AR080327A1 - Tienopirimidinas que contienen heterocicloalquilo inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros. - Google Patents
Tienopirimidinas que contienen heterocicloalquilo inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros.Info
- Publication number
- AR080327A1 AR080327A1 ARP110100601A ARP110100601A AR080327A1 AR 080327 A1 AR080327 A1 AR 080327A1 AR P110100601 A ARP110100601 A AR P110100601A AR P110100601 A ARP110100601 A AR P110100601A AR 080327 A1 AR080327 A1 AR 080327A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- group
- substituted
- phenyl
- 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
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 208000030159 metabolic disease Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004069 aziridinyl group Chemical group 0.000 abstract 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 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
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- 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
- 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
- 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
- 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
-
- 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
- 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
- A61P7/06—Antianaemics
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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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- 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
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)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto caracterizado porque tiene la formula general (1) en la que X es CH o N, R1 es H, halogeno, CN, CH3 o CF3, R2 es un grupo seleccionado de (2) donde el grupo puede estar sustituido en el átomo de nitrogeno con (3) -SO2-(alquilo C1-3), -CO-(alquilo C1-3), -CO-(CH2)n-O-(alquilo C1-3), -CO-(CH2)n-N(alquilo C1-3)2, alquilo C1-4, -(CH2)n-CF3, -(CH2)n-CHF2, -(CH2)n-OH, -(CH2)n-O-(alquilo C1-3), -(CH2)n-CN, (4) y donde puede estar sustituido en un átomo de carbono con un grupo -CH2OH, donde n es 1 o 2, y donde el grupo puede estar sustituido en el átomo de nitrogeno con alquilo (3) C1-4 lineal o ramificado, -(CH2)n-CF3, -(CH2)n-CHF2, -(CH2)n-OH, -(CH2)n-O-(aIquilo C1-3), -(CH2)n-CN, -(CH2)n-CO-N(alquilo C1-3)2, -SO2-(aIquilo C1-3), -CO-(alquilo C1-3), -CO2(alquilo C1-4), -CO2-(CH2)n-CF3, -CO2-(CH2)n-O-(alquilo C1-3), -CO2-(CH2)n-CO-N(alquilo C1-3)2, (4) donde n es 1 o 2, R3 un grupo alquilo C1-2, y R4 es -COOH, -CO2(alquilo C1-3), -CO2-(CH2)n-N(alquilo C1-3)2, -CONH2, -CO-NHR5, -CO-NH-(CH2)p-R6, -CO-NH-(CH2)m-R7, -CO-N(CH3)-(CH2)m-R7, CO-N(CH3)-(CH2)-ciclohexilo, (5), R5 es -CN, -OH, alquilo C1-6 lineal o ramificado, -O(alquilo C1-3), cicloalquilo C3-6, -SO2-(alquilo C1-3); pirazolilo opcionalmente sustituido con metilo; o piperidinilo opcionalmente sustituido con metilo, donde el grupo cicloalquilo C3-6 puede estar sustituido con -NH2, -OH u -OCH3; R6 es -C(CH3)2Cl; -C(CH3)2OH; -CHC3-6 cicloalquilo, que está opcionalmente sustituido con OH; imidazolilo, que está opcionalmente sustituido con metilo; pirrolidinilo, que está opcionalmente sustituido con alquilo C1-3 o con un grupo oxo; tetrahidrofuranilo; tetrahidropiranilo; fenilo, que está opcionalmente sustituido con uno o dos -F, -CI, -CN, -OH, alquilo C1-3 u -O(alquilo C1-3); naftilo; piridinilo; furanilo; tiofenilo; oxazolilo; tiazolilo; pirazolilo; morfolinilo, que está opcionalmente sustituido con metilo; benzotiofenilo; -CO-fenilo; o -SO2-N(alquilo C1-3)2, y R7 es F, -OH, -OCF3, -O-(alquilo C1-3), -O-fenilo, -O(CH2)m-OH, -N(alquilo C1-3)2, -NH-fenilo, piperidinilo, pirrolidinilo, azetedinilo o aziridinilo, y donde el átomo de hidrogeno en los grupos NH puede reemplazarse con alquilo C1-3, donde p es 1, 2 o 3, y m es 2 o 3, o un tautomero, enantiomero, díastereomero o la sal del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10154925 | 2010-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080327A1 true AR080327A1 (es) | 2012-03-28 |
Family
ID=43902874
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100601A AR080327A1 (es) | 2010-02-26 | 2011-02-25 | Tienopirimidinas que contienen heterocicloalquilo inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros. |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8648068B2 (es) |
| EP (1) | EP2539346B1 (es) |
| JP (1) | JP5639197B2 (es) |
| KR (1) | KR20120130052A (es) |
| CN (1) | CN102869669A (es) |
| AR (1) | AR080327A1 (es) |
| AU (1) | AU2011219761A1 (es) |
| BR (1) | BR112012021264A2 (es) |
| CA (1) | CA2791105A1 (es) |
| CL (1) | CL2012002318A1 (es) |
| EA (1) | EA201201193A1 (es) |
| MX (1) | MX2012009409A (es) |
| PH (1) | PH12012501691A1 (es) |
| TW (1) | TW201141482A (es) |
| UY (1) | UY33241A (es) |
| WO (1) | WO2011104337A1 (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1899353A1 (en) * | 2005-06-22 | 2008-03-19 | DeveloGen Aktiengesellschaft | Thienopyrimidines for pharmaceutical compositions |
| JP5302883B2 (ja) | 2006-04-07 | 2013-10-02 | 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 | 医薬組成物用のmnk1/mnk2阻害活性を有するチエノピリミジン |
| EP1889847A1 (en) | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| KR20110045019A (ko) | 2008-08-26 | 2011-05-03 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물을 위한 티에노피리미딘 |
| 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 |
| MX2012009869A (es) | 2010-02-26 | 2012-09-12 | Japan Tobacco Inc | Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih. |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| AR080328A1 (es) * | 2010-02-26 | 2012-03-28 | Boehringer Ingelheim Int | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| CA2873967A1 (en) | 2012-05-21 | 2013-11-28 | Bayer Pharma Aktiengesellschaft | Substituted benzothienopyrimidines |
| EP2852596B1 (en) | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| SG10201610869TA (en) | 2012-06-26 | 2017-02-27 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalacti |
| 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 |
| CA2899665A1 (en) | 2013-02-01 | 2014-08-07 | Bayer Pharma Aktiengesellschaft | Substituted thienopyrimidines and pharmaceutical use thereof |
| EP2951175B1 (en) | 2013-02-01 | 2017-10-04 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolopyrimidinylamino-indazoles |
| WO2014135480A1 (en) | 2013-03-06 | 2014-09-12 | Bayer Pharma Aktiengesellschaft | Substituted thiazolopyrimidines |
| EP2983674A4 (en) | 2013-04-08 | 2017-05-10 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| CN103356626B (zh) * | 2013-08-02 | 2015-01-07 | 上海市第十人民医院 | 吡唑并嘧啶类化合物在制备抗红色毛癣菌感染疾病药物中的应用 |
| CN103356624B (zh) * | 2013-08-02 | 2014-12-31 | 上海市第十人民医院 | 一种嘧啶类化合物在制备抗真菌药物中的应用 |
| CN103417545B (zh) * | 2013-08-02 | 2014-12-31 | 上海市第十人民医院 | 一种吡唑并嘧啶类化合物在制备抗烟曲霉菌感染性疾病药物中的应用 |
| CN103356625B (zh) * | 2013-08-02 | 2014-10-29 | 上海市第十人民医院 | 嗓唑并嘧啶类在近平滑假丝酵母菌感染性疾病应用 |
| CN103356627B (zh) * | 2013-08-02 | 2014-10-29 | 上海市第十人民医院 | 一种药物在光滑假丝酵母菌感染性疾病应用 |
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| US9512084B2 (en) * | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| AU2014359456B2 (en) * | 2013-12-04 | 2019-01-24 | Evotec International Gmbh | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| WO2015091156A1 (en) * | 2013-12-17 | 2015-06-25 | Boehringer Ingelheim International Gmbh | Sulfoximine substituted pyrrolotriazines for pharmaceutical compositions |
| AU2015257917C1 (en) * | 2014-05-07 | 2019-03-14 | Evotec International Gmbh | Sulfoximine substituted quinazolines for pharmaceutical compositions |
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-
2011
- 2011-02-24 UY UY0001033241A patent/UY33241A/es not_active Application Discontinuation
- 2011-02-25 AR ARP110100601A patent/AR080327A1/es unknown
- 2011-02-25 US US13/034,913 patent/US8648068B2/en not_active Expired - Fee Related
- 2011-02-25 BR BR112012021264A patent/BR112012021264A2/pt not_active Application Discontinuation
- 2011-02-25 TW TW100106540A patent/TW201141482A/zh unknown
- 2011-02-25 JP JP2012554347A patent/JP5639197B2/ja not_active Expired - Fee Related
- 2011-02-25 CN CN2011800209929A patent/CN102869669A/zh active Pending
- 2011-02-25 AU AU2011219761A patent/AU2011219761A1/en not_active Abandoned
- 2011-02-25 PH PH1/2012/501691A patent/PH12012501691A1/en unknown
- 2011-02-25 KR KR1020127022310A patent/KR20120130052A/ko not_active Withdrawn
- 2011-02-25 EA EA201201193A patent/EA201201193A1/ru unknown
- 2011-02-25 WO PCT/EP2011/052810 patent/WO2011104337A1/en not_active Ceased
- 2011-02-25 MX MX2012009409A patent/MX2012009409A/es not_active Application Discontinuation
- 2011-02-25 EP EP11707387.4A patent/EP2539346B1/en not_active Ceased
- 2011-02-25 CA CA2791105A patent/CA2791105A1/en not_active Abandoned
-
2012
- 2012-08-21 CL CL2012002318A patent/CL2012002318A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| UY33241A (es) | 2011-09-30 |
| AU2011219761A1 (en) | 2012-08-16 |
| CN102869669A (zh) | 2013-01-09 |
| TW201141482A (en) | 2011-12-01 |
| JP5639197B2 (ja) | 2014-12-10 |
| WO2011104337A1 (en) | 2011-09-01 |
| CL2012002318A1 (es) | 2012-11-23 |
| EP2539346B1 (en) | 2014-04-16 |
| CA2791105A1 (en) | 2011-09-01 |
| JP2013520472A (ja) | 2013-06-06 |
| BR112012021264A2 (pt) | 2016-05-17 |
| KR20120130052A (ko) | 2012-11-28 |
| PH12012501691A1 (en) | 2012-11-05 |
| US20110212102A1 (en) | 2011-09-01 |
| EA201201193A1 (ru) | 2013-04-30 |
| US8648068B2 (en) | 2014-02-11 |
| MX2012009409A (es) | 2012-09-07 |
| EP2539346A1 (en) | 2013-01-02 |
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