BR9809648A - Derivados de piperazinil-benzil-tetrazol antiinflamatórios e intermediários dos mesmos - Google Patents
Derivados de piperazinil-benzil-tetrazol antiinflamatórios e intermediários dos mesmosInfo
- Publication number
- BR9809648A BR9809648A BR9809648-6A BR9809648A BR9809648A BR 9809648 A BR9809648 A BR 9809648A BR 9809648 A BR9809648 A BR 9809648A BR 9809648 A BR9809648 A BR 9809648A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- formula
- benzyl
- inflammatory
- disorders
- Prior art date
Links
- 230000003110 anti-inflammatory effect Effects 0.000 title abstract 2
- WEDPCJWFKWEVDS-UHFFFAOYSA-N 1-[phenyl(2h-tetrazol-5-yl)methyl]piperazine Chemical class C1CNCCN1C(C=1C=CC=CC=1)C1=NNN=N1 WEDPCJWFKWEVDS-UHFFFAOYSA-N 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- KJUGUADJHNHALS-UHFFFAOYSA-N 1H-tetrazole Substances C=1N=NNN=1 KJUGUADJHNHALS-UHFFFAOYSA-N 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 1
- 101100244562 Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM 14847 / LMG 12228 / 1C / PRS 101 / PAO1) oprD gene Proteins 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 108700023159 delta Opioid Receptors Proteins 0.000 abstract 1
- 102000048124 delta Opioid Receptors Human genes 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000004202 respiratory function Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 150000003536 tetrazoles Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- 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
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Surface Acoustic Wave Elements And Circuit Networks Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Patente de Invenção: <B>"DERIVADOS DE PIPERAZINIL-BENZIL-TETRAZOL ANTIINFLAMATóRIOS E INTERMEDIáRIOS DOS MESMOS"<D>. Tetrazóis e seus sais farmaceuticamente aceitáveis que são agonistas seletivos para o receptor de opióide delta, particularmente úteis no tratamento de doenças inflamatórias tais como artrite, psoríase, asma, doença do intestino inflamatório, distúrbios da função respiratória, distúrbios gastrintestinais tais como doença do intestino funcional e distúrbios Gl funcionais, da fórmula: em que R^ 1^ é H, alcanoíla C~ 2~-C~ 6~, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, alquinila C~ 2~-C~ 6~, cicloalquila C~ 3~-C~ 7~, (cicloalquil C~ 3~-C~ 7~)alquila C~ 1~-C~ 4~, (alcóxi C~ 1~-C~ 4~)alquila C~ 1~-C~ 4~, carboxi(alquila C~ 1~-C~ 4~), aril(alquila C~ 1~-C~ 4~) ou heteroaril(alquila C~ 1~-C~ 4~); R^ 2^ e R^ 3^ são cada um independentemente H ou alquila C~ 1~-C~ 4~; R^ 4^ é selecionado dentre (i) H, (ii) um grupo da fórmula R^ 6^-(CH~ 2~)~ m~-Z-(CH~ 2~)~ n~-, onde m é 0, 1, 2 ou 3, n é 1, 2 ou 3, Z é uma ligação direta ou O, e R^ 6^ é -CO~ 2~H ou -CO~ 2~(alquila C~ 1~-C~ 4~), e (iii) um grupo da fórmula onde R^ 7^ é H ou alquila C~ 1~-C~ 4~; e R^ 5^ é hidróxi, alcóxi C~ 1~-C~ 4~ ou -NHSO~ 2~(alquila C~ 1~-C~ 4~); com a condição de que quando Z é O, m é 1, 2 ou 3 e n é 2 ou 3.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9709972.5A GB9709972D0 (en) | 1997-05-19 | 1997-05-19 | Tetrazoles |
| PCT/EP1998/002277 WO1998052929A1 (en) | 1997-05-19 | 1998-04-17 | Anti-inflammatory piperazinyl-benzyl-tetrazole derivatives and intermediates thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9809648A true BR9809648A (pt) | 2000-07-11 |
Family
ID=10812431
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9809648-6A BR9809648A (pt) | 1997-05-19 | 1998-04-17 | Derivados de piperazinil-benzil-tetrazol antiinflamatórios e intermediários dos mesmos |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6514975B1 (pt) |
| EP (1) | EP0983251B1 (pt) |
| JP (1) | JP2000513024A (pt) |
| AR (1) | AR015679A1 (pt) |
| AT (1) | ATE269852T1 (pt) |
| AU (1) | AU7644998A (pt) |
| BR (1) | BR9809648A (pt) |
| CA (1) | CA2290501C (pt) |
| DE (1) | DE69824724T2 (pt) |
| DK (1) | DK0983251T3 (pt) |
| ES (1) | ES2221985T3 (pt) |
| GB (1) | GB9709972D0 (pt) |
| HR (1) | HRP980267A2 (pt) |
| MA (1) | MA26499A1 (pt) |
| PA (1) | PA8451601A1 (pt) |
| PT (1) | PT983251E (pt) |
| TN (1) | TNSN98066A1 (pt) |
| WO (1) | WO1998052929A1 (pt) |
| ZA (1) | ZA984158B (pt) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5985880A (en) | 1996-06-05 | 1999-11-16 | Delta Pharmaceuticals | Compositions and methods for reducing respiratory depression and attendant side effects of mu opioid compounds |
| GB9804734D0 (en) * | 1998-03-05 | 1998-04-29 | Pfizer Ltd | Compounds |
| US6054623A (en) * | 1998-12-18 | 2000-04-25 | Alliedsignal Inc. | Hydroxythiol grignard reaction synthesis |
| US6503905B1 (en) | 1998-12-29 | 2003-01-07 | Pfizer Inc | 3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives |
| US6455055B1 (en) | 1999-02-12 | 2002-09-24 | The Procter & Gamble Company | Cosmetic compositions |
| PE20010623A1 (es) * | 1999-10-05 | 2001-07-07 | Gruenenthal Chemie | Uso de (+)-tramadol y/o o-demetiltramadol para tratamiento de urgencia urinaria incrementada y/o incontinencia urinaria |
| AU2002227135B2 (en) | 2000-10-31 | 2008-01-03 | Rensselaer Polytechnic Institute | 8- substituted-2, 6-methano-3-benzazocines and 3-substituted morphinanes as opioid receptor binding agents |
| BR0213327A (pt) | 2001-10-15 | 2004-10-13 | Janssen Pharmaceutica Nv | Derivados de 4-fenil-4-[1h-imidazol-2-il]-piperidina substituìdos e sua aplicação como agonistas de delta opióides não-peptìdicos seletivos |
| US8575169B2 (en) | 2001-10-29 | 2013-11-05 | Versi Group, Llc | Method of treating sexual dysfunctions with delta opioid receptor agonist compounds |
| US7030124B2 (en) * | 2001-10-29 | 2006-04-18 | Ardent Pharmaceuticals, Inc. | Method of treating depression with delta receptor agonist compounds |
| JP4665379B2 (ja) * | 2002-06-28 | 2011-04-06 | Ｄｉｃ株式会社 | ヘリカルツイスティングパワーの増大方法、光学活性化合物、それを含有した液晶組成物及び液晶表示素子 |
| TW200504033A (en) * | 2002-10-23 | 2005-02-01 | Procter & Gamble | Melanocortin receptor ligands |
| US20090297611A1 (en) * | 2003-07-31 | 2009-12-03 | Robinson Cynthia B | Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a tyrosine kinase inhibitor, delta opioid receptor antagonist, neurokinin receptor antagonist, or vcam inhibitor for treatment of asthma or chronic obstructive pulmonary disease |
| US20050026879A1 (en) * | 2003-07-31 | 2005-02-03 | Robinson Cynthia B. | Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a tyrosine kinase inhibitor, delta opioid receptor antagonist, neurokinin receptor antagonist, or VCAM inhibitor for treatment of asthma or chronic obstructive pulmonary disease |
| US20080045610A1 (en) * | 2004-09-23 | 2008-02-21 | Alexander Michalow | Methods for regulating neurotransmitter systems by inducing counteradaptations |
| CA2580694A1 (en) * | 2004-09-23 | 2006-03-30 | Alexander Michalow | Methods for regulating neurotransmitter systems by inducing counteradaptations |
| TW200724144A (en) * | 2005-04-14 | 2007-07-01 | Ardent Pharmaceuticals Inc | Compositions of novel opioid compounds and method of use thereof |
| US7210814B2 (en) * | 2005-04-29 | 2007-05-01 | Ultradent Products, Inc. | Dental curing light with specially arranged LEDs |
| US20100029681A1 (en) * | 2006-05-26 | 2010-02-04 | Hassan Pajouhesh | Heterocyclic compounds as calcium channel blockers |
| NZ573129A (en) * | 2006-06-28 | 2011-06-30 | Amgen Inc | Piperazine acetic acid glycine transporter-1 inhibitors |
| US8573616B2 (en) | 2009-05-29 | 2013-11-05 | Hydema Produktion A/S | Suspension system with inclination stabilization |
| TR201908514T4 (tr) | 2009-12-04 | 2019-07-22 | Alkermes Pharma Ireland Ltd | İlaç doz aşimi tedavi̇si̇ i̇çi̇n morfi̇nan türevleri̇ |
| US8436175B2 (en) | 2010-03-22 | 2013-05-07 | Rensselaer Polytechnic Institute | Carboxamide bioisosteres of opiates |
| US8778960B2 (en) | 2010-08-23 | 2014-07-15 | Alkermes Pharma Ireland Limited | Methods for treating antipsychotic-induced weight gain |
| WO2012138888A1 (en) | 2011-04-05 | 2012-10-11 | Alkermes, Inc. | Process for the synthesis of quaternary amine compounds |
| WO2013003720A1 (en) | 2011-06-29 | 2013-01-03 | Alkermes, Inc. | Peripherally acting opioid compounds |
| US9211293B2 (en) | 2011-12-15 | 2015-12-15 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| LT3153171T (lt) | 2011-12-15 | 2018-12-10 | Alkermes Pharma Ireland Limited | Samidorfanas (alks 33) derinyje su buprenorfinu, skirtas depresinių sutrikimų gydymui |
| ES2770978T3 (es) | 2013-05-24 | 2020-07-06 | Alkermes Pharma Ireland Ltd | Análogos de morfanos y morfinanos y métodos de uso |
| EP3003311A2 (en) | 2013-05-24 | 2016-04-13 | Alkermes Pharma Ireland Limited | Methods for treating depressive symptoms |
| CN106588873B (zh) * | 2016-11-21 | 2019-11-12 | 云南省药物研究所 | 一种三芳基二甲基哌嗪乙二磺酸盐的多晶型物及其制备方法和应用 |
| EP4243768A1 (en) | 2020-11-12 | 2023-09-20 | Alkermes Pharma Ireland Limited | Immediate release multilayer tablet |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3453285A (en) * | 1967-11-29 | 1969-07-01 | Miles Lab | Tetrazolyl alkanoic acids |
| US5807858A (en) * | 1996-06-05 | 1998-09-15 | Delta Pharmaceutical, Inc. | Compositions and methods for reducing respiratory depression |
| GB9202238D0 (en) * | 1992-02-03 | 1992-03-18 | Wellcome Found | Compounds |
| EP0585500A1 (en) * | 1992-09-04 | 1994-03-09 | Merrell Dow Pharmaceuticals Inc. | Diaryl piperazineacetamides as antimuscarinic agents |
| CN1054850C (zh) * | 1993-07-30 | 2000-07-26 | 德尔塔药物公司 | 用于治疗的哌嗪化合物 |
| JPH07247274A (ja) * | 1994-03-10 | 1995-09-26 | Wakamoto Pharmaceut Co Ltd | ピバル酸 テトラゾリルフェニルエステル誘導体、それらを有効成分として含有するエラスターゼ阻害剤及び肺障害治療剤 |
| SE9504661D0 (sv) * | 1995-12-22 | 1995-12-22 | Astra Pharma Inc | New compounds |
| USH2007H1 (en) * | 1996-01-19 | 2001-12-04 | Fmc Corporation | Insecticidal N-heterocyclylalkyl-or N-[(polycyclyl)alkyl]-N′substituted piperazines |
-
1997
- 1997-05-19 GB GBGB9709972.5A patent/GB9709972D0/en active Pending
-
1998
- 1998-04-17 DK DK98924137T patent/DK0983251T3/da active
- 1998-04-17 BR BR9809648-6A patent/BR9809648A/pt not_active IP Right Cessation
- 1998-04-17 AU AU76449/98A patent/AU7644998A/en not_active Abandoned
- 1998-04-17 JP JP10549851A patent/JP2000513024A/ja not_active Ceased
- 1998-04-17 CA CA002290501A patent/CA2290501C/en not_active Expired - Fee Related
- 1998-04-17 PT PT98924137T patent/PT983251E/pt unknown
- 1998-04-17 AT AT98924137T patent/ATE269852T1/de not_active IP Right Cessation
- 1998-04-17 ES ES98924137T patent/ES2221985T3/es not_active Expired - Lifetime
- 1998-04-17 US US09/367,322 patent/US6514975B1/en not_active Expired - Fee Related
- 1998-04-17 DE DE69824724T patent/DE69824724T2/de not_active Expired - Fee Related
- 1998-04-17 EP EP98924137A patent/EP0983251B1/en not_active Expired - Lifetime
- 1998-04-17 WO PCT/EP1998/002277 patent/WO1998052929A1/en not_active Ceased
- 1998-05-15 PA PA19988451601A patent/PA8451601A1/es unknown
- 1998-05-15 AR ARP980102281A patent/AR015679A1/es unknown
- 1998-05-18 TN TNTNSN98066A patent/TNSN98066A1/fr unknown
- 1998-05-18 ZA ZA9804158A patent/ZA984158B/xx unknown
- 1998-05-18 MA MA25079A patent/MA26499A1/fr unknown
- 1998-05-19 HR HR9709972.5A patent/HRP980267A2/hr not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| WO1998052929A1 (en) | 1998-11-26 |
| EP0983251B1 (en) | 2004-06-23 |
| PT983251E (pt) | 2004-08-31 |
| CA2290501C (en) | 2003-07-08 |
| AR015679A1 (es) | 2001-05-16 |
| US6514975B1 (en) | 2003-02-04 |
| GB9709972D0 (en) | 1997-07-09 |
| MA26499A1 (fr) | 2004-12-20 |
| DE69824724T2 (de) | 2005-08-25 |
| DK0983251T3 (da) | 2004-09-27 |
| JP2000513024A (ja) | 2000-10-03 |
| ES2221985T3 (es) | 2005-01-16 |
| EP0983251A1 (en) | 2000-03-08 |
| DE69824724D1 (de) | 2004-07-29 |
| ATE269852T1 (de) | 2004-07-15 |
| CA2290501A1 (en) | 1998-11-26 |
| HRP980267A2 (en) | 1999-02-28 |
| PA8451601A1 (es) | 2000-05-24 |
| ZA984158B (en) | 1999-11-19 |
| TNSN98066A1 (fr) | 2005-03-15 |
| AU7644998A (en) | 1998-12-11 |
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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 A 9A ANUIDADE. |
|
| 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 1908 DE 31/07/2007. |