ZA200402172B - 3-Azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists - Google Patents
3-Azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists Download PDFInfo
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- ZA200402172B ZA200402172B ZA200402172A ZA200402172A ZA200402172B ZA 200402172 B ZA200402172 B ZA 200402172B ZA 200402172 A ZA200402172 A ZA 200402172A ZA 200402172 A ZA200402172 A ZA 200402172A ZA 200402172 B ZA200402172 B ZA 200402172B
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- South Africa
- Prior art keywords
- alkyl
- aza
- exo
- hydroxy
- phenyl
- Prior art date
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- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 239000002287 radioligand Substances 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 238000005932 reductive alkylation reaction Methods 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 150000005621 tetraalkylammonium salts Chemical class 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- FAQYAMRNWDIXMY-UHFFFAOYSA-N trichloroborane Chemical compound ClB(Cl)Cl FAQYAMRNWDIXMY-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
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- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
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- A—HUMAN NECESSITIES
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A61P25/32—Alcohol-abuse
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/34—Tobacco-abuse
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
- C07D303/02—Compounds containing oxirane rings
- C07D303/04—Compounds containing oxirane rings containing only hydrogen and carbon atoms in addition to the ring oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Otolaryngology (AREA)
- Nutrition Science (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33851101P | 2001-10-22 | 2001-10-22 |
Publications (1)
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|---|---|
| ZA200402172B true ZA200402172B (en) | 2006-09-27 |
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Family Applications (1)
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| ZA200402172A ZA200402172B (en) | 2001-10-22 | 2004-03-18 | 3-Azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists |
Country Status (42)
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1598339T1 (sl) | 2001-04-18 | 2009-12-31 | Euro Celtique Sa | Derivati 1-(4-amino.cikloheksil)-1,3-dihidro-2h-benzimidazol-2-ona in sorodne spojine kot nociceptinski analogi in ORL1 ligandi za zdravljenje bolečine |
| CA2463264C (fr) | 2001-10-22 | 2009-05-26 | Pfizer Products Inc. | Derives 3-azabicyclo (3.1.0) hexane en tant qu'antagonistes de recepteur opioide |
| WO2004089908A2 (fr) * | 2003-04-14 | 2004-10-21 | Pfizer Products Inc. | Derives de 3-azabicyclo[3.2.1]octane |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7153976B2 (en) * | 2003-10-06 | 2006-12-26 | Pfizer Inc. | Purification process for an azabicyclo[3.1.0]hexane compound |
| ES2634841T3 (es) * | 2003-10-14 | 2017-09-29 | Pfizer Products Inc. | Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina |
| AU2004281229A1 (en) * | 2003-10-16 | 2005-04-28 | Pfizer Products Inc. | Preparation of 3-azabicyclo (3.1.0) hexane derivatives |
| US7855298B2 (en) | 2004-02-23 | 2010-12-21 | Glaxo Group Limited | Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors |
| CA2558274A1 (fr) * | 2004-03-05 | 2005-09-15 | Banyu Pharmaceutical Co., Ltd. | Derive cycloalkanopyridine |
| EP1837022A4 (fr) * | 2004-12-14 | 2009-12-16 | Toray Industries | Derive d'indolomorphinane avec carboxy en position 6' |
| GB0512099D0 (en) * | 2005-06-14 | 2005-07-20 | Glaxo Group Ltd | Compounds |
| GB0517191D0 (en) * | 2005-08-22 | 2005-09-28 | Glaxo Group Ltd | Compounds |
| US7592461B2 (en) | 2005-12-21 | 2009-09-22 | Bristol-Myers Squibb Company | Indane modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof |
| MY145633A (en) | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| WO2008075162A2 (fr) * | 2006-12-15 | 2008-06-26 | Pfizer Limited | Composés pour le traitement d'un dysfonctionnement sexuel |
| TWI409067B (zh) | 2007-02-28 | 2013-09-21 | Theravance Inc | ８-氮雜雙環〔３．２．１〕辛烷化合物之結晶型 |
| US7691878B2 (en) * | 2007-08-27 | 2010-04-06 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| TWI423801B (zh) * | 2007-08-27 | 2014-01-21 | Theravance Inc | 作為μ類鴉片受體拮抗劑之８－氮雜雙環〔３．２．１〕辛基－２－羥基苯甲醯胺化合物 |
| WO2009029252A1 (fr) * | 2007-08-27 | 2009-03-05 | Theravance, Inc. | Composés d'amidoalkyle-8-azabicyclo[3.2.1]octane en tant qu'antagonistes du récepteur opioïde mu |
| WO2009029257A1 (fr) * | 2007-08-27 | 2009-03-05 | Theravance, Inc. | Composes d'alkyl-8-azabicyclo[3.2.1.]octane disubstitutes utilises en tant qu'antagonistes du recepteur opioide mu |
| BR112013007566A2 (pt) | 2010-09-28 | 2016-08-02 | Panacea Biotec Ltd | novos compostos bicíclicos |
| DK3072884T3 (da) * | 2013-11-20 | 2020-03-09 | Sanwa Kagaku Kenkyusho Co | 3-azabicyclo[3.1.0]hexanderivat og anvendelse deraf til medicinske formål |
| EP3299357A4 (fr) | 2015-05-20 | 2018-11-14 | Sanwa Kagaku Kenkyusho Co., Ltd. | Cristal de sel de nouveau dérivé de 3-azabicyclo[3.1.0]hexane et son utilisation pharmaceutique |
| US20200237720A1 (en) | 2017-03-02 | 2020-07-30 | Sanwa Kagaku Kenkyusho Co., Ltd. | Therapeutic agent for alcohol use disorders |
Family Cites Families (26)
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| US2099214A (en) * | 1937-11-16 | Process fob forming the sulphuric | ||
| US2099216A (en) * | 1934-05-04 | 1937-11-16 | Frederick H Nass | Metal testing machine |
| US3004340A (en) * | 1959-09-24 | 1961-10-17 | Bernice L Collins | Kitchen utensil |
| US3078282A (en) * | 1960-01-02 | 1963-02-19 | Bayer Ag | Anthraquinone dyestuffs |
| NZ224236A (en) | 1987-04-16 | 1990-08-28 | Lilly Co Eli | Trans 3,4 pyridine derivatives and pharmaceutical compositions |
| JPH04155522A (ja) * | 1990-10-19 | 1992-05-28 | Nec Corp | ファースト・イン・ランダム・アウト回路 |
| US5159081A (en) | 1991-03-29 | 1992-10-27 | Eli Lilly And Company | Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists |
| NZ242117A (en) | 1991-03-29 | 1994-11-25 | Lilly Co Eli | 4-phenylpiperidine derivatives and medicaments containing them |
| GB9725114D0 (en) * | 1997-11-28 | 1998-01-28 | Pfizer Ltd | Treatment of pruritus |
| GB9810671D0 (en) * | 1998-05-18 | 1998-07-15 | Pfizer Ltd | Anti-pruritic agents |
| TWI244481B (en) * | 1998-12-23 | 2005-12-01 | Pfizer | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GB9912410D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912415D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912413D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912411D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| US20020064825A1 (en) * | 2000-05-19 | 2002-05-30 | Lewis Marilyn Evelyn | Novel polypeptide |
| US20030207876A1 (en) * | 2000-06-23 | 2003-11-06 | Banks Bernard Joseph | 3-Azabicyclo[3.1.0]hexane derivatives useful in therapy |
| US20020025948A1 (en) * | 2000-06-23 | 2002-02-28 | Banks Bernard Joseph | 3-azabicyclo[3.1.0]hexane derivatives useful in therapy |
| GB0015562D0 (en) * | 2000-06-23 | 2000-08-16 | Pfizer Ltd | Heterocycles |
| DE10042885A1 (de) * | 2000-08-31 | 2002-03-14 | Heidelberger Druckmasch Ag | Bogentransportzylinder |
| CA2463264C (fr) | 2001-10-22 | 2009-05-26 | Pfizer Products Inc. | Derives 3-azabicyclo (3.1.0) hexane en tant qu'antagonistes de recepteur opioide |
| ATE308522T1 (de) | 2002-05-30 | 2005-11-15 | Lilly Co Eli | Opioidrezeptorantagonisten |
| US20040204453A1 (en) * | 2003-04-14 | 2004-10-14 | Pfizer Inc | 4-Phenyl-piperidine compounds and their use as modulators of opioid receptors |
| US7056930B2 (en) * | 2003-04-14 | 2006-06-06 | Pfizer Inc. | 2-Azabicyclo[3.3.1]nonane derivatives |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7153976B2 (en) * | 2003-10-06 | 2006-12-26 | Pfizer Inc. | Purification process for an azabicyclo[3.1.0]hexane compound |
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2002
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- 2002-09-09 UA UA20040402979A patent/UA75714C2/uk unknown
- 2002-09-09 AT AT02765197T patent/ATE392415T1/de not_active IP Right Cessation
- 2002-09-09 SI SI200230688T patent/SI1440059T1/sl unknown
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- 2002-09-09 EP EP02765197A patent/EP1440059B1/fr not_active Expired - Lifetime
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2004
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- 2004-04-15 MA MA27630A patent/MA27141A1/fr unknown
- 2004-04-20 CR CR7317A patent/CR7317A/es unknown
- 2004-04-21 TN TNP2004000071A patent/TNSN04071A1/fr unknown
- 2004-04-21 NO NO20041626A patent/NO329092B1/no not_active IP Right Cessation
- 2004-04-22 EC EC2004005077A patent/ECSP045077A/es unknown
-
2005
- 2005-02-24 US US11/066,095 patent/US20050171178A1/en not_active Abandoned
- 2005-06-08 HK HK05104840A patent/HK1072052A1/xx not_active IP Right Cessation
-
2006
- 2006-03-01 US US11/366,903 patent/US20070054950A1/en not_active Abandoned
-
2007
- 2007-10-19 JP JP2007272602A patent/JP2008069169A/ja active Pending
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