AR093413A2 - Antagonistas de neuroquinina, composiciones farmaceuticas que los comprenden, y uso de dichos antagonistas en la preparacion de un medicamento - Google Patents

Antagonistas de neuroquinina, composiciones farmaceuticas que los comprenden, y uso de dichos antagonistas en la preparacion de un medicamento

Info

Publication number
AR093413A2
AR093413A2 ARP130104108A ARP130104108A AR093413A2 AR 093413 A2 AR093413 A2 AR 093413A2 AR P130104108 A ARP130104108 A AR P130104108A AR P130104108 A ARP130104108 A AR P130104108A AR 093413 A2 AR093413 A2 AR 093413A2
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
independently selected
attached
Prior art date
Application number
ARP130104108A
Other languages
English (en)
Original Assignee
Opko Health Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23337634&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR093413(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Opko Health Inc filed Critical Opko Health Inc
Publication of AR093413A2 publication Critical patent/AR093413A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—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
    • A61K31/4025—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/4353—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
    • A61K31/437—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/4353—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
    • A61K31/4375—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 nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/40—Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/50—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C07D211/28—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • C07D211/36—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 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
    • C07D211/40—Oxygen atoms
    • C07D211/42—Oxygen atoms attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • C07D211/36—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 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—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
    • C07D211/36—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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—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 one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—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 one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—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
    • C07D401/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—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
    • C07D401/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/10—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 aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—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
    • C07D413/12—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Reproductive Health (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

Un antagonista de neuroquinina de la fórmula (1), o una sal aceptable para uso farmacéutico del mismo, en donde Ar¹ y Ar² se seleccionan cada uno independientemente del grupo que consiste en R¹⁷-heteroarilo y un resto de fórmula (2); X¹ es -O-, -S-, -SO-, -SO₂-, -NR³⁴-, -N(COR¹²)- o -N(SO₂R¹⁵)-; cuando X¹ es -SO-, -SO₂-, -N(COR¹²)- o -N(SO₂R¹⁵)-, entonces: R¹ y R² se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C₁₋₆, hidroxi(alquilo C₁₋₃), cicloalquilo C₁₋₈, -CH₃F, -CHF₂ y -CF₃; o R¹ y R², junto con el átomo de carbono al que ambos están unidos, forman un anillo de alquileno C₃₋₆; o cuando X¹ es -O-, -S- o -NR³⁴ entonces: R¹ y R² se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C₁₋₆, hidroxi(alquilo C₁₋₃), cicloalquilo C₃₋₈, -CH₂F, -CHF₂ y -CF₃; o R¹ y R², junto con el átomo de carbono al que ambos están unidos, forman un anillo de alquileno C₃₋₆; o R¹ y R² junto con el átomo de carbono al que ambos están unidos forman un grupo C=O; R³ se selecciona del grupo que consiste en H, alquilo C₁₋₆, hidroxi(alquilo C₁₋₃), cicloalquilo C₃₋₈, -CH₂F, -CHF₂ y -CF₃; cada R⁶ se selecciona independientemente del grupo que consiste en H, alquilo C₁₋₆ y -OH; cada R⁷ se selecciona independientemente del grupo que consiste en H y alquilo C₁₋₆; n2 es 1 a 4; R⁴ y R⁵ se seleccionan independientemente del grupo que consiste en -(CR²⁸R²⁹)ₙ₁-G, donde, n1 es 0 a 5; y G es -H, -CF₃, -CHF₂, -CH₂F, -OH, -O-(alquilo C₁₋₆), -OCH₂F, -OCHF₂, -OCF₃, -OCH₂CF₃, -O-(cicloalquilo C₃₋₆), -O-alquilo C₁₋₆-(cicloalquilo C₃₋₈), -NR¹³R¹⁴, -SO₂NR¹³R¹⁴, -NR¹²SO₂R¹³, -NR¹²C(O)R¹⁴, -NR¹²C(O)OR¹³, -NR¹²(C(O)NR¹³R¹⁴), -C(O)NR¹³R¹⁴, -C(O)OR¹³, -cicloalquilo C₃₋₈, (R¹⁹)ʳ-arilo, (R¹⁹)ʳ-heteroarilo, -OC(O)R¹⁴, -OC(O)NR¹³R¹⁴, -C(=NOR¹⁴)(R¹³), -C(O)R¹³, -C(OR¹²)(R¹³)(R¹⁴), heterocicloalquenilo opcionalmente sustituido con 1 a 4 sustituyentes independientemente seleccionados del grupo que consiste en R³⁰ y R³¹, o un resto del grupo de fórmulas (3); o R⁴ y R⁵ juntos son =O, =NOR¹²; o R⁴ y R⁵, junto con el átomo de carbono al que ambos están unidos, forman un anillo de heterocicloalquilo o heterocicloalquenilo de 4 a 8 miembros que contiene de 1 a 3 grupos independientemente seleccionados de X², siempre que por lo menos un X² sea -NR³⁵, -O-, -S-, -S(O)- o -SO₂-, el anillo puede sustituirse opcionalmente con 1 a 6 sustituyentes independientemente seleccionados del grupo que consiste en R³⁰ y R³¹; siempre que R⁴ y R⁵ no se seleccionen ambos del grupo que consiste en H, alquilo y cicloalquilo C₃₋₈; siempre que también cuando uno de R⁴ y R⁵ sea -OH, entonces el otro de R⁴ y R⁵ no sea alquilo o (R¹⁹)ʳ-arilo; R⁸, R⁹ y R¹⁰ se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₈, -OR¹², halógeno, -CN, -NO₂, -CF₃, -CHF₂, -CH₂F, -CH₂CF₃, -OCF₃, -OCHF₂, -OCH₂F, -OCH₂CF₃, -COOR¹², -CONR²¹R²², -OC(O)NR²¹R²², -OC(O)R¹², -NR²¹COR¹², -NR²¹CO₂R¹⁵, -NR²¹CONR²¹R²², -NR²¹SO₂R¹⁵, -NR²¹R²², -SO₂NR²¹R²², -S(O)ₙ₆R¹⁵, (R¹⁹)ʳ-arilo y (R¹⁹)ʳ-heteroarilo; R¹² es H, alquilo C₁₋₆ o cicloalquilo C₃₋₈; R¹³ y R¹⁴ se seleccionan cada uno independientemente del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₆, -CH₂CF₃, arilo y heteroarilo; o R¹³ y R¹⁴, junto con el átomo de nitrógeno al que ambos están unidos, forman un anillo saturado o insaturado de 4 a 7 miembros, que está opcionalmente sustituido con -OR¹², en donde uno de los átomos de carbono del anillo se reemplaza opcionalmente por un heteroátomo seleccionado del grupo que consiste en -O-, -S- y -NR³⁴-; n6 es 0, 1 ó 2; R¹⁵ es alquilo C₁₋₆, cicloalquilo C₃₋₈, -CF₃ o -CH₂CF₃; R¹⁶ es H, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₈, hidroxialquilo C₂₋₆ o -P(O)(OH)₂; cada R¹⁹ es un sustituyente del anillo arilo o heteroarilo al que está unido, y se selecciona independientemente del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₈, alcoxi C₁₋₆, -OH, halógeno, -CN, -NO₂, -CF₃, -CHF₂, -CH₂F, -OCF₃, -OCHF₂, -OCH₂F, -O-(alquilo C₁₋₆), -O-(cicloalquilo C₃₋₈), -COOR¹², -CONR²¹R²², -OC(O)NR²¹R²², -OC(O)R¹², -NR²¹R²², -NR²¹COR¹², -NR²¹CO₂R¹², -NR²¹CONR²¹R²², -NR²¹SO₂R¹⁵ y -S(O)ₙ₆R¹⁵; R²¹ y R²² se seleccionan independientemente del grupo que consiste en H, alquilo C₁₋₆, cicloalquilo C₃₋₈ y bencilo; o R²¹ y R²², junto con el átomo de nitrógeno al que ambos están unidos, forman un anillo saturado o insaturado de 4 a 7 miembros, en donde uno de los átomos de carbono del anillo se reemplaza opcionalmente por un heteroátomo seleccionado del grupo que consiste en -O-, -S- y -NR³⁴-; R²³ y R²⁴ se seleccionan cada uno independientemente del grupo que consiste en H y alquilo C₁₋₆; o R²³ y R²⁴, junto con el átomo de carbono al que ambos están unidos, forman un grupo C=O o grupo ciclopropilo; R²⁷ es H, -OH o alquilo C₁₋₆; R²⁸ y R²⁹ se seleccionan cada uno independientemente del grupo que consiste en H y alquilo C₁₋₂; R³⁰ y R³¹ se seleccionan cada uno independientemente del grupo que consiste en H, -OH, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₈ y -C(O)NR¹³R¹⁴; o R³⁰ y R³¹, junto con el átomo de carbono al que ambos están unidos, forman =O, =S, un anillo de ciclopropilo o =NR³⁵; R³² y R³³ se seleccionan cada uno independientemente del grupo que consiste en H y alquilo C₁₋₆; R³⁴ es H, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₈ o hidroxialquilo C₂₋₆; R³⁵ es H, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₈, -P(O)(OH)₂, alilo, hidroxialquilo C₂₋₆, alcoxi C₁₋₆alquilo C₁₋₆, SO₂R¹⁵ o -(CH₂)₂-N(R¹²)-SO₂-R¹⁵; R³⁶ es H, alquilo C₁₋₆, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈alquilo C₁₋₈, -NO₂, -CN u OR¹²; R³⁷ es de 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en H, alquilo C₁₋₆, -OH, alcoxi C₁₋₆ y halógeno; r es 1 a 3; X² es -NR³⁵-, -O-, -S-, -S(O)-, -SO₂-, -CH₂-, -CF₂- o -CR¹²F-; X³ es -NR³⁴-, -N(CONR¹³R¹⁴)-, -N(CO₂R¹³)-, -N(SO₂R¹⁵)-, -N(COR¹²)-, -N(SO₂NHR¹³)-, -O-, -S-, -S(O)-, -SO₂-, -CH₂-, -CF₂- o -CR¹²F-; n3 es 1 a 5; y n5 es 1 a 3; o un diastereómero, enantiómero, estereoisómero, regioestereómero, rotómero, tautómero y prodroga de los mismos.
ARP130104108A 2001-12-18 2013-11-08 Antagonistas de neuroquinina, composiciones farmaceuticas que los comprenden, y uso de dichos antagonistas en la preparacion de un medicamento AR093413A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34145201P 2001-12-18 2001-12-18

Publications (1)

Publication Number Publication Date
AR093413A2 true AR093413A2 (es) 2015-06-03

Family

ID=23337634

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP020104877A AR037851A1 (es) 2001-12-18 2002-12-16 Antagonistas de neuroquinina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos
ARP130104108A AR093413A2 (es) 2001-12-18 2013-11-08 Antagonistas de neuroquinina, composiciones farmaceuticas que los comprenden, y uso de dichos antagonistas en la preparacion de un medicamento

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP020104877A AR037851A1 (es) 2001-12-18 2002-12-16 Antagonistas de neuroquinina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos

Country Status (34)

Country Link
US (6) US7049320B2 (es)
EP (2) EP1882686B1 (es)
JP (4) JP4500984B2 (es)
KR (2) KR20100064394A (es)
CN (1) CN1606545B (es)
AR (2) AR037851A1 (es)
AT (2) ATE522504T1 (es)
AU (1) AU2002357264B2 (es)
BR (2) BR0215158A (es)
CA (1) CA2470476C (es)
CO (1) CO5590915A2 (es)
CY (2) CY1108924T1 (es)
DE (1) DE60225067T2 (es)
DK (1) DK1463716T3 (es)
EC (1) ECSP045159A (es)
ES (2) ES2299637T3 (es)
HU (1) HUP0402679A3 (es)
IL (2) IL162484A0 (es)
LT (1) LTC1463716I2 (es)
LU (1) LUC00043I2 (es)
MX (1) MXPA04005910A (es)
MY (2) MY136697A (es)
NL (1) NL300895I2 (es)
NO (2) NO327976B1 (es)
NZ (2) NZ551997A (es)
PE (1) PE20030762A1 (es)
PL (1) PL216664B1 (es)
PT (1) PT1463716E (es)
RU (1) RU2326120C9 (es)
SG (1) SG180017A1 (es)
SI (1) SI1463716T1 (es)
TW (1) TWI329511B (es)
WO (1) WO2003051840A1 (es)
ZA (1) ZA200404583B (es)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20030762A1 (es) 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
ATE358482T1 (de) * 2002-07-03 2007-04-15 Schering Corp 1-amido-4-phenyl-4-benzyloxymethyl-piperidin derivative und verwandte verbindungen als neurokinin-1 (nk-1) antagonsisten zur behandlung von erbrechen, depressionen, angstzustände und husten
NZ543102A (en) 2003-04-24 2008-12-24 Incyte Corp Aza spiro alkane derivatives as inhibitors of metalloproteases
AU2004308935A1 (en) * 2003-12-22 2005-07-14 Schering Corporation Pharmaceutical compositions
ES2282062T1 (es) 2004-06-04 2007-10-16 Teva Pharmaceutical Industries Ltd. Composicion farmaceutica que contiene irbesartan.
AU2012216435B8 (en) * 2004-07-01 2015-02-19 Opko Health, Inc. Piperidine derivatives as NK1 antagonists
JP2008505107A (ja) * 2004-07-01 2008-02-21 シェーリング　コーポレイション Ｎｋ１アンタゴニストとしてのピペリジン誘導体
US7354922B2 (en) * 2004-12-14 2008-04-08 Schering Corporation Bridged ring NK1 antagonists
WO2007096782A2 (en) * 2006-02-22 2007-08-30 Valorisation Recherche Hscm, Limited Partnership Compositions for disorders associated wtth metachromatic cell activation
SG10201500028RA (en) * 2006-04-05 2015-02-27 Opko Health Inc Pharmaceutical formulations: salts of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
WO2007114922A2 (en) * 2006-04-05 2007-10-11 Schering Corporation Salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and preparation process therefor
EP2662374A1 (en) * 2006-04-05 2013-11-13 OPKO Health, Inc. Salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl) -ethoxy}-methyl]-8-phenyl-1,7 -diaza-spiro[4.5]decan-2-one and preparation process therefor
AR066191A1 (es) 2007-03-22 2009-08-05 Schering Corp Proceso e intermediarios para la sintesis de compuestos 8- [ ( 1- (3,5- bis- ( trifluorometil) fenil) - etoxi ) - metil]- 8 fenil - 1,7- diaza - espiro (4, 5) decan -2 ona
AR065802A1 (es) * 2007-03-22 2009-07-01 Schering Corp Formulaciones de comprimidos que contienen sales de 8- [( 1- ( 3,5- bis- (trifluorometil) fenil) -etoxi ) - metil) -8- fenil -1, 7- diaza- spiro [ 4,5] decan -2- ona y comprimidos elaborados a partir de estas
US7786146B2 (en) * 2007-08-13 2010-08-31 Valeant Pharmaceuticals International Derivatives of 5-amino-4,6-disubstituted indole and 5-amino-4,6-disubstituted indoline as potassium channel modulators
US8138168B1 (en) 2007-09-26 2012-03-20 Takeda Pharmaceutical Company Limited Renin inhibitors
KR101719004B1 (ko) * 2008-09-05 2017-03-22 옵코 헬스, 인크. 8-［｛1-（3,5-비스-（트리플루오로메틸）페닐）-에톡시｝-메틸］-8-페닐-1,7-디아자-스피로［4.5］데칸-2-온 화합물의 합성 방법 및 중간체
CN102573475B (zh) * 2009-08-14 2016-01-20 欧科生医股份有限公司 神经激肽-1拮抗剂的静脉内制剂
WO2011085392A1 (en) * 2010-01-11 2011-07-14 Pro-Dex, Inc. Handheld medical device with thermal padding
WO2013004766A1 (en) 2011-07-04 2013-01-10 Ferrari Giulio Nk-1 receptor antagonists for treating corneal neovascularisation
EP2545905A1 (en) 2011-07-11 2013-01-16 Britannia Pharmaceuticals Limited A new therapeutical composition containing apomorphine as active ingredient
WO2013168176A2 (en) * 2012-03-30 2013-11-14 Glenmark Generics Limited Process for preparation of fosaprepitant and salt thereof
CN105017251B (zh) * 2015-06-30 2018-06-29 齐鲁制药有限公司 一种nk-1受体拮抗剂的制备方法及其中间体
US20180250270A1 (en) 2015-09-11 2018-09-06 Chase Pharmaceuticals Corporation Muscarinic combination and its use for combating hypocholinergic disorders of the central nervous system
CN105367510B (zh) * 2015-11-02 2017-07-21 叶海伟 一种(2R，4S)‑3‑Cbz‑2，4‑二苯基‑1，3‑恶唑烷‑5‑酮的制备方法
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
CN108148060B (zh) * 2016-12-05 2020-06-19 四川科伦博泰生物医药股份有限公司 取代的杂环化合物及其衍生物，其药物组合物、制备方法及用途
IL312486B2 (en) 2017-04-10 2025-05-01 Chase Therapeutics Corp NK1 antagonist combination and method for treating synucleinopathies
CN121221782A (zh) 2017-06-30 2025-12-30 傲拓神经科学公司 用于治疗抑郁的nk-1拮抗剂组合物和方法
CN111465412A (zh) * 2017-12-21 2020-07-28 英特维特国际股份有限公司 Nk-1拮抗剂的口服药物组合物
CN111918647A (zh) 2018-02-26 2020-11-10 圣拉斐尔医院有限公司 用于治疗眼痛的nk-1拮抗剂
WO2020257364A1 (en) 2019-06-17 2020-12-24 DeepMap Inc. Nearest neighbor search using compressed octrees representing high definition maps for autonomous vehicles
EP3991730A4 (en) 2019-06-28 2023-08-09 Shanghai Shengdi Pharmaceutical Co., Ltd NEUROKININ-1 ANTAGONIST
JP2022542063A (ja) * 2019-07-25 2022-09-29 インターベット インターナショナル ベー． フェー． テルマピタントまたは（５ｒ，８ｓ）－８－［［（１ｒ）－１－［３，５－ビス（トリフルオロメチル）フェニル］エトキシ］メチル］－８－フェニル－１，３，７－トリアザスピロ［４．５］デカン－２，４－ジオンの結晶形態
WO2021180885A1 (en) 2020-03-11 2021-09-16 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency
AU2021246889A1 (en) 2020-04-03 2022-10-13 Nerre Therapeutics Limited An NK-1 receptor antagonist for treating a disease selecting from sepsis, septic shock,, acute respiratory distress syndrome (ARDS) or multiple organ dysfunction syndrome (MODS)
CA3177477A1 (en) 2020-06-02 2021-12-09 Nerre Therapeutics Limited Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs
CN111606868B (zh) * 2020-06-23 2023-02-17 温州大学新材料与产业技术研究院 一种双齿噁唑啉手性配体的制备方法
AU2021407138A1 (en) 2020-12-25 2023-06-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Use of nk1 antagonist prodrug compound in combination with 5-ht3 receptor antagonist
US20250059187A1 (en) * 2021-12-22 2025-02-20 The Regents Of The University Of California Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
CN119528985A (zh) 2023-08-28 2025-02-28 科睿迪(南京)医药科技有限公司 神经激肽-1受体拮抗剂化合物

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU678409B2 (en) * 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
US5661162A (en) 1992-12-14 1997-08-26 Merck Sharp & Dohme Limited 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists
GB9317104D0 (en) * 1993-08-17 1993-09-29 Zeneca Ltd Therapeutic heterocycles
ATE170174T1 (de) 1994-01-13 1998-09-15 Merck Sharp & Dohme Gem-bissubstituierte azazyclische tachykinin- antagonisten
WO1996026726A1 (en) 1995-02-28 1996-09-06 Hoechst Marion Roussel, Inc. Pharmaceutical composition for piperidinoalkanol compounds
GB9601680D0 (en) 1996-01-27 1996-03-27 Pfizer Ltd Therapeutic agents
CA2287397A1 (en) 1997-04-24 1998-10-29 Merck Sharp & Dohme Limited Use of an nk-1 receptor antagonist and an ssri for treating obesity
US6380242B1 (en) * 1998-12-23 2002-04-30 Nps Allelix Corp. N-alkylamino-indoles for the treatment of migraine
US6436928B1 (en) * 1999-12-17 2002-08-20 Schering Corporation Selective neurokinin antagonists
ES2258485T3 (es) 1999-12-17 2006-09-01 Schering Corporation Antagonistas selectivos de neuroquinina.
US6499984B1 (en) 2000-05-22 2002-12-31 Warner-Lambert Company Continuous production of pharmaceutical granulation
ATE374183T1 (de) * 2001-11-13 2007-10-15 Schering Corp Nk1-antagonisten
PE20030762A1 (es) * 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
ATE358482T1 (de) * 2002-07-03 2007-04-15 Schering Corp 1-amido-4-phenyl-4-benzyloxymethyl-piperidin derivative und verwandte verbindungen als neurokinin-1 (nk-1) antagonsisten zur behandlung von erbrechen, depressionen, angstzustände und husten
EP1682545B1 (en) 2003-10-03 2007-12-12 Pfizer Limited Imidazopyridine substituted tropane derivatives with ccr5 receptor antagonist activity for the treatment of hiv and inflammation
JP2008505107A (ja) * 2004-07-01 2008-02-21 シェーリング　コーポレイション Ｎｋ１アンタゴニストとしてのピペリジン誘導体
US7354922B2 (en) 2004-12-14 2008-04-08 Schering Corporation Bridged ring NK1 antagonists
EP2662374A1 (en) 2006-04-05 2013-11-13 OPKO Health, Inc. Salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl) -ethoxy}-methyl]-8-phenyl-1,7 -diaza-spiro[4.5]decan-2-one and preparation process therefor
SG10201500028RA (en) * 2006-04-05 2015-02-27 Opko Health Inc Pharmaceutical formulations: salts of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one and treatment methods using the same
AR065802A1 (es) 2007-03-22 2009-07-01 Schering Corp Formulaciones de comprimidos que contienen sales de 8- [( 1- ( 3,5- bis- (trifluorometil) fenil) -etoxi ) - metil) -8- fenil -1, 7- diaza- spiro [ 4,5] decan -2- ona y comprimidos elaborados a partir de estas

Also Published As

Publication number Publication date
PL370841A1 (en) 2005-05-30
NL300895I2 (nl) 2017-11-21
EP1882686A2 (en) 2008-01-30
MY136697A (en) 2008-11-28
AU2002357264B2 (en) 2006-08-24
HK1111157A1 (en) 2008-08-01
PT1463716E (pt) 2008-05-12
DE60225067D1 (de) 2008-03-27
US7049320B2 (en) 2006-05-23
HUP0402679A3 (en) 2011-05-30
MXPA04005910A (es) 2004-09-13
JP2005513068A (ja) 2005-05-12
IL162484A0 (en) 2005-11-20
DE60225067T2 (de) 2009-02-05
EP1882686B1 (en) 2011-08-31
JP4500984B2 (ja) 2010-07-14
NO2017053I2 (no) 2017-10-19
JP2014058549A (ja) 2014-04-03
ECSP045159A (es) 2004-07-23
LTPA2017032I1 (lt) 2017-11-10
KR20100064394A (ko) 2010-06-14
NZ551997A (en) 2008-07-31
EP1463716B1 (en) 2008-02-13
RU2326120C9 (ru) 2008-11-20
US8796299B2 (en) 2014-08-05
CA2470476C (en) 2010-05-25
HUP0402679A2 (hu) 2005-03-29
TW200306179A (en) 2003-11-16
PL216664B1 (pl) 2014-04-30
US20140336158A1 (en) 2014-11-13
ES2299637T3 (es) 2008-06-01
SG180017A1 (en) 2012-05-30
US20130023503A1 (en) 2013-01-24
CY2017030I1 (el) 2018-04-04
US20110098468A1 (en) 2011-04-28
ES2372871T3 (es) 2012-01-27
TWI329511B (en) 2010-09-01
LTC1463716I2 (lt) 2018-06-25
CN1606545A (zh) 2005-04-13
HK1065036A1 (en) 2005-02-08
US20030158173A1 (en) 2003-08-21
JP5860199B2 (ja) 2016-02-16
IL162484A (en) 2012-05-31
AR037851A1 (es) 2004-12-09
ZA200404583B (en) 2006-02-22
AU2002357264A1 (en) 2003-06-30
US20060199815A1 (en) 2006-09-07
US7902366B2 (en) 2011-03-08
CY1108924T1 (el) 2014-07-02
US8273895B2 (en) 2012-09-25
BRPI0215158B1 (pt) 2017-06-27
NO20043041L (no) 2004-07-16
PE20030762A1 (es) 2003-09-05
DK1463716T3 (da) 2008-06-16
ATE522504T1 (de) 2011-09-15
CA2470476A1 (en) 2003-06-26
WO2003051840A1 (en) 2003-06-26
JP2010031053A (ja) 2010-02-12
CY2017030I2 (el) 2018-04-04
MY158859A (en) 2016-11-15
RU2326120C2 (ru) 2008-06-10
SI1463716T1 (sl) 2008-06-30
LUC00043I2 (es) 2017-12-20
US20170283434A1 (en) 2017-10-05
KR100984617B1 (ko) 2010-09-30
JP5823476B2 (ja) 2015-11-25
US9688693B2 (en) 2017-06-27
EP1463716A1 (en) 2004-10-06
CN1606545B (zh) 2013-01-23
RU2004122109A (ru) 2005-06-10
ATE386023T1 (de) 2008-03-15
NZ532975A (en) 2007-02-23
NO2017053I1 (no) 2017-10-19
EP1882686A3 (en) 2008-04-30
BR0215158A (pt) 2004-10-19
CO5590915A2 (es) 2005-12-30
JP2015110657A (ja) 2015-06-18
LUC00043I1 (es) 2017-10-16
KR20040065289A (ko) 2004-07-21
NO327976B1 (no) 2009-11-02

Similar Documents

Publication Publication Date Title
AR093413A2 (es) Antagonistas de neuroquinina, composiciones farmaceuticas que los comprenden, y uso de dichos antagonistas en la preparacion de un medicamento
AR114083A2 (es) AGENTES INDUCTORES DE APOPTOSIS CON SELECTIVIDAD POR Bcl-2 PARA EL TRATAMIENTO DE CÁNCER Y ENFERMEDADES INMUNES
AR111776A1 (es) Heteroarilos inhibidores de las proteínas ras mutantes de g12c
AR117544A1 (es) Heterocíclicos inhibidores de mat2a y métodos de uso para el tratamiento del cáncer
AR127892A1 (es) Compuestos y composiciones para la administración de agentes terapéuticos
AR110139A1 (es) COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV
AR088989A1 (es) Derivados biciclicos de dihidroisoquinolin-1-ona
AR043190A1 (es) Derivados de quinoleina como inhibidores del factor inhibidor de la migracion de macrofagos y metodos para su identificacion. sintesis y composiciones farmaceuticas.
AR094684A1 (es) Triterpenoides de c-19 modificados, con actividad inhibidora de la maduración del vih
AR049284A1 (es) Compuestos derivados de 1,3-tiazol; composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades asociadas a la actividad de los ppard
AR128379A1 (es) Inhibidores de la proteína tirosina fosfatasa, composiciones y métodos de uso
AR094174A1 (es) Lactamas fusionadas de arilo y heteroarilo
AR103252A1 (es) Compuestos de quinazolina
AR092607A1 (es) Pirrolopirimidinilamino-benzotiazolonas sustituidas
AR089285A1 (es) Derivados de betulina
AR121913A1 (es) Compuestos terapéuticos
AR102799A1 (es) Profármacos de agonistas fenólicos de trpv1
AR120652A1 (es) Antagonistas de sstr5
AR113887A1 (es) Derivados de indol macrocíclicos sustituidos con cloro
AR088014A1 (es) Derivados de alcoholes 1-fenil-2-piridinil alquilicos como inhibidores de la fosfodiesterasa
AR099988A1 (es) Derivados de dihidropirrolopirimidina
AR101479A1 (es) Derivados de 6-alquinil-piridina
AR033680A1 (es) Compuestos triciclicos utiles como inhibidores de la farnesil proteino transferasa y su uso para la manufactura de medicamentos como agentes antitumorales
AR090323A1 (es) Imidazopiridazinas sustituidas, procesos e intermediarios para su obtencion y su uso en el tratamiento de enfermedades mediadas por la quinasa mps-1
AR042284A1 (es) Derivados de piperidina, preparacion y composiciones farmaceuticas que las contienen; y uso de los mismos para la fabricacion de medicamentos

Legal Events

Date Code Title Description
FB Suspension of granting procedure