BR0111062A - Derivados de 1,4-diazepan-2,5-diona e seu uso como antagonistas receptores de nk-1 - Google Patents
Derivados de 1,4-diazepan-2,5-diona e seu uso como antagonistas receptores de nk-1Info
- Publication number
- BR0111062A BR0111062A BR0111062-4A BR0111062A BR0111062A BR 0111062 A BR0111062 A BR 0111062A BR 0111062 A BR0111062 A BR 0111062A BR 0111062 A BR0111062 A BR 0111062A
- Authority
- BR
- Brazil
- Prior art keywords
- lower alkyl
- heteroaryl
- diazepan
- halogen
- hydrogen
- Prior art date
Links
- 102000002002 Neurokinin-1 Receptors Human genes 0.000 title abstract 3
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 title abstract 3
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- XMOKZLVOWBOPCO-UHFFFAOYSA-N 1,4-diazepane-2,5-dione Chemical class O=C1CCNC(=O)CN1 XMOKZLVOWBOPCO-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 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
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
"DERIVADOS DE 1,4-DIAZEPAN-2,5-DIONA E SEU USO COMO ANTAGONISTAS RECEPTORES DE NK-1". A invenção refere-se a compostos da fórmula, geral (I) em que R^ 1^, R^ 2^ são independentemente um do outro arila ou heteroarila, em que o grupo heteroarila contém um ou dois heteroátomos, selecionados de N, O ou S, e em que os grupos arila ou heteroarila são opcionalmente substituídos por 1 a 3 substituintes, que são independentemente um do outro halogênio, CF~ 3~ alcóxi inferior ou alquila inferior; R^ 3^ é hidrogênio, alquila inferior, -(CH~ 2~)~ n~N(R)~ 2~, -(CH~ 2~)~ n~-heteroarila ou é um heterociclo -(CH~ 2~)~ n~-não aromático, cujos heteroclos são opcionalmente substituídos por halogênio, CF~ 3~ alcóxi inferior ou alquila inferior; R^ 4^ é =O, =N(CH~ 2~)~ n~CH~ 3~ ou =N(CH~ 2~)~ n~N(R)~ 2~; R^ 3^ e R^ 4^ podem ser juntamente com os átomos N e C aos quais eles são ligados o grupo -CR^ 5^=N-N=; R^ 5^ é hidrogênio, -(CH~ 2~)~ n~N(R)~ 2~, -(CH ~2~)~ n~-heteroarila ou é um heterociclo -(CH~ 2~)~ n~-não aromático, cujos heterociclos são opcionalmente substituídos por halogênio, CF ~3~, alcóxi inferior ou alquila inferior; R é hidrogênio ou alquila inferior; n é 0, 1, 2 ou 3; e a sais de adição de ácido farmaceuticamente aceitáveis e suas formas enancioméricas. Os compostos são úteis no tratamento de doenças, relacionadas ao receptor de NK-1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00111249 | 2000-05-25 | ||
| PCT/EP2001/005723 WO2001090083A1 (en) | 2000-05-25 | 2001-05-18 | 1,4-diazepan-2,5-dione derivatives and their use as nk-1 receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0111062A true BR0111062A (pt) | 2003-06-10 |
Family
ID=8168838
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0111062-4A BR0111062A (pt) | 2000-05-25 | 2001-05-18 | Derivados de 1,4-diazepan-2,5-diona e seu uso como antagonistas receptores de nk-1 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6452001B2 (pt) |
| EP (1) | EP1296961B1 (pt) |
| JP (1) | JP4060596B2 (pt) |
| KR (1) | KR100526696B1 (pt) |
| CN (1) | CN1178923C (pt) |
| AR (1) | AR028607A1 (pt) |
| AT (1) | ATE353881T1 (pt) |
| AU (2) | AU2001281778B2 (pt) |
| BR (1) | BR0111062A (pt) |
| CA (1) | CA2409842C (pt) |
| DE (1) | DE60126614T2 (pt) |
| DK (1) | DK1296961T3 (pt) |
| ES (1) | ES2280392T3 (pt) |
| MX (1) | MXPA02011464A (pt) |
| PE (1) | PE20011266A1 (pt) |
| PT (1) | PT1296961E (pt) |
| WO (1) | WO2001090083A1 (pt) |
| ZA (1) | ZA200208940B (pt) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ560232A (en) | 2005-02-25 | 2010-11-26 | Hoffmann La Roche | Tablets with improved drug substance dispersibility |
| US20080033167A1 (en) | 2005-12-29 | 2008-02-07 | Gilles Guichard | Compositions and methods for synthesizing heterocyclic therapeutic compounds |
| ATE477021T1 (de) * | 2005-12-29 | 2010-08-15 | Immupharma France Sa | 1,3,5-triazepin-dionen zur behandlung von malaria |
| AU2006331357B2 (en) * | 2005-12-29 | 2012-05-17 | Immupharma France Sa | Compositions and methods for synthesizing novel heterocyclic therapeutics |
| CN101395143A (zh) * | 2005-12-29 | 2009-03-25 | 安姆弗拉玛法国股份公司 | 用于治疗疟疾或aids的氮杂杂环化合物 |
| CN101405276A (zh) * | 2005-12-29 | 2009-04-08 | 安姆弗拉玛法国股份公司 | 用于抑制磷脂酶a2的组合物和方法 |
| RU2008150752A (ru) * | 2006-05-26 | 2010-07-10 | Новартис АГ (CH) | Ингибиторы альдостеронсинтазы и/или 11-гидроксилазы |
| JP2010516731A (ja) | 2007-01-24 | 2010-05-20 | グラクソ グループ リミテッド | ２−メトキシ−５−（５−トリフルオロメチル−テトラゾール−１−イル）−ベンジル］−（２ｓ−フェニル−ピペリジン−３ｓ−イル）−アミンを含む医薬組成物 |
| KR101044833B1 (ko) * | 2010-02-10 | 2011-06-28 | (주)혜성나노텍 | 무차광 온실 보온커텐 종형 개폐장치 |
| EP2610252A4 (en) | 2010-08-26 | 2013-09-04 | Kowa Co | NOVEL PROCESS FOR THE PRODUCTION OF ISOQUINOLINE DERIVATIVES AND THEIR SALTS |
| RU2014102107A (ru) | 2011-06-24 | 2015-08-10 | Констракшн Рисёрч Энд Текнолоджи Гмбх | Цементирующая композиция и присадка |
| CN108358893A (zh) * | 2018-02-10 | 2018-08-03 | 安徽唯诗杨信息科技有限公司 | 一种一锅法合成四氢化苯并-[1,4]-二氮杂环庚烷衍生物的方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4022765A (en) | 1975-01-06 | 1977-05-10 | E. R. Squibb & Sons, Inc. | Triazolo[4,3-d][1,4]benzodiazepine-6-ones |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| DE69434063D1 (de) | 1993-12-29 | 2004-11-11 | Merck Sharp & Dohme | Substituierte Morpholinderivate und ihre Verwendung als therapeutische Mittel |
| IL112778A0 (en) | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
| US5719156A (en) | 1995-05-02 | 1998-02-17 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5972938A (en) | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
-
2001
- 2001-05-14 US US09/854,885 patent/US6452001B2/en not_active Expired - Fee Related
- 2001-05-18 CA CA002409842A patent/CA2409842C/en not_active Expired - Fee Related
- 2001-05-18 AU AU2001281778A patent/AU2001281778B2/en not_active Ceased
- 2001-05-18 BR BR0111062-4A patent/BR0111062A/pt not_active Application Discontinuation
- 2001-05-18 EP EP01960225A patent/EP1296961B1/en not_active Expired - Lifetime
- 2001-05-18 CN CNB018099335A patent/CN1178923C/zh not_active Expired - Fee Related
- 2001-05-18 AU AU8177801A patent/AU8177801A/xx active Pending
- 2001-05-18 ES ES01960225T patent/ES2280392T3/es not_active Expired - Lifetime
- 2001-05-18 AT AT01960225T patent/ATE353881T1/de not_active IP Right Cessation
- 2001-05-18 JP JP2001586272A patent/JP4060596B2/ja not_active Expired - Fee Related
- 2001-05-18 PT PT01960225T patent/PT1296961E/pt unknown
- 2001-05-18 DK DK01960225T patent/DK1296961T3/da active
- 2001-05-18 WO PCT/EP2001/005723 patent/WO2001090083A1/en not_active Ceased
- 2001-05-18 KR KR10-2002-7015837A patent/KR100526696B1/ko not_active Expired - Fee Related
- 2001-05-18 DE DE60126614T patent/DE60126614T2/de not_active Expired - Lifetime
- 2001-05-18 MX MXPA02011464A patent/MXPA02011464A/es active IP Right Grant
- 2001-05-21 PE PE2001000458A patent/PE20011266A1/es not_active Application Discontinuation
- 2001-05-23 AR ARP010102436A patent/AR028607A1/es unknown
-
2002
- 2002-11-04 ZA ZA200208940A patent/ZA200208940B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20030003759A (ko) | 2003-01-10 |
| ES2280392T3 (es) | 2007-09-16 |
| DK1296961T3 (da) | 2007-06-04 |
| CN1430611A (zh) | 2003-07-16 |
| JP4060596B2 (ja) | 2008-03-12 |
| DE60126614D1 (de) | 2007-03-29 |
| EP1296961B1 (en) | 2007-02-14 |
| PE20011266A1 (es) | 2001-12-14 |
| JP2003534332A (ja) | 2003-11-18 |
| ATE353881T1 (de) | 2007-03-15 |
| CA2409842C (en) | 2008-07-29 |
| AR028607A1 (es) | 2003-05-14 |
| KR100526696B1 (ko) | 2005-11-08 |
| AU8177801A (en) | 2001-12-03 |
| CN1178923C (zh) | 2004-12-08 |
| WO2001090083A1 (en) | 2001-11-29 |
| CA2409842A1 (en) | 2001-11-29 |
| PT1296961E (pt) | 2007-05-31 |
| US6452001B2 (en) | 2002-09-17 |
| DE60126614T2 (de) | 2007-11-22 |
| ZA200208940B (en) | 2004-02-04 |
| MXPA02011464A (es) | 2003-04-25 |
| US20020010174A1 (en) | 2002-01-24 |
| AU2001281778B2 (en) | 2005-06-02 |
| EP1296961A1 (en) | 2003-04-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B11B | Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements |