BR0016638A - Análogos de homopiperidilbenzimidazóis substituìdos como relaxantes fúndicos - Google Patents
Análogos de homopiperidilbenzimidazóis substituìdos como relaxantes fúndicosInfo
- Publication number
- BR0016638A BR0016638A BR0016638-3A BR0016638A BR0016638A BR 0016638 A BR0016638 A BR 0016638A BR 0016638 A BR0016638 A BR 0016638A BR 0016638 A BR0016638 A BR 0016638A
- Authority
- BR
- Brazil
- Prior art keywords
- aryl
- alkyl
- substituted
- optionally substituted
- hydrogen
- Prior art date
Links
- 239000002249 anxiolytic agent Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- -1 homopiperidinyl Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 abstract 2
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 2
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 abstract 1
- 241000233866 Fungi Species 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 150000001412 amines Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002950 deficient Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 230000001771 impaired effect Effects 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P1/06—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (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)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cosmetics (AREA)
Abstract
"ANáLOGOS DE HOMOPIPERIDILBENZIMIDAZóIS SUBSTITUìDOS COMO RELAXANTES FúNDICOS". A presente invenção refere-se a compostos com atividade de relaxamento fúndico de fórmula (I) suas pró-drogas, N-óxidos, sais de adição, aminas quaternárias e formas estereoquimicamente isoméricas em que o radical bivalente representa uma homopiperidinila saturada ou não-saturada tendo uma ligação dupla, e em que o referido radical bivalente é substituído com R^ 2^ sendo hidrogênio, hidróxi, C~ 1-4~alquila, ou C~ 1-4~alquilóxi; -a^ 1^=a^ 2^-a^ 3^=a^ 4^ representa um radical bivalente opcionalmente substituído; R^ 1^ é hidrogênio, C~ 1-6~alquila, arila^ 1^, C~ 1-6~alquila substituída com arila^ 1^, C~ 1-4~ alquiloxicarbonila, aril^ 1^carbonila, aril^ 1^C~ 1-6~alquilcarbonila, C~ 1-4~ alquilcarbonila, trifluorometila, trifluorometilcarbonila, C~ 1-6~alquilsulfonila, aril^ 1^sulfonila, metanossulfonila, benzenossulfonila, trifluorometanossulfonila ou dimetilsulfamoíla; X representa O, S ou NR^ 3^ em que R^ 3^ é hidrogênio, C~ 1-6~alquila, metanossulfonila, benzenossulfonila, trifluorometanossulfonila, dimetilsulfamoíla, C~ 1-4~alquila substituída com arila^ 2^ e opcionalmente com hidróxi, C~ 1-4~alquilcarbonilC~ 1-4~ alquila substituída com arila^ 2^; arila^ 1^ é fenila opcionalmente substituída, piridinila opcionalmente substituída, naftila, quinolinila ou 1,3-benzodioxolila; arila^ 2^ é fenila opcionalmente substituída. Processos para preparação dos referidos produtos, formulações compreendendo os referidos produtos e seu uso como medicamento são descritos, em particular para tratamento de sintomas dispépticos, síndrome de intestino irritável e outras condições relacionadas com relaxamento dificultado ou deficiente do fundo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99204441 | 1999-12-21 | ||
| PCT/EP2000/012858 WO2001046189A1 (en) | 1999-12-21 | 2000-12-14 | Substituted homopiperidinyl benzimidazole analogues as fundic relaxants |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR0016638A true BR0016638A (pt) | 2002-10-01 |
| BR0016638B1 BR0016638B1 (pt) | 2013-02-05 |
| BRPI0016638B8 BRPI0016638B8 (pt) | 2017-04-25 |
Family
ID=8241040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0016638A BRPI0016638B8 (pt) | 1999-12-21 | 2000-12-14 | compostos análogos de homopiperidilbenzimidazóis substituídos como relaxantes fúndicos, processo para preparar os mesmos, composição farmacêutica e processo para prepará-la. |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US7304052B2 (pt) |
| EP (1) | EP1250337B1 (pt) |
| JP (1) | JP4852210B2 (pt) |
| KR (1) | KR100715351B1 (pt) |
| CN (1) | CN100343251C (pt) |
| AT (1) | ATE416174T1 (pt) |
| AU (1) | AU781144B2 (pt) |
| BG (1) | BG65784B1 (pt) |
| BR (1) | BRPI0016638B8 (pt) |
| CA (1) | CA2393158C (pt) |
| CY (1) | CY1108844T1 (pt) |
| CZ (1) | CZ299803B6 (pt) |
| DE (1) | DE60041001D1 (pt) |
| DK (1) | DK1250337T3 (pt) |
| EA (1) | EA005851B1 (pt) |
| EE (1) | EE05182B1 (pt) |
| ES (1) | ES2317856T3 (pt) |
| HK (1) | HK1053109B (pt) |
| HR (1) | HRP20020518B1 (pt) |
| HU (1) | HU229929B1 (pt) |
| IL (2) | IL150310A0 (pt) |
| MX (1) | MXPA02006346A (pt) |
| MY (1) | MY127758A (pt) |
| NO (1) | NO322362B1 (pt) |
| NZ (1) | NZ518816A (pt) |
| PL (1) | PL199678B1 (pt) |
| PT (1) | PT1250337E (pt) |
| SI (1) | SI1250337T1 (pt) |
| SK (1) | SK287113B6 (pt) |
| TW (1) | TWI225488B (pt) |
| UA (1) | UA73963C2 (pt) |
| WO (1) | WO2001046189A1 (pt) |
| ZA (1) | ZA200204983B (pt) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI225488B (en) | 1999-12-21 | 2004-12-21 | Janssen Pharmaceutica Nv | Derivatives of homopiperidinyl substituted benzimidazole analogues |
| JO2352B1 (en) * | 2000-06-22 | 2006-12-12 | جانسين فارماسيوتيكا ان. في | Compounds for the treatment of non-adaptation of the bottom of the uterus |
| CA2473236A1 (en) | 2002-01-10 | 2003-07-24 | Neurogen Corporation | Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1h-benzoimidazole analogues |
| CA2555409A1 (en) * | 2004-02-19 | 2005-09-01 | Banyu Pharmaceutical Co., Ltd. | Novel sulfone amide derivative |
| EP2121683B1 (en) * | 2007-01-25 | 2011-08-31 | Janssen Pharmaceutica, N.V. | 2-piperazin-1-yl-3h-imidazo[4,5-b]pyridine derivatives |
| ES2700542T3 (es) | 2010-06-24 | 2019-02-18 | Gilead Sciences Inc | Composición farmacéutica que comprende un derivado de pirazolo[1,5-A]pirimidina como un agente antiviral |
| WO2012070069A2 (en) * | 2010-11-24 | 2012-05-31 | Sequent Scientific Limited | A process for preparation of albendazole |
| JP2014159375A (ja) * | 2011-06-15 | 2014-09-04 | Takeda Chem Ind Ltd | アゼパン化合物 |
| JP6122868B2 (ja) | 2011-12-22 | 2017-04-26 | ギリアード サイエンシーズ， インコーポレイテッド | 抗ウイルス剤としてのピラゾロ［１，５−ａ］ピリミジン |
| IN2014DN09173A (pt) | 2012-04-17 | 2015-07-10 | Gilead Sciences Inc | |
| WO2015091584A1 (en) * | 2013-12-18 | 2015-06-25 | F. Hoffmann-La Roche Ag | Thiazolopyridine compounds, compositions and their use as tyk2 kinase inhibitors |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2060197C3 (de) | 1970-12-08 | 1979-02-22 | Bayer Ag, 5090 Leverkusen | Verfahren zur Herstellung von 2-Aminobenzothiazol und dessen N-Alkylsubstitutionsprodukten |
| US4093726A (en) * | 1976-12-02 | 1978-06-06 | Abbott Laboratories | N-(2-benzimidazolyl)-piperazines |
| ES482789A0 (es) * | 1978-08-25 | 1980-12-01 | Thomae Gmbh Dr K | Procedimiento para la preparacion de nuevos bencimidazoles sustituidos en posicion 5 o 6 con un anillo de piridazinona |
| JPS5879983A (ja) * | 1981-11-06 | 1983-05-13 | Kanebo Ltd | 新規なベンズイミダゾ−ル誘導体、その製造法およびその医薬組成物 |
| FR2528526A1 (fr) * | 1982-06-09 | 1983-12-16 | Sfr Sa Robinetterie | Butee se fixant dans un alesage d'un dispositif |
| DE3224512A1 (de) * | 1982-07-01 | 1984-01-05 | Dr. Karl Thomae Gmbh, 7950 Biberach | Neue imidazolderivate, ihre herstellung und diese verbindungen enthaltende arzneimittel |
| PH23995A (en) * | 1984-01-09 | 1990-02-09 | Janssen Pharmaceutica Nv | 4((bicycle heterocyclyl)-methyl and hetero)piperidines |
| DE3634066A1 (de) * | 1986-10-07 | 1988-04-21 | Boehringer Mannheim Gmbh | Neue 5-alkylbenzimidazole, verfahren zu ihrer herstellung sowie arzneimittel |
| JPH0260197A (ja) * | 1988-08-26 | 1990-02-28 | Nec Corp | パッケージ構造 |
| FR2674856B1 (fr) * | 1991-04-05 | 1993-07-30 | Esteve Labor Dr | Nouveaux antihistaminiques non sedatifs, derives de benzimidazole, leur procede de preparation et leur utilisation en tant que medicaments. |
| IL101851A (en) * | 1991-06-13 | 1996-05-14 | Janssen Pharmaceutica Nv | History 01 -) 4 - Pipridinyl - and Pipridinylidene (- Imidazo] A-1,2 [Pirolo, Thiano or Purano (] 3,2 [Azpin, their preparation and pharmaceutical preparations containing them and composition |
| DE4237656A1 (de) * | 1992-06-13 | 1993-12-16 | Merck Patent Gmbh | Benzimidazolderivate |
| KR0144793B1 (ko) * | 1992-07-08 | 1998-07-15 | 제임스 클리프튼 보올딩 | 돼지에서 위궤양을 완화시키기 위한 벤즈이미다졸 |
| ES2048109B1 (es) * | 1992-07-20 | 1994-12-16 | Espanola Prod Quimicos | Procedimiento de preparacion de nuevos derivados piperidicos del bencimidazol. |
| WO1995032960A1 (fr) * | 1994-05-31 | 1995-12-07 | Mitsui Toatsu Chemicals, Incorporated | Derive de benzimidazol |
| FR2766822B1 (fr) * | 1997-07-30 | 2001-02-23 | Adir | Nouveaux derives de benzimidazole, de benzoxazole et de benzothiazole, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US6150379A (en) * | 1997-11-26 | 2000-11-21 | Axys Pharmaceuticals, Inc. | Compounds and compositions as anticoagulants |
| TWI225488B (en) | 1999-12-21 | 2004-12-21 | Janssen Pharmaceutica Nv | Derivatives of homopiperidinyl substituted benzimidazole analogues |
-
2000
- 2000-12-11 TW TW089126315A patent/TWI225488B/zh not_active IP Right Cessation
- 2000-12-14 CN CNB008174458A patent/CN100343251C/zh not_active Expired - Fee Related
- 2000-12-14 EE EEP200200326A patent/EE05182B1/xx not_active IP Right Cessation
- 2000-12-14 WO PCT/EP2000/012858 patent/WO2001046189A1/en active IP Right Grant
- 2000-12-14 SK SK854-2002A patent/SK287113B6/sk not_active IP Right Cessation
- 2000-12-14 ES ES00985180T patent/ES2317856T3/es not_active Expired - Lifetime
- 2000-12-14 SI SI200031019T patent/SI1250337T1/sl unknown
- 2000-12-14 CZ CZ20022055A patent/CZ299803B6/cs not_active IP Right Cessation
- 2000-12-14 NZ NZ518816A patent/NZ518816A/xx not_active IP Right Cessation
- 2000-12-14 KR KR1020027006004A patent/KR100715351B1/ko not_active IP Right Cessation
- 2000-12-14 EP EP00985180A patent/EP1250337B1/en not_active Expired - Lifetime
- 2000-12-14 BR BRPI0016638A patent/BRPI0016638B8/pt not_active IP Right Cessation
- 2000-12-14 IL IL15031000A patent/IL150310A0/xx unknown
- 2000-12-14 PL PL355442A patent/PL199678B1/pl unknown
- 2000-12-14 MX MXPA02006346A patent/MXPA02006346A/es active IP Right Grant
- 2000-12-14 JP JP2001547099A patent/JP4852210B2/ja not_active Expired - Fee Related
- 2000-12-14 DE DE60041001T patent/DE60041001D1/de not_active Expired - Lifetime
- 2000-12-14 UA UA2002065092A patent/UA73963C2/uk unknown
- 2000-12-14 US US10/169,011 patent/US7304052B2/en not_active Expired - Fee Related
- 2000-12-14 AT AT00985180T patent/ATE416174T1/de active
- 2000-12-14 AU AU21673/01A patent/AU781144B2/en not_active Ceased
- 2000-12-14 CA CA2393158A patent/CA2393158C/en not_active Expired - Fee Related
- 2000-12-14 EA EA200200700A patent/EA005851B1/ru not_active IP Right Cessation
- 2000-12-14 DK DK00985180T patent/DK1250337T3/da active
- 2000-12-14 HU HU0203847A patent/HU229929B1/hu unknown
- 2000-12-14 PT PT00985180T patent/PT1250337E/pt unknown
- 2000-12-20 MY MYPI20006015A patent/MY127758A/en unknown
-
2002
- 2002-05-29 BG BG106749A patent/BG65784B1/bg unknown
- 2002-06-13 HR HR20020518A patent/HRP20020518B1/xx not_active IP Right Cessation
- 2002-06-19 IL IL150310A patent/IL150310A/en not_active IP Right Cessation
- 2002-06-20 NO NO20022977A patent/NO322362B1/no not_active IP Right Cessation
- 2002-06-20 ZA ZA200204983A patent/ZA200204983B/en unknown
-
2003
- 2003-07-23 HK HK03105325.2A patent/HK1053109B/zh not_active IP Right Cessation
-
2009
- 2009-03-03 CY CY20091100243T patent/CY1108844T1/el unknown
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