BR0213186A - 4-(2-furoil)aminopiperidinas, intermediários na sìntese dos mesmos, processo para produzir os mesmos e uso medicinal dos mesmos - Google Patents
4-(2-furoil)aminopiperidinas, intermediários na sìntese dos mesmos, processo para produzir os mesmos e uso medicinal dos mesmosInfo
- Publication number
- BR0213186A BR0213186A BR0213186-2A BR0213186A BR0213186A BR 0213186 A BR0213186 A BR 0213186A BR 0213186 A BR0213186 A BR 0213186A BR 0213186 A BR0213186 A BR 0213186A
- Authority
- BR
- Brazil
- Prior art keywords
- group
- chem
- furoyl
- formula
- aminopiperidines
- Prior art date
Links
- HZOLDANSZVXETR-UHFFFAOYSA-N (1-aminopiperidin-4-yl)-(furan-2-yl)methanone Chemical class C1CN(N)CCC1C(=O)C1=CC=CO1 HZOLDANSZVXETR-UHFFFAOYSA-N 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 206010010774 Constipation Diseases 0.000 abstract 2
- 208000003251 Pruritus Diseases 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 206010021333 Ileus paralytic Diseases 0.000 abstract 1
- 201000005081 Intestinal Pseudo-Obstruction Diseases 0.000 abstract 1
- 206010028813 Nausea Diseases 0.000 abstract 1
- 206010054048 Postoperative ileus Diseases 0.000 abstract 1
- 206010047700 Vomiting Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 230000003042 antagnostic effect Effects 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 102000051367 mu Opioid Receptors Human genes 0.000 abstract 1
- OFIYCVSDCXIQFF-UHFFFAOYSA-N n-piperidin-4-ylfuran-2-carboxamide Chemical class C=1C=COC=1C(=O)NC1CCNCC1 OFIYCVSDCXIQFF-UHFFFAOYSA-N 0.000 abstract 1
- 230000008693 nausea Effects 0.000 abstract 1
- 201000007620 paralytic ileus Diseases 0.000 abstract 1
- 108020001612 μ-opioid receptors Proteins 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- 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
-
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- C07D211/58—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
"4-(2-FUROIL)AMINOPIPERIDINAS, INTERMEDIáRIOS NA SìNTESE DOS MESMOS, PROCESSO PARA PRODUZIR OS MESMOS E USO MEDICINAL DOS MESMOS". A invenção refere-se a novas 4-(2-furoil)aminopiperidinas representadas pela fórmula geral (I), seus intermediários sintéticos, processos para sua preparação e medicamentos contendo-as. Na fórmula acima, X é CH ou N e Y é um grupo seguinte fórmula geral (II), fórmula (II-a) ou fórmula (III): nas quais: a, b e c são cada qual um número inteiro de 0 a 6; Z é CH~ 2~ ou NH; W é O ou S; T é O ou N-R^ 15^ onde R^ 15^ é H, um grupo C~ 1~-C~ 6~ alquila, um grupo benzila ou um grupo fenetila; e R^ 1^ é H, um grupo C1-C6 alcoxicarbonila, um grupo benzilóxi-carbonila ou similares. Os derivados de 4-(2-furoil)aminopiperidina de acordo com esta invenção possui atividade antagonística <109> opióide e são úteis para o tratamento ou prevenção de efeitos colaterais que são causados por agonista de receptores <109> e que são selecionados de constipação, náusea/êmese ou sarna ou para o tratamento ou prevenção de constipação idiopática, íleo pós-operatório, íleo paralítico, síndrome do intestino irritável ou prurido crónico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001311828 | 2001-10-09 | ||
| PCT/JP2002/010449 WO2003035645A1 (fr) | 2001-10-09 | 2002-10-08 | Nouvelles 4-(2-furoyl)aminopiperidines, intermediaires utilises dans la synthese de ces dernieres, leur procede de production et leur utilisation medicale |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0213186A true BR0213186A (pt) | 2004-08-10 |
Family
ID=19130581
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0213186-2A BR0213186A (pt) | 2001-10-09 | 2002-10-08 | 4-(2-furoil)aminopiperidinas, intermediários na sìntese dos mesmos, processo para produzir os mesmos e uso medicinal dos mesmos |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US7375115B2 (pt) |
| EP (1) | EP1443046B1 (pt) |
| JP (1) | JP4009251B2 (pt) |
| KR (1) | KR100938369B1 (pt) |
| CN (1) | CN1326853C (pt) |
| AT (1) | ATE417845T1 (pt) |
| BR (1) | BR0213186A (pt) |
| CA (1) | CA2468529C (pt) |
| DE (1) | DE60230437D1 (pt) |
| DK (1) | DK1443046T3 (pt) |
| ES (1) | ES2319879T3 (pt) |
| MX (1) | MXPA04003330A (pt) |
| PT (1) | PT1443046E (pt) |
| WO (1) | WO2003035645A1 (pt) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004099194A1 (ja) * | 2003-05-08 | 2004-11-18 | Kyorin Pharmaceutical Co. Ltd. | 掻痒治療薬として有用な4-(2-フロイル)アミノピペリジン類 |
| JP2004352714A (ja) * | 2003-05-08 | 2004-12-16 | Kyorin Pharmaceut Co Ltd | 新規な4−(2−フロイル)アミノピペリジン誘導体 |
| EP1622613A4 (en) * | 2003-05-14 | 2008-04-02 | Cytokinetics Inc | COMPOUNDS, COMPOSITIONS AND METHODS |
| JO2769B1 (en) | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
| AR057959A1 (es) * | 2005-12-01 | 2007-12-26 | Elan Pharm Inc | 5-pirazolpiperidinas-(sustituidas) |
| MY145633A (en) | 2006-03-01 | 2012-03-15 | Theravance Inc | 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| JP4898287B2 (ja) * | 2006-05-17 | 2012-03-14 | 杏林製薬株式会社 | [1−[2−[4−[n−(5−メチルピリジン−2−イル)−2−フランカルボキサミド]ピペリジン−1−イル]エチル]シクロヘキシル]アセトヒドロキサム酸の製造方法 |
| JO2642B1 (en) | 2006-12-08 | 2012-06-17 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| MX2009011416A (es) | 2007-04-23 | 2009-11-05 | Janssen Pharmaceutica Nv | Tia(di)azoles como antagonistas del receptor de dopamina 2 de disociacion rapida. |
| RS52518B (sr) | 2007-04-23 | 2013-04-30 | Janssen Pharmaceutica N.V. | Derivati 4-alkoksipiridazina kao brzo disocirajući dopamin 2 receptorski antagonisti |
| US20100137368A1 (en) * | 2007-04-23 | 2010-06-03 | Janssen Pharmaceutica N.V. | Pyridine derivatives as fast dissociating dopamine 2 receptor antagonists |
| CA2729313C (en) | 2008-07-03 | 2016-08-30 | Janssen Pharmaceutica Nv | Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists |
| ES2622161T3 (es) | 2008-07-31 | 2017-07-05 | Janssen Pharmaceutica, N.V. | Piridinas sustituidas con piperazin-1-il-trifluorometilo como antagonistas del receptor de la dopamina 2 de disociación rápida |
| WO2010135731A1 (en) * | 2009-05-22 | 2010-11-25 | Kaufman Herbert E | Preparations and methods for ameliorating or reducing presbyopia |
| US8299079B2 (en) | 2009-05-22 | 2012-10-30 | Kaufman Herbert E | Preparations and methods for ameliorating or reducing presbyopia |
| US20120142932A1 (en) * | 2009-09-08 | 2012-06-07 | Koji Kawamura | Method for manufacturing 4-(5-methylpyridin-2-ylamino)piperidine-1-carboxylic acid derivative |
| JP2013537240A (ja) * | 2010-09-20 | 2013-09-30 | カリウス セラピューティクス エスエー | 糖尿病および脂質異常症の処置のための方法および組成物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59112984A (ja) * | 1982-12-21 | 1984-06-29 | Shionogi & Co Ltd | 1,4−ベンゾジアゼピン誘導体 |
| US4584303A (en) * | 1984-04-09 | 1986-04-22 | The Boc Group, Inc. | N-aryl-N-(4-piperidinyl)amides and pharmaceutical compositions and method employing such compounds |
| US4912109A (en) * | 1987-02-02 | 1990-03-27 | Boc, Inc. | N-heterocyclic-N-(4-piperidinyl) amides and pharmaceutical compositions and methods employing such compounds |
| US4791112A (en) * | 1987-02-02 | 1988-12-13 | The Boc Group, Inc. | N-heterocyclic-N-(4-piperidyl)amides and pharmaceutical compositions and methods employing such compounds |
| JPH09501404A (ja) | 1993-05-26 | 1997-02-10 | スミスクライン・ビーチャム・ラボラトワール・ファルマソーティク | 新規化合物 |
-
2002
- 2002-10-08 EP EP02772984A patent/EP1443046B1/en not_active Expired - Lifetime
- 2002-10-08 BR BR0213186-2A patent/BR0213186A/pt not_active IP Right Cessation
- 2002-10-08 KR KR1020047005180A patent/KR100938369B1/ko not_active Expired - Fee Related
- 2002-10-08 CA CA2468529A patent/CA2468529C/en not_active Expired - Fee Related
- 2002-10-08 MX MXPA04003330A patent/MXPA04003330A/es active IP Right Grant
- 2002-10-08 US US10/492,065 patent/US7375115B2/en not_active Expired - Fee Related
- 2002-10-08 CN CNB028241568A patent/CN1326853C/zh not_active Expired - Fee Related
- 2002-10-08 WO PCT/JP2002/010449 patent/WO2003035645A1/ja not_active Ceased
- 2002-10-08 ES ES02772984T patent/ES2319879T3/es not_active Expired - Lifetime
- 2002-10-08 DK DK02772984T patent/DK1443046T3/da active
- 2002-10-08 PT PT02772984T patent/PT1443046E/pt unknown
- 2002-10-08 DE DE60230437T patent/DE60230437D1/de not_active Expired - Lifetime
- 2002-10-08 AT AT02772984T patent/ATE417845T1/de active
- 2002-10-08 JP JP2003538161A patent/JP4009251B2/ja not_active Expired - Fee Related
-
2008
- 2008-03-20 US US12/077,687 patent/US20080194826A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2468529C (en) | 2011-03-01 |
| ATE417845T1 (de) | 2009-01-15 |
| CN1582286A (zh) | 2005-02-16 |
| EP1443046A4 (en) | 2005-11-16 |
| DE60230437D1 (de) | 2009-01-29 |
| ES2319879T3 (es) | 2009-05-14 |
| KR20040039495A (ko) | 2004-05-10 |
| CA2468529A1 (en) | 2003-05-01 |
| EP1443046B1 (en) | 2008-12-17 |
| DK1443046T3 (da) | 2009-04-14 |
| JPWO2003035645A1 (ja) | 2005-02-10 |
| MXPA04003330A (es) | 2004-07-08 |
| WO2003035645A1 (fr) | 2003-05-01 |
| JP4009251B2 (ja) | 2007-11-14 |
| US20080194826A1 (en) | 2008-08-14 |
| PT1443046E (pt) | 2009-02-26 |
| US20050085508A1 (en) | 2005-04-21 |
| CN1326853C (zh) | 2007-07-18 |
| KR100938369B1 (ko) | 2010-01-22 |
| US7375115B2 (en) | 2008-05-20 |
| EP1443046A1 (en) | 2004-08-04 |
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