ATE327974T1 - Modulatoren des glucocorticoid-rezeptors - Google Patents
Modulatoren des glucocorticoid-rezeptorsInfo
- Publication number
- ATE327974T1 ATE327974T1 AT01309064T AT01309064T ATE327974T1 AT E327974 T1 ATE327974 T1 AT E327974T1 AT 01309064 T AT01309064 T AT 01309064T AT 01309064 T AT01309064 T AT 01309064T AT E327974 T1 ATE327974 T1 AT E327974T1
- Authority
- AT
- Austria
- Prior art keywords
- glucocorticoid receptor
- compounds
- modulators
- present
- provides
- Prior art date
Links
- 102000003676 Glucocorticoid Receptors Human genes 0.000 title abstract 2
- 108090000079 Glucocorticoid Receptors Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 2
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 abstract 1
- 229940117965 Glucocorticoid receptor modulator Drugs 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 108010085012 Steroid Receptors Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 abstract 1
- 229940126013 glucocorticoid receptor antagonist Drugs 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000004031 partial agonist Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 102000005969 steroid hormone receptors Human genes 0.000 abstract 1
- 230000003637 steroidlike Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/205—Radicals derived from carbonic acid
-
- 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
- A61P25/28—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
- 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
- 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
- A61P3/08—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
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
- C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/44—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
- C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/52—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Electrochromic Elements, Electrophoresis, Or Variable Reflection Or Absorption Elements (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24399300P | 2000-10-28 | 2000-10-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE327974T1 true ATE327974T1 (de) | 2006-06-15 |
Family
ID=22920962
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT01309064T ATE327974T1 (de) | 2000-10-28 | 2001-10-25 | Modulatoren des glucocorticoid-rezeptors |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20020107235A1 (de) |
| EP (1) | EP1201649B1 (de) |
| JP (1) | JP2002193911A (de) |
| AT (1) | ATE327974T1 (de) |
| BR (1) | BR0104831A (de) |
| CA (1) | CA2360308C (de) |
| DE (1) | DE60120077T2 (de) |
| ES (1) | ES2262612T3 (de) |
| MX (1) | MXPA01010961A (de) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL146057A (en) * | 2000-10-27 | 2007-09-20 | Pfizer Prod Inc | A process for the preparation of modulators of a non-steroidal glucocorticoid receptor |
| EP1349546A2 (de) * | 2000-12-20 | 2003-10-08 | BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG | Dissoziierte glucocorticoid-rezeptorantagonisten zur behandlung von nebenwirkungen von glucocorticoiden |
| BR0214967A (pt) | 2001-12-14 | 2005-05-10 | Novo Nordisk As | Composto, sal famaceuticamente aceitável, processo para a preparação de um composto, composição farmacêutica, uso de um composto e método de tratar um distúrbio de um paciente |
| WO2004005229A1 (en) * | 2002-07-08 | 2004-01-15 | Pfizer Products Inc. | Modulators of the glucocorticoid receptor |
| US20040220153A1 (en) * | 2002-09-24 | 2004-11-04 | Jost-Price Edward Roydon | Methods and reagents for the treatment of diseases and disorders associated with increased levels of proinflammatory cytokines |
| US7091196B2 (en) | 2002-09-26 | 2006-08-15 | Rib-X Pharmaceuticals, Inc. | Bifunctional heterocyclic compounds and methods of making and using same |
| BR0314872A (pt) * | 2002-10-18 | 2005-08-02 | Pfizer Prod Inc | Ligandos do receptor canabinóide e usos dos mesmos |
| FR2847471B1 (fr) * | 2002-11-25 | 2006-12-29 | Expanscience Lab | Composition comprenant au moins un derive d'acide carbamique ,son utilisation cosmetique et comme medicament |
| TW200517114A (en) | 2003-10-15 | 2005-06-01 | Combinatorx Inc | Methods and reagents for the treatment of immunoinflammatory disorders |
| JP2007512337A (ja) | 2003-11-21 | 2007-05-17 | コンビナトアールエックス インコーポレーティッド | 炎症性障害の治療のための方法および試薬 |
| EP2716647A3 (de) | 2004-02-27 | 2014-08-20 | Rib-X Pharmaceuticals, Inc. | Makrocyclische Verbindungen Und Verfahren Zu Deren Herstellung Und Anwendung |
| US20050267141A1 (en) | 2004-05-28 | 2005-12-01 | Phytogen Life Sciences Inc. | Process to prepare camptothecin derivatives |
| US8067433B2 (en) | 2005-11-09 | 2011-11-29 | Zalicus Inc. | Methods, compositions, and kits for the treatment of ophthalmic disorders |
| UZ4378C (en) * | 2007-02-02 | 2011-07-29 | Pfizer Prod Inc | Tricyclic compounds and their use as glucocorticoid receptor modulators |
| DK2114970T3 (da) | 2007-02-02 | 2011-09-19 | Pfizer Prod Inc | Tricykliske forbindelser og deres anvendelse som glucocorticoidreceptormodulatorer |
| BRPI0917212A2 (pt) | 2008-07-28 | 2015-11-10 | Pfizer | compostos de fenantrenona, seus usos na preparação de composições, e composições compreendendo os referidos compostos |
| US20100092479A1 (en) * | 2008-08-18 | 2010-04-15 | Combinatorx (Singapore) Pte. Ltd. | Compositions and methods for treatment of viral diseases |
| ES2745628T3 (es) | 2008-11-07 | 2020-03-03 | Univ Sheffield | Medicamento y método de diagnóstico |
| EP2525831B1 (de) | 2010-01-22 | 2019-05-15 | Ascendis Pharma A/S | Trägerverknüpfte carbamat-prodrug-linker |
| TW201422590A (zh) | 2012-09-07 | 2014-06-16 | Abbvie Inc | 雜環核激素受體調節劑 |
| EP2935284A4 (de) | 2012-12-21 | 2016-04-27 | Abbvie Inc | Heterocyclische nuklearhormonrezeptormodulatoren |
| US20170260131A1 (en) * | 2014-11-25 | 2017-09-14 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists |
| US11634384B2 (en) * | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
| CA3025268A1 (en) | 2016-05-25 | 2017-11-30 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
| US10717712B2 (en) | 2018-07-27 | 2020-07-21 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL122740A (en) * | 1997-01-15 | 2003-09-17 | Akzo Nobel Nv | 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them |
| PL207610B1 (pl) * | 1999-04-30 | 2011-01-31 | Pfizer Prod Inc | Związki modulujące receptory glukokortykoidowe, ich zastosowanie do wytwarzania leku i środek farmaceutyczny |
| IL146057A (en) * | 2000-10-27 | 2007-09-20 | Pfizer Prod Inc | A process for the preparation of modulators of a non-steroidal glucocorticoid receptor |
-
2001
- 2001-10-25 EP EP01309064A patent/EP1201649B1/de not_active Expired - Lifetime
- 2001-10-25 DE DE60120077T patent/DE60120077T2/de not_active Expired - Fee Related
- 2001-10-25 AT AT01309064T patent/ATE327974T1/de not_active IP Right Cessation
- 2001-10-25 JP JP2001328050A patent/JP2002193911A/ja active Pending
- 2001-10-25 ES ES01309064T patent/ES2262612T3/es not_active Expired - Lifetime
- 2001-10-26 CA CA002360308A patent/CA2360308C/en not_active Expired - Fee Related
- 2001-10-26 BR BR0104831-7A patent/BR0104831A/pt not_active IP Right Cessation
- 2001-10-26 MX MXPA01010961A patent/MXPA01010961A/es unknown
- 2001-10-26 US US10/006,215 patent/US20020107235A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DE60120077D1 (de) | 2006-07-06 |
| CA2360308C (en) | 2006-02-07 |
| US20020107235A1 (en) | 2002-08-08 |
| MXPA01010961A (es) | 2002-05-24 |
| JP2002193911A (ja) | 2002-07-10 |
| ES2262612T3 (es) | 2006-12-01 |
| CA2360308A1 (en) | 2002-04-28 |
| EP1201649B1 (de) | 2006-05-31 |
| BR0104831A (pt) | 2002-08-20 |
| DE60120077T2 (de) | 2006-11-02 |
| EP1201649A1 (de) | 2002-05-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |