AR073209A1 - Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen. - Google Patents
Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen.Info
- Publication number
- AR073209A1 AR073209A1 ARP090103272A ARP090103272A AR073209A1 AR 073209 A1 AR073209 A1 AR 073209A1 AR P090103272 A ARP090103272 A AR P090103272A AR P090103272 A ARP090103272 A AR P090103272A AR 073209 A1 AR073209 A1 AR 073209A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- heteroatom selected
- heterocyclyl
- heteroaryl
- Prior art date
Links
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 title 1
- 101710139011 MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 title 1
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 title 1
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 208000027866 inflammatory disease Diseases 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 208000030159 metabolic disease Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 16
- 229910052760 oxygen Inorganic materials 0.000 abstract 14
- 125000005842 heteroatom Chemical group 0.000 abstract 13
- 229910052717 sulfur Inorganic materials 0.000 abstract 13
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- VUEMIUIJBHSNBW-UHFFFAOYSA-N 4-(2-methoxyanilino)-5-methylthieno[2,3-d]pyrimidine-6-carboxylic acid Chemical compound COC1=CC=CC=C1NC1=NC=NC2=C1C(C)=C(C(O)=O)S2 VUEMIUIJBHSNBW-UHFFFAOYSA-N 0.000 abstract 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 101100295741 Gallus gallus COR4 gene Proteins 0.000 abstract 1
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- 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
-
- 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
- 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
- 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
-
- 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
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial 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
-
- 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
- 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
-
- 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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- 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
- A61P7/10—Antioedematous agents; Diuretics
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Reivindicacion 1: Un compuesto caracterizado porque tiene la formula general (1) en la que X se selecciona entre CH o N; R2 se selecciona entre H, CN, CF3, CON(R4)2; O-alquilo C1-8 opcionalmente sustituido con R3; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; y alquilo C1-8 opcionalmente sustituido con R6; y cuando X es CH, R2 también puede ser F, CI, SO2NH2; Y se selecciona entre alquilo C1-8 de cadena lineal o ramificada, opcionalmente sustituido con uno o más de R3; cicloalquilo C3-8, opcionalmente sustituido con uno o más de R9; y sistemas heterocíclicos seleccionados entre una cualquiera de las formulas (2) opcionalmente sustituido con uno o más de R9, donde n es independientemente 1 a 3 U es independientemente O o NR5; R1 se selecciona entre H; CI; y alquilo C1-8, opcionalmente sustituido con N(R4)2 o F; R3 se selecciona entre OH, OR4 y N(R4)2 desde el segundo átomo de carbono de la cadena alquilo al que se une R3 en adelante; F; CO2H; CON(R4)2; SO2N(R4)2; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O donde el átomo de nitrogeno puede estar sustituido con H o alquilo C1-3; y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; R4 se selecciona entre H y alquilo C1-8; R5 se selecciona entre H; alquilo C1-8, alquenilo C2-8, cicloalquilo C3 -10; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; heteroarilo C5-10 que comprende al menos un heteroátomo seleccionada entre N, S y O; COR6, CO2R4; CONH(CH2)mR6; (CH2)mR6; CO(CH2)mR6; (CH2)mC(O)R6; SO2R4; y SO2(CH2)mR6; donde m es 1-4; R6 se selecciona entre H; OH; OR4; OC(O)R4; N(R4)2; F; CO2H; CON(R4)2; SO2N(R4)2; heterociclilo que comprende al menos un heteroátomo seleccionado entre N, S y O; y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O y que está opcionalmente sustituido con alquilo C1-3 o N(R4)2; W se selecciona entre F; CI; Br; I; CN; -(CH2)1-2NR7R8; -C(S)NH2; -CONR7R8; -C(=NR7)NR7R8; -CO2R7; y -SO2NR7R8; o W junto con R1 puede formar un anillo heterocíclico de cinco o siete miembros que comprende al menos un heteroátomo seleccionado entre N, S y O, donde el átomo de nitrogeno puede estar sustituido con H, -C(O)-O-alquilo C1-4, -CO-(CH2)1-2-NH2, -CO-(CH2)1-2-NH(alquilo C1-3) o -CO-(CH2)1-2-N(alquilo C1-3)2; R7se selecciona entre H y alquilo C1-8; R8 se selecciona entre H; alquilo C1-8 opcionalmente sustituido con R3; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O, opcionalmente sustituido con alquilo C1-3, y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; R9 se selecciona entre OH, OR4, N(R4)2, N(R4)COR4, NR4SO2R4 y N(R4)-(CH2)m-R4 sobre cualquier átomo de carbono distinto del unido a O o N; F; CO2H; CON(R4)2; SO2N(R4)2; SO2R4; (CH2)mOR4; (CH2)mN(R4)2; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; con la condicion de que se excluya el compuesto 4-(2-metoxifenilamino)-5-metiltieno[2,3-d]pirimidina-6-carboxilato de etilo; o un tautomero, metabolito, profármaco o una al farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08015049 | 2008-08-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR073209A1 true AR073209A1 (es) | 2010-10-20 |
Family
ID=40266066
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090103272A AR073209A1 (es) | 2008-08-26 | 2009-08-25 | Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen. |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8486953B2 (es) |
| EP (1) | EP2331551B1 (es) |
| JP (1) | JP5675614B2 (es) |
| KR (1) | KR20110045019A (es) |
| CN (1) | CN102186857A (es) |
| AR (1) | AR073209A1 (es) |
| AU (1) | AU2009286734A1 (es) |
| BR (1) | BRPI0918971A2 (es) |
| CA (1) | CA2735361A1 (es) |
| CL (1) | CL2011000409A1 (es) |
| ES (1) | ES2593495T3 (es) |
| IL (1) | IL211008A0 (es) |
| MX (1) | MX2011001938A (es) |
| NZ (1) | NZ591113A (es) |
| RU (1) | RU2011110908A (es) |
| TW (1) | TW201014864A (es) |
| UY (1) | UY32072A (es) |
| WO (1) | WO2010023181A1 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1899353A1 (en) * | 2005-06-22 | 2008-03-19 | DeveloGen Aktiengesellschaft | Thienopyrimidines for pharmaceutical compositions |
| EA200802118A1 (ru) | 2006-04-07 | 2009-04-28 | Девелоджен Ациенгезельшафт | Обладающие ингибирующей активностью в отношении mnk1/mnk2 тиенопиримидины, предназначенные для применения в фармацевтических композициях |
| EP1889847A1 (en) | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| NZ591113A (en) | 2008-08-26 | 2012-07-27 | Boehringer Ingelheim Int | Thienopyrimidine linked to phenyl or pyridine via an nh amine for pharmaceutical compositions |
| EA201201191A1 (ru) * | 2010-02-26 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций |
| UY33241A (es) * | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| JP5575275B2 (ja) | 2010-02-26 | 2014-08-20 | 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 | 医薬組成物のための置換アルキル基含有チエノピリミジン |
| US20130065914A1 (en) * | 2010-02-26 | 2013-03-14 | Boehringer Ingelheim International Gmbh | Halogen or cyano substituted thieno [2,3-d]pyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions |
| MX343138B (es) * | 2011-07-29 | 2016-10-25 | K Hansson Göran | Terapia de ácido 3-hidroxiantranílico (3-haa) para la prevención y el tratamiento de hiperlipidemia y sus complicaciones cardiovasculares. |
| AR090037A1 (es) * | 2011-11-15 | 2014-10-15 | Xention Ltd | Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio |
| JP6109193B2 (ja) * | 2012-01-10 | 2017-04-05 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | チエノピリミジン化合物 |
| US9540392B2 (en) | 2012-05-21 | 2017-01-10 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| EP2852595B1 (en) | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Substituted benzothienopyrimidines |
| US20150182490A1 (en) | 2012-06-26 | 2015-07-02 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| TW201412740A (zh) | 2012-09-20 | 2014-04-01 | Bayer Pharma AG | 經取代之吡咯并嘧啶胺基苯并噻唑酮 |
| EP2917185B1 (en) * | 2012-11-09 | 2017-05-10 | Evotec International GmbH | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| WO2014118226A1 (en) | 2013-02-01 | 2014-08-07 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolopyrimidinylamino-indazoles |
| EP2951187A1 (en) | 2013-02-01 | 2015-12-09 | Bayer Pharma Aktiengesellschaft | Substituted thienopyrimidines and pharmaceutical use thereof |
| WO2014135480A1 (en) | 2013-03-06 | 2014-09-12 | Bayer Pharma Aktiengesellschaft | Substituted thiazolopyrimidines |
| KR20160061911A (ko) | 2013-04-08 | 2016-06-01 | 데니스 엠. 브라운 | 최적하 투여된 화학 화합물의 치료 효과 |
| US10167296B2 (en) * | 2014-05-07 | 2019-01-01 | Evotec International Gmbh | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| JP2017519737A (ja) * | 2014-05-26 | 2017-07-20 | バイエル・ファルマ・アクティエンゲゼルシャフト | 置換テトラヒドロピリドチエノピリミジン |
| TWI713455B (zh) * | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | MnK抑制劑及其相關方法 |
| CA2982984C (en) | 2015-04-20 | 2023-10-17 | Effector Therapeutics, Inc. | Inhibitors of immune checkpoint modulators for use in treating cancer and infections |
| GB201520500D0 (en) * | 2015-11-20 | 2016-01-06 | Medical Res Council Technology | Compounds |
| WO2017117052A1 (en) | 2015-12-31 | 2017-07-06 | Effector Therapeutics, Inc. | Mnk biomarkers and uses thereof |
| US11690847B2 (en) | 2016-11-30 | 2023-07-04 | Case Western Reserve University | Combinations of 15-PGDH inhibitors with corticosteroids and/or TNF inhibitors and uses thereof |
| NZ796735A (en) | 2017-02-06 | 2025-12-19 | Univ Case Western Reserve | Compositions and methods of modulating short-chain dehydrogenase activity |
| EA201991894A1 (ru) * | 2017-02-14 | 2020-02-05 | Эффектор Терапьютикс, Инк. | ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ |
| FI3802517T3 (fi) | 2018-06-07 | 2023-03-23 | Idorsia Pharmaceuticals Ltd | Alkoksisubstituoituja pyridinyylijohdannaisia LPA1-reseptoriantagonisteina ja niiden käyttö fibroosin hoidossa |
| JP2022505846A (ja) | 2018-10-24 | 2022-01-14 | イーフェクター セラピューティクス, インコーポレイテッド | Mnk阻害剤の結晶形態 |
| CN120463720A (zh) | 2018-11-21 | 2025-08-12 | 卡斯西部储备大学 | 调节短链脱氢酶活性的组合物和方法 |
| AR119162A1 (es) | 2019-06-18 | 2021-12-01 | Idorsia Pharmaceuticals Ltd | Derivados de piridin-3-ilo |
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-
2009
- 2009-08-24 NZ NZ591113A patent/NZ591113A/en not_active IP Right Cessation
- 2009-08-24 RU RU2011110908/04A patent/RU2011110908A/ru not_active Application Discontinuation
- 2009-08-24 ES ES09782115.1T patent/ES2593495T3/es active Active
- 2009-08-24 BR BRPI0918971A patent/BRPI0918971A2/pt not_active IP Right Cessation
- 2009-08-24 EP EP09782115.1A patent/EP2331551B1/en active Active
- 2009-08-24 UY UY0001032072A patent/UY32072A/es not_active Application Discontinuation
- 2009-08-24 AU AU2009286734A patent/AU2009286734A1/en not_active Abandoned
- 2009-08-24 KR KR1020117004371A patent/KR20110045019A/ko not_active Withdrawn
- 2009-08-24 CA CA2735361A patent/CA2735361A1/en not_active Abandoned
- 2009-08-24 US US13/060,731 patent/US8486953B2/en not_active Expired - Fee Related
- 2009-08-24 MX MX2011001938A patent/MX2011001938A/es active IP Right Grant
- 2009-08-24 JP JP2011524346A patent/JP5675614B2/ja not_active Expired - Fee Related
- 2009-08-24 WO PCT/EP2009/060876 patent/WO2010023181A1/en not_active Ceased
- 2009-08-24 CN CN2009801406895A patent/CN102186857A/zh active Pending
- 2009-08-25 AR ARP090103272A patent/AR073209A1/es unknown
- 2009-08-25 TW TW098128547A patent/TW201014864A/zh unknown
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2011
- 2011-02-02 IL IL211008A patent/IL211008A0/en unknown
- 2011-02-24 CL CL2011000409A patent/CL2011000409A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8486953B2 (en) | 2013-07-16 |
| EP2331551A1 (en) | 2011-06-15 |
| CN102186857A (zh) | 2011-09-14 |
| KR20110045019A (ko) | 2011-05-03 |
| ES2593495T3 (es) | 2016-12-09 |
| TW201014864A (en) | 2010-04-16 |
| RU2011110908A (ru) | 2012-10-10 |
| WO2010023181A1 (en) | 2010-03-04 |
| IL211008A0 (en) | 2011-04-28 |
| JP2012500825A (ja) | 2012-01-12 |
| MX2011001938A (es) | 2011-03-29 |
| UY32072A (es) | 2010-03-26 |
| CA2735361A1 (en) | 2010-03-04 |
| JP5675614B2 (ja) | 2015-02-25 |
| BRPI0918971A2 (pt) | 2015-12-01 |
| US20120128686A1 (en) | 2012-05-24 |
| EP2331551B1 (en) | 2016-06-29 |
| NZ591113A (en) | 2012-07-27 |
| AU2009286734A1 (en) | 2010-03-04 |
| CL2011000409A1 (es) | 2011-07-29 |
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