TWI377206B - Crystalline form of a quinolinone-carboxamide compound - Google Patents
Crystalline form of a quinolinone-carboxamide compound Download PDFInfo
- Publication number
- TWI377206B TWI377206B TW095110607A TW95110607A TWI377206B TW I377206 B TWI377206 B TW I377206B TW 095110607 A TW095110607 A TW 095110607A TW 95110607 A TW95110607 A TW 95110607A TW I377206 B TWI377206 B TW I377206B
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- Prior art keywords
- acid
- crystalline
- oxo
- isopropyl
- salt form
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- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 210000001578 tight junction Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 230000037317 transdermal delivery Effects 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 238000013022 venting Methods 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
Classifications
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61P1/10—Laxatives
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Nutrition Science (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US66878005P | 2005-04-06 | 2005-04-06 |
Publications (2)
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|---|---|
| TW200643020A TW200643020A (en) | 2006-12-16 |
| TWI377206B true TWI377206B (en) | 2012-11-21 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW095110607A TWI377206B (en) | 2005-04-06 | 2006-03-27 | Crystalline form of a quinolinone-carboxamide compound |
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| JP (2) | JP5230407B2 (enExample) |
| KR (1) | KR101322873B1 (enExample) |
| CN (1) | CN101151264B (enExample) |
| AR (2) | AR053208A1 (enExample) |
| AT (1) | ATE479682T1 (enExample) |
| AU (1) | AU2006232129B2 (enExample) |
| BR (1) | BRPI0610657A2 (enExample) |
| CA (1) | CA2603654C (enExample) |
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| DE (1) | DE602006016586D1 (enExample) |
| DK (1) | DK1874766T3 (enExample) |
| EA (1) | EA012115B1 (enExample) |
| ES (1) | ES2350495T3 (enExample) |
| HR (1) | HRP20100629T1 (enExample) |
| IL (1) | IL186023A (enExample) |
| MA (1) | MA29403B1 (enExample) |
| MX (1) | MX2007012438A (enExample) |
| MY (1) | MY151075A (enExample) |
| NO (1) | NO339699B1 (enExample) |
| NZ (1) | NZ561900A (enExample) |
| PE (1) | PE20061310A1 (enExample) |
| PL (1) | PL1874766T3 (enExample) |
| PT (1) | PT1874766E (enExample) |
| SI (1) | SI1874766T1 (enExample) |
| TW (1) | TWI377206B (enExample) |
| WO (1) | WO2006108127A2 (enExample) |
| ZA (1) | ZA200708071B (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7063671B2 (en) * | 2002-06-21 | 2006-06-20 | Boston Scientific Scimed, Inc. | Electronically activated capture device |
| US7728006B2 (en) * | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| TWI351282B (en) | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| DE602005016446D1 (de) * | 2004-11-05 | 2009-10-15 | Theravance Inc | 5-HT4-Rezeptoragonistenverbindungen |
| DE602005014566D1 (de) | 2004-11-05 | 2009-07-02 | Theravance Inc | Chinolinon-carboxamid-verbindungen |
| TWI377206B (en) * | 2005-04-06 | 2012-11-21 | Theravance Inc | Crystalline form of a quinolinone-carboxamide compound |
| PT2404919E (pt) | 2005-11-08 | 2013-10-22 | Vertex Pharma | Composto heterocíclico útil como um modulador de transportadores de cassete de ligação a atp |
| JP2010527357A (ja) * | 2007-05-17 | 2010-08-12 | セラヴァンス， インコーポレーテッド | 腸の前処置のための運動促進剤 |
| CH698729B1 (de) * | 2007-05-30 | 2009-10-15 | Cerbios Pharma Sa | Stabile, kristalline (6S)-N(5)-Methyl-5, 6,7,8-tetrahydrofolsäure. |
| HUE049642T2 (hu) * | 2007-12-07 | 2020-09-28 | Vertex Pharma | 3-(6-(1-(2,2-Difluorbenzo[d][1,3]dioxol-5-il)-ciklopropánkarboxamido)-3-metilpiridin-2-il)-benzoesav szilárd formái |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| LT2419104T (lt) | 2009-04-13 | 2018-02-12 | Theravance Biopharma R&D Ip, Llc | 5-ht4 receptoriaus agonistų ir acetilcholinesterazės inhibitorių deriniai, skirti pažinimo sutrikimų gydymui |
| CN102762572A (zh) | 2010-02-01 | 2012-10-31 | 诺瓦提斯公司 | 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物 |
| AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
| EP2531490B1 (en) | 2010-02-02 | 2014-10-15 | Novartis AG | Cyclohexyl amide derivatives as crf receptor antagonists |
| ES2900353T3 (es) | 2010-04-07 | 2022-03-16 | Vertex Pharma | Composiciones farmacéuticas de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiriidin-2-il)benzoico y administración de las mismas |
| NZ727015A (en) | 2012-01-25 | 2017-12-22 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| CA2930199C (en) | 2013-11-12 | 2022-10-25 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases |
| CA3069989C (en) | 2017-07-31 | 2025-05-06 | Alfasigma S.P.A. | METHODS FOR TREATING GASTROPARESIA SYMPTOMS USING VELUSETRAG |
| US10570127B1 (en) | 2018-11-05 | 2020-02-25 | Renexxion, Llc | Material and methods for the treatment of gastro-intestinal disorders |
| US20260124194A1 (en) | 2022-09-20 | 2026-05-07 | Alfasigma S.P.A. | Velusetrag for use in the treatment of chronic intestinal pseudo-obstruction (cipo) |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3122671B2 (ja) | 1990-05-23 | 2001-01-09 | 協和醗酵工業株式会社 | 複素環式化合物 |
| DE69113284T2 (de) * | 1990-12-28 | 1996-02-22 | Kyowa Hakko Kogyo Co., Ltd., Tokio/Tokyo | Chinolinderivat. |
| WO1994012497A1 (fr) | 1992-11-20 | 1994-06-09 | Taisho Pharmaceutical Co., Ltd. | Compose heterocyclique |
| JP3829879B2 (ja) | 1994-05-18 | 2006-10-04 | 大正製薬株式会社 | キノリンカルボン酸誘導体 |
| TW402591B (en) * | 1997-07-11 | 2000-08-21 | Janssen Pharmaceutica Nv | Monocyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives |
| US7105195B2 (en) * | 2003-07-25 | 2006-09-12 | General Mills, Inc. | Reduced trans fat product |
| ES2338882T3 (es) | 2003-11-24 | 2010-05-13 | Pfizer, Inc. | Compuestos de acido quinolona-carboxilico que tienen actividad agonista del receptor 5-ht4. |
| US7728006B2 (en) | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| TWI351282B (en) | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| DE602005016446D1 (de) | 2004-11-05 | 2009-10-15 | Theravance Inc | 5-HT4-Rezeptoragonistenverbindungen |
| DE602005014566D1 (de) | 2004-11-05 | 2009-07-02 | Theravance Inc | Chinolinon-carboxamid-verbindungen |
| US20060183901A1 (en) | 2005-02-17 | 2006-08-17 | Theravance, Inc. | Crystalline form of an indazole-carboxamide compound |
| BRPI0608392A2 (pt) | 2005-03-02 | 2009-12-29 | Theravance Inc | compostos de quinolinona como agonistas do receptor 5-ht4 |
| TWI377206B (en) * | 2005-04-06 | 2012-11-21 | Theravance Inc | Crystalline form of a quinolinone-carboxamide compound |
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- 2006-04-03 MY MYPI20061482 patent/MY151075A/en unknown
- 2006-04-03 PE PE2006000360A patent/PE20061310A1/es not_active Application Discontinuation
- 2006-04-05 JP JP2008505559A patent/JP5230407B2/ja not_active Expired - Lifetime
- 2006-04-05 DE DE602006016586T patent/DE602006016586D1/de not_active Expired - Lifetime
- 2006-04-05 HR HR20100629T patent/HRP20100629T1/hr unknown
- 2006-04-05 MX MX2007012438A patent/MX2007012438A/es active IP Right Grant
- 2006-04-05 PL PL06740692T patent/PL1874766T3/pl unknown
- 2006-04-05 DK DK06740692.6T patent/DK1874766T3/da active
- 2006-04-05 AU AU2006232129A patent/AU2006232129B2/en not_active Expired
- 2006-04-05 AT AT06740692T patent/ATE479682T1/de active
- 2006-04-05 NZ NZ561900A patent/NZ561900A/en unknown
- 2006-04-05 CA CA2603654A patent/CA2603654C/en not_active Expired - Lifetime
- 2006-04-05 CN CN2006800107676A patent/CN101151264B/zh not_active Expired - Lifetime
- 2006-04-05 BR BRPI0610657-9A patent/BRPI0610657A2/pt not_active Application Discontinuation
- 2006-04-05 SI SI200630833T patent/SI1874766T1/sl unknown
- 2006-04-05 WO PCT/US2006/012978 patent/WO2006108127A2/en not_active Ceased
- 2006-04-05 EP EP06740692A patent/EP1874766B1/en not_active Expired - Lifetime
- 2006-04-05 EA EA200702161A patent/EA012115B1/ru not_active IP Right Cessation
- 2006-04-05 ES ES06740692T patent/ES2350495T3/es not_active Expired - Lifetime
- 2006-04-05 KR KR1020077025632A patent/KR101322873B1/ko not_active Expired - Lifetime
- 2006-04-05 PT PT06740692T patent/PT1874766E/pt unknown
- 2006-04-05 US US11/398,119 patent/US7728004B2/en active Active
- 2006-04-06 AR ARP060101375A patent/AR053208A1/es not_active Application Discontinuation
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2007
- 2007-09-18 IL IL186023A patent/IL186023A/en active IP Right Grant
- 2007-09-19 ZA ZA200708071A patent/ZA200708071B/xx unknown
- 2007-10-25 MA MA30317A patent/MA29403B1/fr unknown
- 2007-11-02 NO NO20075574A patent/NO339699B1/no not_active IP Right Cessation
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2010
- 2010-04-13 US US12/759,080 patent/US8658671B2/en active Active
- 2010-11-25 CY CY20101101076T patent/CY1111275T1/el unknown
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- 2012-05-17 JP JP2012113464A patent/JP2012153725A/ja not_active Withdrawn
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- 2014-01-08 US US14/150,059 patent/US9126994B2/en not_active Expired - Lifetime
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| MM4A | Annulment or lapse of patent due to non-payment of fees |