PE20161315A1 - Compuestos de pirazolona y usos de los mismos - Google Patents
Compuestos de pirazolona y usos de los mismosInfo
- Publication number
- PE20161315A1 PE20161315A1 PE2016001440A PE2016001440A PE20161315A1 PE 20161315 A1 PE20161315 A1 PE 20161315A1 PE 2016001440 A PE2016001440 A PE 2016001440A PE 2016001440 A PE2016001440 A PE 2016001440A PE 20161315 A1 PE20161315 A1 PE 20161315A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- optionally substituted
- pyrazol
- phenoxy
- dihydro
- Prior art date
Links
- ZRHUHDUEXWHZMA-UHFFFAOYSA-N 1,4-dihydropyrazol-5-one Chemical class O=C1CC=NN1 ZRHUHDUEXWHZMA-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- -1 1- (4- (tert-butyl) benzyl) -4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-3-yl Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 102000023984 PPAR alpha Human genes 0.000 abstract 1
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 abstract 1
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 208000036142 Viral infection Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 230000009385 viral infection Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
-
- 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
- C07D401/10—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 aromatic rings
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invencion se refiere a compuestos de la formula I o sales farmaceuticamente aceptables de los mismos, donde: R1 y R2 son cada uno -C1-6 alquilo o CH3 opcionalmente sustituidos por halogeno o R1 y R2 forman juntos -C3-6 cicloalquilo opcionalmente sustituido por halogeno, C1-6 alquilo y -CF3; R3 es un arilo, heteroarilo opcionalmente sustituido, entre otros; R4 es un heteroarilo, -C1-2alquilo-arilo, opcionalmente sustituido, entre otros. Son compuestos preferidos: acido 2-(4-(3-(1-(4-(ter-butil)bencil)-4,4-dimetil-5-oxo-4,5-dihidro-1H-pirazol-3-il)propil)fenoxi)-2-metilpropanoico; 2-(4-(3-(1-(4-(ter-butil)bencil)-4,4-dimetil-5-oxo-4,5-dihidro-1H-pirazol-3-il)propil)fenoxi)-2-metil-N-(fenilsulfonil)propanamida, entre otros. Tambien se refiere a una composicion y un metodo de tratamiento. Dichos compuestos actuan como antagonistas selectivos del peroxisoma proliferador activado del receptor a (PPARalfa) siendo utiles en el tratamiento de cancer de prostata, mama, entre otros, e infecciones virales tales como VIH y VHC
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461939955P | 2014-02-14 | 2014-02-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20161315A1 true PE20161315A1 (es) | 2016-12-25 |
Family
ID=53800550
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016001440A PE20161315A1 (es) | 2014-02-14 | 2015-02-09 | Compuestos de pirazolona y usos de los mismos |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9862708B2 (es) |
| EP (1) | EP3105205A4 (es) |
| JP (1) | JP2017505804A (es) |
| KR (1) | KR20160115996A (es) |
| CN (1) | CN106029640B (es) |
| AU (1) | AU2015217450A1 (es) |
| BR (1) | BR112016017781A2 (es) |
| CA (1) | CA2937542A1 (es) |
| EA (1) | EA201691342A1 (es) |
| IL (1) | IL247148A0 (es) |
| MX (1) | MX2016010436A (es) |
| NZ (1) | NZ722345A (es) |
| PE (1) | PE20161315A1 (es) |
| SG (1) | SG11201606149YA (es) |
| WO (1) | WO2015123133A1 (es) |
| ZA (1) | ZA201605222B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3128377A1 (en) * | 2019-02-01 | 2020-08-06 | University Of South Carolina | Bicyclic pyridine compositions and methods of using the same for cancer therapy |
| WO2021204589A1 (en) | 2020-04-07 | 2021-10-14 | Bayer Aktiengesellschaft | Substituted thiazolopyridines, salts thereof and their use as herbicidally active substances |
| WO2022194843A1 (en) | 2021-03-19 | 2022-09-22 | Bayer Aktiengesellschaft | Substituted 1,2,4-thiadiazoles, salts thereof and their use as herbicidally active substances |
| AR125453A1 (es) | 2021-04-27 | 2023-07-19 | Bayer Ag | Piridazinonas sustituidas, sales o n-óxidos de las mismas y su uso como sustancias herbicidamente activas |
| AU2022330302A1 (en) | 2021-08-17 | 2024-02-22 | Bayer Aktiengesellschaft | Substituted 1,2,4-thiadiazolyl nicotinamides, salts or n-oxides thereof and their use as herbicidally active substances |
| TW202328150A (zh) | 2021-09-07 | 2023-07-16 | 德商拜耳廠股份有限公司 | 經取代之噻唑并吡啶、其鹽及其作為除草活性物質之用途 |
| TW202328151A (zh) | 2021-09-07 | 2023-07-16 | 德商拜耳廠股份有限公司 | 經取代之2,3-二氫[1,3]噻唑并[4,5-b]吡啶、其鹽及其作為除草活性物質之用途 |
| AR127618A1 (es) | 2021-11-29 | 2024-02-14 | Bayer Ag | Dihidropiranopiridinas sustituidas, sales o n-óxidos de las mismas y su uso como sustancias herbicidamente activas |
| EP4238973A1 (en) | 2022-03-04 | 2023-09-06 | Bayer AG | Substituted 1,2,4-thiadiazolyl isonicotinamides, salts or n-oxides thereof and their use as herbicidally active substances |
| EP4238972A1 (en) | 2022-03-04 | 2023-09-06 | Bayer AG | Substituted 1,2,4-thiadiazolyl picolinamides, salts or n-oxides thereof and their use as herbicidally active substances |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3244593A (en) | 1963-06-12 | 1966-04-05 | Endo Lab | Pharmaceutically active substituted 5-pyrazolones |
| US4719175A (en) | 1982-05-03 | 1988-01-12 | Polaroid Corporation | Novel pyrazole compounds having silver halide development groups |
| DE3312581A1 (de) * | 1983-04-08 | 1984-10-11 | Bayer Ag, 5090 Leverkusen | Verwendung von pyrazolonderivaten bei der bekaempfung des wachstums von tumorzellen und der metastasenbildung, arzneimittel hierfuer und verfahren zu deren herstellung |
| JPH02229168A (ja) | 1989-03-01 | 1990-09-11 | Takeda Chem Ind Ltd | ピラゾロン誘導体 |
| EP0491218A1 (en) * | 1990-12-17 | 1992-06-24 | F. Hoffmann-La Roche Ag | Benzodiazepinones |
| FR2725988B1 (fr) | 1994-10-24 | 1997-01-24 | Roussel Uclaf | Nouveaux derives de pyrazolones et pyrazoles acides, leur procede de preparation, les nouveaux intermediaires obtenus, leur application a titre de medicaments et les compositions pharmaceutiques les renfermant |
| US5484940A (en) | 1994-11-28 | 1996-01-16 | Grant; Francine S. | Substituted 3-indolyl-5-pyrazolone compounds |
| DE19518082A1 (de) | 1995-05-17 | 1996-11-21 | Merck Patent Gmbh | 4(-Arylaminomethylen)-2,4-dihydropyrazol-3-one |
| DE19914140A1 (de) | 1999-03-27 | 2000-09-28 | Bayer Ag | Substituierte Benzoylpyrazole |
| US7060822B1 (en) | 1999-07-30 | 2006-06-13 | Abbott Gmbh & Co. Kg | 2-pyrazolin-5-ones |
| CN1193026C (zh) | 1999-07-30 | 2005-03-16 | 艾博特股份有限两合公司 | 2-吡唑啉-5-酮 |
| US6455525B1 (en) * | 1999-11-04 | 2002-09-24 | Cephalon, Inc. | Heterocyclic substituted pyrazolones |
| EP1778669A2 (en) | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| WO2006071730A1 (en) | 2004-12-27 | 2006-07-06 | Astrazeneca Ab | Pyrazolone compounds as metabotropic glutamate receptor agonists for the treatment of neurological and psychiatric disorders |
| JPWO2006129583A1 (ja) | 2005-05-30 | 2009-01-08 | 株式会社ジーンケア研究所 | ピラゾロン誘導体 |
| WO2006129587A1 (ja) | 2005-05-30 | 2006-12-07 | Genecare Research Institute Co., Ltd. | ピラゾロン誘導体を含有する医薬組成物 |
| EP2054062A1 (en) | 2006-08-18 | 2009-05-06 | Syngenta Limited | Use of hppd inhibitors in the treatment of depression and/or withdrawal symptoms associated with addictive drugs |
| KR20090031331A (ko) | 2007-09-21 | 2009-03-25 | 주식회사 엘지생명과학 | 옥소 디하이드로 피라졸을 포함하는 신규한 베타 세크리타제 저해용 화합물 |
| AU2009318098B2 (en) | 2008-11-20 | 2015-07-16 | Northwestern University | Treatment of amyotrophic lateral sclerosis |
| WO2012020738A1 (ja) | 2010-08-09 | 2012-02-16 | 武田薬品工業株式会社 | 複素環化合物およびその用途 |
| CN103237793B (zh) | 2010-12-01 | 2015-06-10 | 日产化学工业株式会社 | 具有多发性骨髓瘤的治疗效果的吡唑化合物 |
| WO2012074068A1 (ja) | 2010-12-01 | 2012-06-07 | 日産化学工業株式会社 | ピラゾール化合物による造血幹細胞の製造方法 |
| WO2013134562A1 (en) * | 2012-03-09 | 2013-09-12 | Inception 2, Inc. | Triazolone compounds and uses thereof |
-
2015
- 2015-02-09 KR KR1020167025019A patent/KR20160115996A/ko not_active Withdrawn
- 2015-02-09 CN CN201580008005.1A patent/CN106029640B/zh not_active Expired - Fee Related
- 2015-02-09 CA CA2937542A patent/CA2937542A1/en not_active Abandoned
- 2015-02-09 WO PCT/US2015/015000 patent/WO2015123133A1/en not_active Ceased
- 2015-02-09 JP JP2016552317A patent/JP2017505804A/ja active Pending
- 2015-02-09 EP EP15748977.4A patent/EP3105205A4/en not_active Withdrawn
- 2015-02-09 AU AU2015217450A patent/AU2015217450A1/en not_active Abandoned
- 2015-02-09 NZ NZ722345A patent/NZ722345A/en not_active IP Right Cessation
- 2015-02-09 MX MX2016010436A patent/MX2016010436A/es unknown
- 2015-02-09 BR BR112016017781A patent/BR112016017781A2/pt not_active IP Right Cessation
- 2015-02-09 SG SG11201606149YA patent/SG11201606149YA/en unknown
- 2015-02-09 EA EA201691342A patent/EA201691342A1/ru unknown
- 2015-02-09 US US15/118,402 patent/US9862708B2/en not_active Expired - Fee Related
- 2015-02-09 PE PE2016001440A patent/PE20161315A1/es not_active Application Discontinuation
-
2016
- 2016-07-27 ZA ZA2016/05222A patent/ZA201605222B/en unknown
- 2016-08-07 IL IL247148A patent/IL247148A0/en unknown
-
2017
- 2017-12-01 US US15/829,514 patent/US20180079745A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| IL247148A0 (en) | 2016-09-29 |
| CN106029640A (zh) | 2016-10-12 |
| MX2016010436A (es) | 2016-10-31 |
| BR112016017781A2 (pt) | 2017-08-08 |
| CN106029640B (zh) | 2018-08-24 |
| EP3105205A1 (en) | 2016-12-21 |
| SG11201606149YA (en) | 2016-09-29 |
| US20180079745A1 (en) | 2018-03-22 |
| AU2015217450A8 (en) | 2016-09-08 |
| JP2017505804A (ja) | 2017-02-23 |
| AU2015217450A1 (en) | 2016-08-11 |
| NZ722345A (en) | 2018-02-23 |
| CA2937542A1 (en) | 2015-08-20 |
| WO2015123133A1 (en) | 2015-08-20 |
| EP3105205A4 (en) | 2017-08-02 |
| KR20160115996A (ko) | 2016-10-06 |
| ZA201605222B (en) | 2019-02-27 |
| EA201691342A1 (ru) | 2016-12-30 |
| US9862708B2 (en) | 2018-01-09 |
| US20170174666A1 (en) | 2017-06-22 |
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