AU2009277057A1 - Pyrazinone modulator of corticotropin-releasing factor receptor activity - Google Patents
Pyrazinone modulator of corticotropin-releasing factor receptor activity Download PDFInfo
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- AU2009277057A1 AU2009277057A1 AU2009277057A AU2009277057A AU2009277057A1 AU 2009277057 A1 AU2009277057 A1 AU 2009277057A1 AU 2009277057 A AU2009277057 A AU 2009277057A AU 2009277057 A AU2009277057 A AU 2009277057A AU 2009277057 A1 AU2009277057 A1 AU 2009277057A1
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- Prior art keywords
- cyclopropyl
- crf
- mmol
- methoxyethyl
- pct
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- 108010056643 Corticotropin-Releasing Hormone Receptors Proteins 0.000 title description 6
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- 230000003938 response to stress Effects 0.000 description 1
- 238000007363 ring formation reaction Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 230000035939 shock 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
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000012321 sodium triacetoxyborohydride Substances 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 210000000278 spinal cord Anatomy 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
- 230000004936 stimulating effect Effects 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 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
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- XHVSCKNABCCCAC-UHFFFAOYSA-N trimethylsilyl 2,2-difluoro-2-fluorosulfonylacetate Chemical compound C[Si](C)(C)OC(=O)C(F)(F)S(F)(=O)=O XHVSCKNABCCCAC-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 238000007514 turning Methods 0.000 description 1
- 230000009452 underexpressoin Effects 0.000 description 1
- 229940072690 valium Drugs 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
- 238000010792 warming Methods 0.000 description 1
- 238000005406 washing Methods 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
- MMSLSKDMIZOHRX-WYDAWZGFSA-N α-helical crf(9-41) Chemical compound OC(=O)C[C@H](N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(N)=O MMSLSKDMIZOHRX-WYDAWZGFSA-N 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8523008P | 2008-07-31 | 2008-07-31 | |
| US61/085,230 | 2008-07-31 | ||
| PCT/US2009/041793 WO2010014280A1 (en) | 2008-07-31 | 2009-04-27 | Pyrazinone modulator of corticotropin-releasing factor receptor activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2009277057A1 true AU2009277057A1 (en) | 2010-02-04 |
Family
ID=40651774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2009277057A Abandoned AU2009277057A1 (en) | 2008-07-31 | 2009-04-27 | Pyrazinone modulator of corticotropin-releasing factor receptor activity |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7932256B2 (https=) |
| EP (1) | EP2303867B1 (https=) |
| JP (1) | JP5396474B2 (https=) |
| KR (1) | KR20110040870A (https=) |
| CN (1) | CN102171205B (https=) |
| AR (1) | AR072639A1 (https=) |
| AU (1) | AU2009277057A1 (https=) |
| MX (1) | MX2011000754A (https=) |
| TW (1) | TW201008926A (https=) |
| WO (1) | WO2010014280A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | Methods and compositions for treating schizophrenia |
| US10077443B2 (en) | 2012-11-15 | 2018-09-18 | Roche Innovation Center Copenhagen A/S | Oligonucleotide conjugates |
| CN104955952A (zh) | 2013-01-30 | 2015-09-30 | 弗·哈夫曼-拉罗切有限公司 | Lna寡核苷酸碳水化合物缀合物 |
| WO2015112642A1 (en) | 2014-01-21 | 2015-07-30 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonists for the treatment of congenital adrenal hyperplasia |
| CA3121920A1 (en) | 2018-12-07 | 2020-06-11 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| 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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6159980A (en) * | 1996-09-16 | 2000-12-12 | Dupont Pharmaceuticals Company | Pyrazinones and triazinones and their derivatives thereof |
| CN1231473C (zh) * | 2000-02-16 | 2005-12-14 | 神经能质公司 | 取代的芳基吡嗪 |
| RU2003136151A (ru) * | 2001-06-12 | 2005-05-20 | Ньюроджин Корпорейшн (US) | 2, 5-диарилпиразины, 2, 5-диарилпиридины и 2, 5-диарилпиримидины в качестве модуляторов рецептора кортикотропин-рилизинг-фактора 1 (крф1) |
| WO2004046136A1 (en) | 2002-11-21 | 2004-06-03 | 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 EP EP09789614.6A patent/EP2303867B1/en not_active Not-in-force
- 2009-04-27 CN CN2009801386016A patent/CN102171205B/zh not_active Expired - Fee Related
- 2009-04-27 JP JP2011521135A patent/JP5396474B2/ja not_active Expired - Fee Related
- 2009-04-27 AU AU2009277057A patent/AU2009277057A1/en not_active Abandoned
- 2009-04-27 KR KR1020117002253A patent/KR20110040870A/ko not_active Withdrawn
- 2009-04-27 WO PCT/US2009/041793 patent/WO2010014280A1/en not_active Ceased
- 2009-04-27 MX MX2011000754A patent/MX2011000754A/es active IP Right Grant
- 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 |
|---|---|
| US7932256B2 (en) | 2011-04-26 |
| CN102171205A (zh) | 2011-08-31 |
| CN102171205B (zh) | 2013-08-07 |
| JP5396474B2 (ja) | 2014-01-22 |
| US20110166160A1 (en) | 2011-07-07 |
| AR072639A1 (es) | 2010-09-08 |
| TW201008926A (en) | 2010-03-01 |
| KR20110040870A (ko) | 2011-04-20 |
| MX2011000754A (es) | 2011-02-24 |
| EP2303867B1 (en) | 2014-12-17 |
| WO2010014280A1 (en) | 2010-02-04 |
| EP2303867A1 (en) | 2011-04-06 |
| US20100029684A1 (en) | 2010-02-04 |
| US8372847B2 (en) | 2013-02-12 |
| JP2011529886A (ja) | 2011-12-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK4 | Application lapsed section 142(2)(d) - no continuation fee paid for the application |