BR0209035A - Antagonistas de receptor crf - Google Patents
Antagonistas de receptor crfInfo
- Publication number
- BR0209035A BR0209035A BR0209035-0A BR0209035A BR0209035A BR 0209035 A BR0209035 A BR 0209035A BR 0209035 A BR0209035 A BR 0209035A BR 0209035 A BR0209035 A BR 0209035A
- Authority
- BR
- Brazil
- Prior art keywords
- halo
- alkyl
- alkoxy
- alkynyl
- alkenyl
- Prior art date
Links
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- 108010056643 Corticotropin-Releasing Hormone Receptors Proteins 0.000 title 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102400000739 Corticotropin Human genes 0.000 abstract 1
- 101800000414 Corticotropin Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 abstract 1
- 229960000258 corticotropin Drugs 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- -1 halo C1-C6 alkoxy Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 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
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-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
- C07D471/06—Peri-condensed systems
-
- 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
- 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
- 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
- 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
-
- 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
- C07D487/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
"ANTAGONISTAS DE RECEPTOR CRF". A presente invenção diz respeito a compostos de pirimidinas tricíclicas de fórmula (I), incluindo esteroisómeros, profármacos e sais ou solvatos farmaceuticamente aceitáveis destes, em que R é arila ou heteroarila, em que, em cada um dos grupos apresentados, R pode ser substituído por 1 a 4 substituintes selecionados independentemente do grupo que consiste de: halogênio, C1-C6 alquila, C1-C6 alcóxi, halo C1-C6 alquila, C1-C6 alquenila, C1-C6 alquinila, halo C1-C6 alcóxi, C1-C6 mono ou dialquilamino, nitro, ciano e um grupo R~ 4~; R~ 1~ é hidrogênio, C1-C6 alquila, C1-C6 alquenila, C1-C6 alquinila, halo C1-C6 alquila, halo C1-C6 alcóxi, NH~ 2~, halogênio ou ciano; R~ 2~ é hidrogênio ou C(H)~ n~n(R~ 5~)~ q~(CH~ 2~)pZR~ 6~: R~ 1~ é hidrogênio, C2-C6 alquenila, C2-C6 alquinila ou [CH (R~ 5~) (CH~ 2~)]~ m~ZR~ 6~; R~ 4~ é C3 -C7 cicloalquila, que pode conter uma ou mais ligações duplas; arila; ou um heterociclo 5-6 membrado; em que, em cada um dos grupos apresentados, R~ 4~ pode ser substituído por um ou mais grupos selecionados de: halogênio, C1-C6 alquila, C1-C6 alcóxi, halo C1-C6 alquila, C2-C6 alquenila, C2-C6 alquinila, halo C1-C6 alcóxi, C1-C6 mona ou dialquilamino, nitro, e ciano; R~ 5~ é hidrogênio, C2-C6 alquenila, C2-C6 alquinila ou (CH~ 2~)pZR~ 6~; R~ 6~ é C1-C6 alquila, que pode ser substituído por um ou mais grupos selecionados de halogênio, halo C1-C6 alquila, C2-C6 alquenila, C2-C6 alquinila, halo C1-C6 alcóxi, C1-C6 alcóxi, C1-C6 mono ou dialquilamino, nitro, ciano e um grupo R~ 4~; Y e X são independentemente carbono ou nitrogênio; m e n são independentemente 0 ou 1; p é 0 ou um número inteiro de 1 a 4; q é 1 ou 2; Z é uma ligação 0, NH ou S; a processos para sua preparação, a composições farmacêuticas que os contém e seus usos no tratamento de condições mediadas por fator de liberação de corticotropina (CRF).
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0110566A GB0110566D0 (en) | 2001-04-30 | 2001-04-30 | Chemical compounds |
| GB0110579A GB0110579D0 (en) | 2001-04-30 | 2001-04-30 | Chemical compounds |
| GB0117423A GB0117423D0 (en) | 2001-07-17 | 2001-07-17 | Chemical compounds |
| GB0203203A GB0203203D0 (en) | 2002-02-11 | 2002-02-11 | Chemical compounds |
| PCT/GB2002/001981 WO2002087573A1 (en) | 2001-04-30 | 2002-04-30 | Crf receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0209035A true BR0209035A (pt) | 2004-08-10 |
Family
ID=27447943
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0209035-0A BR0209035A (pt) | 2001-04-30 | 2002-04-30 | Antagonistas de receptor crf |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7329667B2 (pt) |
| EP (1) | EP1383498B1 (pt) |
| JP (1) | JP2004528342A (pt) |
| KR (1) | KR20040015205A (pt) |
| CN (1) | CN1512883A (pt) |
| AR (1) | AR033296A1 (pt) |
| AT (1) | ATE320254T1 (pt) |
| AU (1) | AU2002249474B2 (pt) |
| BR (1) | BR0209035A (pt) |
| CA (1) | CA2446497A1 (pt) |
| CZ (1) | CZ20032945A3 (pt) |
| DE (1) | DE60209885T2 (pt) |
| ES (1) | ES2255610T3 (pt) |
| HU (1) | HUP0304035A2 (pt) |
| IL (1) | IL158063A0 (pt) |
| MX (1) | MXPA03009930A (pt) |
| NO (1) | NO20034837L (pt) |
| NZ (1) | NZ528364A (pt) |
| PL (1) | PL366854A1 (pt) |
| TW (1) | TWI236908B (pt) |
| WO (1) | WO2002087573A1 (pt) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0308208D0 (en) | 2003-04-09 | 2003-05-14 | Glaxo Group Ltd | Chemical compounds |
| CA2764885C (en) | 2009-06-08 | 2018-05-15 | Takeda Pharmaceutical Company Limited | Dihydropyrrolonaphtyridinone compounds as inhibitors of jak |
| RU2498986C2 (ru) * | 2011-07-20 | 2013-11-20 | Учреждение Российской Академии Наук Институт Проблем Химической Физики Ран (Ипхф Ран) | ТЕТРАЦИАНОЗАМЕЩЕННЫЕ 1,4,9b-ТРИАЗАФЕНАЛЕНЫ И СПОСОБ ИХ ПОЛУЧЕНИЯ |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6403599B1 (en) * | 1995-11-08 | 2002-06-11 | Pfizer Inc | Corticotropin releasing factor antagonists |
| ZA973884B (en) * | 1996-05-23 | 1998-11-06 | Du Pont Merck Pharma | Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders |
| IL143105A0 (en) * | 1998-11-12 | 2002-04-21 | Neurocrine Biosciences Inc | Fused polycyclic heterocyclic compounds and pharmaceutical compositions containing the same |
| KR20010080990A (ko) | 1998-11-12 | 2001-08-25 | 추후기재 | Ｃｒｆ 수용체 길항제 및 그와 관련된 방법 |
| GB0117395D0 (en) | 2001-07-17 | 2001-09-05 | Glaxo Group Ltd | Chemical compounds |
-
2002
- 2002-04-30 AT AT02718405T patent/ATE320254T1/de not_active IP Right Cessation
- 2002-04-30 ES ES02718405T patent/ES2255610T3/es not_active Expired - Lifetime
- 2002-04-30 AR ARP020101598A patent/AR033296A1/es unknown
- 2002-04-30 PL PL02366854A patent/PL366854A1/xx not_active Application Discontinuation
- 2002-04-30 CA CA002446497A patent/CA2446497A1/en not_active Abandoned
- 2002-04-30 JP JP2002584918A patent/JP2004528342A/ja active Pending
- 2002-04-30 DE DE60209885T patent/DE60209885T2/de not_active Expired - Fee Related
- 2002-04-30 BR BR0209035-0A patent/BR0209035A/pt not_active IP Right Cessation
- 2002-04-30 US US10/476,441 patent/US7329667B2/en not_active Expired - Fee Related
- 2002-04-30 MX MXPA03009930A patent/MXPA03009930A/es active IP Right Grant
- 2002-04-30 HU HU0304035A patent/HUP0304035A2/hu unknown
- 2002-04-30 NZ NZ528364A patent/NZ528364A/en unknown
- 2002-04-30 IL IL15806302A patent/IL158063A0/xx unknown
- 2002-04-30 WO PCT/GB2002/001981 patent/WO2002087573A1/en not_active Ceased
- 2002-04-30 KR KR10-2003-7014159A patent/KR20040015205A/ko not_active Withdrawn
- 2002-04-30 AU AU2002249474A patent/AU2002249474B2/en not_active Ceased
- 2002-04-30 EP EP02718405A patent/EP1383498B1/en not_active Expired - Lifetime
- 2002-04-30 TW TW091108900A patent/TWI236908B/zh not_active IP Right Cessation
- 2002-04-30 CZ CZ20032945A patent/CZ20032945A3/cs unknown
- 2002-04-30 CN CNA028107454A patent/CN1512883A/zh active Pending
-
2003
- 2003-10-29 NO NO20034837A patent/NO20034837L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| DE60209885T2 (de) | 2006-08-10 |
| NZ528364A (en) | 2005-12-23 |
| WO2002087573A1 (en) | 2002-11-07 |
| TWI236908B (en) | 2005-08-01 |
| ATE320254T1 (de) | 2006-04-15 |
| MXPA03009930A (es) | 2004-01-29 |
| CA2446497A1 (en) | 2002-11-07 |
| AU2002249474B2 (en) | 2006-01-12 |
| JP2004528342A (ja) | 2004-09-16 |
| EP1383498B1 (en) | 2006-03-15 |
| IL158063A0 (en) | 2004-03-28 |
| AR033296A1 (es) | 2003-12-10 |
| DE60209885D1 (de) | 2006-05-11 |
| US20040235871A1 (en) | 2004-11-25 |
| KR20040015205A (ko) | 2004-02-18 |
| PL366854A1 (en) | 2005-02-07 |
| US7329667B2 (en) | 2008-02-12 |
| NO20034837L (no) | 2003-12-09 |
| CN1512883A (zh) | 2004-07-14 |
| NO20034837D0 (no) | 2003-10-29 |
| EP1383498A1 (en) | 2004-01-28 |
| CZ20032945A3 (cs) | 2004-02-18 |
| HUP0304035A2 (hu) | 2004-04-28 |
| ES2255610T3 (es) | 2006-07-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE 6A., 7A. E 8A. ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2060 DE 29/06/2010. |