AR074021A1 - Compuestos heterociclicos fusionados como moduladores del canal ionico - Google Patents
Compuestos heterociclicos fusionados como moduladores del canal ionicoInfo
- Publication number
- AR074021A1 AR074021A1 ARP090104206A ARP090104206A AR074021A1 AR 074021 A1 AR074021 A1 AR 074021A1 AR P090104206 A ARP090104206 A AR P090104206A AR P090104206 A ARP090104206 A AR P090104206A AR 074021 A1 AR074021 A1 AR 074021A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- optionally substituted
- aryl
- alkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 108090000862 Ion Channels Proteins 0.000 title 1
- 102000004310 Ion Channels Human genes 0.000 title 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 10
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- -1 -C (O) R Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Su uso en el tratamiento de diversos estados patologicos, que incluyen enfermedades cardiovasculares y diabetes. Composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de la formula (1), en donde: R1 es hidrogeno o alquilo C1-6 opcionalmente sustituido con 1, 2 o 3 grupos seleccionados de hidroxilo, alcoxi, halo, -C(O)R, arilo, cicloalquilo, heterociclilo y heteroarilo, en donde dichos grupos arilo, cicloalquilo, heterociclilo o heteroarilo están opcionalmente sustituidos con uno, dos o tres grupos seleccionados, de modo independiente, de halo, hidroxilo, alquilo, -C(O)R, haloalquilo, alcoxi, arilo o cicloalquilo; en donde R es hidroxi, alcoxi o -NH2; R2 y R3 son cada uno, de modo independiente, hidrogeno, halo, alcoxi C1-6, opcionalmente sustituido alquilo C1-6, -CF3, -O-CF 3 o -CN, o R2 y R3, tomados junto con el carbono al que ambos están unidos, forman un cicloalquilo opcionalmente sustituido; R4 es fenilo opcionalmente sustituido con 1, 2 o 3 sustituyentes de modo independiente, seleccionados del grupo que consiste en alquilo C1-6, cicloalquilo, arilo, heteroarilo, heterociclilo, halo, -NO2, -CF3, -O-CF3, -CN, -O-R8, -S-R8, -N(R8)(R9), -S(=O)-R8, -S(=O)2R8, -S(=O)2-N(R8)(R9), -S(=O)2-O-R8, -N(R8)-C(O)-R9, -N(R8)-C(O)-O-R9, -N(R8)-C(O)-NR8)(R9), -C(O)-R8, -C(O)-O-R8, -C(O)-N(R8)(R9) y -N(R8)-S(=O)2-R9, en donde cada uno de dichos alquilo, cicloalquilo, arilo, heteroarilo y heterociclilo también está opcionalmente sustituido con halo, -NO2, -CF3, -O-CF3, -N(R8)(R9), -C(O)-R8, -C(O)-O-R8, -C(O)-N(R8)(R9), -CN, o -O-R8; en donde R8 y R9 están seleccionados, de modo independiente, del grupo que consiste en hidrogeno, alquilo C1-6, heterociclilo, arilo y heteroarilo, en donde el alquilo, heterociclilo, arilo y heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados, de modo independiente, de halo, alquilo, mono- o dialquilamino, alquilo o arilo, R5 y R6 son cada uno, de modo independiente, hidrogeno, halo, alcoxi, opcionalmente sustituido alquilo C1-6, -CF3, -O-CF3 o -CN, o R5 y R6, tomados junto con el carbono al que ambos están unidos, forman un cicloalquilo opcionalmente sustituido; R7 es hidrogeno, halo, ciano o alquilo C1-6 opcionalmente sustituido con hidroxilo, alcoxi, halo o -C(O)R, X1 y X2 son, de modo independiente, -N= o -C(R10)=, en donde R10 está seleccionado de hidrogeno, halo, hidroxilo, alquilo C1-6, alcoxi C1-6, -CF3, -O-CF3, -CN, o -N(R8)(R9); o una de sus sales, ésteres, profármacos o solvatos farmacéuticamente aceptables.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10978808P | 2008-10-30 | 2008-10-30 | |
| US16101109P | 2009-03-17 | 2009-03-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR074021A1 true AR074021A1 (es) | 2010-12-15 |
Family
ID=41683383
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104206A AR074021A1 (es) | 2008-10-30 | 2009-10-30 | Compuestos heterociclicos fusionados como moduladores del canal ionico |
Country Status (4)
| Country | Link |
|---|---|
| US (3) | US20100113514A1 (es) |
| AR (1) | AR074021A1 (es) |
| TW (1) | TW201028382A (es) |
| WO (1) | WO2010074807A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090247535A1 (en) * | 2008-03-26 | 2009-10-01 | Duke University | Use of ranolazine for non-cardiovascular disorders |
| GB201106750D0 (en) * | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| KR20140033377A (ko) | 2011-05-10 | 2014-03-18 | 길리애드 사이언시즈, 인코포레이티드 | 나트륨 채널 조절제로서의 융합된 헤테로시클릭 화합물 |
| NO3175985T3 (es) | 2011-07-01 | 2018-04-28 | ||
| TW201837023A (zh) | 2011-07-01 | 2018-10-16 | 美商基利科學股份有限公司 | 作為離子通道調節劑之稠合雜環化合物 |
| AU2013203252B2 (en) | 2012-01-27 | 2015-08-20 | Gilead Sciences, Inc. | Combination therapies using late sodium ion channel blockers and potassium ion channel blockers |
| AU2014364783B2 (en) | 2013-12-19 | 2017-01-05 | Gilead Sciences, Inc. | Fused heterocyclic compounds as ion channel modulators |
| EP3092227B1 (en) * | 2014-01-09 | 2018-07-11 | Orion Corporation | Bicyclic heterocyclic derivatives as bromodomain inhibitors |
| WO2018098491A1 (en) | 2016-11-28 | 2018-05-31 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| ES2992063T3 (es) | 2016-11-28 | 2024-12-09 | Praxis Prec Medicines Inc | Compuestos y procedimientos de uso de los mismos |
| US11492345B2 (en) | 2017-02-13 | 2022-11-08 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| WO2018187480A1 (en) | 2017-04-04 | 2018-10-11 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| WO2019035951A1 (en) | 2017-08-15 | 2019-02-21 | Praxis Precision Medicines, Inc. | COMPOUNDS AND THEIR METHODS OF USE |
| CN112423760A (zh) | 2018-05-30 | 2021-02-26 | 普拉克西斯精密药物股份有限公司 | 离子通道调节剂 |
| EA202092908A1 (ru) | 2018-09-28 | 2021-05-14 | Праксис Пресижн Медсинз, Инк. | Модуляторы ионных каналов |
| US11773099B2 (en) | 2019-05-28 | 2023-10-03 | Praxis Precision Medicines, Inc. | Compounds and their methods of use |
| US11505554B2 (en) | 2019-05-31 | 2022-11-22 | Praxis Precision Medicines, Inc. | Substituted pyridines as ion channel modulators |
| US11279700B2 (en) | 2019-05-31 | 2022-03-22 | Praxis Precision Medicines, Inc. | Ion channel modulators |
| US11767325B2 (en) | 2019-11-26 | 2023-09-26 | Praxis Precision Medicines, Inc. | Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US4902514A (en) | 1988-07-21 | 1990-02-20 | Alza Corporation | Dosage form for administering nilvadipine for treating cardiovascular symptoms |
| EP0556393B1 (en) | 1990-11-06 | 2000-07-26 | Yamanouchi Pharmaceutical Co. Ltd. | Fused pyrazine derivative |
| US5250679A (en) | 1991-10-18 | 1993-10-05 | Genentech, Inc. | Nonpeptidyl platelet aggregation inhibitors having specificity for the GPIIb III.sub. receptor |
| JPH06228112A (ja) | 1993-02-05 | 1994-08-16 | Yamanouchi Pharmaceut Co Ltd | （１ｈ，４ｈ）キノキサリン誘導体 |
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| CN1067387C (zh) | 1994-09-27 | 2001-06-20 | 山之内制药株式会社 | 1,2,3,4－四氢喹喔啉二酮衍生物 |
| DE19624808A1 (de) | 1996-06-21 | 1998-01-02 | Basf Ag | Pyrrolylchinoxalindione, ihre Herstellung und Verwendung |
| SE9800836D0 (sv) | 1998-03-13 | 1998-03-13 | Astra Ab | New Compounds |
| JP2000281676A (ja) | 1999-01-25 | 2000-10-10 | Yamanouchi Pharmaceut Co Ltd | Ａｍｐａ拮抗化合物の新規製造法 |
| JP2000309586A (ja) | 1999-02-26 | 2000-11-07 | Kyorin Pharmaceut Co Ltd | ６−置換−７−ヘテロキノキサリンカルボン酸誘導体とその付加塩及びそれらの製造方法 |
| US6498154B1 (en) * | 1999-05-04 | 2002-12-24 | Wyeth | Cyclic regimens using quinazolinone and benzoxazine derivatives |
| US6358948B1 (en) * | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| WO2000066560A1 (en) * | 1999-05-04 | 2000-11-09 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| AU2002220241A1 (en) | 2000-12-01 | 2002-06-11 | Iconix Pharmaceuticals, Inc. | Parb inhibitors |
| EP1377559A4 (en) * | 2001-03-08 | 2005-09-28 | Incyte San Diego Inc | MOLECULES ACTIVATING AN RXR RECEPTOR |
| US20030114448A1 (en) | 2001-05-31 | 2003-06-19 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| US20030220344A1 (en) * | 2002-04-04 | 2003-11-27 | Luiz Belardinelli | Method of treating arrhythmias |
| AR043059A1 (es) | 2002-11-12 | 2005-07-13 | Bayer Pharmaceuticals Corp | Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos |
| WO2005092894A1 (en) | 2004-03-01 | 2005-10-06 | Eli Lilly And Company | Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms |
| CN101365696A (zh) | 2004-07-28 | 2009-02-11 | Irm责任有限公司 | 作为类固醇激素核受体调节剂的化合物和组合物 |
| EP1874753A2 (en) * | 2005-04-14 | 2008-01-09 | Smithkline Beecham Corporation | Compounds, compositions and methods |
| CN101316821A (zh) * | 2005-09-30 | 2008-12-03 | 詹森药业有限公司 | 作为rxr激动剂用于治疗异常脂肪血症、高胆固醇血症和糖尿病的二氢-[1h]-喹啉-2-酮衍生物 |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| WO2008144483A2 (en) | 2007-05-18 | 2008-11-27 | Armgo Pharma, Inc. | Agents for treating disorders involving modulation of ryanodine receptors |
-
2009
- 2009-10-28 US US12/607,823 patent/US20100113514A1/en not_active Abandoned
- 2009-10-28 WO PCT/US2009/062386 patent/WO2010074807A1/en not_active Ceased
- 2009-10-30 TW TW098136971A patent/TW201028382A/zh unknown
- 2009-10-30 AR ARP090104206A patent/AR074021A1/es unknown
-
2012
- 2012-12-06 US US13/706,786 patent/US8664379B2/en active Active
-
2013
- 2013-12-10 US US14/101,740 patent/US8952007B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2010074807A1 (en) | 2010-07-01 |
| US8952007B2 (en) | 2015-02-10 |
| US8664379B2 (en) | 2014-03-04 |
| US20130096122A1 (en) | 2013-04-18 |
| US20100113514A1 (en) | 2010-05-06 |
| TW201028382A (en) | 2010-08-01 |
| US20140094460A1 (en) | 2014-04-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |