension, menopause, diabetic neuropathy, arthritis, and pain; Antibiotics, anti-infectives, anti-inflammatories, anti-fungals, anti-virals, oral and injectable pharmaceutical contraceptives, human vaccines; Pharmaceutical preparations for the prevention and treatment of smoking habits and addictions; Pharmaceutical preparations for the prevention and treatment of renal disease and disorders; Pharmaceutical preparations for the prevention and treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; Pharmaceutical preparations for the prevention and treatment of muscular atrophy; Pharmaceutical preparations for the prevention and treatment of inflammatory diseases, namely inflammatory bowel diseases, inflammatory joint diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; Pharmaceutical preparations for the prevention and treatment of metabolic diseases and disorders, namely diabetes, hypoglycemia, muscular dystrophy, sickle cell disease, and anemia
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the prevention and treatment of cranial and facial nerve disorders, connective tissue injuries, diseases and disorders, bone and cartilage injuries, diseases and disorders; Pharmaceutical preparations for the prevention and treatment of neuromuscular and neurological diseases and disorders, namely, central nervous system diseases and disorders, namely central nervous system infections, brain diseases, central nervous system movement disorders, muscle diseases and disorders, namely inflammatory muscle diseases and disorders and muscular dystrophy, ocular motility and spinal cord infections, injuries and diseases, and seizure disorders; Pharmaceutical preparations for the prevention and treatment of genitourinary diseases, namely, inflammatory pelvic, urological and reproductive system diseases, disorders and infections, sexually transmitted diseases, erectile and sexual dysfunction, infertility and incontinence; Pharmaceutical preparations for the prevention and treatment of auto-immune, cardiovascular, gastrointestinal, blood, oncological, ophthalmological and respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of allergies, hypertension, menopause, diabetic neuropathy, arthritis, and pain; Antibiotics, anti-infectives, anti-inflammatories, anti-fungals, anti-virals, oral and injectable pharmaceutical contraceptives, human vaccines; Pharmaceutical preparations for the prevention and treatment of smoking habits and addictions; Pharmaceutical preparations for the prevention and treatment of renal disease and disorders; Pharmaceutical preparations for the prevention and treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; Pharmaceutical preparations for the prevention and treatment of muscular atrophy; Pharmaceutical preparations for the prevention and treatment of inflammatory diseases, namely inflammatory bowel diseases, inflammatory joint diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; Pharmaceutical preparations for the prevention and treatment of metabolic diseases and disorders, namely diabetes, hypoglycemia, muscular dystrophy, sickle cell disease, and anemia
The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I):
A receptor. They are useful in the treatment of a number of conditions, including pain.
The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a sulfonamide URAT1inhibitor of formula (I), or a pharmaceutically acceptable salt thereof for use as a medicament, wherein R1, X1 and m as defined in the description, and to certain new sulfonamide URAT1 inhibitors. URAT1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout.
C07C 311/21 - Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R and R6 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
The present invention relates to compounds of Formula (I) described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.
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 401/12 - 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 407/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 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 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
A61K 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
A device for dispensing individual doses of powder from respective pockets of a disc-shaped carrier by outwardly rupturing a lidding foil by means of pressure on an opposite side surface, the device providing individual respective deaggregation flow paths for each pocket, split airstreams allowing improved entrainment of powder, a cam mechanism for outwardly rupturing the pockets, an indexing mechanism linked to the cam mechanism and a dose counter.
B65D 83/04 - Containers or packages with special means for dispensing contents for dispensing annular, disc-shaped, spherical or like small articles, e.g. tablets or pills
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): or pharmaceutically acceptable salt thereofs, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout.
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
Chemical Compounds The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5- c]pyridazine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R 2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I):
A receptor. They are useful in the treatment of a number of conditions, including pain.
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
C07D 487/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups
31.
IMIDAZOPYRIDAZINE DERIVATIVES AS GABAA RECEPTOR MODULATORS
Chemical Compounds The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5- c]pyridazine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R 2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
The present invention relates to compounds of Formula (IA) and (IB) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
Various embodiments relate to a device for dispensing a plurality of unitary doses of dry powder. The device includes: a casing; first and second supports respectively for two carriers each having a plurality of housings for respective unitary doses adapted to be connected to the mouthpiece for inhalation of the dose, the first and second supports being moveably mounted within the casing for sequentially connecting the housings to the mouthpiece; an indexing mechanism adapted to engage and move the first and second supports; and a changeover mechanism adapted to cause the device to pass from a first dispensing state to a second dispensing state and lock the second support in its stationary position while the device is in the first dispensing state, and to lock the first support in its stationary position while the device is in the second dispensing state.
The present invention relates to a solid molecular dispersion of from 3:97 to 12:88 weight % ratio of fesoterodine hydrogen fumarate and a polymeric binder selected from the group consisting of an alkyl hydroxyalkylcellulose ether, a hydroxyalkylcellulose ether, an ester of either thereof, and a mixture of any two or more thereof.
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon 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 401/12 - 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 237/08 - Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav 1.7 inhibitors of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07C 307/06 - Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 213/64 - One oxygen atom attached in position 2 or 6
C07D 213/65 - One oxygen atom attached in position 3 or 5
C07D 213/89 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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
The invention relates to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole Nav1.8 modulators of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/417 - Imidazole-alkylamines, e.g. histamine, phentolamine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The invention provides 4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2- fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide or a pharmaceutically acceptable salt thereof for the treatment of a disease associated with elevated blood uric acid levels, such as hyperuricemia or gout. In another aspect the invention provides the tosylate salt of 4-[2-(5-amino-1H-pyrazol-4- yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide.
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
48.
INTERMEDIATE AND PROCESS FOR THE PREPARATION OF A SULFONAMIDE DERIVATIVE
The invention relates to a crystalline form of 2-chloro-N-{2-[3-(2-{[(4'-hydroxybiphenyl-3- yl)methyl]amino}-2-oxoethyl)phenyl]-1,1-dimethylethyl}acetamide, a process for preparing the same and its use in the preparation of the 2 agonist N-[(4'-hydroxybiphenyl-3- yl)methyl]-2-(3-{2-[((2R)-2-hydroxy-2-{4-hydroxy-3- [(methylsulfonyl)amino]phenyl}ethyl)amino]-2-methylpropyl} phenyl)acetamide which is useful in the treatment of respiratory diseases.
C07C 237/22 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
C07C 303/40 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
C07C 311/08 - Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
The present invention relates to compounds of formula (I) to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.
The invention relates to a novel crystallisation process for preparing fluticasone propionate as crystalline form 1 polymorph with controlled particle size and suitable for micronisation. Said process comprises the step of dissolving fluticasone propionate in acetone or in a mixture of acetone and water and then adding this solution to water or to a mixture of water 10 and acetone, thereby causing fluticasone propionate to crystallise out of the solution as crystalline form
Device for dispensing a plurality of unitary doses (2) of dry powder, includes at least one support comprising conduits each defining a flow path for an airstream carrying one of the unitary dose (2), the support having first (26) and second (27) members secured to one another so that a first conduit portion (29) of the first member faces a second conduit portions (43) of the second member to define one of the conduits, and a first separation portion (30) of the first member faces a second separation portions (45) of the second member, the support comprising a plurality of barrier-forming elements (31, 46) each arranged between corresponding first (30) and second (45) separation portions to prevent dry powder from passing from one of the conduits to one of the adjacent conduits.
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
Injection system (1) comprising a pen-injector (2) including: - a shell (3) having an elongated outer surface and proximal and distal sections, and - an actuator (10) slidably mounted on the proximal section of the shell (3), wherein said injection system further comprises an actuating device (15) comprising: - a lever (30) pivotally connected to the proximal section of the shell (3) and adapted to cover and press at least a part of the actuator (10) when actuated by a patient, - a holding member (50) radially protruding from the outer surface of the shell (3) and adapted to bear on a patient's finger (61) while enabling the patient to actuate the lever (30) with another finger (62).
The invention provides a compound of the formula (I): wherein A, R1, R2 and R3 are as defined herein, or a pharmaceutically acceptable salt thereof. Such compounds are small molecule TRPM8 blockers and therefore useful in the propylaxis or treatment of a wide range of diseases, conditions or syndromes, including cold allodynia and Raynaulds syndrome.
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 209/42 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 215/48 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 215/54 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
C07D 217/26 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 235/08 - Radicals containing only hydrogen and carbon atoms
C07D 235/16 - 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
C07D 241/42 - Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
C07D 241/44 - Benzopyrazines 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 carbon atoms of the hetero ring
C07D 271/12 - Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 277/68 - Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
The present invention relates to a method of treating hepatis C and/or liver fibroisis with 3-cycloalkylaminopyrrolidine derivatives of the present invention.
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
The present invention relates to solid molecular dispersion of fesoterodine hydrogen fumarate and a polymeric binder. The invention also relates to an inert core bead or particle which is coated with said solid molecular dispersion and to pharmaceutical formulations comprising such coated beads or particles.
The invention relates to acyl sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new acyl sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein U, V, W, X, Y, R° and R1 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
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 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 451/04 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring system
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 25/00 - Drugs for disorders of the nervous system
61.
Dose unit, pack of dose units and inhaler for inhalation of combination of drugs
Various embodiments relate to a dose unit for a dry powder inhaler including: a dose carrier including a plurality of pockets each adapted to contain a dose of medication powder suitable for inhalation, the pockets being sequentially arranged such that the content of the pockets can be sequentially exposed to a flow of air for successive inhalations and a plurality of medication powder doses arranged in the pockets of the dose carrier. The doses are regularly distributed in the pockets according to a sequence of identical groups, each group including at least one blank pocket and one pocket containing a dose of medication powder. Various embodiments also relate to a pack including one such dose unit and one further dose unit with all pockets containing a medication powder. Various embodiments further relate to a dry powder inhaler including such a pack of dose units.
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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 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
PC71695A Abstract Chemical Compounds The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I): (I) or a pharmaceutically acceptable salt thereof, wherein Z, R 1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07D 213/64 - One oxygen atom attached in position 2 or 6
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 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
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 25/04 - Centrally acting analgesics, e.g. opioids
66.
SULFONAMIDE DERIVATIVES AS NAV1.7 INHIBITORS FOR THE TREATMENT OF PAIN
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07C 311/00 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 31/427 - Thiazoles not condensed and containing further heterocyclic rings
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 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 25/04 - Centrally acting analgesics, e.g. opioids
68.
BENZENE SULFONAMIDES AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly 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
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly 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
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 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 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 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof; to compositions containing such compounds; and to the of such compounds as inhibitors of HCV replication.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61P 31/22 - Antivirals for DNA viruses for herpes viruses
The invention relates to compounds of formula
processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
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 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
Device for dispensing a plurality of unitary doses of dry powder, comprising: - first (25a) and second (25b) supports, - an indexing mechan ism adapted to move the first and second supports (25), the indexing mechanism and the supports (25a, 25b) being configured so that in a first dispensing state of the device, the first (25a) and second (25b) supports are respectively in engagement with and disengaged from the indexing mechanism, in a second dispensing state of the device, the second (25b) and first (25a) supports are respectively in engagement with and disengaged from the indexing mechanism - a changeover mechanism (90) adapted to cause the device to pass from the first dispensing state to the second dispensing state, to lock the second support (25b) while the device is in the first dispensing state, and to lock the first support (25a) while the device is in the second dispensing state.
Device for dispensing a plurality of unitary doses (2) of dry powder, comprising at least one support comprising conduits each defining a flow path for an airstream carrying one of the unitary dose (2), the support having first (26) and second (27) members secured to one another so that a first conduit portion (29) of the first member faces a second conduit portions (43) of the second member to define one of the conduits, and a first separation portion (30) of the first member faces a second separation portions (45) of the second member, the support comprising a plurality of barrier-forming elements (31, 46) each arranged between corresponding first (30) and second (45) separation portions to prevent dry powder from passing from one of the conduits to one of the adjacent conduits.
A device for dispensing a plurality of unitary doses of dry powder includes: first and second supports, an indexing mechanism adapted to move the first and second supports, the indexing mechanism and the supports being configured so that in a first dispensing state of the device, the first and second supports are respectively in engagement with and disengaged from the indexing mechanism, in a second dispensing state of the device, the second and first supports are respectively in engagement with and disengaged from the indexing mechanism, and a changeover mechanism for causing the device to pass from the first dispensing state to the second dispensing state, to lock the second support while the device is in the first dispensing state, and to lock the first support while the device is in the second dispensing state.
This invention relates to the hydrochloride salt of biphenyl-2-yl-carbamic acid -{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl-amino]-nonyl}-piperidin-4-yl ester and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, said compound. The invention also relates to the hydrates, solvates and polymorphs of the hydrochloride salt of Biphenyl-2-yl-carbamic acid 1-{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl- amino]-nonyl}-piperidin-4-yl ester.
The present invention provides an interferon-alpha immunoglobulin Fc fusion protein and use of the fusion protein in the treatment of a condition alleviated by the administration of interferon- alpha, such as a liver disorder, for example hepatitis and in particular hepatitis C.
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
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 403/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The invention relates to a dose unit for a dry powder inhaler comprising: - a dose carrier including a plurality of pockets (17) each adapted to contain a dose of medication powder suitable for inhalation, said pockets being sequentially arranged such that the content of the pockets (17) can be sequentially exposed to a flow of air for successive inhalations and - a plurality of medication powder doses (X) arranged in pockets (17) of the dose carrier (15). The doses are regularly distributed in the pockets according to a sequence of identical groups, each group including at least one blank pocket (B) and one pocket containing a dose of medication powder (X). The invention also relates to a pack (105) comprised of one such dose unit (105a) and one further dose unit (105b) with all pockets containing a medication powder (Y). The invention further relates to a dry powder inhaler including such a pack (105) of dose units.
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
C07J 3/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by one carbon atom
C07J 5/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, and substituted in position 21 by only one singly bound oxygen atom
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
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 systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives 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
A61P 5/44 - GlucocorticosteroidsDrugs increasing or potentiating the activity of glucocorticosteroids
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
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 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
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 453/06 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing iso-quinuclidine ring systems
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
The present invention relates to compounds of the formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly inflammatory conditions.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
The present invention relates to the use of an anti-NGF antibody in the treatment or prevention of pain and/or a lower urinary tract symptom (LUTS) associated with interstitial cystitis and/or painful bladder syndrome and/or bladder pain syndrome.
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts, solvates or tautomers therof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment 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
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 275/03 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings 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
This invention relates to a class of pyrrolidine compounds of formula (I), and pharmaceutical ly acceptable derivatives thereof, to their use in med icine, to compositions containing them, and to processes for their preparation. It also relates to intermediates used in the preparation of such compounds and derivatives. In particular the compounds of formula (I) are useful for the treatment of EP2-mediated conditions, such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), chronic pelvic pain syndrome, polycystic kidney disease and polycystic ovarian syndrome.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
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
A61P 43/00 - Drugs for specific purposes, not provided for in groups
90.
Hydrochloride salt of 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide
This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament.
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
91.
NOVEL USES FOR ESREBOXETINE AND RACEMIC REBOXETINE
A norepinephrine reuptake inhibitor, or a pharmaceutically acceptable salt thereof, preferably esreboxetine or racemic reboxetine, more preferably esreboxetine, to improve cognitive function, in particular to improve in cognitive function in patients with fibromyalgia is provided. Also provided are methods of treatment of the same.
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds in the treatment of pain.
A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituted by one or more substituents each independently selected from Rf), C3-5 cycloalkyl (optionally substituted by one or more halogen), CN or halogen; where Rf represents halogen or phenyl: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.
C07D 231/14 - 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 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 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/04 - 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 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 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
The invention provides a diisopropylamine derivative selected from: (a) a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof; and (b) a pharmaceutically acceptable ester prodrug of the compound of formula I, and its pharmaceutically acceptable salts and solvates; for use in the treatment of stress urinary incontinence or mixed urinary incontinence. A preferred diisopropylamine derivative is fesoterodine, or a pharmaceutically acceptable salt thereof.
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, L and n are as defined in the specification. These compounds are useful as MC4 agonists.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The invention relates to compounds of formula
processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
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
C07D 295/22 - 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 hetero atoms directly attached to ring nitrogen atoms
98.
NOVEL COMPOUNDS ACTIVE AS MUSCARINIC RECEPTOR ANTAGONISTS
The invention relates to compounds of formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.
The invention relates to compounds of formula (I), processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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 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 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - 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 31/4709 - Non-condensed quinolines containing further heterocyclic 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 11/00 - Drugs for disorders of the respiratory system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
