AR077898A1 - Metilpirrolopirimidincarboxamidas - Google Patents
MetilpirrolopirimidincarboxamidasInfo
- Publication number
- AR077898A1 AR077898A1 ARP100103064A ARP100103064A AR077898A1 AR 077898 A1 AR077898 A1 AR 077898A1 AR P100103064 A ARP100103064 A AR P100103064A AR P100103064 A ARP100103064 A AR P100103064A AR 077898 A1 AR077898 A1 AR 077898A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkoxy
- hydroxyl
- alkyl
- optionally substituted
- hydrogen
- Prior art date
Links
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 14
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 11
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 102000011016 Type 5 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 abstract 1
- 108010037581 Type 5 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 abstract 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000003709 fluoroalkyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Los compuesto de la presente son inhibidores efectivos de la fosfodiesteresa tipo 5 Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) en donde R1 es -CH2-cicloalquilo C3-6 o alquilo C1-4 que está opcionalmente sustituido por R11; R11 es alcoxilo C1-4 o hidroxilo; R2 es hidrogeno o alquilo C1-4; R21 es hidrogeno o fluor; R22 es hidrogeno, halogeno, alquilo C1-4, alcoxilo C1-4, hidroxilo, fluoroalcoxilo C1-4, -C(O)-alquilo C1-4, o fluoroalquilo C1-4; o R21 y R22 se combinan para formar un grupo -O-CH2-O-; R23 es hidrogeno, halogeno, alquilo C1-4, alcoxilo C1-4, hidroxilo o fluoroalcoxilo C1-4; o R22 y R23 se combinan para formar un grupo -O-CH2-O-; R24 es hidrogeno; Y es -(CH2)n-, n es 0 o 1; R3 es un anillo heterocíclico saturado de 4 a 7 miembros que contiene un átomo de nitrogeno y opcionalmente un átomo de oxígeno, estando dicho anillo heterocíclico opcionalmente sustituido por R4 y/o por uno o dos sustituyentes R5, o un grupo cicloalquilo C3-6 sustituido por R6 y opcionalmente sustituido por R61; R4 es -C(O)-H, -C(O)-alquilo C1-4, en donde el grupo alquilo C1-4 está opcionalmente sustituido por R41, -C(O)-cicloalquilo C3-6, en donde el grupo cicloalquilo C3-6 está opcionalmente sustituido por R42, o -C(O)-O-alquilo C1-4, en donde el grupo alquilo C1-4 está opcionalmente sustituido por R43; R41 es alcoxilo C1-4 o hidroxilo; R42 es alcoxilo C1-4 o hidroxilo; R43 es alcoxilo C1-4 o hidroxilo; si solamente un sustituyente R5 está presente entonces R5 es alcoxilo C1-4, halogeno, alquilo C1-4 o hidroxilo, si dos sustituyentes R5 están presentes, éstos son idénticos y están unidos al mismo átomo de carbono y son seleccionados de halogeno o alquilo C1-4 o conjuntamente con el átomo de carbono, al cual se encuentran unidos, forman un anillo ciclopropano unido a espiro; R6 es -NH-C(O)-R7, -C(O)-NR8R9, halogeno, hidroxilo o NH2; R61 es halogeno, alquilo C1-4 o hidroxilo; R7 es hidrogeno, alquilo C1-4, que está opcionalmente sustituido por R71, cicloalquilo C3-6, que está opcionalmente sustituido por R72, o alcoxilo C1-4, que está opcionalmente sustituido por R73; R71 es alcoxilo C1-4 o hidroxilo; R72 es alcoxilo C1-4 o hidroxilo; R73 es alcoxilo C1-4 o hidroxilo; R8 es hidrogeno; R9 es alquilo C1-4, que está opcionalmente sustituido por R91, o cicloalquilo C3-6, que está opcionalmente sustituido por R92; R91 es alcoxilo C1-4 o hidroxilo; R92 es alcoxilo C1-4 o hidroxilo; una sal del mismo, o un estereoisomero del compuesto o una sal del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09168685 | 2009-08-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077898A1 true AR077898A1 (es) | 2011-09-28 |
Family
ID=41698276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103064A AR077898A1 (es) | 2009-08-26 | 2010-08-23 | Metilpirrolopirimidincarboxamidas |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US8927557B2 (es) |
| EP (1) | EP2470536B1 (es) |
| JP (1) | JP5791606B2 (es) |
| KR (1) | KR101762884B1 (es) |
| CN (1) | CN102574861B (es) |
| AR (1) | AR077898A1 (es) |
| AU (1) | AU2010288550B2 (es) |
| BR (1) | BR112012003616A8 (es) |
| CA (1) | CA2771938A1 (es) |
| CL (1) | CL2012000271A1 (es) |
| CO (1) | CO6491110A2 (es) |
| EA (1) | EA021103B1 (es) |
| EC (1) | ECSP12011678A (es) |
| ES (1) | ES2529563T3 (es) |
| IL (1) | IL218126A (es) |
| MX (1) | MX2012002432A (es) |
| MY (1) | MY159031A (es) |
| NZ (1) | NZ598777A (es) |
| PE (1) | PE20121133A1 (es) |
| SG (1) | SG178481A1 (es) |
| TN (1) | TN2012000034A1 (es) |
| TW (1) | TWI471327B (es) |
| UA (1) | UA106628C2 (es) |
| WO (1) | WO2011023693A1 (es) |
| ZA (1) | ZA201200616B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
| JP5980318B2 (ja) * | 2011-06-17 | 2016-08-31 | タケダ ゲー・エム・ベー・ハーＴａｋｅｄａ ＧｍｂＨ | 新規のフタラジノン−ピロロピリミジンカルボキサミド誘導体 |
| WO2014128109A1 (en) | 2013-02-21 | 2014-08-28 | Bayer Pharma Aktiengesellschaft | Forms of methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridino-3-yl]pyrimidino-5-yl}methyl carbamate |
| JP2020097527A (ja) * | 2017-03-31 | 2020-06-25 | 武田薬品工業株式会社 | 複素環化合物 |
| CN107286160A (zh) * | 2017-06-05 | 2017-10-24 | 毛佳婧 | 一种抗肝炎药物的哌啶并吡啶并吡唑‑锌配合物的制备方法 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2754260B1 (fr) | 1996-10-04 | 1998-10-30 | Adir | Nouveaux derives substitues de biphenyle ou de phenylpyridine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US6187777B1 (en) * | 1998-02-06 | 2001-02-13 | Amgen Inc. | Compounds and methods which modulate feeding behavior and related diseases |
| WO2001094350A1 (en) | 2000-06-07 | 2001-12-13 | Almirall Prodesfarma S.A. | 6-phenylpyrrolopyrimidinedione derivatives |
| WO2002064598A1 (en) | 2001-02-14 | 2002-08-22 | Warner-Lambert Company Llc | Thieno'2,3-d pyrimidindione derivatives as matrix metalloproteinase inhibitors |
| CN100374441C (zh) * | 2003-06-06 | 2008-03-12 | 天津倍方科技发展有限公司 | 二氢吡咯[2，3-d]嘧啶-4-酮衍生物，其制备方法及其制药用途 |
| US20050124623A1 (en) * | 2003-11-26 | 2005-06-09 | Bender John A. | Diazaindole-dicarbonyl-piperazinyl antiviral agents |
| DK1807072T3 (da) | 2004-10-29 | 2009-03-16 | Lilly Co Eli | Cycloalkyllactamderivater som inhibitorer af 11-beta-hydroxysteroid-dehydrogenase 1 |
| WO2006095009A1 (en) * | 2005-03-09 | 2006-09-14 | Nycomed Gmbh | Amido-substituted 6-phenylphenanthridines |
| AU2007293774C1 (en) | 2006-09-07 | 2014-12-18 | Albert Einstein College Of Medicine, Inc. | Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases |
| JP4837701B2 (ja) * | 2007-04-20 | 2011-12-14 | 田辺三菱製薬株式会社 | 医薬組成物 |
| AR070454A1 (es) * | 2008-02-27 | 2010-04-07 | Nycomed Gmbh | Pirrolopirimidincarboxamidas y composiciones farmaceuticas que las comprenden |
-
2010
- 2010-08-23 AR ARP100103064A patent/AR077898A1/es unknown
- 2010-08-24 US US13/390,940 patent/US8927557B2/en not_active Expired - Fee Related
- 2010-08-24 BR BR112012003616A patent/BR112012003616A8/pt not_active Application Discontinuation
- 2010-08-24 CA CA2771938A patent/CA2771938A1/en not_active Abandoned
- 2010-08-24 MY MYPI2012000701A patent/MY159031A/en unknown
- 2010-08-24 JP JP2012526038A patent/JP5791606B2/ja not_active Expired - Fee Related
- 2010-08-24 SG SG2012011219A patent/SG178481A1/en unknown
- 2010-08-24 NZ NZ598777A patent/NZ598777A/xx not_active IP Right Cessation
- 2010-08-24 KR KR1020127006983A patent/KR101762884B1/ko not_active Expired - Fee Related
- 2010-08-24 AU AU2010288550A patent/AU2010288550B2/en not_active Ceased
- 2010-08-24 MX MX2012002432A patent/MX2012002432A/es active IP Right Grant
- 2010-08-24 ES ES10744949.8T patent/ES2529563T3/es active Active
- 2010-08-24 PE PE2012000214A patent/PE20121133A1/es not_active Application Discontinuation
- 2010-08-24 EP EP10744949.8A patent/EP2470536B1/en active Active
- 2010-08-24 EA EA201200322A patent/EA021103B1/ru not_active IP Right Cessation
- 2010-08-24 UA UAA201203246A patent/UA106628C2/uk unknown
- 2010-08-24 WO PCT/EP2010/062329 patent/WO2011023693A1/en not_active Ceased
- 2010-08-24 CN CN201080046838.4A patent/CN102574861B/zh not_active Expired - Fee Related
- 2010-08-25 TW TW99128511A patent/TWI471327B/zh not_active IP Right Cessation
-
2012
- 2012-01-24 TN TNP2012000034A patent/TN2012000034A1/en unknown
- 2012-01-25 ZA ZA2012/00616A patent/ZA201200616B/en unknown
- 2012-02-01 CL CL2012000271A patent/CL2012000271A1/es unknown
- 2012-02-02 CO CO12018550A patent/CO6491110A2/es unknown
- 2012-02-15 EC ECSP12011678 patent/ECSP12011678A/es unknown
- 2012-02-15 IL IL218126A patent/IL218126A/en not_active IP Right Cessation
-
2014
- 2014-11-19 US US14/547,938 patent/US9376442B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR129635A2 (es) | Moduladores de tetrahidropiridopirazina de gpr6 | |
| AR066155A1 (es) | Compuestos de pirazol, simil tiroideo, composicion farmaceutica, proceso y uso en terapia | |
| PE20130155A1 (es) | Derivados de ariletinilo | |
| PE20160608A1 (es) | Compuestos de quinolina selectivamente sustituida | |
| MX2022008434A (es) | Herbicidas de piridazinona. | |
| AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| PE20121159A1 (es) | DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR | |
| AR070454A1 (es) | Pirrolopirimidincarboxamidas y composiciones farmaceuticas que las comprenden | |
| PE20190656A1 (es) | Compuestos de tiazolo-piridina sustituida como inhibidores de malt1 | |
| PE20130375A1 (es) | Compuestos de triazolopiridinas y triazolopirazinas inhibidores de c-met y composiciones de los mismos | |
| AR086983A1 (es) | Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak | |
| AR054621A1 (es) | 1-aril-4-ciclopropilpirazoles sustituidos | |
| AR061923A1 (es) | Compuestos derivados de benzofuran-piperidina | |
| EA200970510A1 (ru) | Гетеромоноциклическое соединение и его применение | |
| AR056536A1 (es) | Compuestos de 2-amino-5- [4-(difluormetoxi)fenil]-5-fenilimidazolona como inhibidores de la beta secretasa (bace) | |
| MX2017002241A (es) | Compuestos de aminopirimidina como inhibidores de jak. | |
| AR075854A1 (es) | Inhibidores de beta- secretasa | |
| CO6210701A2 (es) | Derivados de amidas del acido 6,7-dihidro-5h-imidazo[1,2-a]imidazol-3-carboxilico | |
| AR097024A1 (es) | Derivados sustituidos de quinazolin-4-ona | |
| AR087288A1 (es) | Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a | |
| AR059622A1 (es) | Quinolonas utiles como inhibidores de la sintetasa del oxido nitrico inducibles | |
| AR075951A1 (es) | Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mek | |
| AR061603A1 (es) | Derivados de etenilcarboxamidas microbicidas | |
| AR061369A1 (es) | Derivados de pirimidina y composiciones farmaceuticas que los comprenden | |
| AR075583A1 (es) | Derivados de isoxazol/o-piridina con eslabon etilo o etenilo |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |