JP2012102102A5 - - Google Patents
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- Publication number
- JP2012102102A5 JP2012102102A5 JP2011261145A JP2011261145A JP2012102102A5 JP 2012102102 A5 JP2012102102 A5 JP 2012102102A5 JP 2011261145 A JP2011261145 A JP 2011261145A JP 2011261145 A JP2011261145 A JP 2011261145A JP 2012102102 A5 JP2012102102 A5 JP 2012102102A5
- Authority
- JP
- Japan
- Prior art keywords
- methoxy
- benzoylamino
- aza
- piperidin
- bicyclo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 10
- -1 bicyclo [2.2.2] oct-3-yl Chemical group 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 5
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- 206010052105 Gastrointestinal hypomotility Diseases 0.000 claims 1
- 201000005081 Intestinal Pseudo-Obstruction Diseases 0.000 claims 1
- 206010054048 Postoperative ileus Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 1
- 230000005176 gastrointestinal motility Effects 0.000 claims 1
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 230000008673 vomiting Effects 0.000 claims 1
- HTSGKJQDMSTCGS-UHFFFAOYSA-N 1,4-bis(4-chlorophenyl)-2-(4-methylphenyl)sulfonylbutane-1,4-dione Chemical compound C1=CC(C)=CC=C1S(=O)(=O)C(C(=O)C=1C=CC(Cl)=CC=1)CC(=O)C1=CC=C(Cl)C=C1 HTSGKJQDMSTCGS-UHFFFAOYSA-N 0.000 description 2
- 0 CO*1C(*NC(c(cc(c(N)c2)Cl)c2OC)=O)*CCN(CCCCCC(O[C@@]2C(CC3)CCN3C2)=O)C1 Chemical compound CO*1C(*NC(c(cc(c(N)c2)Cl)c2OC)=O)*CCN(CCCCCC(O[C@@]2C(CC3)CCN3C2)=O)C1 0.000 description 2
- OMLDMGPCWMBPAN-YPMHNXCESA-N norcisapride Chemical compound CO[C@H]1CNCC[C@H]1NC(=O)C1=CC(Cl)=C(N)C=C1OC OMLDMGPCWMBPAN-YPMHNXCESA-N 0.000 description 2
- IVLICPVPXWEGCA-UHFFFAOYSA-N 3-quinuclidinol Chemical compound C1C[C@@H]2C(O)C[N@]1CC2 IVLICPVPXWEGCA-UHFFFAOYSA-N 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- FKLJPTJMIBLJAV-UHFFFAOYSA-N Compound IV Chemical compound O1N=C(C)C=C1CCCCCCCOC1=CC=C(C=2OCCN=2)C=C1 FKLJPTJMIBLJAV-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- DCSUBABJRXZOMT-IRLDBZIGSA-N cisapride Chemical compound C([C@@H]([C@@H](CC1)NC(=O)C=2C(=CC(N)=C(Cl)C=2)OC)OC)N1CCCOC1=CC=C(F)C=C1 DCSUBABJRXZOMT-IRLDBZIGSA-N 0.000 description 1
- 229960005132 cisapride Drugs 0.000 description 1
- DCSUBABJRXZOMT-UHFFFAOYSA-N cisapride Natural products C1CC(NC(=O)C=2C(=CC(N)=C(Cl)C=2)OC)C(OC)CN1CCCOC1=CC=C(F)C=C1 DCSUBABJRXZOMT-UHFFFAOYSA-N 0.000 description 1
- 230000001268 conjugating effect Effects 0.000 description 1
- NLFBCYMMUAKCPC-KQQUZDAGSA-N ethyl (e)-3-[3-amino-2-cyano-1-[(e)-3-ethoxy-3-oxoprop-1-enyl]sulfanyl-3-oxoprop-1-enyl]sulfanylprop-2-enoate Chemical compound CCOC(=O)\C=C\SC(=C(C#N)C(N)=O)S\C=C\C(=O)OCC NLFBCYMMUAKCPC-KQQUZDAGSA-N 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53489204P | 2004-01-07 | 2004-01-07 | |
| US60/534,892 | 2004-01-07 | ||
| US56093804P | 2004-04-09 | 2004-04-09 | |
| US60/560,938 | 2004-04-09 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006549435A Division JP5200288B2 (ja) | 2004-01-07 | 2005-01-07 | 胃腸疾患および中枢神経系疾患の治療のための立体異性体化合物と方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012102102A JP2012102102A (ja) | 2012-05-31 |
| JP2012102102A5 true JP2012102102A5 (https=) | 2013-02-21 |
| JP5524939B2 JP5524939B2 (ja) | 2014-06-18 |
Family
ID=34798839
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006549435A Expired - Lifetime JP5200288B2 (ja) | 2004-01-07 | 2005-01-07 | 胃腸疾患および中枢神経系疾患の治療のための立体異性体化合物と方法 |
| JP2011261145A Expired - Lifetime JP5524939B2 (ja) | 2004-01-07 | 2011-11-30 | 胃腸疾患および中枢神経系疾患の治療のための立体異性体化合物と方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006549435A Expired - Lifetime JP5200288B2 (ja) | 2004-01-07 | 2005-01-07 | 胃腸疾患および中枢神経系疾患の治療のための立体異性体化合物と方法 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US7176218B2 (https=) |
| EP (2) | EP1704146B1 (https=) |
| JP (2) | JP5200288B2 (https=) |
| KR (1) | KR101240464B1 (https=) |
| CN (1) | CN101824033B (https=) |
| AT (1) | ATE464308T1 (https=) |
| AU (2) | AU2005205531B2 (https=) |
| BR (1) | BRPI0506736B1 (https=) |
| CA (1) | CA2551686C (https=) |
| CY (1) | CY1110901T1 (https=) |
| DE (1) | DE602005020580D1 (https=) |
| DK (2) | DK2194053T3 (https=) |
| ES (2) | ES2344568T3 (https=) |
| IL (1) | IL176569A (https=) |
| MX (1) | MXPA06007853A (https=) |
| NO (1) | NO337741B1 (https=) |
| PT (2) | PT2194053E (https=) |
| RU (1) | RU2374244C2 (https=) |
| WO (1) | WO2005068461A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0211230D0 (en) | 2002-05-16 | 2002-06-26 | Medinnova Sf | Treatment of heart failure |
| US8524736B2 (en) | 2004-01-07 | 2013-09-03 | Armetheon, Inc. | Stereoisomeric compounds and methods for the treatment of gastrointestinal and central nervous system disorders |
| DK2194053T3 (da) * | 2004-01-07 | 2013-07-01 | Armetheon Inc | Methoxypiperidinderivater til brug i behandling af gastrointestinale forstyrrelser og forstyrrelser i centralnervesystemet. |
| US8138204B2 (en) | 2004-01-07 | 2012-03-20 | Aryx Therapeutics, Inc. | Stereoisomeric compounds and methods for the treatment of gastrointestinal and central nervous system disorders |
| MY150958A (en) | 2005-06-16 | 2014-03-31 | Astrazeneca Ab | Compounds for the treatment of multi-drug resistant bacterial infections |
| CN101258151B (zh) * | 2005-08-31 | 2012-10-10 | ARYx医疗有限公司 | 用于治疗胃肠系统和中枢神经系统疾病的立体异构化合物的合成方法及中间体 |
| RU2418798C2 (ru) * | 2005-08-31 | 2011-05-20 | Арикс Терапьютикс, Инк. | Способы синтеза и промежуточные соединения при синтезе стереоизомерных соединений, пригодных для лечения желудочно-кишечных расстройств и расстройств центральной нервной системы |
| GB0525068D0 (en) | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
| AU2006327313A1 (en) * | 2005-12-23 | 2007-06-28 | Astrazeneca Ab | Heterocyclic GABA-B modulators |
| US20080085915A1 (en) * | 2006-06-23 | 2008-04-10 | Cyrus Becker | Compounds and methods for the treatment of gastrointestinal and central nervous system disorders |
| CN101402633A (zh) | 2007-09-11 | 2009-04-08 | 上海恒瑞医药有限公司 | 苯甲酰胺类衍生物、其制备方法及其在医药上的用途 |
| WO2010062959A1 (en) * | 2008-11-26 | 2010-06-03 | Aryx Therapeutics, Inc. | 5-ht4 receptor agonists for treating irritable bowel syndrome and colonic hypersensitivity |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
| WO2011092290A1 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists |
| EP2531490B1 (en) | 2010-02-02 | 2014-10-15 | Novartis AG | Cyclohexyl amide derivatives as crf receptor antagonists |
| AR086554A1 (es) | 2011-05-27 | 2014-01-08 | Novartis Ag | Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina |
| PL395470A1 (pl) * | 2011-06-29 | 2013-01-07 | Adamed Spólka Z Ograniczona Odpowiedzialnoscia | Sulfonamidowe pochodne amin alicyklicznych do leczenia chorób osrodkowego ukladu nerwowego |
| JP2015525202A (ja) | 2012-05-03 | 2015-09-03 | ノバルティス アーゲー | グレリン受容体アゴニストとしての２，７−ジアザ−スピロ［４，５］デカ−７−イル誘導体のｌ−リンゴ酸塩およびその結晶形態 |
| TW202026002A (zh) * | 2014-05-16 | 2020-07-16 | 日商拉夸里亞創藥股份有限公司 | 用於胃輕癱之5-ht4受體激動劑 |
| US10376145B2 (en) | 2015-02-24 | 2019-08-13 | Elira, Inc. | Systems and methods for enabling a patient to achieve a weight loss objective using an electrical dermal patch |
| US10864367B2 (en) | 2015-02-24 | 2020-12-15 | Elira, Inc. | Methods for using an electrical dermal patch in a manner that reduces adverse patient reactions |
| US20220062621A1 (en) | 2015-02-24 | 2022-03-03 | Elira, Inc. | Electrical Stimulation-Based Weight Management System |
| EP3261712B1 (en) | 2015-02-24 | 2024-04-03 | Elira, Inc. | System for enabling appetite modulation and/or improving dietary compliance using an electro-dermal patch |
| US10765863B2 (en) | 2015-02-24 | 2020-09-08 | Elira, Inc. | Systems and methods for using a transcutaneous electrical stimulation device to deliver titrated therapy |
| US10335302B2 (en) | 2015-02-24 | 2019-07-02 | Elira, Inc. | Systems and methods for using transcutaneous electrical stimulation to enable dietary interventions |
| US9956393B2 (en) | 2015-02-24 | 2018-05-01 | Elira, Inc. | Systems for increasing a delay in the gastric emptying time for a patient using a transcutaneous electro-dermal patch |
| US11495028B2 (en) * | 2018-09-28 | 2022-11-08 | Intel Corporation | Obstacle analyzer, vehicle control system, and methods thereof |
| US10570127B1 (en) | 2018-11-05 | 2020-02-25 | Renexxion, Llc | Material and methods for the treatment of gastro-intestinal disorders |
| WO2020096911A1 (en) * | 2018-11-05 | 2020-05-14 | Renexxion, Llc | Methods of producing naronapride trihydrate |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| GB1425706A (en) | 1972-06-30 | 1976-02-18 | Wyeth John & Brother Ltd | Piperidine derivatives |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US5137896A (en) | 1981-10-01 | 1992-08-11 | Janssen Pharmaceutica N.V. | N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
| CA1183847A (en) | 1981-10-01 | 1985-03-12 | Georges Van Daele | N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
| US5057525A (en) * | 1981-10-01 | 1991-10-15 | Janssen Pharmaceutica N.V. | Novel N-(3-hydroxy-4-piperidinyl) benzamide derivatives |
| US4962115A (en) * | 1981-10-01 | 1990-10-09 | Janssen Pharmaceutica N.V. | Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
| GB8519707D0 (en) * | 1985-08-06 | 1985-09-11 | Fordonal Sa | Chemical compounds |
| US4870074A (en) | 1986-04-30 | 1989-09-26 | Dainippon Pharmaceutical Co., Ltd. | Substituted benzamide derivatives, for enhancing gastrointestinal motility |
| NZ225152A (en) * | 1987-07-17 | 1990-04-26 | Janssen Pharmaceutica Nv | Heterocyclically substituted piperidinyl benzamides as pharmaceuticals |
| CA1317940C (en) | 1987-09-25 | 1993-05-18 | Georges H. P. Van Daele | Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides |
| US4975439A (en) | 1987-09-25 | 1990-12-04 | Janssen Pharmaceutical N.V. | Novel substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides |
| US5041454A (en) | 1987-09-25 | 1991-08-20 | Janssen Pharmaceutica N.V. | Novel substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides |
| US5395832A (en) | 1991-02-15 | 1995-03-07 | Hokuriku Seiyaku Co., Ltd. | Benzamide derivatives |
| JP3104142B2 (ja) * | 1991-02-15 | 2000-10-30 | 北陸製薬株式会社 | ベンズアミド誘導体 |
| TW243449B (https=) | 1991-02-15 | 1995-03-21 | Hokuriku Pharmaceutical | |
| IT1260485B (it) | 1992-05-29 | 1996-04-09 | Procedimento e dispositivo per il trattamento dell'obesita' di un paziente | |
| CA2139638A1 (en) | 1992-07-07 | 1994-01-20 | Nancy M. Gray | Methods of using (-) cisapride for the treatment of gastro-esophageal reflux disease and other disorders |
| EP0651639A4 (en) | 1992-07-07 | 1996-06-26 | Sepracor Inc | METHODS OF USING CISAPRIDE (+) FOR THE TREATMENT OF GASTROSOPHAGIC REFLUX AND OTHER DISORDERS. |
| NZ257545A (en) | 1992-11-05 | 1997-01-29 | Smithkline Beecham Plc | Heterocyclic (especially piperidine) derivatives and pharmaceutical compositions |
| US5472866A (en) | 1992-12-24 | 1995-12-05 | Synaptic Pharmaceutical Corporation | DNA encoding 5-HT4A serotonin receptors |
| US5705798A (en) * | 1994-12-16 | 1998-01-06 | Mastercard International Inc. | System and method for processing a customized financial transaction card |
| US5712293A (en) | 1995-06-07 | 1998-01-27 | Sepracor, Inc. | Methods for treating gastro-esophageal reflux disease and other disorders associated with the digestive tract using optically pure (-) norcisapride |
| US5739151A (en) | 1996-07-19 | 1998-04-14 | Sepracor Inc. | Method for treating emesis and central nervous system disorders using optically pure (+) norcisapride |
| US6147093A (en) | 1996-07-19 | 2000-11-14 | Sepracor Inc. | Methods for treating gastroesophageal reflux disease |
| TR200000020T2 (tr) | 1997-07-11 | 2000-09-21 | Janssen Pharmaceutica N.V. | 5-HT3 ve 5-HT4 aracılı bozuklar için faydalı (+)-norsisaprit. |
| JPH11292846A (ja) | 1998-02-10 | 1999-10-26 | Hokuriku Seiyaku Co Ltd | ベンズアミド誘導体及びそれを含有する医薬 |
| AR022338A1 (es) | 1999-02-04 | 2002-09-04 | Hokuriku Pharmaceutical | Un compuesto de benzamida, medicamento que lo contiene, y uso para la manufactura de un medicamento para el tratamiento o prevencion de una enfermedad digestiva o para mejorar la movilidad del tracto gastrointestinal. |
| DE19933926A1 (de) | 1999-07-20 | 2001-01-25 | Boehringer Ingelheim Pharma | Biphenylderivate, ihre Herstellung und ihre Verwendung als Arzneimittel |
| US20040092511A1 (en) | 1999-12-10 | 2004-05-13 | Billstein Stephan Anthony | Pharmaceutical combinations and their use in treating gastrointestinal and abdominal viscera disorders |
| JP2004513071A (ja) | 2000-05-23 | 2004-04-30 | ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク | 肺の弾性繊維損傷に関連した呼吸器疾患の治療方法 |
| AU2001275326C1 (en) | 2000-06-07 | 2006-09-21 | Aryx Therapeutics | Treatment of gastroesophageal reflux disease using piperidine derivatives |
| MXPA03000145A (es) * | 2002-01-07 | 2003-07-15 | Pfizer | Compuestos de oxo u oxi-piridina como moduladores de receptores 5-ht4. |
| DK2194053T3 (da) * | 2004-01-07 | 2013-07-01 | Armetheon Inc | Methoxypiperidinderivater til brug i behandling af gastrointestinale forstyrrelser og forstyrrelser i centralnervesystemet. |
-
2005
- 2005-01-07 DK DK10153093.9T patent/DK2194053T3/da active
- 2005-01-07 ES ES05705267T patent/ES2344568T3/es not_active Expired - Lifetime
- 2005-01-07 AU AU2005205531A patent/AU2005205531B2/en not_active Expired
- 2005-01-07 KR KR1020067015208A patent/KR101240464B1/ko not_active Expired - Lifetime
- 2005-01-07 BR BRPI0506736-7A patent/BRPI0506736B1/pt active IP Right Grant
- 2005-01-07 DK DK05705267.2T patent/DK1704146T3/da active
- 2005-01-07 MX MXPA06007853A patent/MXPA06007853A/es active IP Right Grant
- 2005-01-07 PT PT101530939T patent/PT2194053E/pt unknown
- 2005-01-07 CA CA2551686A patent/CA2551686C/en not_active Expired - Lifetime
- 2005-01-07 ES ES10153093T patent/ES2415830T3/es not_active Expired - Lifetime
- 2005-01-07 EP EP05705267A patent/EP1704146B1/en not_active Expired - Lifetime
- 2005-01-07 RU RU2006128589/04A patent/RU2374244C2/ru active
- 2005-01-07 PT PT05705267T patent/PT1704146E/pt unknown
- 2005-01-07 AT AT05705267T patent/ATE464308T1/de active
- 2005-01-07 US US11/031,623 patent/US7176218B2/en not_active Expired - Lifetime
- 2005-01-07 CN CN2010101640045A patent/CN101824033B/zh not_active Expired - Lifetime
- 2005-01-07 DE DE602005020580T patent/DE602005020580D1/de not_active Expired - Lifetime
- 2005-01-07 WO PCT/US2005/000510 patent/WO2005068461A1/en not_active Ceased
- 2005-01-07 EP EP10153093A patent/EP2194053B1/en not_active Expired - Lifetime
- 2005-01-07 JP JP2006549435A patent/JP5200288B2/ja not_active Expired - Lifetime
- 2005-03-23 US US11/087,167 patent/US7282509B2/en not_active Expired - Lifetime
-
2006
- 2006-06-26 IL IL176569A patent/IL176569A/en active IP Right Grant
- 2006-08-07 NO NO20063568A patent/NO337741B1/no unknown
-
2008
- 2008-11-13 AU AU2008243243A patent/AU2008243243B2/en not_active Expired
-
2010
- 2010-07-05 CY CY20101100615T patent/CY1110901T1/el unknown
-
2011
- 2011-11-30 JP JP2011261145A patent/JP5524939B2/ja not_active Expired - Lifetime
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