ZA200409053B - (S)-4-Amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofuryl-carbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamin de, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor. - Google Patents
(S)-4-Amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofuryl-carbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamin de, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor. Download PDFInfo
- Publication number
- ZA200409053B ZA200409053B ZA200409035A ZA200409053A ZA200409053B ZA 200409053 B ZA200409053 B ZA 200409053B ZA 200409035 A ZA200409035 A ZA 200409035A ZA 200409053 A ZA200409053 A ZA 200409053A ZA 200409053 B ZA200409053 B ZA 200409053B
- Authority
- ZA
- South Africa
- Prior art keywords
- compound
- amino
- pharmaceutically acceptable
- addition salt
- piperidinylmethyl
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- ZUSSTQCWRDLYJA-UHFFFAOYSA-N n-hydroxy-5-norbornene-2,3-dicarboximide Chemical compound C1=CC2CC1C1C2C(=O)N(O)C1=O ZUSSTQCWRDLYJA-UHFFFAOYSA-N 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 210000001577 neostriatum Anatomy 0.000 description 1
- 208000015238 neurotic disease Diseases 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- BOTREHHXSQGWTR-UHFFFAOYSA-N oxolane-3-carboxylic acid Chemical compound OC(=O)C1CCOC1 BOTREHHXSQGWTR-UHFFFAOYSA-N 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 229960003540 oxyquinoline Drugs 0.000 description 1
- 201000007620 paralytic ileus Diseases 0.000 description 1
- 229960001412 pentobarbital Drugs 0.000 description 1
- 208000000689 peptic esophagitis Diseases 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- NMHMNPHRMNGLLB-UHFFFAOYSA-N phloretic acid Chemical compound OC(=O)CCC1=CC=C(O)C=C1 NMHMNPHRMNGLLB-UHFFFAOYSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
- 229950008882 polysorbate Drugs 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229940068984 polyvinyl alcohol Drugs 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 201000007847 postgastrectomy syndrome Diseases 0.000 description 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 description 1
- 235000015497 potassium bicarbonate Nutrition 0.000 description 1
- 239000011736 potassium bicarbonate Substances 0.000 description 1
- 229940086066 potassium hydrogencarbonate Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960004063 propylene glycol Drugs 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
- 230000001012 protector Effects 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000001226 reprecipitation Methods 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical class O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 210000003568 synaptosome Anatomy 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- KAQZZWSBZVORPS-UHFFFAOYSA-N tert-butyl n-[1-(piperidin-4-ylmethyl)piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OC(C)(C)C)CCN1CC1CCNCC1 KAQZZWSBZVORPS-UHFFFAOYSA-N 0.000 description 1
- UJJLJRQIPMGXEZ-UHFFFAOYSA-N tetrahydro-2-furoic acid Chemical compound OC(=O)C1CCCO1 UJJLJRQIPMGXEZ-UHFFFAOYSA-N 0.000 description 1
- UJJLJRQIPMGXEZ-SCSAIBSYSA-N tetrahydrofuran-2-carboxylic acid Chemical compound OC(=O)[C@H]1CCCO1 UJJLJRQIPMGXEZ-SCSAIBSYSA-N 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 208000009935 visceral pain Diseases 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- 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
-
- 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
- A61P1/14—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2002141262 | 2002-05-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200409053B true ZA200409053B (en) | 2005-07-12 |
Family
ID=29267809
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200409035A ZA200409053B (en) | 2002-05-16 | 2004-11-09 | (S)-4-Amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofuryl-carbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamin de, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor. |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US6696468B2 (de) |
| EP (1) | EP1362857B1 (de) |
| JP (1) | JP3643107B2 (de) |
| KR (1) | KR20040107520A (de) |
| CN (1) | CN1653063A (de) |
| AR (1) | AR040021A1 (de) |
| AT (1) | ATE273304T1 (de) |
| AU (1) | AU2003230245A1 (de) |
| BR (1) | BR0309933A (de) |
| CA (1) | CA2483368A1 (de) |
| CZ (1) | CZ20041084A3 (de) |
| DE (1) | DE60300021T2 (de) |
| DK (1) | DK1362857T3 (de) |
| ES (1) | ES2227500T3 (de) |
| HK (1) | HK1060118A1 (de) |
| HU (1) | HUP0501016A2 (de) |
| IL (1) | IL165012A0 (de) |
| MX (1) | MXPA04011332A (de) |
| NO (1) | NO20045469L (de) |
| PL (1) | PL372724A1 (de) |
| PT (1) | PT1362857E (de) |
| RU (1) | RU2004136853A (de) |
| SK (1) | SK50192004A3 (de) |
| TR (1) | TR200403020T2 (de) |
| TW (1) | TW200400186A (de) |
| WO (1) | WO2003097638A1 (de) |
| ZA (1) | ZA200409053B (de) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9904377D0 (sv) * | 1999-12-01 | 1999-12-01 | Astra Pharma Prod | Pharmaceutical combinations |
| SE0200844D0 (sv) | 2002-03-19 | 2002-03-19 | Astrazeneca Ab | Chemical compounds |
| SE0200843D0 (sv) | 2002-03-19 | 2002-03-19 | Astrazeneca Ab | Chemical compounds |
| SE0300957D0 (sv) | 2003-04-01 | 2003-04-01 | Astrazeneca Ab | Chemical compounds |
| TW200533348A (en) * | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| TWI351282B (en) * | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| US8309575B2 (en) | 2004-04-07 | 2012-11-13 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| US7728006B2 (en) * | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| ES2327142T3 (es) * | 2004-11-05 | 2009-10-26 | Theravance, Inc. | Compuestos de quinolinona-carboxamida. |
| DE602005016446D1 (de) * | 2004-11-05 | 2009-10-15 | Theravance Inc | 5-HT4-Rezeptoragonistenverbindungen |
| RU2404179C2 (ru) * | 2004-12-22 | 2010-11-20 | Тереванс, Инк. | Индазол-карбоксамидные соединения |
| CN101163701A (zh) * | 2005-03-02 | 2008-04-16 | 施万制药 | 作为5-ht4受体激动剂的喹啉酮化合物 |
| US7256294B2 (en) * | 2005-05-25 | 2007-08-14 | Theravance, Inc. | Crystalline form of a benzimidazole-carboxamide medicinal compound |
| MY147756A (en) * | 2005-05-25 | 2013-01-15 | Theravance Inc | Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists |
| US20080200505A1 (en) * | 2005-05-27 | 2008-08-21 | Astrazeneca Ab | Piperidines for the Treatment of Chemokine Mediated Diseases |
| TW200722419A (en) * | 2005-05-27 | 2007-06-16 | Astrazeneca Ab | Chemical compounds |
| US8314127B2 (en) | 2005-07-21 | 2012-11-20 | Astrazeneca Ab | Piperidine derivatives |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| TWI423967B (zh) * | 2008-02-21 | 2014-01-21 | Dainippon Sumitomo Pharma Co | 醯胺衍生物及含有其之醫藥組合物 |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| EP2531510B1 (de) | 2010-02-01 | 2014-07-23 | Novartis AG | Pyrazolo-[5,1b-]oxazol-derivate als crf-1-rezeptor-antagonisten |
| WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| ES2527849T3 (es) | 2010-02-02 | 2015-01-30 | Novartis Ag | Derivados de ciclohexilamida como antagonistas del receptor de CRF |
| US8546416B2 (en) | 2011-05-27 | 2013-10-01 | Novartis Ag | 3-spirocyclic piperidine derivatives as ghrelin receptor agonists |
| EA201491990A1 (ru) | 2012-05-03 | 2015-02-27 | Новартис Аг | L-малатная соль 2,7-диазаспиро[4.5]дец-7-иловых производных и их кристаллические формы в качестве агонистов грелиновых рецепторов |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH111472A (ja) | 1996-04-30 | 1999-01-06 | Dainippon Pharmaceut Co Ltd | ベンズアミド誘導体及びそれを含有する医薬組成物 |
| WO1999055674A1 (fr) | 1998-04-28 | 1999-11-04 | Dainippon Pharmaceutical Co., Ltd. | Derives de 1-[(1-substituee-4-piperidinyle)methyle]-4-piperidine, procede de production de ceux-ci, compositions medicinales contenant ces composes et intermediaires de ces composes |
| JP2000080081A (ja) | 1998-06-24 | 2000-03-21 | Dainippon Pharmaceut Co Ltd | １―〔（１―置換―４―ピペリジニル）メチル〕―４―ピペリジン誘導体及びそれを含有する医薬組成物 |
| JP2001122784A (ja) | 1999-10-27 | 2001-05-08 | Dainippon Pharmaceut Co Ltd | １−［（１−置換−４−ピペリジニル）メチル］−４−ピペリジン誘導体からなる医薬 |
-
2002
- 2002-12-18 US US10/321,615 patent/US6696468B2/en not_active Expired - Fee Related
-
2003
- 2003-01-03 ES ES03250050T patent/ES2227500T3/es not_active Expired - Lifetime
- 2003-01-03 PT PT03250050T patent/PT1362857E/pt unknown
- 2003-01-03 DK DK03250050T patent/DK1362857T3/da active
- 2003-01-03 AT AT03250050T patent/ATE273304T1/de not_active IP Right Cessation
- 2003-01-03 DE DE60300021T patent/DE60300021T2/de not_active Expired - Fee Related
- 2003-01-03 EP EP03250050A patent/EP1362857B1/de not_active Expired - Lifetime
- 2003-05-08 TW TW092112525A patent/TW200400186A/zh unknown
- 2003-05-15 JP JP2003137413A patent/JP3643107B2/ja not_active Expired - Fee Related
- 2003-05-15 WO PCT/JP2003/006051 patent/WO2003097638A1/en not_active Application Discontinuation
- 2003-05-15 MX MXPA04011332A patent/MXPA04011332A/es unknown
- 2003-05-15 BR BR0309933-4A patent/BR0309933A/pt not_active Application Discontinuation
- 2003-05-15 CN CNA03811089XA patent/CN1653063A/zh active Pending
- 2003-05-15 HU HU0501016A patent/HUP0501016A2/hu unknown
- 2003-05-15 AR ARP030101702A patent/AR040021A1/es unknown
- 2003-05-15 RU RU2004136853/04A patent/RU2004136853A/ru not_active Application Discontinuation
- 2003-05-15 IL IL16501203A patent/IL165012A0/xx unknown
- 2003-05-15 SK SK5019-2004A patent/SK50192004A3/sk unknown
- 2003-05-15 KR KR10-2004-7018158A patent/KR20040107520A/ko not_active Application Discontinuation
- 2003-05-15 CA CA002483368A patent/CA2483368A1/en not_active Abandoned
- 2003-05-15 CZ CZ20041084A patent/CZ20041084A3/cs unknown
- 2003-05-15 AU AU2003230245A patent/AU2003230245A1/en not_active Abandoned
- 2003-05-15 TR TR2004/03020T patent/TR200403020T2/xx unknown
- 2003-05-15 PL PL03372724A patent/PL372724A1/xx not_active Application Discontinuation
-
2004
- 2004-04-22 HK HK04102812A patent/HK1060118A1/xx not_active IP Right Cessation
- 2004-11-09 ZA ZA200409035A patent/ZA200409053B/en unknown
- 2004-12-15 NO NO20045469A patent/NO20045469L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003230245A1 (en) | 2003-12-02 |
| RU2004136853A (ru) | 2005-06-27 |
| AR040021A1 (es) | 2005-03-09 |
| TW200400186A (en) | 2004-01-01 |
| PT1362857E (pt) | 2004-11-30 |
| IL165012A0 (en) | 2005-12-18 |
| DE60300021T2 (de) | 2005-09-08 |
| DE60300021D1 (de) | 2004-09-16 |
| ES2227500T3 (es) | 2005-04-01 |
| CZ20041084A3 (cs) | 2005-02-16 |
| US6696468B2 (en) | 2004-02-24 |
| PL372724A1 (en) | 2005-07-25 |
| BR0309933A (pt) | 2005-02-09 |
| NO20045469L (no) | 2005-02-16 |
| MXPA04011332A (es) | 2005-02-14 |
| HK1060118A1 (en) | 2004-07-30 |
| SK50192004A3 (sk) | 2005-04-01 |
| US20030216433A1 (en) | 2003-11-20 |
| JP3643107B2 (ja) | 2005-04-27 |
| ATE273304T1 (de) | 2004-08-15 |
| WO2003097638A1 (en) | 2003-11-27 |
| DK1362857T3 (da) | 2004-12-20 |
| EP1362857A1 (de) | 2003-11-19 |
| CN1653063A (zh) | 2005-08-10 |
| JP2004043453A (ja) | 2004-02-12 |
| HUP0501016A2 (en) | 2006-02-28 |
| TR200403020T2 (tr) | 2005-05-23 |
| EP1362857B1 (de) | 2004-08-11 |
| KR20040107520A (ko) | 2004-12-20 |
| CA2483368A1 (en) | 2003-11-27 |
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