AR072008A1 - Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 - Google Patents
Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38Info
- Publication number
- AR072008A1 AR072008A1 ARP090102007A ARP090102007A AR072008A1 AR 072008 A1 AR072008 A1 AR 072008A1 AR P090102007 A ARP090102007 A AR P090102007A AR P090102007 A ARP090102007 A AR P090102007A AR 072008 A1 AR072008 A1 AR 072008A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- ring
- conditions
- halo
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000005764 inhibitory process Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 206010061218 Inflammation Diseases 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 230000004054 inflammatory process Effects 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- MZAGXDHQGXUDDX-JSRXJHBZSA-N (e,2z)-4-ethyl-2-hydroxyimino-5-nitrohex-3-enamide Chemical compound [O-][N+](=O)C(C)C(/CC)=C/C(=N/O)/C(N)=O MZAGXDHQGXUDDX-JSRXJHBZSA-N 0.000 abstract 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 abstract 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010010741 Conjunctivitis Diseases 0.000 abstract 1
- 201000004624 Dermatitis Diseases 0.000 abstract 1
- 201000005569 Gout Diseases 0.000 abstract 1
- 206010018634 Gouty Arthritis Diseases 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 239000012826 P38 inhibitor Substances 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010042496 Sunburn Diseases 0.000 abstract 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 abstract 1
- 230000002917 arthritic effect Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 201000006549 dyspepsia Diseases 0.000 abstract 1
- 208000024798 heartburn Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos son inhibidores de p38 y son utiles en el tratamiento de inflamacion tal como en el tratamiento de asma, COPD, ARDS, artritis reumatoide, espondilitis reumatoide, osteoartritis, artritis gotosa y otras afecciones artr¡ticas; articulaciones inflamadas, eccema, psoriasis u otras afecciones inflamatorias de la piel tales como quemaduras solares; afecciones inflamatorias oculares incluyendo conjuntivitis, pirosis, dolor y otras afecciones asociadas con la inflamacion. Composiciones farmaceuticas que las contienen. Reivindicacion 1: Un compuesto representado por la formula qu¡mica (1) o una sal farmaceuticamente aceptable del mismo, donde: L se selecciona entre el grupo que consiste en (a) -C(O)-, (b) -CH(OH)-, (c) -CH(NR3R4)-, (d) -C(=NOR3)-, (e) -CH2-, y (f) -S(O)n-, donde n es 0, 1 o 2; Ar1 es un anillo arom tico o heteroarom tico, opcionalmente mono-, di- o trisustituido, de 6 tomos, donde el anillo heteroarom tico puede contener 1, 2 o 3 hetero tomos seleccionados entre N, S y O, donde los sustituyentes se seleccionan independientemente entre el grupo que consiste en (a) halo, (b) -alquilo C1-4, (c) -O-alquilo C1-4, (d) -CF3, (e) -NH2, (f) -NH-CH3, (g) -CN, (h) -C(O)NH2, y (i) -S(O)n-CH3; Ar2 es un anillo heteroc¡clico, 5,6-bic¡clico, condensado, opcionalmente mono-, di- o tri-sustituido, seleccionado entre el grupo de formulas (2) o un N-oxido del mismo, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en (a) halo, (b) -alquilo C1-4, (c) -O-alquilo C1-4, (d) -CF3, (e) -NH2, y (f) -NH2-CH3, (g) -NH2-CH2CF3, (h) -C(O)-morfolinilo, (i) -C(O)-NR1R2, (j) -C(O)OH, (k) -CN, (l) un anillo heteroarom tico o heteroc¡clico, de 5 o 6 miembros, que contiene 1, 2 o 3 hetero tomos seleccionados entre el grupo que consiste en S, O y N; R1, R2, R3 y R4 se seleccionan independientemente entre el grupo que consiste en (a) hidrogeno, y (b) alquilo C1-4, o R1 y R2 o R3 y R4 pueden unirse para formar un anillo saturado de 5 o 6 miembros, conteniendo dicho anillo opcionalmente un hetero tomo seleccionado entre S, N y O.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13192808P | 2008-06-13 | 2008-06-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072008A1 true AR072008A1 (es) | 2010-07-28 |
Family
ID=40864629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102007A AR072008A1 (es) | 2008-06-13 | 2009-06-04 | Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US20110105430A1 (es) |
| EP (1) | EP2300485B1 (es) |
| JP (1) | JP5511805B2 (es) |
| CN (1) | CN102203101B (es) |
| AR (1) | AR072008A1 (es) |
| AT (1) | ATE541850T1 (es) |
| AU (1) | AU2009257712B2 (es) |
| CA (1) | CA2727315A1 (es) |
| ES (1) | ES2380120T3 (es) |
| MX (1) | MX2010013629A (es) |
| TW (1) | TW200951133A (es) |
| WO (1) | WO2009152072A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR072008A1 (es) * | 2008-06-13 | 2010-07-28 | Merck & Co Inc | Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 |
| NZ599597A (en) | 2009-10-30 | 2013-05-31 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| AU2011213557B2 (en) | 2010-02-05 | 2015-05-07 | Phosphagenics Limited | Carrier comprising non-neutralised tocopheryl phosphate |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| CN102372707B (zh) * | 2010-08-16 | 2015-08-19 | 上海药明康德新药开发有限公司 | 6-甲基-4-溴-1,6-二氢吡咯[2,3-c]吡啶-7-酮的合成方法 |
| US9003783B2 (en) * | 2010-09-30 | 2015-04-14 | Electro-Motive Diesel, Inc. | Burner arrangement for a two-stroke locomotive diesel engine having an exhaust aftertreatment system |
| TWI541241B (zh) * | 2010-12-16 | 2016-07-11 | 健生科學愛爾蘭無限公司 | 作為呼吸道融合病毒抗病毒劑之咪唑并吡啶類 |
| EP2655362A1 (en) | 2010-12-22 | 2013-10-30 | Abbvie Inc. | Hepatitis c inhibitors and uses thereof |
| US9561243B2 (en) * | 2011-03-15 | 2017-02-07 | Phosphagenics Limited | Composition comprising non-neutralised tocol phosphate and a vitamin A compound |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| WO2014001314A1 (en) | 2012-06-26 | 2014-01-03 | Janssen Pharmaceutica Nv | Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| KR20150027267A (ko) | 2012-06-29 | 2015-03-11 | 화이자 인코포레이티드 | LRRK2 억제제로서의 4-(치환된-아미노)-7H-피롤로[2,3-d]피리미딘 |
| AU2013289284B2 (en) | 2012-07-09 | 2017-03-30 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| KR102244719B1 (ko) | 2013-03-15 | 2021-04-26 | 플렉시콘 인코퍼레이티드 | 헤테로시클릭 화합물 및 그의 용도 |
| GB201321738D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| US9695171B2 (en) | 2013-12-17 | 2017-07-04 | Pfizer Inc. | 3,4-disubstituted-1 H-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazines as LRRK2 inhibitors |
| GB201506660D0 (en) * | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| JP6873980B2 (ja) | 2015-09-14 | 2021-05-19 | ファイザー・インク | ＬＲＲＫ２阻害薬としての新規のイミダゾ［４，５−ｃ］キノリンおよびイミダゾ［４，５−ｃ］［１，５］ナフチリジン誘導体 |
| CN108601732A (zh) | 2015-12-09 | 2018-09-28 | 磷肌酸有限公司 | 药物制剂 |
| IL267006B2 (en) | 2016-12-21 | 2024-11-01 | Phosphagenics Ltd | Process for phosphorylation of a complex alcohol with p4o10 at high temperatures, and products thereof |
| TWI795440B (zh) | 2017-09-15 | 2023-03-11 | 美商佛瑪治療公司 | 作為ＣＢＰ／ｐ３００抑制劑之四氫─咪唑並喹啉化合物 |
| 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 |
| EP3692144A1 (en) | 2017-10-05 | 2020-08-12 | Fulcrum Therapeutics, Inc. | Use of p38 inhibitors to reduce expression of dux4 |
| AU2018348241B2 (en) | 2017-10-13 | 2023-01-12 | Opna Bio SA | Solid forms of a compound for modulating kinases |
| BR112020026783A2 (pt) | 2018-06-29 | 2021-03-30 | Forma Therapeutics, Inc. | Inibição da proteína de ligação creb (cbp) |
| EP3937940A4 (en) | 2019-03-15 | 2022-12-21 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (creb) |
| US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
| US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000071535A1 (en) * | 1999-05-21 | 2000-11-30 | Scios Inc. | INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE |
| GB0222743D0 (en) * | 2002-10-01 | 2002-11-06 | Celltech R&D Ltd | Chemical compounds |
| AR045595A1 (es) * | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| UA95244C2 (ru) * | 2005-06-22 | 2011-07-25 | Плексикон, Инк. | Соединения и способ модулирования активности киназ, и показания для их применения |
| KR20080080211A (ko) * | 2005-12-23 | 2008-09-02 | 아스트라제네카 아베 | 항박테리아성 피롤로피리딘, 피롤로피리미딘 및피롤로아제핀 |
| MX2009005264A (es) * | 2006-12-06 | 2009-05-28 | Boehringer Ingelheim Int | Mimeticos de glucocorticoides, metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos. |
| AR072008A1 (es) * | 2008-06-13 | 2010-07-28 | Merck & Co Inc | Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38 |
-
2009
- 2009-06-04 AR ARP090102007A patent/AR072008A1/es unknown
- 2009-06-06 TW TW098118954A patent/TW200951133A/zh unknown
- 2009-06-08 AT AT09763363T patent/ATE541850T1/de active
- 2009-06-08 AU AU2009257712A patent/AU2009257712B2/en not_active Ceased
- 2009-06-08 EP EP09763363A patent/EP2300485B1/en active Active
- 2009-06-08 ES ES09763363T patent/ES2380120T3/es active Active
- 2009-06-08 MX MX2010013629A patent/MX2010013629A/es active IP Right Grant
- 2009-06-08 WO PCT/US2009/046551 patent/WO2009152072A1/en not_active Ceased
- 2009-06-08 JP JP2011513599A patent/JP5511805B2/ja not_active Expired - Fee Related
- 2009-06-08 US US12/997,524 patent/US20110105430A1/en not_active Abandoned
- 2009-06-08 CA CA2727315A patent/CA2727315A1/en not_active Abandoned
- 2009-06-08 CN CN200980131581.XA patent/CN102203101B/zh not_active Expired - Fee Related
- 2009-06-10 US US12/481,614 patent/US8017605B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP5511805B2 (ja) | 2014-06-04 |
| TW200951133A (en) | 2009-12-16 |
| US20110105430A1 (en) | 2011-05-05 |
| EP2300485B1 (en) | 2012-01-18 |
| CN102203101B (zh) | 2014-12-03 |
| EP2300485A1 (en) | 2011-03-30 |
| WO2009152072A1 (en) | 2009-12-17 |
| CA2727315A1 (en) | 2009-12-17 |
| AU2009257712A1 (en) | 2009-12-17 |
| CN102203101A (zh) | 2011-09-28 |
| ES2380120T3 (es) | 2012-05-08 |
| ATE541850T1 (de) | 2012-02-15 |
| MX2010013629A (es) | 2011-01-14 |
| AU2009257712B2 (en) | 2014-06-12 |
| JP2011524354A (ja) | 2011-09-01 |
| US20090325953A1 (en) | 2009-12-31 |
| US8017605B2 (en) | 2011-09-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |