PE20200447A1 - Compuestos de biheteroarilo y usos de los mismos - Google Patents
Compuestos de biheteroarilo y usos de los mismosInfo
- Publication number
- PE20200447A1 PE20200447A1 PE2019002479A PE2019002479A PE20200447A1 PE 20200447 A1 PE20200447 A1 PE 20200447A1 PE 2019002479 A PE2019002479 A PE 2019002479A PE 2019002479 A PE2019002479 A PE 2019002479A PE 20200447 A1 PE20200447 A1 PE 20200447A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidin
- biheteroaril
- compounds
- compound
- dlk
- Prior art date
Links
Classifications
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/33—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
- A61K31/5386—1,4-Oxazines, e.g. morpholine 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
- A61K35/30—Nerves; Brain; Eyes; Corneal cells; Cerebrospinal fluid; Neuronal stem cells; Neuronal precursor cells; Glial cells; Oligodendrocytes; Schwann cells; Astroglia; Astrocytes; Choroid plexus; Spinal cord tissue
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/08—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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—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
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
-
- 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
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- 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
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—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 C07D415/00
- C07D417/14—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 C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged 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
- C07D487/08—Bridged 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-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
- C07D487/12—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 three hetero rings
- C07D487/18—Bridged 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
- C07D491/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Virology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Psychology (AREA)
- Developmental Biology & Embryology (AREA)
- Cell Biology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Biotechnology (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Vascular Medicine (AREA)
- AIDS & HIV (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Anesthesiology (AREA)
- Urology & Nephrology (AREA)
Abstract
Referido a un compuesto de formula (I-I) o sus sales, en el que R1, R2 y R3 son cada uno independientemente H, F, Cl, Br, I, alquilo C1-6 o haloalquilo C1-6; X1 es N; X2 es N o CH; y A y Cy se selecciona entre el grupo que consiste en pirrolidina, piperidina, azetidina, entre otros. Un compuesto preferido es 5-[2-(3,3-difluoro-1-piperidil)-6-[(1S,4S)-2-oxa-5-azabiciclo[2.2.1]heptan-5-il]pirimidin-4-il]pirimidin-2-amina. Estos compuestos biheteroarilos inhiben la actividad de la doble quinasa de cremallera de leucina (DLK), siendo util para el tratamiento de enfermedades neurodegenerativas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361817966P | 2013-05-01 | 2013-05-01 | |
| PCT/CN2014/076654 WO2014177060A1 (en) | 2013-05-01 | 2014-04-30 | Biheteroaryl compounds and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20200447A1 true PE20200447A1 (es) | 2020-02-28 |
Family
ID=51841525
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019002479A PE20200447A1 (es) | 2013-05-01 | 2014-04-30 | Compuestos de biheteroarilo y usos de los mismos |
| PE2016000335A PE20161063A1 (es) | 2013-05-01 | 2014-04-30 | Compuestos de biheteroarilo y usos de los mismos |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016000335A PE20161063A1 (es) | 2013-05-01 | 2014-04-30 | Compuestos de biheteroarilo y usos de los mismos |
Country Status (22)
| Country | Link |
|---|---|
| US (8) | US9266862B2 (es) |
| EP (1) | EP2991978B1 (es) |
| JP (4) | JP6229042B2 (es) |
| KR (2) | KR101836431B1 (es) |
| CN (2) | CN110003178B (es) |
| AR (1) | AR096151A1 (es) |
| AU (2) | AU2014261894C1 (es) |
| BR (1) | BR112015027055B1 (es) |
| CA (1) | CA2911051C (es) |
| CL (1) | CL2015003147A1 (es) |
| CR (2) | CR20200177A (es) |
| EA (3) | EA029568B8 (es) |
| IL (2) | IL296526B2 (es) |
| MA (3) | MA48577A1 (es) |
| MX (1) | MX2015015130A (es) |
| MY (1) | MY182082A (es) |
| PE (2) | PE20200447A1 (es) |
| PH (2) | PH12015502410B1 (es) |
| SG (2) | SG11201509027WA (es) |
| TW (3) | TWI622587B (es) |
| UA (1) | UA121016C2 (es) |
| WO (1) | WO2014177060A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2844652B1 (en) * | 2012-05-03 | 2019-03-13 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| CN104918934B (zh) | 2013-01-18 | 2017-12-22 | 霍夫曼-拉罗奇有限公司 | 3‑取代的吡唑及其作为dlk抑制剂的用途 |
| KR20160002850A (ko) * | 2013-05-01 | 2016-01-08 | 에프. 호프만-라 로슈 아게 | C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도 |
| MX2015015130A (es) * | 2013-05-01 | 2016-02-18 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos. |
| MX2016008110A (es) * | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
| CN104926716A (zh) * | 2015-06-10 | 2015-09-23 | 哈尔滨工业大学 | 吡啶衍生物2,6-二[(6-甲氧基吡啶-2-基)甲基]吡啶及其合成方法 |
| KR20190040068A (ko) * | 2016-08-29 | 2019-04-16 | 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 | 질환의 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 저해제 |
| ES2895257T3 (es) | 2016-12-08 | 2022-02-18 | Univ Texas | Inhibidores de biciclo[1.1.1]pentano de cremallera de leucina doble cinasa (DLK) para el tratamiento de una enfermedad |
| CA3067944C (en) | 2017-07-14 | 2023-03-14 | F. Hoffmann-La Roche Ag | Bicyclic ketone compounds and methods of use thereof |
| JP7362600B2 (ja) | 2017-10-11 | 2023-10-17 | エフ. ホフマン-ラ ロシュ アーゲー | Rip1キナーゼ阻害剤として使用するための二環式化合物 |
| JP7274473B2 (ja) * | 2017-10-17 | 2023-05-16 | パラウ ファルマ,エス.エル.ユー. | 4-アミノピリミジン化合物の合成 |
| CA3078688A1 (en) | 2017-10-31 | 2019-05-09 | F. Hoffmann-La Roche Ag | Bicyclic sulfones and sulfoxides and methods of use thereof |
| EP3781571B1 (en) | 2018-04-20 | 2024-01-17 | F. Hoffmann-La Roche AG | N-[4-oxo-2,3-dihydro-pyrido[3,2-b][1,4]oxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs) |
| US11993586B2 (en) | 2018-10-22 | 2024-05-28 | Novartis Ag | Crystalline forms of potassium channel modulators |
| WO2020132045A1 (en) | 2018-12-19 | 2020-06-25 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| AR119673A1 (es) | 2019-01-11 | 2022-01-05 | Hoffmann La Roche | Compuestos bicíclicos de cetona y métodos para utilizarlos |
| JP2022518603A (ja) * | 2019-01-31 | 2022-03-15 | 中国医▲薬▼研究▲開▼▲発▼中心有限公司 | 芳香環又は芳香族複素環化合物、その製造方法及び医薬使用 |
| US11560366B2 (en) | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
| JP2021070684A (ja) * | 2019-10-30 | 2021-05-06 | 東ソー株式会社 | ハロゲン化合物の製造方法 |
| CN115335050B (zh) * | 2020-01-29 | 2024-05-17 | 卡玛瑞制药有限公司 | 用于治疗皮肤病症的化合物和组合物 |
| EP4222154A1 (en) * | 2020-10-02 | 2023-08-09 | Genentech, Inc. | Process for the preparation of biheteroaryl compounds and crystal forms thereof |
| US20250032489A1 (en) * | 2021-09-01 | 2025-01-30 | The U.S.A., As Represented By The Secretary, Department Of Health And Human Services | Mixed lineage kinase inhibitors and methods of use |
| WO2023067550A1 (en) * | 2021-10-20 | 2023-04-27 | Yousef Najajreh | Allosteric inhibitor compounds for overcoming cancer resistance |
| TW202435863A (zh) | 2023-01-28 | 2024-09-16 | 芬蘭商奧利安公司 | Cbl-b抑制劑 |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| EP0102324A3 (de) | 1982-07-29 | 1984-11-07 | Ciba-Geigy Ag | Lipide und Tenside in wässriger Phase |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| HUT35524A (en) | 1983-08-02 | 1985-07-29 | Hoechst Ag | Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance |
| US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| EP0652775B1 (en) | 1992-07-27 | 2000-04-19 | THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES | Targeting of liposomes to the blood-brain barrier |
| US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
| AU2001286930A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The Leland Stanford Junior University | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
| DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
| DE60234057D1 (de) | 2001-07-25 | 2009-11-26 | Raptor Pharmaceutical Inc | Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke |
| US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
| ATE411996T1 (de) | 2002-09-30 | 2008-11-15 | Bayer Healthcare Ag | Kondensierte azolpyrimidinderivate |
| US7220833B2 (en) | 2002-12-03 | 2007-05-22 | Thomas Nelson | Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier |
| JP2007505142A (ja) | 2003-09-10 | 2007-03-08 | セダーズ−シナイ メディカル センター | 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達 |
| GB0508471D0 (en) | 2005-04-26 | 2005-06-01 | Celltech R&D Ltd | Therapeutic agents |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| WO2008064244A2 (en) | 2006-11-20 | 2008-05-29 | The Trustees Of Columbia University In The City Of New York | Phosphoinositide modulation for the treatment of neurodegenerative diseases |
| CA2675558A1 (en) * | 2007-02-06 | 2008-08-14 | Novartis Ag | Pi 3-kinase inhibitors and methods of their use |
| US8293747B2 (en) | 2007-07-19 | 2012-10-23 | Merck Sharp & Dohme Corp. | Heterocyclic amide compounds as protein kinase inhibitors |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| US20100056609A1 (en) | 2008-08-26 | 2010-03-04 | Washington University | Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway |
| MX2011004585A (es) * | 2008-10-31 | 2011-06-01 | Novartis Ag | Combinacion de un inhibidor de fosfatidilinositol-3-cinasa (p13k) y un inhibidor de mtor. |
| GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
| KR20120063515A (ko) | 2009-09-09 | 2012-06-15 | 아빌라 테라퓨틱스, 인크. | Pi3 키나제 억제제 및 이들의 용도 |
| RU2012120783A (ru) * | 2009-10-22 | 2013-11-27 | Женентек, Инк. | Модуляция дегенерации аксона |
| GB201004200D0 (en) | 2010-03-15 | 2010-04-28 | Univ Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
| WO2011149950A2 (en) | 2010-05-24 | 2011-12-01 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| WO2012122383A2 (en) * | 2011-03-09 | 2012-09-13 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| MX2015015130A (es) | 2013-05-01 | 2016-02-18 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos. |
| CN103483345B (zh) | 2013-09-25 | 2016-07-06 | 中山大学 | Pi3k激酶抑制剂、包含其的药物组合物及其应用 |
| JP5920747B1 (ja) | 2015-04-07 | 2016-05-18 | エイピーエス.エスエイ | アプリケーションプログラムおよびカード |
-
2014
- 2014-04-30 MX MX2015015130A patent/MX2015015130A/es unknown
- 2014-04-30 AU AU2014261894A patent/AU2014261894C1/en active Active
- 2014-04-30 WO PCT/CN2014/076654 patent/WO2014177060A1/en not_active Ceased
- 2014-04-30 SG SG11201509027WA patent/SG11201509027WA/en unknown
- 2014-04-30 CN CN201910136846.0A patent/CN110003178B/zh active Active
- 2014-04-30 MA MA48577A patent/MA48577A1/fr unknown
- 2014-04-30 PH PH1/2015/502410A patent/PH12015502410B1/en unknown
- 2014-04-30 MY MYPI2015002684A patent/MY182082A/en unknown
- 2014-04-30 PH PH1/2019/502378A patent/PH12019502378A1/en unknown
- 2014-04-30 TW TW103115649A patent/TWI622587B/zh active
- 2014-04-30 TW TW107105054A patent/TWI710558B/zh active
- 2014-04-30 PE PE2019002479A patent/PE20200447A1/es unknown
- 2014-04-30 SG SG10201707002VA patent/SG10201707002VA/en unknown
- 2014-04-30 AR ARP140101782A patent/AR096151A1/es active IP Right Grant
- 2014-04-30 PE PE2016000335A patent/PE20161063A1/es unknown
- 2014-04-30 MA MA42164A patent/MA42164B1/fr unknown
- 2014-04-30 EA EA201592060A patent/EA029568B8/ru not_active IP Right Cessation
- 2014-04-30 UA UAA201511803A patent/UA121016C2/uk unknown
- 2014-04-30 KR KR1020157034239A patent/KR101836431B1/ko active Active
- 2014-04-30 KR KR1020187006149A patent/KR102002265B1/ko active Active
- 2014-04-30 CA CA2911051A patent/CA2911051C/en active Active
- 2014-04-30 EP EP14791795.9A patent/EP2991978B1/en active Active
- 2014-04-30 EA EA201991064A patent/EA038235B1/ru unknown
- 2014-04-30 TW TW106110366A patent/TW201800403A/zh unknown
- 2014-04-30 BR BR112015027055-7A patent/BR112015027055B1/pt active IP Right Grant
- 2014-04-30 MA MA38624A patent/MA38624A1/fr unknown
- 2014-04-30 JP JP2016510926A patent/JP6229042B2/ja active Active
- 2014-04-30 CR CR20200177A patent/CR20200177A/es unknown
- 2014-04-30 IL IL296526A patent/IL296526B2/en unknown
- 2014-04-30 EA EA201792471A patent/EA033084B1/ru not_active IP Right Cessation
- 2014-04-30 CN CN201480024257.9A patent/CN105431420B/zh active Active
- 2014-05-01 US US14/267,011 patent/US9266862B2/en active Active
-
2015
- 2015-10-19 IL IL242164A patent/IL242164B/en active IP Right Grant
- 2015-10-23 CR CR20150589A patent/CR20150589A/es unknown
- 2015-10-26 CL CL2015003147A patent/CL2015003147A1/es unknown
- 2015-10-29 US US14/927,267 patent/US10010549B2/en active Active
-
2016
- 2016-02-11 US US15/041,375 patent/US10028954B2/en active Active
-
2017
- 2017-10-16 JP JP2017200127A patent/JP6655052B2/ja active Active
- 2017-12-22 US US15/852,235 patent/US20180117044A1/en not_active Abandoned
-
2018
- 2018-01-11 US US15/868,301 patent/US20180133219A1/en not_active Abandoned
- 2018-02-22 US US15/902,746 patent/USRE47848E1/en active Active
-
2019
- 2019-01-15 AU AU2019200249A patent/AU2019200249B2/en active Active
- 2019-09-11 US US16/568,130 patent/US20200171029A1/en not_active Abandoned
- 2019-10-28 US US16/666,273 patent/US11129832B2/en active Active
-
2020
- 2020-01-31 JP JP2020014468A patent/JP2020079264A/ja active Pending
-
2022
- 2022-10-28 JP JP2022173436A patent/JP2023011775A/ja active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20200447A1 (es) | Compuestos de biheteroarilo y usos de los mismos | |
| PE20130184A1 (es) | Compuesto heterociclico | |
| PE20141974A1 (es) | Compuestos de heterociclilo | |
| PE20181145A1 (es) | Compuestos de piridina | |
| PE20160995A1 (es) | Inhibidores de syk | |
| AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| PE20171177A1 (es) | Compuestos aminopirimidinilo inhibidores de jak | |
| PE20191613A1 (es) | Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret | |
| PE20161443A1 (es) | Compuestos | |
| PE20150230A1 (es) | Nuevos diazaespirocicloalcanos y azaespirocicloalcanos | |
| PE20190337A1 (es) | NUEVOS DERIVADOS DE PIRROLO [2,3-d]PIRIMIDA, UN PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN | |
| PE20190339A1 (es) | 1h-pirazolo[4,3-b] piridinas como inhibidores de pde1 | |
| PE20161405A1 (es) | Analogos de cortistatina y sintesis y usos de los mismos | |
| PE20200700A1 (es) | Compuestos macrociclicos y usos de los mismos | |
| NZ749437A (en) | Processes and intermediates for making a jak inhibitor | |
| AR088449A1 (es) | Benzilindazoles sustituidos | |
| PE20161292A1 (es) | Compuestos de nicotinamida sustituida con heteroarilo | |
| PE20141855A1 (es) | Benzotienilo-pirrolotriazinas disustituidas y sus usos | |
| PE20180552A1 (es) | Nuevos compuestos biciclicos como inhibidores duales de atx/ca | |
| AR093184A1 (es) | Compuesto de pirimidina sustituida como inhibidor de quinurenina-3-monooxigenasa y composicion farmaceutica que lo comprenden | |
| UY40181A (es) | Pesticidas de azol bicíclico sustituido con heterociclos | |
| UY32531A (es) | Nuevos compuestos para el tratamiento de trastornos del snc | |
| UY32096A (es) | Derivados de 2-carboxamida - cicloamino - urea especìficos, sus sales farmacèuticamente aceptables, composiciones contenièndolos, pro-farmacos de los mismos, procesos para su produciòn y aplicaciones | |
| PE20141691A1 (es) | Compuestos con actividad nematicida | |
| PE20170682A1 (es) | Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias |