AR074049A1 - Formas cristalinas de sales de (1r*,2r*,4r*)-2-(2-{[3-(4,7-dimetoxi-1h-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il ester de ácido isobutirico, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por bloqueadores del ca - Google Patents
Formas cristalinas de sales de (1r*,2r*,4r*)-2-(2-{[3-(4,7-dimetoxi-1h-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il ester de ácido isobutirico, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por bloqueadores del caInfo
- Publication number
- AR074049A1 AR074049A1 ARP090104038A ARP090104038A AR074049A1 AR 074049 A1 AR074049 A1 AR 074049A1 AR P090104038 A ARP090104038 A AR P090104038A AR P090104038 A ARP090104038 A AR P090104038A AR 074049 A1 AR074049 A1 AR 074049A1
- Authority
- AR
- Argentina
- Prior art keywords
- acid
- 2thita
- benzoimidazol
- amino
- bicyclo
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 abstract 7
- 238000010586 diagram Methods 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- KQNPFQTWMSNSAP-UHFFFAOYSA-N isobutyric acid Chemical compound CC(C)C(O)=O KQNPFQTWMSNSAP-UHFFFAOYSA-N 0.000 abstract 4
- 238000002441 X-ray diffraction Methods 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 3
- 239000000843 powder Substances 0.000 abstract 3
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 3
- 230000005855 radiation Effects 0.000 abstract 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 abstract 1
- 108090000312 Calcium Channels Proteins 0.000 abstract 1
- 102000003922 Calcium Channels Human genes 0.000 abstract 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 abstract 1
- 229940092714 benzenesulfonic acid Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 abstract 1
- 239000001530 fumaric acid Substances 0.000 abstract 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 1
- 239000011976 maleic acid Substances 0.000 abstract 1
- 229940098779 methanesulfonic acid Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-N naphthalene-2-sulfonic acid Chemical compound C1=CC=CC2=CC(S(=O)(=O)O)=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/14—Radicals substituted by nitrogen atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Cardiology (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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Sales cristalinas de (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico, los procesos para la preparacion del mismo, composiciones farmacéuticas que contienen dichas sales cristalinas, y su uso como medicamentos, en especial como bloqueadores de los canales de calcio. Reivindicacion 1: Una sal cristalina del compuesto (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico; en donde dicha sal cristalina consiste en: - 1 equivalente de (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico; - un componente ácido que consiste en 1 a 2 equivalentes de un ácido seleccionado desde el grupo que consiste en ácido bromhídrico, ácido sulfurico, ácido maleico, ádico fumárico, ácido metansulfonico, ácido paratoluensulfonico, ácido bencensulfonico, ácido naftalen-1,5-didulfonico, ácido naftalen-2-sulfonico, y ácido etansulfonico; y - 0 a 5 equivalentes de agua. Reivindicacion 7: Una sal cristalina del compuesto (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico de acuerdo con la reivindicacion 5, caracterizada por la presencia de máximos en el diagrama de difraccion de rayos X de polvo en los siguientes ángulos de refraccion 2thita: 5,07°, 8,19°, 10,15°, 15,26°, 17,61°, 20,39°, 22,63°, 23,93°, 24,27°, y 25,61°; en el cual dicho diagrama de difraccion de rayos X de polvo es obtenido mediante el uso de radiacion Cu Kalfa1; y la precision de los valores 2thita se encuentra en el rango de 2thita +/- 0,2°. Reivindicacion 12: Una sal cristalina del compuesto (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico de acuerdo con la reivindicacion 11, caracterizada por la presencia de máximos en el diagrama de difraccion de rayos X de polvo en los siguientes ángulos de refraccion 2thita: 5,27°, 8,05°, y 20,61°; en el cual dicho diagrama de difraccion de rayos X de polvo es obtenido mediante el uso de radiacion Cu Kalfa1; y la precision de los valores 2thita se encuentra en el rango de 2thita +/- 0,2°. Reivindicacion 14: Una sal cristalina del compuesto (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimetoxi-1H-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il éster de ácido isobutírico de acuerdo con la reivindicacion 13, caracterizada por la presencia de máximos en el diagrama de difraccion de rayos X de polvo en los siguiente ángulos de refraccion 2thita: 9,3°, 15,6°, y 17,3°; en el cual dicho diagrama de difraccion de rayos X de polvo es obtenido mediante el uso de radiacion Cu Kalfa1; y la precision de los valores 2thita se encuentra en el rango de 2thita +/- 0,2°.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IB2008054351 | 2008-10-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074049A1 true AR074049A1 (es) | 2010-12-22 |
Family
ID=41403088
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104038A AR074049A1 (es) | 2008-10-22 | 2009-10-21 | Formas cristalinas de sales de (1r*,2r*,4r*)-2-(2-{[3-(4,7-dimetoxi-1h-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il ester de ácido isobutirico, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por bloqueadores del ca |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US8492555B2 (es) |
| EP (1) | EP2344461B1 (es) |
| JP (1) | JP4913926B2 (es) |
| KR (1) | KR101331291B1 (es) |
| CN (1) | CN102186828B (es) |
| AR (1) | AR074049A1 (es) |
| AU (1) | AU2009306002B2 (es) |
| BR (1) | BRPI0920635B8 (es) |
| CA (1) | CA2740722C (es) |
| CL (1) | CL2011000921A1 (es) |
| DK (1) | DK2344461T3 (es) |
| ES (1) | ES2618178T3 (es) |
| HU (1) | HUE032044T2 (es) |
| IL (1) | IL212405A (es) |
| MA (1) | MA32817B1 (es) |
| MX (1) | MX342043B (es) |
| MY (1) | MY160597A (es) |
| NZ (1) | NZ592996A (es) |
| RU (1) | RU2516247C2 (es) |
| TW (1) | TWI463981B (es) |
| WO (1) | WO2010046857A1 (es) |
| ZA (1) | ZA201103734B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102186828B (zh) | 2008-10-22 | 2014-07-16 | 埃科特莱茵药品有限公司 | 异丁酸(1r*,2r*,4r*)-2-(2-{[3-(4,7-二甲氧基-1h-苯并咪唑-2-基)-丙基]-甲基-胺基}-乙基)-5-苯基-二环[2.2.2]辛-5-烯-2-基酯的盐 |
| KR101836552B1 (ko) * | 2010-10-20 | 2018-03-08 | 아이도시아 파마수티컬즈 리미티드 | 바이시클로[2.2.2]옥탄-2-온 화합물의 부분입체선택적 제조 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4129603A1 (de) * | 1991-09-06 | 1993-03-11 | Thomae Gmbh Dr K | Kondensierte 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| US6268377B1 (en) * | 1998-09-28 | 2001-07-31 | Merck & Co., Inc. | Method for treating androgen-related conditions |
| CA2462913A1 (en) * | 2001-10-10 | 2003-04-17 | Aryx Therapeutics | Mibefradil-based compounds as calcium channel blockers useful in the treatment of hypertension and angina |
| WO2008132679A1 (en) * | 2007-04-27 | 2008-11-06 | Actelion Pharmaceuticals Ltd | Bridged six-membered ring compounds |
| BRPI0911538B1 (pt) | 2008-04-25 | 2021-05-18 | Idorsia Pharmaceuticals Ltd | Composição farmacêutica contendo um composto derivado de benzimidazol e uso do composto |
| CN102186828B (zh) | 2008-10-22 | 2014-07-16 | 埃科特莱茵药品有限公司 | 异丁酸(1r*,2r*,4r*)-2-(2-{[3-(4,7-二甲氧基-1h-苯并咪唑-2-基)-丙基]-甲基-胺基}-乙基)-5-苯基-二环[2.2.2]辛-5-烯-2-基酯的盐 |
| US8314253B2 (en) | 2008-10-22 | 2012-11-20 | Actelion Pharmaceuticals Ltd. | Bridged tetrahydronaphthalene derivatives |
| WO2010046729A2 (en) | 2008-10-23 | 2010-04-29 | Actelion Pharmaceuticals Ltd | Tetrahydronaphthalene compounds |
-
2009
- 2009-10-21 CN CN200980141248.7A patent/CN102186828B/zh not_active Expired - Fee Related
- 2009-10-21 NZ NZ592996A patent/NZ592996A/xx not_active IP Right Cessation
- 2009-10-21 EP EP09752894.7A patent/EP2344461B1/en active Active
- 2009-10-21 AR ARP090104038A patent/AR074049A1/es unknown
- 2009-10-21 CA CA2740722A patent/CA2740722C/en active Active
- 2009-10-21 HU HUE09752894A patent/HUE032044T2/en unknown
- 2009-10-21 MX MX2011004138A patent/MX342043B/es active IP Right Grant
- 2009-10-21 KR KR1020117011728A patent/KR101331291B1/ko not_active Expired - Fee Related
- 2009-10-21 JP JP2011532754A patent/JP4913926B2/ja not_active Expired - Fee Related
- 2009-10-21 BR BRPI0920635A patent/BRPI0920635B8/pt not_active IP Right Cessation
- 2009-10-21 US US13/125,443 patent/US8492555B2/en not_active Expired - Fee Related
- 2009-10-21 RU RU2011120042/04A patent/RU2516247C2/ru active
- 2009-10-21 AU AU2009306002A patent/AU2009306002B2/en not_active Ceased
- 2009-10-21 WO PCT/IB2009/054637 patent/WO2010046857A1/en not_active Ceased
- 2009-10-21 TW TW098135673A patent/TWI463981B/zh not_active IP Right Cessation
- 2009-10-21 DK DK09752894.7T patent/DK2344461T3/en active
- 2009-10-21 MY MYPI2011001766A patent/MY160597A/en unknown
- 2009-10-21 ES ES09752894.7T patent/ES2618178T3/es active Active
-
2011
- 2011-04-17 IL IL212405A patent/IL212405A/en active IP Right Grant
- 2011-04-21 CL CL2011000921A patent/CL2011000921A1/es unknown
- 2011-05-20 MA MA33872A patent/MA32817B1/fr unknown
- 2011-05-20 ZA ZA2011/03734A patent/ZA201103734B/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2563323T3 (es) | Procedimiento para la preparación de un sólido cristalino a partir de derivados de ácido glicin-N,N-diacético | |
| AR083870A1 (es) | Inhibidores de la replicacion del vih | |
| UY32490A (es) | Inhibidores de beta-secretasa | |
| BR112014010576B8 (pt) | compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos | |
| HRP20220182T1 (hr) | Kristalni oblici inhibitora prolil hidroksilaze | |
| BR112015012425A2 (pt) | composto, composição farmacêutica, método e medicamento para o tratamento de doenças medicadas pela proteína parp-1 e uso do composto | |
| AR066130A1 (es) | Formas cristalinas de saxagliptina y procesos para preparar las mismas | |
| HN2010002121A (es) | 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak | |
| UY33044A (es) | Derivados del acido carbamoil-metil-amino-acetico sustituido como inhibidores de nep novedosos | |
| AR088091A1 (es) | Derivados de isoxazol-5-il-pirazin-2-amina como inhibidores de la quinasa atr y polimorfos de los mismos | |
| DOP2013000194A (es) | Imidazo[5,1-f][1,2,4] triazinas para el tratamiento de trastornos neurologicos | |
| CO6311106A2 (es) | Derivados novedosos del acido oleanólico con saturacion del anillo c | |
| CL2012000953A1 (es) | Procedimientos de preparacion de derivados espiro[furo[2,3-f][1,3]benzodioxol-7,3`-indol]-2`(1`h)-onas. | |
| PE20130246A1 (es) | COMPUESTOS DEL COMPLEJO DE Fe(III) PARA EL TRATAMIENTO Y PROFILAXIS DE LOS SINTOMAS DE DEFICIENCIA DE HIERRO Y LAS ANEMIAS POR DEFICIENCIA DE HIERRO | |
| PE20080131A1 (es) | Agentes antifungicos | |
| PE20140002A1 (es) | Proceso de elaboracion para derivados de pirimidina | |
| CO6852073A2 (es) | Antagonistas trpm8 y su uso en tratamientos | |
| BR112014014060A2 (pt) | processo para a preparação de travoprosta | |
| CU20130116A7 (es) | Derivados de heteroarilo como moduladores de nachr alfa 7 | |
| EA201391371A1 (ru) | Фармацевтическая композиция ситаглиптина | |
| AR074049A1 (es) | Formas cristalinas de sales de (1r*,2r*,4r*)-2-(2-{[3-(4,7-dimetoxi-1h-benzoimidazol-2-il)-propil]-metil-amino}-etil)-5-fenil-biciclo[2.2.2]oct-5-en-2-il ester de ácido isobutirico, composicion farmaceutica que las comprende y su uso en el tratamiento de enfermedades mediadas por bloqueadores del ca | |
| BR112014009266A2 (pt) | processo para a preparação de ácidos isoxazolil-metóxi-nicotínicos | |
| PE20131327A1 (es) | Forma cristalina delta de la sal de arginina de perindoprilo, su procedimiento de preparacion, y las composiciones farmaceuticas que la contienen | |
| AR083818A1 (es) | Procedimiento para la preparacion de derivados de acido 3-(6-amino-piridin-3-il)-2-acrilico | |
| AR085163A1 (es) | Compuesto de 4-amino-2-butenamida, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion y usos |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |