TW201008926A - Pyrazinone modulator of corticotropin-releasing factor receptor activity - Google Patents
Pyrazinone modulator of corticotropin-releasing factor receptor activity Download PDFInfo
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- TW201008926A TW201008926A TW098124751A TW98124751A TW201008926A TW 201008926 A TW201008926 A TW 201008926A TW 098124751 A TW098124751 A TW 098124751A TW 98124751 A TW98124751 A TW 98124751A TW 201008926 A TW201008926 A TW 201008926A
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- cyclopropyl
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- 239000010452 phosphate Substances 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 210000003635 pituitary gland Anatomy 0.000 description 1
- 206010036067 polydipsia Diseases 0.000 description 1
- 239000004926 polymethyl methacrylate Substances 0.000 description 1
- 208000028173 post-traumatic stress disease Diseases 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 239000013014 purified material Substances 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- WHMDPDGBKYUEMW-UHFFFAOYSA-N pyridine-2-thiol Chemical compound SC1=CC=CC=N1 WHMDPDGBKYUEMW-UHFFFAOYSA-N 0.000 description 1
- 238000011552 rat model Methods 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 238000006268 reductive amination reaction Methods 0.000 description 1
- 238000006894 reductive elimination reaction Methods 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 229910052707 ruthenium Inorganic materials 0.000 description 1
- 239000000523 sample Substances 0.000 description 1
- 239000004576 sand Substances 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 230000000391 smoking effect Effects 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 208000020431 spinal cord injury Diseases 0.000 description 1
- NYKCGQQJNVPOLU-ONTIZHBOSA-N spiradoline Chemical compound C([C@@H]([C@H](C1)N2CCCC2)N(C)C(=O)CC=2C=C(Cl)C(Cl)=CC=2)C[C@]21CCCO2 NYKCGQQJNVPOLU-ONTIZHBOSA-N 0.000 description 1
- 229950006495 spiradoline Drugs 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000012353 t test Methods 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 235000007586 terpenes Nutrition 0.000 description 1
- BVYMBBLLDIFXQT-UHFFFAOYSA-N tert-butyl 2-(6-methoxy-5-methyl-3-nitropyridin-2-yl)acetate Chemical compound COC1=NC(CC(=O)OC(C)(C)C)=C([N+]([O-])=O)C=C1C BVYMBBLLDIFXQT-UHFFFAOYSA-N 0.000 description 1
- FQFILJKFZCVHNH-UHFFFAOYSA-N tert-butyl n-[3-[(5-bromo-2-chloropyrimidin-4-yl)amino]propyl]carbamate Chemical compound CC(C)(C)OC(=O)NCCCNC1=NC(Cl)=NC=C1Br FQFILJKFZCVHNH-UHFFFAOYSA-N 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- RLUJQBLWUQZMDG-UHFFFAOYSA-N toluene;hydrochloride Chemical compound Cl.CC1=CC=CC=C1 RLUJQBLWUQZMDG-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- GPRLSGONYQIRFK-MNYXATJNSA-N triton Chemical compound [3H+] GPRLSGONYQIRFK-MNYXATJNSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 229940072690 valium Drugs 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 230000009278 visceral effect Effects 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical class [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- 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
- A61P25/22—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
- A61P25/30—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8523008P | 2008-07-31 | 2008-07-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW201008926A true TW201008926A (en) | 2010-03-01 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW098124751A TW201008926A (en) | 2008-07-31 | 2009-07-22 | Pyrazinone modulator of corticotropin-releasing factor receptor activity |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7932256B2 (enExample) |
| EP (1) | EP2303867B1 (enExample) |
| JP (1) | JP5396474B2 (enExample) |
| KR (1) | KR20110040870A (enExample) |
| CN (1) | CN102171205B (enExample) |
| AR (1) | AR072639A1 (enExample) |
| AU (1) | AU2009277057A1 (enExample) |
| MX (1) | MX2011000754A (enExample) |
| TW (1) | TW201008926A (enExample) |
| WO (1) | WO2010014280A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6440625B2 (ja) | 2012-11-14 | 2018-12-19 | ザ・ジョンズ・ホプキンス・ユニバーシティー | 精神分裂病を処置するための方法および組成物 |
| RU2015119411A (ru) | 2012-11-15 | 2017-01-10 | Рош Инновейшен Сентер Копенгаген А/С | Конъюгаты антисмысловых соединений, направленные на аполипопротеин в |
| WO2014118267A1 (en) | 2013-01-30 | 2014-08-07 | Santaris Pharma A/S | Lna oligonucleotide carbohydrate conjugates |
| CN106102740A (zh) | 2014-01-21 | 2016-11-09 | 纽罗克里生物科学有限公司 | 治疗先天性肾上腺增生的crf1受体拮抗剂 |
| EP3984523B1 (en) | 2018-12-07 | 2025-09-03 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| WO2021062246A1 (en) | 2019-09-27 | 2021-04-01 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| IT201900021216A1 (it) | 2019-11-14 | 2021-05-14 | Isagro Spa | Processo per la preparazione di derivati piridinici e corrispondenti piridil-formammidine |
| CN112552184B (zh) * | 2020-12-18 | 2022-05-10 | 诚达药业股份有限公司 | 一种含环丙基手性胺盐酸盐的合成方法 |
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| ATE213495T1 (de) | 1996-09-16 | 2002-03-15 | Du Pont Pharm Co | Eine resorbierbare röntgenopake markierung enthaltendes chirurgisches implantat und verfahren zum verriegeln desselben in einem körper |
| NZ520484A (en) * | 2000-02-16 | 2005-03-24 | Neurogen Corp | Substituted arylpyrazines that are modulators of CRF (corticotropin releasing factor) receptor and methods of treatment using them |
| HRP20031096A2 (en) * | 2001-06-12 | 2005-08-31 | Neurogen Corporation | 2,5-diarylpyrazines, 2,5-diarylpyridines and 2,5-diarylpyrimidines as crf1 receptor modulators |
| AU2003278542A1 (en) | 2002-11-21 | 2004-06-15 | Pharmacia & Upjohn Company Llc | Pyrazine compounds as crf modulators |
-
2009
- 2009-04-24 US US12/429,810 patent/US7932256B2/en active Active
- 2009-04-27 CN CN2009801386016A patent/CN102171205B/zh not_active Expired - Fee Related
- 2009-04-27 KR KR1020117002253A patent/KR20110040870A/ko not_active Withdrawn
- 2009-04-27 AU AU2009277057A patent/AU2009277057A1/en not_active Abandoned
- 2009-04-27 JP JP2011521135A patent/JP5396474B2/ja not_active Expired - Fee Related
- 2009-04-27 EP EP09789614.6A patent/EP2303867B1/en not_active Not-in-force
- 2009-04-27 MX MX2011000754A patent/MX2011000754A/es active IP Right Grant
- 2009-04-27 WO PCT/US2009/041793 patent/WO2010014280A1/en not_active Ceased
- 2009-07-22 TW TW098124751A patent/TW201008926A/zh unknown
- 2009-07-30 AR ARP090102928A patent/AR072639A1/es not_active Application Discontinuation
-
2011
- 2011-03-21 US US13/052,458 patent/US8372847B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2011529886A (ja) | 2011-12-15 |
| US20110166160A1 (en) | 2011-07-07 |
| US8372847B2 (en) | 2013-02-12 |
| EP2303867B1 (en) | 2014-12-17 |
| KR20110040870A (ko) | 2011-04-20 |
| CN102171205B (zh) | 2013-08-07 |
| AU2009277057A1 (en) | 2010-02-04 |
| MX2011000754A (es) | 2011-02-24 |
| CN102171205A (zh) | 2011-08-31 |
| WO2010014280A1 (en) | 2010-02-04 |
| US20100029684A1 (en) | 2010-02-04 |
| JP5396474B2 (ja) | 2014-01-22 |
| AR072639A1 (es) | 2010-09-08 |
| EP2303867A1 (en) | 2011-04-06 |
| US7932256B2 (en) | 2011-04-26 |
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