HRP20100629T1 - Kristalni oblik spoja kinolinon-karboksamida - Google Patents
Kristalni oblik spoja kinolinon-karboksamida Download PDFInfo
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- HRP20100629T1 HRP20100629T1 HR20100629T HRP20100629T HRP20100629T1 HR P20100629 T1 HRP20100629 T1 HR P20100629T1 HR 20100629 T HR20100629 T HR 20100629T HR P20100629 T HRP20100629 T HR P20100629T HR P20100629 T1 HRP20100629 T1 HR P20100629T1
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- Prior art keywords
- compound
- crystalline salt
- crystalline
- salt
- peak values
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- 150000001875 compounds Chemical class 0.000 claims abstract 32
- 150000003839 salts Chemical class 0.000 claims abstract 30
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims abstract 6
- 239000012453 solvate Substances 0.000 claims abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- 206010010774 Constipation Diseases 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000004899 motility Effects 0.000 claims 3
- 206010051153 Diabetic gastroparesis Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 206010021518 Impaired gastric emptying Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 201000006549 dyspepsia Diseases 0.000 claims 2
- 210000005095 gastrointestinal system Anatomy 0.000 claims 2
- 208000013617 idiopathic gastroparesis Diseases 0.000 claims 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 239000011541 reaction mixture Substances 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 238000007707 calorimetry Methods 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- UUCJNYSXZJNSLE-UHFFFAOYSA-N 2-oxo-1-propan-2-ylquinoline-3-carboxylic acid Chemical compound C1=CC=C2C=C(C(O)=O)C(=O)N(C(C)C)C2=C1 UUCJNYSXZJNSLE-UHFFFAOYSA-N 0.000 abstract 1
- -1 methanesulfonyl-methyl-amino Chemical group 0.000 abstract 1
Classifications
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- 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
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- 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)
Abstract
Spoj u obliku kristalne soli, naznačen time, da je to klorovodična sol spoja 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-8-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amid ili njegov solvat. Patent sadrži još 19 patentnih zahtjeva.
Claims (20)
1. Spoj u obliku kristalne soli, naznačen time, da je to klorovodična sol spoja 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-8-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amid ili njegov solvat.
2. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 1, naznačen time, da je taj spoj u obliku kristalne soli kristalna klorovodična sol.
3. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 2, naznačen time, da taj spoj u obliku kristalne soli karakterizira obrazac rentgenske difrakcije u prašku s dvije ili više vršnih vrijednosti na 2θ, odabranih između: 4.41±0.2, 8.82±0.2, 9.08±0.2, 11.21±0.2, 14.40±0.2, 16.42±0.2, 17.35±0.2, 17.61±0.2, 18.14±0.2, 19.04±0.2, 19.95±0.2, 20.20±0.2, 21.23±0.2, 22.13±0.2, 22.48±0.2, 22.83±0.2, 24.16±0.2, 25.37±0.2, 25.56±0.2, 26.22±0.2, 27.33±0.2, 29.08±0.2 i 29.61±0.2.
4. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 3, naznačen time, da obrazac rentgenske difrakcije u prašku sadrži dvije ili više vršnih vrijednosti na 2θ, odabranih između: 14.40±0.2, 7.35±0.2, 17.61±0.2, 19.04±0.2, 21.23±0.2 i 22.13±0.2.
5. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 2, naznačen time, da taj spoj u obliku kristalne soli karakterizira obrazac rentgenske difrakcije u prašku u kojem se pozicije vršnih vrijednosti u znatnoj mjeri poklapaju s pozicijama vršnih vrijednosti iz obrasca prikazanog na Slici 1.
6. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 2, naznačen time, da taj spoj u obliku kristalne soli karakterizira trag diferencijalne pretražne kalorimetrije koji iskazuje najvišu vrijednost endotermnog toplinskog toka na temperaturi višoj od oko 230 °C.
7. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 2, naznačen time, da taj spoj u obliku kristalne soli karakterizira trag diferencijalne pretražna kalorimetrija koji se u znatnoj mjeri poklapa s onim koji je prikazan na Slici 2.
8. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 1, naznačen time, da je spoj u obliku kristalne soli hidrat.
9. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 8, naznačen time, da taj spoj u obliku kristalne soli karakterizira obrazac rentgenske difrakcije u prašku s dvije ili više vršnih vrijednosti na 2θ, odabranih između: 5.30±0.2, 7.43±0.2, 8.72±0.2, 10.52±0.2, 13.85±0.2, 14.11±0.2, 15.80*0.2, 15.99±0.2, 17.26±0.2, 19.53±0.2, 20.08±0.2, 21.06*0.2, 21.48±0.2, 21.92±0.2, 22.85±0.2, 23.91±0.2, 25.28±0.2, 26.06±0.2, 27.34±0.2, 27.51±0.2 i 29.67±0.2.
10. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 9, naznačen time, da obrazac rentgenske difrakcije u prašku sadrži dvije ili više vršnih vrijednosti na 2θ, odabranih između: 10.52±0.2, 13.85±0.2, 15.80±0.2, 17.26±0.2 i 21.06±0.2.
11. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 8, naznačen time, da taj spoj u obliku kristalne soli karakterizira obrazac rentgenske difrakcije u prašku u kojem se pozicije vršnih vrijednosti u znatnoj mjeri poklapaju s pozicijama vršnih vrijednosti iz obrasca prikazanog na Slici 4.
12. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 8, naznačen time, da taj spoj u obliku kristalne soli karakterizira trag diferencijalne pretražne kalorimetrije koji se u znatnoj mjeri poklapa s onim koji je prikazan na Slici 5.
13. Farmaceutski pripravak, naznačen time, da sadrži farmaceutski prihvatljiv nosač i spoj u obliku kristalne soli iz bilo kojeg od patentnih zahtjeva 1 do 12.
14. Spoj u obliku kristalne soli za koji se zahtijeva patentna zaštita u bilo kojem od patentnih zahtjeva 1 do 12, naznačen time, da je namijenjen terapijskoj uporabi.
15. Spoj u obliku kristalne soli za koji se zahtijeva patentna zaštita u patentnom zahtjevu 14, naznačen time, da je namijenjen liječenju poremećaja smanjenog motiliteta gastrointestinalnog sustava u sisavaca.
16. Spoj u obliku kristalne soli u skladu s patentnim zahtjevom 15, naznačen time, da je poremećaj smanjenog motiliteta odabran između sljedećeg: kronična konstipacija, sindrom nadraženog crijeva s predominantnom konstipacijom, dijabetička i idiopatska gastropareza i funkcionalna dispepsija.
17. Uporaba spoja u obliku kristalne soli iz bilo kojeg od patentnih zahtjeva 1 do 12, naznačena time, da se ta uporaba odnosi na proizvodnju lijeka za liječenje medicinskog stanja u sisavaca, a to medicinsko stanje je poremećaj ili smanjeni motilitet gastrointestinalnog sustava.
18. Uporaba u skladu s patentnim zahtjevom 17, naznačena time, da je dotično medicinsko stanje odabrano iz sljedećeg: kronična konstipacija, sindrom nadraženog crijeva s predominantnom konstipacijom, dijabetička i idiopatska gastropareza i funkcionalna dispepsija.
19. Postupak za pripravu kristalne klorovodične soli spoja 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-8-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amida, naznačen time, da dotični postupak uključuje:
(a) izlaganje spoja 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-8-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]okt-3-il}amida djelovanju klorovodične kiselina, čime se dobiva reakcijska smjesa; i
(b) izdvajanje kristalne klorovodične soli iz rekacijske smjese.
20. Postupak za pripravu kristalne klorovodične soli spoja 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-S-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]oct-3-il}amida, naznačen time, da dotični postupak uključuje:
(a) otapanje 1-izopropil-2-okso-1,2-dihidrokinolion-3-karboksilna kiselina {(1S,3R,5R)-8-[(R)-2-hidroksi-3-(metansulfonil-metil-amino)propil]-8-azabiciklo[3.2.1]oct-3-il}amid klorovodika u vodi u koncentraciji većoj od oko 50 miligrama na mililitar, čime se dobiva suspenzija; i
(b) izdvajanje kristalnog hidrata iz suspenzije.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US66878005P | 2005-04-06 | 2005-04-06 | |
| PCT/US2006/012978 WO2006108127A2 (en) | 2005-04-06 | 2006-04-05 | Crystalline form of a quinolinone-carboxamide compound |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20100629T1 true HRP20100629T1 (hr) | 2010-12-31 |
Family
ID=37074104
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100629T HRP20100629T1 (hr) | 2005-04-06 | 2010-11-19 | Kristalni oblik spoja kinolinon-karboksamida |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US7728004B2 (hr) |
| EP (1) | EP1874766B1 (hr) |
| JP (2) | JP5230407B2 (hr) |
| KR (1) | KR101322873B1 (hr) |
| CN (1) | CN101151264B (hr) |
| AR (2) | AR053208A1 (hr) |
| AT (1) | ATE479682T1 (hr) |
| AU (1) | AU2006232129B2 (hr) |
| BR (1) | BRPI0610657A2 (hr) |
| CA (1) | CA2603654C (hr) |
| CY (1) | CY1111275T1 (hr) |
| DE (1) | DE602006016586D1 (hr) |
| DK (1) | DK1874766T3 (hr) |
| EA (1) | EA012115B1 (hr) |
| ES (1) | ES2350495T3 (hr) |
| HK (1) | HK1110866A1 (hr) |
| HR (1) | HRP20100629T1 (hr) |
| IL (1) | IL186023A (hr) |
| MA (1) | MA29403B1 (hr) |
| MX (1) | MX2007012438A (hr) |
| MY (1) | MY151075A (hr) |
| NO (1) | NO339699B1 (hr) |
| NZ (1) | NZ561900A (hr) |
| PE (1) | PE20061310A1 (hr) |
| PL (1) | PL1874766T3 (hr) |
| PT (1) | PT1874766E (hr) |
| SI (1) | SI1874766T1 (hr) |
| TW (1) | TWI377206B (hr) |
| WO (1) | WO2006108127A2 (hr) |
| ZA (1) | ZA200708071B (hr) |
Families Citing this family (19)
| 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 |
| SI2395002T1 (sl) | 2005-11-08 | 2014-10-30 | Vertex Pharmaceuticals Incorporated | Farmacevtski sestavek, vsebujoč heterociklični modulator prenašalcev z ATP-vezavno kaseto |
| 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. |
| SI2225230T1 (sl) * | 2007-12-07 | 2017-03-31 | Vertex Pharmaceuticals Incorporated | Trdne oblike 3-(6-(1-2,2-difluorobenzo(d)(1,3)dioxol-5-il)ciklopropan- karboksamido)-3-metilpiridin-2-il) benzojske kisline |
| US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
| PL2419104T3 (pl) * | 2009-04-13 | 2018-04-30 | Theravance Biopharma R&D Ip, Llc | Kombinacje agonistów receptora 5-HT4 i inhibitorów acetylocholinoesterazy do leczenia zaburzeń poznawczych |
| JP2013518085A (ja) | 2010-02-01 | 2013-05-20 | ノバルティス アーゲー | ＣＲＦ−１受容体アンタゴニストとしてのピラゾロ［５，１ｂ］オキサゾール誘導体 |
| WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| WO2011095450A1 (en) | 2010-02-02 | 2011-08-11 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の医薬組成物およびその投与 |
| RU2016122882A (ru) | 2013-11-12 | 2017-12-19 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний |
| US11642339B2 (en) * | 2017-07-31 | 2023-05-09 | Theravance Biopharma R&D Ip, Llc | Methods of treating symptoms of gastroparesis using velusetrag |
| WO2024061960A1 (en) | 2022-09-20 | 2024-03-28 | Alfasigma S.P.A. | Velusetrag for use in the treatment of chronic intestinal pseudo-obstruction (cipo) |
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| 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 |
| ES2080482T3 (es) * | 1990-12-28 | 1996-02-01 | Kyowa Hakko Kogyo Kk | Derivado de quinoleina. |
| US5571820A (en) | 1992-11-20 | 1996-11-05 | Taisho Pharmaceutical Co., Ltd. | Heterocyclic compound |
| 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. |
| TWI351282B (en) | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| US7728006B2 (en) | 2004-04-07 | 2010-06-01 | Theravance, Inc. | Quinolinone-carboxamide compounds as 5-HT4 receptor agonists |
| 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 |
| JP2008530225A (ja) | 2005-02-17 | 2008-08-07 | セラヴァンス， インコーポレーテッド | インダゾール−カルボキサミド化合物の結晶型 |
| NZ560828A (en) | 2005-03-02 | 2011-01-28 | Theravance Inc | Quinolinone compounds as 5-HT4 receptor agonists |
| TWI377206B (en) * | 2005-04-06 | 2012-11-21 | Theravance Inc | Crystalline form of a quinolinone-carboxamide compound |
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