AR078833A1 - Derivados de heteroarilos que contienen nitrogeno como inhibidores dela cinasa jak3 - Google Patents
Derivados de heteroarilos que contienen nitrogeno como inhibidores dela cinasa jak3Info
- Publication number
- AR078833A1 AR078833A1 ARP100103999A ARP100103999A AR078833A1 AR 078833 A1 AR078833 A1 AR 078833A1 AR P100103999 A ARP100103999 A AR P100103999A AR P100103999 A ARP100103999 A AR P100103999A AR 078833 A1 AR078833 A1 AR 078833A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- cyanoalkyl
- haloalkyl
- hydroxyalkyl
- Prior art date
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 title abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 title abstract 5
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 title abstract 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 16
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 8
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 8
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 8
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000002619 bicyclic group Chemical group 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000002950 monocyclic group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
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- 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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
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- 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
- A61P37/02—Immunomodulators
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- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
- C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
-
- 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
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- 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
- C07D519/06—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 containing at least one condensed beta-lactam ring system, provided for by groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00, e.g. a penem or a cepham system
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Derivados de heteroarilo nitrogenados de formula (1) o (2), donde los significados para los distintos sustituyentes son los indicados en la descripcion. Estos compuestos son utiles como inhibidores de cinasas JAK, particularmente JAK3. Se provee además un proceso para su preparacion. Reivindicacion 1: Un compuesto caracterizado por la formula (1) o (2) donde: A es carbono y B es nitrogeno, o A es nitrogeno y B es carbono; W es CH o N; R1 y R2 son, independientemente, hidrogeno, alquilo C1-4, haloalquilo C1-4, hidroxialquilo C1-4, cianoalquilo C1-4, alcoxi C1-4alquilo C1-4, halogeno, -CN, -OR8 o -SR8; R3 es alquilo C1-4, R9-alquilo C1-4, Cy1 o Cy2-alquilo C1-4, donde Cy1 y Cy2 están opcionalmente sustituidos por uno o más R10; R4 es hidrogeno, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4, cianoalquilo C1-4, R12R7N-alquilo C0-4, R13CONR7-alquilo C0-4, R13R7NCO-alquilo C0-4, R12R7NCONR7-alquilo C0-4, R13CO2NR7-alquilo C0-4, R13SO2NR7-alquilo C0-4, -OR12 o Cy2-alquilo C0-4; donde Cy2 está opcionalmente sustituido por uno o más R11; R5 es hidrogeno, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4, cianoalquilo C1-4, halogeno, -CN, -OR12, -NR7R12, o Cy2-alquilo C0-4, donde Cy2 está opcionalmente sustituido por uno o más R11; R6 es hidrogeno, alquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4, R12R7N-alquilo C1-4, R16CO-alquilo C0-4, R16CO2-alquilo C0-4, R16CO-O-alquilo C1-4, cianoalquilo C1-4, Cy1 o Cy2-alquilo C1-4, donde Cy1 y Cy2 están opcionalmente sustituidos por uno o más R11; R7 es hidrogeno o aIquilo C1-4; R8 es hidrogeno, alquilo C1-4, haloalquilo C1-4, hidroxialquilo C1-4, o alcoxi C1-4alquilo C1-4; R9 es halogeno, -CN, -CONR7R12, -COR13, -CO2R12, -OR12, -OCONR7R12, -SO2R13, -SO2NR7R12, -NR7R12, -NR7COR12, -NR7CONR7R12, -NR7CO2R13 o -NR7SO2R13; R10 es alquilo C1-4 o R9-alquilo C0-4; R11 es alquilo C1-4, haloalquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4, cianoalquilo C1-4, halogeno, -CN, -CONR7R14, -COR14, -CO2R15, -OR14, -OCONR7R14, -SO2R15, -SO2NR7R14, -NR7R14, -NR7COR14, -NR7CONR7R14, -NR7CO2R15 o -NR7SO2R15; R12 es hidrogeno o R13; R13 es alquilo C1-5, haloalquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4, cianoalquilo C1-4, Cy2-alquilo C0-4 o R14R7N-alquilo C1-4; donde Cy2 está opcionalmente sustituido por uno o más R11; R14 es hidrogeno o R15; R15 es alquilo C1-4, haloalquilo C1-4, alcoxi C1-4alquilo C1-4, hidroxialquilo C1-4 o cianoalquilo C1-4; R16 es alquilo C1-4, haloalquilo C1-4, alcoxi C1-4alquilo C1-4 o cianoalquilo C1-4; Cy1 es un anillo monocíclico de 3 a 7 miembros o bicíclico de 6 a 11 miembros, que es saturado, parcialmente insaturado o aromático, y que es carbocíclico o heterocíclico que contiene de 1 a 4 heteroátomos seleccionados independientemente de N, S y O, donde dicho anillo está unido al resto de la molécula a través de cualquier átomo de C disponible, y donde uno o más átomos de C o S del anillo están opcionalmente oxidados formando CO, SO o SO2; y Cy2 es un anillo monocíclico de 3 a 7 miembros o bicíclico de 6 a 11 miembros, que es saturado, parcialmente insaturado o aromático, y que es carbocíclico o heterocíclico que contiene de 1 a 4 heteroátomos seleccionados independientemente de N, S y O, donde dicho anillo está unido al resto de la molécula a través de cualquier átomo de C o N disponible, y donde uno o más átomos de C o S están opcionalmente oxidados formando CO, SO o SO2; o una sal del mismo.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09382233 | 2009-10-29 | ||
| US29105109P | 2009-12-30 | 2009-12-30 | |
| US32992710P | 2010-04-30 | 2010-04-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078833A1 true AR078833A1 (es) | 2011-12-07 |
Family
ID=41571618
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100103999A AR078833A1 (es) | 2009-10-29 | 2010-10-29 | Derivados de heteroarilos que contienen nitrogeno como inhibidores dela cinasa jak3 |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US8501735B2 (es) |
| EP (1) | EP2493895B1 (es) |
| JP (1) | JP5759471B2 (es) |
| KR (1) | KR101675614B1 (es) |
| CN (1) | CN102712658B (es) |
| AR (1) | AR078833A1 (es) |
| AU (1) | AU2010311378B2 (es) |
| BR (1) | BR112012010186B8 (es) |
| CA (1) | CA2778680C (es) |
| DK (1) | DK2493895T3 (es) |
| ES (1) | ES2629006T3 (es) |
| IL (1) | IL219385A0 (es) |
| MX (1) | MX2012005100A (es) |
| PE (1) | PE20121352A1 (es) |
| PL (1) | PL2493895T3 (es) |
| PT (1) | PT2493895T (es) |
| RU (1) | RU2553681C2 (es) |
| SI (1) | SI2493895T1 (es) |
| TW (1) | TWI478714B (es) |
| UA (1) | UA109775C2 (es) |
| WO (1) | WO2011051452A1 (es) |
| ZA (1) | ZA201203090B (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| EP2397482A1 (en) * | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Heteroaryl imidazolone derivatives as jak inhibitors |
| WO2012003576A1 (en) * | 2010-07-06 | 2012-01-12 | Université de Montréal | Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| US9018395B2 (en) | 2011-01-27 | 2015-04-28 | Université de Montréal | Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| WO2013025628A1 (en) * | 2011-08-15 | 2013-02-21 | Ligand Pharmaceuticals Incorporated | Janus kinase inhibitor compounds and methods |
| AU2012340869B2 (en) | 2011-11-23 | 2017-03-02 | Cancer Research Technology Limited | Thienopyrimidine inhibitors of atypical protein kinase C |
| UY34616A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias. |
| WO2013117649A1 (en) * | 2012-02-10 | 2013-08-15 | Galapagos Nv | Imidazo [4, 5 -c] pyridine derivatives useful for the treatment of degenerative and inflammatory diseases |
| TW201513861A (zh) * | 2013-01-17 | 2015-04-16 | Galapagos Nv | 用於治療退化性及發炎疾病之新穎化合物 |
| EP2970277B1 (en) | 2013-03-15 | 2021-07-28 | Knopp Biosciences LLC | Imidazo(4,5-b) pyridin-2-yl amides as kv7 channel activators |
| TWI731317B (zh) | 2013-12-10 | 2021-06-21 | 美商健臻公司 | 原肌球蛋白相關之激酶（ｔｒｋ）抑制劑 |
| TWI705967B (zh) | 2014-03-20 | 2020-10-01 | 美商卡佩拉醫療公司 | 苯并咪唑衍生物及其醫藥組合物及使用方法 |
| SI3572405T1 (sl) | 2014-09-12 | 2023-12-29 | Biohaven Therapeutics Ltd. | Amidi benzoimidazol-1,2-il kot aktivatorji kanalov kv 7 |
| MA40698A3 (fr) | 2014-12-18 | 2020-01-31 | Genzyme Corp | Formulations pharmaceutiques d'inhibiteurs de kinase associée à la tropomyosine (trk) |
| EP3053927A1 (en) | 2015-02-05 | 2016-08-10 | Vectura Limited | Novel polymorphs |
| US10155757B2 (en) | 2015-03-10 | 2018-12-18 | Vectura Limited | Crystalline form of a JAK3 kinase inhibitor |
| AU2016356694B2 (en) | 2015-11-20 | 2021-07-29 | Forma Therapeutics, Inc. | Purinones as ubiquitin-specific protease 1 inhibitors |
| ES2946551T3 (es) | 2017-10-17 | 2023-07-20 | Palau Pharma S L U | Síntesis de compuestos de 4-aminopirimidina |
| TWI820146B (zh) * | 2018-06-15 | 2023-11-01 | 瑞典商阿斯特捷利康公司 | 嘌呤酮化合物及其在治療癌症中之用途 |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| JP2023528223A (ja) | 2020-05-13 | 2023-07-04 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症を処置するための抗ヘモジュベリン（ｈｊｖ）抗体 |
| CN112724133B (zh) * | 2021-01-12 | 2022-03-25 | 湖南复瑞生物医药技术有限责任公司 | 6-溴吡唑并[1,5-a]吡啶的制备方法 |
| WO2023248010A2 (en) | 2022-06-23 | 2023-12-28 | Synovo Gmbh | Targeted modulators of jak3 for treatment of inflammatory and autoimmune diseases |
| US20240261224A1 (en) | 2022-12-02 | 2024-08-08 | Kinaset Therapeutics, Inc. | Formulation of a pan-jak inhibitor |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9718913D0 (en) * | 1997-09-05 | 1997-11-12 | Glaxo Group Ltd | Substituted oxindole derivatives |
| WO2004039796A1 (de) | 2002-10-28 | 2004-05-13 | Bayer Healthcare Ag | Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren |
| EP1505064A1 (en) | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| AR050188A1 (es) * | 2004-08-03 | 2006-10-04 | Uriach Y Compania S A J | Compuestos heterociclicos condensados utiles en terapia como inhibidores de quinasas p38 y composiciones farmaceuticas que los contienen |
| AU2005278292B2 (en) * | 2004-08-31 | 2011-09-08 | Msd K.K. | Novel substituted imidazole derivatives |
| WO2006053109A1 (en) | 2004-11-10 | 2006-05-18 | Synta Pharmaceuticals Corp. | Heteroaryl compounds |
| RU2007140903A (ru) | 2005-04-05 | 2009-05-20 | Фармакопия, Инк. (Us) | Производные пурина и имидазопиридина для иммуносупрессии |
| US7884109B2 (en) | 2005-04-05 | 2011-02-08 | Wyeth Llc | Purine and imidazopyridine derivatives for immunosuppression |
| JP2008535866A (ja) | 2005-04-08 | 2008-09-04 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | ピリミジン誘導体 |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| EP1931674B1 (en) * | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| TWI398252B (zh) | 2006-05-26 | 2013-06-11 | Novartis Ag | 吡咯并嘧啶化合物及其用途 |
| AR063142A1 (es) | 2006-10-04 | 2008-12-30 | Pharmacopeia Inc | Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen. |
| US7902187B2 (en) | 2006-10-04 | 2011-03-08 | Wyeth Llc | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| WO2008043019A1 (en) * | 2006-10-04 | 2008-04-10 | Pharmacopeia, Inc | 8-substituted 2-(benzimidazolyl) purine derivatives for immunosuppression |
| ES2631003T3 (es) | 2006-10-19 | 2017-08-25 | Signal Pharmaceuticals, Llc | Compuestos heteroarilo, sus composiciones y métodos de tratamiento con ellos |
| MX2009005194A (es) | 2006-11-16 | 2009-11-10 | Pharmacopeia Llc | Derivados de purina 7-sustituidos para inmunosupresion. |
| US20080119496A1 (en) * | 2006-11-16 | 2008-05-22 | Pharmacopeia Drug Discovery, Inc. | 7-Substituted Purine Derivatives for Immunosuppression |
| PE20090996A1 (es) * | 2007-04-02 | 2009-07-15 | Palau Pharma Sa | Derivados de pirrolopirimidina como inhibidores de cinasa jak3 |
| CN101679412A (zh) | 2007-05-23 | 2010-03-24 | 药典有限责任公司 | 作为PKC-θ抑制剂的嘌呤酮类和1H-咪唑并吡啶酮类 |
| US8648069B2 (en) * | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| WO2009048474A1 (en) | 2007-10-12 | 2009-04-16 | Pharmacopeia, Inc. | 2,7,9-substituted purinone derivatives for immunosuppression |
| PE20091035A1 (es) | 2007-11-30 | 2009-07-16 | Palau Pharma Sa | Derivados de 2-aminopirimidina |
| WO2009077608A1 (en) | 2007-12-19 | 2009-06-25 | Palau Pharma, S. A. | 2 -aminopyrimidine derivatives as histamine h4 antagonists |
| RU2489430C2 (ru) | 2007-12-21 | 2013-08-10 | Палау Фарма, С.А. | Производные 4-аминопиримидина |
| GB0815369D0 (en) | 2008-08-22 | 2008-10-01 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| PE20121505A1 (es) | 2009-12-23 | 2012-11-05 | Medicis Pharmaceutical Corp | Derivados de aminoalquilpirimidina como antagonistas del receptor h4 de histamina |
| JP2011136925A (ja) * | 2009-12-28 | 2011-07-14 | Dainippon Sumitomo Pharma Co Ltd | 含窒素二環性化合物 |
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