JP5930278B2 - Mlk阻害剤および使用方法 - Google Patents
Mlk阻害剤および使用方法 Download PDFInfo
- Publication number
- JP5930278B2 JP5930278B2 JP2011537733A JP2011537733A JP5930278B2 JP 5930278 B2 JP5930278 B2 JP 5930278B2 JP 2011537733 A JP2011537733 A JP 2011537733A JP 2011537733 A JP2011537733 A JP 2011537733A JP 5930278 B2 JP5930278 B2 JP 5930278B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- mmol
- pyrrolo
- pyridin
- phenyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
- QTKBXPVTDMTPMZ-UHFFFAOYSA-N CN(C)c(cc1)ncc1-c(cc12)cnc1[nH]cc2-c(cc1)cc(Cl)c1F Chemical compound CN(C)c(cc1)ncc1-c(cc12)cnc1[nH]cc2-c(cc1)cc(Cl)c1F QTKBXPVTDMTPMZ-UHFFFAOYSA-N 0.000 description 1
- NMMATNQHSAAIGY-UHFFFAOYSA-N COc(cc(cc1OC)-c(nc2N3c(cc4)cc5c4[nH]cc5)cnc2NC3=O)c1OC Chemical compound COc(cc(cc1OC)-c(nc2N3c(cc4)cc5c4[nH]cc5)cnc2NC3=O)c1OC NMMATNQHSAAIGY-UHFFFAOYSA-N 0.000 description 1
- KHWMQOUQPHPQOU-GXHSKWEDSA-N COc(cc(cc1OC)-c2cnc3[nH]cc(/C(/C=N\C(N)=C)=C/N)c3c2)c1OC Chemical compound COc(cc(cc1OC)-c2cnc3[nH]cc(/C(/C=N\C(N)=C)=C/N)c3c2)c1OC KHWMQOUQPHPQOU-GXHSKWEDSA-N 0.000 description 1
- ZUMBBARLJHSZAM-UHFFFAOYSA-N C[n](cc1)c(cc2)c1cc2N(c1nc(-c(cc2)ccc2O)cnc1N1)C1=O Chemical compound C[n](cc1)c(cc2)c1cc2N(c1nc(-c(cc2)ccc2O)cnc1N1)C1=O ZUMBBARLJHSZAM-UHFFFAOYSA-N 0.000 description 1
- KVLOJNGWRWUDLV-UHFFFAOYSA-N Nc(cc1)ccc1-c(c1c2)c[nH]c1ncc2-c(cc1)cnc1N Chemical compound Nc(cc1)ccc1-c(c1c2)c[nH]c1ncc2-c(cc1)cnc1N KVLOJNGWRWUDLV-UHFFFAOYSA-N 0.000 description 1
- KPUJWYPWMBTFGE-UHFFFAOYSA-N Nc(cc1)ccc1-c(cc12)cnc1[nH]cc2-c(cc1)cc2c1[nH]cc2 Chemical compound Nc(cc1)ccc1-c(cc12)cnc1[nH]cc2-c(cc1)cc2c1[nH]cc2 KPUJWYPWMBTFGE-UHFFFAOYSA-N 0.000 description 1
- MPTRQLXNBJOFSI-UHFFFAOYSA-N Nc(nc1)ncc1-c(cc12)cnc1[nH]cc2-c(cc1)cc2c1[nH]cc2 Chemical compound Nc(nc1)ncc1-c(cc12)cnc1[nH]cc2-c(cc1)cc2c1[nH]cc2 MPTRQLXNBJOFSI-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/4353—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
- A61K31/438—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
- A61K31/4427—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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
- A61K31/495—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
- A61K31/55—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
- 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
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P25/04—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
- A61P25/14—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
- A61P25/24—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
- 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
- A61P27/16—Otologicals
-
- 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
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- 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
- C07D471/04—Ortho-condensed 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
- C07D471/02—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
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11795008P | 2008-11-25 | 2008-11-25 | |
| US61/117,950 | 2008-11-25 | ||
| US14875509P | 2009-01-30 | 2009-01-30 | |
| US14877809P | 2009-01-30 | 2009-01-30 | |
| US61/148,755 | 2009-01-30 | ||
| US61/148,778 | 2009-01-30 | ||
| PCT/US2009/065878 WO2010068483A2 (en) | 2008-11-25 | 2009-11-25 | Mlk inhibitors and methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014232195A Division JP5873544B2 (ja) | 2008-11-25 | 2014-11-14 | Mlk阻害剤および使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012509903A JP2012509903A (ja) | 2012-04-26 |
| JP2012509903A5 JP2012509903A5 (cg-RX-API-DMAC7.html) | 2013-01-17 |
| JP5930278B2 true JP5930278B2 (ja) | 2016-06-08 |
Family
ID=42243278
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011537733A Active JP5930278B2 (ja) | 2008-11-25 | 2009-11-25 | Mlk阻害剤および使用方法 |
| JP2014232195A Active JP5873544B2 (ja) | 2008-11-25 | 2014-11-14 | Mlk阻害剤および使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014232195A Active JP5873544B2 (ja) | 2008-11-25 | 2014-11-14 | Mlk阻害剤および使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (4) | US8877772B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP3037421A3 (cg-RX-API-DMAC7.html) |
| JP (2) | JP5930278B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN102264743B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2009324894B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2744498C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2554375T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2010068483A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8227603B2 (en) | 2006-08-01 | 2012-07-24 | Cytokinetics, Inc. | Modulating skeletal muscle |
| PL2583970T3 (pl) | 2006-08-02 | 2016-05-31 | Cytokinetics Inc | Określone cząstki chemiczne, kompozycje i sposoby zawierające imidazopirymidyny |
| US8299248B2 (en) | 2006-08-02 | 2012-10-30 | Cytokinetics, Incorporated | Certain 1H-imidazo[4,5-b]pyrazin-2(3H)-ones and 1H-imidazo[4,5-b]pyrazin-2-ols and methods for their use |
| MX337906B (es) | 2006-10-19 | 2016-03-28 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| US7998976B2 (en) | 2008-02-04 | 2011-08-16 | Cytokinetics, Inc. | Certain chemical entities, compositions and methods |
| BRPI0907502A2 (pt) | 2008-02-04 | 2019-01-15 | Cytokinetics Inc | pelo menos um entidade química, composição, e, métodos para tratar um paciente tendo uma condição, para aumentar a função ou atividade do músculo esquelético, para aumentar a eficiência do músculo esquelético, parab aumentar o tempo da fadiga de fibra muscular esquelética rápida, para sensibilizar uma fibra muscular esquelética rápida para produzir força em resposta a baixas concentreações de íons cálcio e para aumentar o tempo de fadiga muscular esquelética |
| WO2010016490A1 (ja) | 2008-08-05 | 2010-02-11 | 第一三共株式会社 | イミダゾピリジン-2-オン誘導体 |
| EP2370424A1 (en) | 2008-11-10 | 2011-10-05 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP3037421A3 (en) * | 2008-11-25 | 2016-11-30 | University Of Rochester | Mlk inhibitors and methods of use |
| SI3354650T1 (sl) | 2008-12-19 | 2022-06-30 | Vertex Pharmaceuticals Incorporated | Spojine, uporabne kot zaviralci ATR kinaze |
| CN106117213B (zh) | 2009-10-26 | 2022-03-18 | 西格诺药品有限公司 | 杂芳基化合物及其合成和纯化方法 |
| EP2568984A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| AU2011253021A1 (en) | 2010-05-12 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | 2 -aminopyridine derivatives useful as inhibitors of ATR kinase |
| AU2011253025A1 (en) | 2010-05-12 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2569287B1 (en) | 2010-05-12 | 2014-07-09 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| JP2013529200A (ja) | 2010-05-12 | 2013-07-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
| WO2011143419A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
| WO2011149950A2 (en) * | 2010-05-24 | 2011-12-01 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| AU2011270807A1 (en) | 2010-06-23 | 2013-01-31 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of ATR kinase |
| DE102010049877A1 (de) * | 2010-11-01 | 2012-05-03 | Merck Patent Gmbh | 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate |
| EP2487159A1 (en) * | 2011-02-11 | 2012-08-15 | MSD Oss B.V. | RorgammaT inhibitors |
| MX2013011450A (es) | 2011-04-05 | 2014-02-03 | Vertex Pharma | Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
| EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| JP2014522818A (ja) | 2011-06-22 | 2014-09-08 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
| JP2014517079A (ja) | 2011-06-22 | 2014-07-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atrキナーゼ阻害剤として有用な化合物 |
| PH12014500094A1 (en) | 2011-07-13 | 2014-03-17 | Cytokinetics Inc | Combination als therapy |
| BR112014007690B1 (pt) | 2011-09-30 | 2022-10-04 | Vertex Pharmaceuticals Incorporated | Usos de inibidores de atr no tratamento de câncer pancreático e câncer de pulmão de células não pequenas |
| JP6212045B2 (ja) | 2011-09-30 | 2017-10-11 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Atrキナーゼの阻害剤として有用な化合物を作製するためのプロセス |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| MX2014003796A (es) | 2011-09-30 | 2015-01-16 | Vertex Pharma | Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
| EP2751088B1 (en) | 2011-09-30 | 2016-04-13 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| PH12014500869A1 (en) | 2011-10-19 | 2014-06-30 | Signal Pharm Llc | Treatment of cancer with tor kinase inhibitors |
| EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8841449B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| KR102040997B1 (ko) | 2011-12-02 | 2019-11-27 | 시그날 파마소티칼 엘엘씨 | 7-(6-(2-히드록시프로판-2-일)피리딘-3-일)-1-((트랜스)-4-메톡시시클로헥실)-3,4-디히드로피라지노[2,3-b]피라진-2(1H)-온, 그의 고체 형태의 제약 조성물 및 그의 사용 방법 |
| TWI615143B (zh) | 2012-02-24 | 2018-02-21 | 標誌製藥公司 | 使用tor激酶抑制劑組合療法以治療癌症之方法 |
| CN102627646A (zh) * | 2012-03-19 | 2012-08-08 | 苏州四同医药科技有限公司 | 一种3-碘-5-溴-4,7-二氮杂吲哚的制备方法 |
| DK2833973T3 (en) | 2012-04-05 | 2018-01-02 | Vertex Pharma | Compounds useful as ATR kinase inhibitors and combination therapies thereof |
| WO2014026329A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof |
| WO2014026330A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| WO2014026327A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| WO2014085795A1 (en) * | 2012-11-30 | 2014-06-05 | University Of Rochester | Mixed lineage kinase inhibitors for hiv/aids therapies |
| EP3418281B1 (en) | 2012-12-07 | 2020-09-30 | Vertex Pharmaceuticals Inc. | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of atr kinase for the treatment of cancer diseases |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| CA2895905A1 (en) | 2012-12-21 | 2014-06-26 | Zenith Epigenetics Corp. | Novel heterocyclic compounds as bromodomain inhibitors |
| JP2016505041A (ja) | 2013-01-16 | 2016-02-18 | シグナル ファーマシューティカルズ,エルエルシー | 置換型ピロロピリミジン化合物、その組成物、およびこれらを用いた治療方法 |
| CN105431148A (zh) * | 2013-03-07 | 2016-03-23 | 加利菲亚生物公司 | 混合谱系激酶抑制剂及治疗方法 |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| BR112015026021A2 (pt) | 2013-04-17 | 2017-07-25 | Signal Pharm Llc | terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer |
| KR102240356B1 (ko) | 2013-04-17 | 2021-04-14 | 시그날 파마소티칼 엘엘씨 | Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법 |
| KR102271344B1 (ko) | 2013-04-17 | 2021-07-01 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| CN105377260B (zh) | 2013-04-17 | 2020-06-12 | 西格诺药品有限公司 | 二氢吡嗪并-吡嗪类化合物在制备治疗癌症的药物中的应用 |
| ES2744198T3 (es) | 2013-04-17 | 2020-02-24 | Signal Pharm Llc | Formulaciones farmacéuticas, procesos, formas sólidas y procedimientos de uso relacionados con 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3, 4 dihidropirazino[2,3-b]pirazin-2(1H)-ona |
| JP6382947B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ,エルエルシー | 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法 |
| CN105392499B (zh) | 2013-04-17 | 2018-07-24 | 西格诺药品有限公司 | 用于治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法 |
| WO2014181813A1 (ja) * | 2013-05-10 | 2014-11-13 | 武田薬品工業株式会社 | 複素環化合物 |
| WO2014193912A1 (en) | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| HRP20200854T1 (hr) | 2013-06-21 | 2020-08-21 | Zenith Epigenetics Ltd. | Novi biciklički inhibitori bromodomene |
| WO2015004534A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. | ブロモドメイン阻害剤としての新規キナゾリノン |
| EP3077397B1 (en) | 2013-12-06 | 2019-09-18 | Vertex Pharmaceuticals Inc. | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| WO2015160868A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| WO2015160882A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) PYRIDIN-3-YL)-1-(TRANS)-4-METHOXYCYCLOHEXYL)-3, 4-DIHYDROPYRAZINO[2,3-b] PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| ES2777608T3 (es) | 2014-06-05 | 2020-08-05 | Vertex Pharma | Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo |
| CA2950780C (en) | 2014-06-17 | 2023-05-16 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr inhibitors |
| US9623028B2 (en) | 2014-07-14 | 2017-04-18 | Signal Pharmaceuticals, Llc | Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof |
| NZ629796A (en) | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
| USRE49517E1 (en) | 2014-08-15 | 2023-05-02 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10179125B2 (en) | 2014-12-01 | 2019-01-15 | Zenith Epigenetics Ltd. | Substituted pyridines as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| WO2016097863A1 (en) | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Inhibitors of bromodomains |
| EP3256450B1 (en) | 2015-02-11 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof |
| WO2016164641A1 (en) * | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| WO2017059357A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
| EP3368539B1 (en) | 2015-10-27 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted indazole compounds as ror gamma t inhibitors and uses thereof |
| JP2018531958A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としてのヘテロアリール置換安息香酸及びその使用 |
| JP2018531957A (ja) | 2015-10-27 | 2018-11-01 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | RORγT阻害薬としての置換二環式ピラゾール化合物及びその使用 |
| CN109071488B (zh) | 2016-02-10 | 2021-08-13 | 詹森药业有限公司 | 取代的1,2,3-三唑作为nr2b-选择性nmda调节剂 |
| TW201819376A (zh) * | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之1H-咪唑並[4,5-b]吡啶-2(3H)-酮及其作為GLUN2B受體調節劑之用途 |
| US11447503B2 (en) | 2019-06-14 | 2022-09-20 | Janssen Pharmaceutica Nv | Pyridine carbamates and their use as GLUN2B receptor modulators |
| EA202090103A1 (ru) | 2017-06-22 | 2020-04-24 | Селджин Корпорейшн | Лечение гепатоцеллюлярной карциномы, которая характеризуется вирусной инфекцией гепатита b |
| AU2019226571A1 (en) | 2018-03-01 | 2020-10-01 | The Trustees Of Columbia University In The City Of New York | Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress |
| JP7346441B2 (ja) | 2018-04-04 | 2023-09-19 | ヤンセン ファーマシューティカ エヌ.ベー. | 置換ピリジン及びピリミジン並びにglun2b受容体調節物質としてのそれらの使用 |
| CN113015526A (zh) * | 2018-09-19 | 2021-06-22 | 豪夫迈·罗氏有限公司 | 螺环2,3-二氢-7-氮杂吲哚化合物及其用途 |
| US20220220206A1 (en) * | 2019-05-20 | 2022-07-14 | Mayo Foundation For Medical Education And Research | Treating chronic liver disease |
| KR20220020917A (ko) | 2019-06-14 | 2022-02-21 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로[4,3-b]피리딘 및 GLUN2B 수용체 조절제로서의 이들의 용도 |
| TW202112774A (zh) | 2019-06-14 | 2021-04-01 | 比利時商健生藥品公司 | 經取代之吡唑并-吡啶醯胺及其作為glun2b受體調節劑之用途 |
| MX2021015500A (es) | 2019-06-14 | 2022-02-10 | Janssen Pharmaceutica Nv | Pirazolo-pirazinas sustituidas y su uso como moduladores del receptor glun2b. |
| PH12021552839A1 (en) | 2019-06-14 | 2022-10-03 | Janssen Pharmaceutica Nv | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
| CA3142998A1 (en) | 2019-06-14 | 2020-12-17 | Janssen Pharmaceutica Nv | Pyrazine carbamates and their use as glun2b receptor modulators |
| JP2022536424A (ja) | 2019-06-14 | 2022-08-16 | ヤンセン ファーマシューティカ エヌ.ベー. | 置換ヘテロ芳香族ピラゾロピリジン及びglun2b受容体調節因子としてのそれらの使用 |
| CN114555595B (zh) * | 2019-08-30 | 2023-12-26 | Tsd生命科学有限公司 | 咪唑并吡啶衍生物及将其作为有效成分的药学组合物 |
| WO2021237111A1 (en) * | 2020-05-21 | 2021-11-25 | Stemsynergy Therapeutics, Inc. | Notch inhibitors and uses thereof |
| WO2023050323A1 (en) * | 2021-09-30 | 2023-04-06 | Citrix Systems, Inc. | Automated transfer of peripheral device operations |
| US11479541B1 (en) | 2022-01-31 | 2022-10-25 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating thereof |
| US11661409B1 (en) * | 2022-01-31 | 2023-05-30 | Pioneura Corporation | Acid addition salts, compositions, and methods of treating |
| WO2023207911A1 (zh) * | 2022-04-24 | 2023-11-02 | 上海医药集团股份有限公司 | 一种双环杂环化合物、药物组合物和应用 |
| CN117050075A (zh) * | 2022-05-05 | 2023-11-14 | 中国药科大学 | 一类联芳环类bet抑制剂及合成方法与用途 |
| CN117447392B (zh) * | 2023-09-13 | 2024-11-26 | 广州大学 | 一种荧光材料及其制备方法和应用 |
Family Cites Families (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4933438A (en) | 1984-02-29 | 1990-06-12 | University Of Florida | Brain-specific analogues of centrally acting amines |
| US6150354A (en) | 1987-01-15 | 2000-11-21 | Bonnie Davis | Compounds for the treatment of Alzheimer's disease |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| US5312817A (en) | 1991-05-14 | 1994-05-17 | Ernir Snorrason | Treatment of fatigue syndrome |
| IT1250421B (it) | 1991-05-30 | 1995-04-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato con proprieta' bio-adesive. |
| US6537579B1 (en) | 1993-02-22 | 2003-03-25 | American Bioscience, Inc. | Compositions and methods for administration of pharmacologically active compounds |
| FR2710265B1 (fr) | 1993-09-22 | 1995-10-20 | Adir | Composition pharmaceutique bioadhésive pour la libération contrôlée de principes actifs. |
| US5618819A (en) | 1994-07-07 | 1997-04-08 | Adir Et Compagnie | 1,3-dihydro-2H-pyrrolo[2,3-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-(3H)-one compounds |
| US6548084B2 (en) | 1995-07-20 | 2003-04-15 | Smithkline Beecham Plc | Controlled release compositions |
| US6245347B1 (en) | 1995-07-28 | 2001-06-12 | Zars, Inc. | Methods and apparatus for improved administration of pharmaceutically active compounds |
| DE19541260A1 (de) | 1995-11-06 | 1997-05-07 | Lohmann Therapie Syst Lts | Therapeutische Zubereitung zur transdermalen Applikation von Wirkstoffen durch die Haut |
| US6512010B1 (en) | 1996-07-15 | 2003-01-28 | Alza Corporation | Formulations for the administration of fluoxetine |
| EA002806B1 (ru) | 1997-09-11 | 2002-10-31 | Нюкомед Данмарк А/С | Многоединичные композиции с модифицированным высвобождением нестероидных противовоспалительных лекарственных веществ (nsaid) |
| US6624200B2 (en) | 1998-08-25 | 2003-09-23 | Columbia Laboratories, Inc. | Bioadhesive progressive hydration tablets |
| GB9721437D0 (en) | 1997-10-10 | 1997-12-10 | Glaxo Group Ltd | Heteroaromatic compounds and their use in medicine |
| US6607751B1 (en) | 1997-10-10 | 2003-08-19 | Intellipharamaceutics Corp. | Controlled release delivery device for pharmaceutical agents incorporating microbial polysaccharide gum |
| US6403597B1 (en) | 1997-10-28 | 2002-06-11 | Vivus, Inc. | Administration of phosphodiesterase inhibitors for the treatment of premature ejaculation |
| US6248864B1 (en) | 1997-12-31 | 2001-06-19 | Adherex Technologies, Inc. | Compounds and methods and modulating tissue permeability |
| US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
| US6312717B1 (en) | 1998-07-07 | 2001-11-06 | Bristol-Myers Squibb Company | Method for treatment of anxiety and depression |
| US20020009478A1 (en) | 1998-08-24 | 2002-01-24 | Douglas Joseph Dobrozsi | Oral liquid mucoadhesive compositions |
| SE9802864D0 (sv) | 1998-08-27 | 1998-08-27 | Pharmacia & Upjohn Ab | Transdermally administered tolterodine as antimuscarinic agent for the treatment of overactive bladder |
| DE69923200T2 (de) | 1998-10-01 | 2005-12-22 | Novartis Ag | Neue oral anzuwendende arzneizubereitungen für rivastigmine mit kontrollierter wirkstoffabgabe |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US6498176B1 (en) | 1999-03-04 | 2002-12-24 | Smithklinebeecham Corporation | 3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors |
| US6624171B1 (en) | 1999-03-04 | 2003-09-23 | Smithkline Beecham Corporation | Substituted aza-oxindole derivatives |
| GB9904933D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Compounds |
| GB9904995D0 (en) | 1999-03-04 | 1999-04-28 | Glaxo Group Ltd | Substituted aza-oxindole derivatives |
| FR2792527B1 (fr) | 1999-04-22 | 2004-08-13 | Ethypharm Lab Prod Ethiques | Microgranules de ketoprofene, procede de preparation et compositions pharmaceutiques |
| US6541020B1 (en) | 1999-07-09 | 2003-04-01 | Trimeris, Inc. | Methods and compositions for administration of therapeutic reagents |
| PT1202994E (pt) | 1999-07-21 | 2004-08-31 | Astrazeneca Ab | Novos compostos |
| US6562375B1 (en) | 1999-08-04 | 2003-05-13 | Yamanouchi Pharmaceuticals, Co., Ltd. | Stable pharmaceutical composition for oral use |
| AU781048B2 (en) | 1999-09-02 | 2005-05-05 | Nostrum Pharmaceuticals, Inc. | Controlled release pellet formulation |
| US6544548B1 (en) | 1999-09-13 | 2003-04-08 | Keraplast Technologies, Ltd. | Keratin-based powders and hydrogel for pharmaceutical applications |
| US6080736A (en) | 1999-10-27 | 2000-06-27 | Janus Pharmaceuticals, Inc. | Methods and compositions for treating and preventing anxiety and anxiety disorders using optically pure (R) tofisopam |
| US6461631B1 (en) | 1999-11-16 | 2002-10-08 | Atrix Laboratories, Inc. | Biodegradable polymer composition |
| AU2463701A (en) | 1999-12-29 | 2001-07-09 | Nanodelivery, Inc. | Drug delivery system exhibiting permeability control |
| US6589549B2 (en) | 2000-04-27 | 2003-07-08 | Macromed, Incorporated | Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles |
| US6524621B2 (en) | 2000-05-01 | 2003-02-25 | Aeropharm Technology Inc. | Core formulation |
| US6482440B2 (en) | 2000-09-21 | 2002-11-19 | Phase 2 Discovery, Inc. | Long acting antidepressant microparticles |
| US6524615B2 (en) | 2001-02-21 | 2003-02-25 | Kos Pharmaceuticals, Incorporated | Controlled release pharmaceutical composition |
| CA2439263C (en) | 2001-03-02 | 2012-10-23 | Frank Becker | Three hybrid assay system |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| EP2295433A3 (en) * | 2003-03-06 | 2011-07-06 | Eisai R&D Management Co., Ltd. | JNK inhibitors |
| GB2400101A (en) * | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| JP2007516180A (ja) * | 2003-07-02 | 2007-06-21 | スゲン,インコーポレイティド | c−Met阻害薬としてのアリールメチルトリアゾロおよびイミダゾピラジン類 |
| AR045595A1 (es) * | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| PL2332940T3 (pl) * | 2004-03-30 | 2013-03-29 | Vertex Pharma | Azaindole użyteczne jako inhibitory JAK i innych kinaz białkowych |
| US20060011139A1 (en) | 2004-07-16 | 2006-01-19 | Applied Materials, Inc. | Heated substrate support for chemical vapor deposition |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| WO2006015123A1 (en) * | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7709645B2 (en) * | 2004-07-27 | 2010-05-04 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361764B2 (en) * | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| CN101027302B (zh) * | 2004-07-27 | 2011-05-11 | Sgx药物公司 | 吡咯并吡啶激酶调节剂 |
| CN101065016A (zh) * | 2004-09-24 | 2007-10-31 | 詹森药业有限公司 | 蛋白激酶的抑制剂咪唑并[4,5-b]吡嗪酮 |
| AU2005302707A1 (en) | 2004-10-27 | 2006-05-11 | Janssen Pharmaceutica N.V. | Pyridine imidazoles and aza-indoles as progesterone receptor modulators |
| EP1828180A4 (en) * | 2004-12-08 | 2010-09-15 | Glaxosmithkline Llc | 1H-pyrrolo [2,3-BETA] PYRIDINE |
| EP1858895B1 (en) | 2005-02-16 | 2012-06-20 | Schering Corporation | Piperazine-piperidines with cxcr3 antagonist activity |
| CN102603581B (zh) * | 2005-06-22 | 2015-06-24 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
| JP2007108926A (ja) | 2005-10-12 | 2007-04-26 | Denso Corp | 運転支援装置及びプログラム |
| US20090252757A1 (en) | 2005-12-08 | 2009-10-08 | Irm Llc | Methods and compositions for inhibiting hiv infection |
| EP2236620A3 (en) | 2006-05-05 | 2011-05-25 | George Mason Intellectual Properties, Inc. | Compositions for treating HIV infection |
| WO2007135398A1 (en) * | 2006-05-22 | 2007-11-29 | Astrazeneca Ab | Indole derivatives |
| US7732447B2 (en) * | 2006-06-22 | 2010-06-08 | Cephalon, Inc. | Fused [d]pyridazin-7-ones |
| PL2583970T3 (pl) | 2006-08-02 | 2016-05-31 | Cytokinetics Inc | Określone cząstki chemiczne, kompozycje i sposoby zawierające imidazopirymidyny |
| MX337906B (es) * | 2006-10-19 | 2016-03-28 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| GB0706168D0 (en) | 2007-03-29 | 2007-05-09 | Glaxo Group Ltd | Compounds |
| CA2683398A1 (en) | 2007-04-10 | 2008-10-16 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| KR101524817B1 (ko) | 2007-04-18 | 2015-06-01 | 깃세이 야쿠힌 고교 가부시키가이샤 | 질소 함유 축합환 유도체, 그것을 함유하는 의약 조성물 및 그 의약 용도 |
| AU2008317406B2 (en) | 2007-10-25 | 2013-07-18 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| MX2010008198A (es) | 2008-02-25 | 2010-08-23 | Hoffmann La Roche | Inhibidores de cinasa de pirrolopirazina. |
| WO2010016490A1 (ja) * | 2008-08-05 | 2010-02-11 | 第一三共株式会社 | イミダゾピリジン-2-オン誘導体 |
| JP2012509342A (ja) * | 2008-11-20 | 2012-04-19 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 置換ピロロ[2,3−b]−ピリジンおよび−ピラジン |
| EP3037421A3 (en) * | 2008-11-25 | 2016-11-30 | University Of Rochester | Mlk inhibitors and methods of use |
| WO2010068899A1 (en) | 2008-12-12 | 2010-06-17 | Creighton University | Nanoparticles comprising combinations of antiretroviral agents and use thereof |
| WO2011149950A2 (en) | 2010-05-24 | 2011-12-01 | University Of Rochester | Bicyclic heteroaryl kinase inhibitors and methods of use |
| JP2013542945A (ja) | 2010-11-02 | 2013-11-28 | ボード オブ リージェンツ オブ ザ ユニバーシティ オブ ネブラスカ | 治療を送達するための組成物および方法 |
| WO2014085795A1 (en) | 2012-11-30 | 2014-06-05 | University Of Rochester | Mixed lineage kinase inhibitors for hiv/aids therapies |
-
2009
- 2009-11-25 EP EP15186751.2A patent/EP3037421A3/en not_active Withdrawn
- 2009-11-25 WO PCT/US2009/065878 patent/WO2010068483A2/en not_active Ceased
- 2009-11-25 AU AU2009324894A patent/AU2009324894B2/en active Active
- 2009-11-25 ES ES09832359.5T patent/ES2554375T3/es active Active
- 2009-11-25 CN CN200980152665.1A patent/CN102264743B/zh active Active
- 2009-11-25 JP JP2011537733A patent/JP5930278B2/ja active Active
- 2009-11-25 EP EP09832359.5A patent/EP2379561B1/en active Active
- 2009-11-25 US US13/131,193 patent/US8877772B2/en active Active
- 2009-11-25 CA CA2744498A patent/CA2744498C/en active Active
-
2014
- 2014-10-07 US US14/508,566 patent/US9181247B2/en active Active
- 2014-11-14 JP JP2014232195A patent/JP5873544B2/ja active Active
-
2015
- 2015-10-06 US US14/876,345 patent/US20160024087A1/en not_active Abandoned
-
2016
- 2016-06-03 US US15/172,355 patent/US9814704B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP5873544B2 (ja) | 2016-03-01 |
| US9181247B2 (en) | 2015-11-10 |
| EP2379561A4 (en) | 2012-10-03 |
| CA2744498A1 (en) | 2010-06-17 |
| AU2009324894B2 (en) | 2015-04-09 |
| CN102264743B (zh) | 2015-02-11 |
| CN102264743A (zh) | 2011-11-30 |
| EP3037421A3 (en) | 2016-11-30 |
| JP2015052009A (ja) | 2015-03-19 |
| AU2009324894A1 (en) | 2011-11-24 |
| CA2744498C (en) | 2017-10-24 |
| JP2012509903A (ja) | 2012-04-26 |
| US9814704B2 (en) | 2017-11-14 |
| ES2554375T3 (es) | 2015-12-18 |
| US20120053175A1 (en) | 2012-03-01 |
| EP3037421A1 (en) | 2016-06-29 |
| EP2379561A2 (en) | 2011-10-26 |
| US8877772B2 (en) | 2014-11-04 |
| US20160317509A1 (en) | 2016-11-03 |
| EP2379561B1 (en) | 2015-11-04 |
| US20150105401A1 (en) | 2015-04-16 |
| US20160024087A1 (en) | 2016-01-28 |
| WO2010068483A3 (en) | 2010-09-30 |
| WO2010068483A2 (en) | 2010-06-17 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5873544B2 (ja) | Mlk阻害剤および使用方法 | |
| JP6086326B2 (ja) | 二環式ヘテロアリールキナーゼ阻害剤および使用方法 | |
| US11932643B2 (en) | Substituted heterocyclic inhibitors of PTPN11 | |
| EP2925319B1 (en) | Mixed lineage kinase inhibitors for hiv/aids therapies | |
| US12186324B2 (en) | Imidazopiperazine inhibitors of transcription activating proteins | |
| CA3142239A1 (en) | Anticancer combination therapy | |
| US11046649B2 (en) | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20121121 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20121122 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20140205 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20140206 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20140502 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20140513 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140520 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20140714 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20141114 |
|
| A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20150202 |
|
| A912 | Re-examination (zenchi) completed and case transferred to appeal board |
Free format text: JAPANESE INTERMEDIATE CODE: A912 Effective date: 20150220 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160215 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20160420 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 5930278 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |