AR056582A1 - COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDE - Google Patents
COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDEInfo
- Publication number
- AR056582A1 AR056582A1 ARP060104595A ARP060104595A AR056582A1 AR 056582 A1 AR056582 A1 AR 056582A1 AR P060104595 A ARP060104595 A AR P060104595A AR P060104595 A ARP060104595 A AR P060104595A AR 056582 A1 AR056582 A1 AR 056582A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- optionally substituted
- halo
- cycloalkyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical class NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 abstract 2
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 206010027476 Metastases Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010054094 Tumour necrosis Diseases 0.000 abstract 1
- -1 carbamate compound Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229940104302 cytosine Drugs 0.000 abstract 1
- 229940043355 kinase inhibitor Drugs 0.000 abstract 1
- 230000009401 metastasis Effects 0.000 abstract 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 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
- C07D401/12—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
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D401/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compuesto de pirazolil carbamato de formula I: donde: Z se selecciona del grupo que consiste de grupo de formulas (2) X se selecciona del grupo que consiste de grupo de formulas (3) R1 es alquilo C1-C7 opcionalmente sustituido con uno a seis sustituyentes seleccionados del grupo que consiste en halo, y alquilhalo C1-C4; cicloalquilo C3-C6 opcionalmente sustituido con uno o dos sustituyentes seleccionados del grupo que consiste de alquilo C1-C4 y trifluoremetilo; o trimetilsililo; R2 es fenilo opcionalmente sustituido con alquilo C1-C4, o piridinilo opcionalmente sustituido con alquilo C1-C4; Y es hidrogeno, alquilo C1-C4, halo o alquilhalo C1-C4; R3 es alquilo C1-C7 opcionalmente sustituido con cicloalquilo C3-C6; alcoxi C1-C4; alquilhalo C1-C4; cicloalquilo C3-C6 opcionalmente sustituído con uno a cuatro sustituyentes seleccionados del grupo que consiste de alquilo C1-C4 y trifluorometilo; o piridilo, fenilo o tienilo cada uno opcionalmente sustituido con un primer sustituyente seleccionado del grupo que consiste de: halo, ciano, alquilo C1-C4, alquilhalo C1-C4 y alcoxi C1-C4, y opcionalmente sustituido adicional con un segundo sustituyente seleccionado del grupo de alquilo C1-C4 y halo; y R4 es hidrogeno o alquilo C1-C4; o una sal del mismo farmacéuticamente aceptable. Preferentemente, el compuesto es: 1-(5-terc-butil-2-p-ptolil-2H-pirazol-3-il)-3-{6-[4-(2,6-difluoro-benzoil)-piperazin-1-il]-2-metil-piperidin-3-il}-urea. Composicion farmacéutica que lo comprende. Se emplea como inhibidor de cinasa p38, especialmente en el tratamiento dolencias derivadas de excesiva produccion de citosina tales como necrosis de tumores, neoplasmas, metastasis o artritis reumatoide.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73160405P | 2005-10-28 | 2005-10-28 | |
| EP06380151 | 2006-06-02 | ||
| US82196306P | 2006-08-10 | 2006-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR056582A1 true AR056582A1 (es) | 2007-10-10 |
Family
ID=43298635
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060104595A AR056582A1 (es) | 2005-10-28 | 2006-10-20 | COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDE |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7652015B2 (es) |
| EP (1) | EP1943243B1 (es) |
| KR (1) | KR101004156B1 (es) |
| AR (1) | AR056582A1 (es) |
| AT (1) | ATE493403T1 (es) |
| AU (1) | AU2006309044B2 (es) |
| BR (1) | BRPI0616901A2 (es) |
| CA (1) | CA2627673A1 (es) |
| DK (1) | DK1943243T3 (es) |
| DO (1) | DOP2006000234A (es) |
| EA (1) | EA015189B1 (es) |
| PE (1) | PE20070795A1 (es) |
| PL (1) | PL1943243T3 (es) |
| PT (1) | PT1943243E (es) |
| RS (1) | RS51949B (es) |
| SI (1) | SI1943243T1 (es) |
| TN (1) | TNSN08191A1 (es) |
| TW (1) | TWI325423B (es) |
| WO (1) | WO2007053394A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0905955D0 (en) | 2009-04-06 | 2009-05-20 | Respivert Ltd | Novel compounds |
| JP5787977B2 (ja) | 2010-04-08 | 2015-09-30 | レスピバート・リミテツド | Ｐ３８ｍａｐキナーゼ阻害剤 |
| US8933228B2 (en) | 2010-06-17 | 2015-01-13 | Respivert, Ltd. | Respiratory formulations and compounds for use therein |
| EP2736899A1 (en) | 2011-07-26 | 2014-06-04 | Grünenthal GmbH | Substituted bicyclic aromatic carboxamide and urea derivatives as vanilloid receptor ligands |
| EP2890460B1 (en) | 2012-08-29 | 2017-02-22 | Respivert Limited | Kinase inhibitors |
| WO2014033447A2 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| WO2014033449A1 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| WO2014076484A1 (en) | 2012-11-16 | 2014-05-22 | Respivert Limited | Kinase inhibitors |
| CN105408315B (zh) | 2013-04-02 | 2018-09-14 | 瑞斯比维特有限公司 | 激酶抑制剂 |
| WO2014162121A1 (en) | 2013-04-02 | 2014-10-09 | Topivert Pharma Limited | Kinase inhibitors based upon n-alkyl pyrazoles |
| US9890185B2 (en) | 2013-12-20 | 2018-02-13 | Respivert Limited | Urea derivatives useful as kinase inhibitors |
| AU2015226855C1 (en) | 2014-03-07 | 2021-02-11 | Biocryst Pharmaceuticals, Inc. | Human plasma kallikrein inhibitors |
| MA40774A (fr) | 2014-10-01 | 2017-08-08 | Respivert Ltd | Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38 |
| CA3015978A1 (en) | 2016-04-06 | 2017-10-12 | Topivert Pharma Limited | Kinase inhibitors |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| WO2019071144A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION |
| SI3700902T1 (sl) | 2017-10-27 | 2023-10-30 | Boehringer Ingelheim International Gmbh | Inhibitorji trpc6 |
| JP2023537963A (ja) | 2020-08-13 | 2023-09-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 統合失調症に伴う認知機能障害に対する処置法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1043995T1 (de) * | 1997-12-22 | 2001-06-07 | Bayer Corp., Pittsburgh | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYLSUBSTITUIERTEN HARNSTOFFEN |
| PT1761520E (pt) * | 2004-06-23 | 2008-09-15 | Lilly Co Eli | Inibidores de quinase |
-
2006
- 2006-10-20 PE PE2006001275A patent/PE20070795A1/es not_active Application Discontinuation
- 2006-10-20 DO DO2006000234A patent/DOP2006000234A/es unknown
- 2006-10-20 AR ARP060104595A patent/AR056582A1/es unknown
- 2006-10-20 TW TW095138670A patent/TWI325423B/zh not_active IP Right Cessation
- 2006-10-25 EP EP06826650A patent/EP1943243B1/en active Active
- 2006-10-25 CA CA002627673A patent/CA2627673A1/en not_active Abandoned
- 2006-10-25 RS RS20110112A patent/RS51949B/en unknown
- 2006-10-25 PL PL06826650T patent/PL1943243T3/pl unknown
- 2006-10-25 PT PT06826650T patent/PT1943243E/pt unknown
- 2006-10-25 DK DK06826650.1T patent/DK1943243T3/da active
- 2006-10-25 KR KR1020087010062A patent/KR101004156B1/ko not_active IP Right Cessation
- 2006-10-25 BR BRPI0616901-5A patent/BRPI0616901A2/pt not_active IP Right Cessation
- 2006-10-25 WO PCT/US2006/041644 patent/WO2007053394A1/en active Application Filing
- 2006-10-25 AT AT06826650T patent/ATE493403T1/de active
- 2006-10-25 AU AU2006309044A patent/AU2006309044B2/en not_active Expired - Fee Related
- 2006-10-25 US US12/088,526 patent/US7652015B2/en not_active Expired - Fee Related
- 2006-10-25 EA EA200801199A patent/EA015189B1/ru not_active IP Right Cessation
- 2006-10-25 SI SI200630950T patent/SI1943243T1/sl unknown
-
2008
- 2008-04-25 TN TNP2008000191A patent/TNSN08191A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0616901A2 (pt) | 2011-07-05 |
| US20080269244A1 (en) | 2008-10-30 |
| KR20080053394A (ko) | 2008-06-12 |
| RS51949B (en) | 2012-02-29 |
| KR101004156B1 (ko) | 2010-12-27 |
| AU2006309044B2 (en) | 2011-10-13 |
| EP1943243B1 (en) | 2010-12-29 |
| US7652015B2 (en) | 2010-01-26 |
| TW200800184A (en) | 2008-01-01 |
| EA200801199A1 (ru) | 2008-08-29 |
| PL1943243T3 (pl) | 2011-05-31 |
| DOP2006000234A (es) | 2007-05-31 |
| CA2627673A1 (en) | 2007-05-10 |
| TWI325423B (en) | 2010-06-01 |
| WO2007053394A1 (en) | 2007-05-10 |
| AU2006309044A1 (en) | 2007-05-10 |
| TNSN08191A1 (en) | 2009-10-30 |
| EP1943243A1 (en) | 2008-07-16 |
| PT1943243E (pt) | 2011-01-11 |
| SI1943243T1 (sl) | 2011-04-29 |
| ATE493403T1 (de) | 2011-01-15 |
| EA015189B1 (ru) | 2011-06-30 |
| PE20070795A1 (es) | 2007-08-24 |
| DK1943243T3 (da) | 2011-03-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |