AR090292A1 - Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizan - Google Patents
Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizanInfo
- Publication number
- AR090292A1 AR090292A1 ARP130100765A ARP130100765A AR090292A1 AR 090292 A1 AR090292 A1 AR 090292A1 AR P130100765 A ARP130100765 A AR P130100765A AR P130100765 A ARP130100765 A AR P130100765A AR 090292 A1 AR090292 A1 AR 090292A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- cyano
- or1c
- optionally substituted
- hydrocarbyl
- Prior art date
Links
Classifications
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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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Composiciones que comprenden a dichos compuestos y métodos para su uso en el tratamiento, control y/o prevención de enfermedades y trastornos, mediados por la actividad de la quinasa asociada a adaptador 1. Reivindicación 1: Un método para inhibir la actividad de una quinasa asociada a adaptador 1 (AAK1), que comprende poner en contacto la AAK1 con un compuesto de la fórmula (1) o con una sal farmacéuticamente aceptable del mismo, en donde: R¹ es R¹A o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de R¹A; cada R¹A es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano, halo o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos ,en donde la sustitución opcional es con uno o más de R¹B; cada R¹B es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano o halo; cada R¹C, es de manera independiente, hidrógeno o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de ciano, halo o hidroxilo; R² es -NR²AR²B, en donde R²A es hidrógeno y R²B es hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más R²C; o R²A y R²B se toman juntos para formar un heterociclo de 4 - 7 miembros, opcionalmente sustituido con uno o más R²C; cada R²C es, de manera independiente, -OR²D, -N(R²D)₂, -C(O)R²D, -C(O)OR²D, -C(O)N(R²D)₂, -N(R²D)C(O)OR²D, ciano, halo o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de amino, ciano, halo, hidroxilo o R²D; cada R²D es, de manera independiente, hidrógeno o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de amino, ciano, halo, o hidroxilo; y R³ es hidrógeno o alquilo C₁₋₆, opcionalmente sustituido con uno o más de ciano, halo o hidroxilo. Reivindicación 33: Un compuesto de la fórmula (2) o una sal farmacéuticamente aceptable del mismo, en donde: A es hidrocarbilo C₁₋₁₂ cíclico o heterociclo de 4 - 7 miembros; D es heterociclo de 4 - 7 miembros; cada R¹A es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano, halo o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de R¹B; cada R¹B es, de manera independiente, -OR¹C, -N(R¹C)₂, -C(O)R¹C, -C(O)OR¹C, -C(O)N(R¹C)₂, -N(R¹C)C(O)OR¹C, ciano o halo; cada R¹C es, de manera independiente, hidrógeno o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de ciano, halo o hidroxilo; cada R²C es, de manera independiente, -OR²D, -N(R²D)₂, -C(O)R²D, -C(O)OR²D, -C(O)N(R²D)₂, -N(R²D)C(O)OR²D, ciano, halo, o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituidos, en donde la sustitución opcional es con uno o más de amino, ciano, halo, hidroxilo o R²D; cada R²D es, de manera independiente, hidrógeno o hidrocarbilo C₁₋₁₂ o heterocarbilo de 2 - 12 miembros, opcionalmente sustituido, en donde la sustitución opcional es con uno o más de amino, ciano, halo, hidroxilo; n es 1 - 3; y m es 0 - 3; con la salvedad de que cuando D es piperidinilo, A es fenilo y R²C es -N(R²D)₂, R²D no es etilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261608765P | 2012-03-09 | 2012-03-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR090292A1 true AR090292A1 (es) | 2014-11-05 |
Family
ID=47892052
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP130100765A AR090292A1 (es) | 2012-03-09 | 2013-03-11 | Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizan |
Country Status (26)
Country | Link |
---|---|
US (3) | US8946415B2 (es) |
EP (1) | EP2834243B1 (es) |
JP (1) | JP6418950B2 (es) |
KR (1) | KR101965025B1 (es) |
CN (1) | CN104302649B (es) |
AR (1) | AR090292A1 (es) |
AU (1) | AU2013230128B2 (es) |
BR (1) | BR112014022000A8 (es) |
CA (1) | CA2866143C (es) |
DK (1) | DK2834243T3 (es) |
ES (1) | ES2676224T3 (es) |
HK (1) | HK1201257A1 (es) |
HU (1) | HUE038786T2 (es) |
IL (1) | IL234486A (es) |
IN (1) | IN2014DN07384A (es) |
MX (1) | MX345830B (es) |
NZ (1) | NZ630721A (es) |
PL (1) | PL2834243T3 (es) |
PT (1) | PT2834243T (es) |
RU (1) | RU2014140735A (es) |
SG (1) | SG11201405561RA (es) |
TR (1) | TR201808280T4 (es) |
TW (1) | TW201341386A (es) |
UY (1) | UY34668A (es) |
WO (1) | WO2013134228A1 (es) |
ZA (1) | ZA201406149B (es) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
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MX345830B (es) | 2012-03-09 | 2017-02-17 | Lexicon Pharmaceuticals Inc | Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y metodos para su uso. |
JP6418949B2 (ja) | 2012-03-09 | 2018-11-07 | レクシコン ファーマシューティカルズ インコーポレイテッド | イミダゾ[1,2−b]ピリダジン系化合物、それを含む組成物、及びそれらを使用する方法 |
US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
JP2016509066A (ja) | 2013-02-22 | 2016-03-24 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | アダプター関連キナーゼ1(aak1)の阻害剤としての5h−クロメノ[3,4−c]ピリジン |
TW201542550A (zh) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
US9737542B2 (en) | 2013-10-11 | 2017-08-22 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
CN110317214B (zh) | 2014-01-24 | 2022-11-22 | 特普医药公司 | 作为蛋白质激酶的调节剂的二芳基巨环 |
US9932320B2 (en) * | 2014-01-31 | 2018-04-03 | Bristol-Myers Squibb Company | Quinoline-based kinase inhibitors |
TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法 |
US20170239249A1 (en) * | 2014-09-30 | 2017-08-24 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
CA2971024C (en) * | 2014-12-15 | 2023-09-26 | Handok Inc. | Fused ring heteroaryl compounds and their use as trk inhibitors |
WO2016164295A2 (en) | 2015-04-10 | 2016-10-13 | Bristol-Myers Squibb Company | Fused pyridines as kinase inhibitors |
AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
EP4397665A3 (en) | 2015-07-06 | 2024-08-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
AU2016296878B2 (en) | 2015-07-21 | 2020-12-17 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
EA036851B1 (ru) * | 2015-11-02 | 2020-12-28 | Янссен Фармацевтика Нв | [1,2,4]триазоло[1,5-a]пиримидин-7-ильное соединение |
RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
TWI764950B (zh) | 2016-11-02 | 2022-05-21 | 比利時商健生藥品公司 | Pde2抑制劑 |
JP7018944B2 (ja) | 2016-11-02 | 2022-02-14 | ヤンセン ファーマシューティカ エヌ.ベー. | PDE2阻害剤としての[1,2,4]トリアゾロ[1,5-a]ピリミジン化合物 |
AU2017353315B2 (en) | 2016-11-02 | 2021-09-16 | Janssen Pharmaceutica Nv | (1,2,4)triazolo(1,5-a)pyrimidine compounds as PDE2 inhibitors |
TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
EP3658148B1 (en) | 2017-07-28 | 2024-07-10 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
AU2018306444B2 (en) | 2017-07-28 | 2022-11-17 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
ES2929467T3 (es) | 2017-12-19 | 2022-11-29 | Turning Point Therapeutics Inc | Compuestos macrocíclicos para tratar enfermedades |
CN111362949B (zh) | 2017-12-22 | 2021-12-21 | 深圳市塔吉瑞生物医药有限公司 | 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途 |
US11345703B2 (en) | 2018-01-23 | 2022-05-31 | Shenzhen Targetrx, Inc. | Substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound |
EP3856743A4 (en) * | 2018-09-27 | 2022-06-15 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS |
EP3866789A4 (en) * | 2018-10-15 | 2022-07-06 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
EP4138844A1 (en) * | 2020-04-21 | 2023-03-01 | Lexicon Pharmaceuticals, Inc. | 4-(3-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine for use in the the treatment of cov-229e or cov-oc43 coronaviruses infections |
CA3175970A1 (en) | 2020-04-21 | 2021-10-28 | Suma GOPINATHAN | Aak1 inhibitors for use in treating viral infections |
US11478733B2 (en) | 2020-11-24 | 2022-10-25 | Caterpillar Inc. | Filter interlock with tabs mating with a pedestal or a housing |
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ES2548135T3 (es) * | 2008-05-13 | 2015-10-14 | Novartis Ag | Heterociclos condensados que contienen nitrógeno y composiciones de los mismos como inhibidores de quinasa |
KR102037619B1 (ko) * | 2008-10-22 | 2019-10-28 | 어레이 바이오파마 인크. | TRK 키나아제 억제제로서 치환된 피라졸로[1,5a] 피리미딘 화합물 |
AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
TW201113286A (en) | 2009-09-03 | 2011-04-16 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors |
WO2011087999A1 (en) * | 2010-01-14 | 2011-07-21 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidines as mark inhibitors |
PL3409278T3 (pl) * | 2011-07-21 | 2021-02-22 | Sumitomo Pharma Oncology, Inc. | Heterocykliczne inhibitory kinazy białkowej |
MX345830B (es) | 2012-03-09 | 2017-02-17 | Lexicon Pharmaceuticals Inc | Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y metodos para su uso. |
JP6418949B2 (ja) | 2012-03-09 | 2018-11-07 | レクシコン ファーマシューティカルズ インコーポレイテッド | イミダゾ[1,2−b]ピリダジン系化合物、それを含む組成物、及びそれらを使用する方法 |
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TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法 |
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2013
- 2013-03-05 MX MX2014010589A patent/MX345830B/es active IP Right Grant
- 2013-03-05 JP JP2014561024A patent/JP6418950B2/ja active Active
- 2013-03-05 SG SG11201405561RA patent/SG11201405561RA/en unknown
- 2013-03-05 PL PL13710250T patent/PL2834243T3/pl unknown
- 2013-03-05 KR KR1020147028071A patent/KR101965025B1/ko active IP Right Grant
- 2013-03-05 AU AU2013230128A patent/AU2013230128B2/en active Active
- 2013-03-05 CN CN201380012483.0A patent/CN104302649B/zh active Active
- 2013-03-05 EP EP13710250.5A patent/EP2834243B1/en active Active
- 2013-03-05 ES ES13710250.5T patent/ES2676224T3/es active Active
- 2013-03-05 BR BR112014022000A patent/BR112014022000A8/pt not_active Application Discontinuation
- 2013-03-05 IN IN7384DEN2014 patent/IN2014DN07384A/en unknown
- 2013-03-05 HU HUE13710250A patent/HUE038786T2/hu unknown
- 2013-03-05 CA CA2866143A patent/CA2866143C/en active Active
- 2013-03-05 NZ NZ630721A patent/NZ630721A/en unknown
- 2013-03-05 TR TR2018/08280T patent/TR201808280T4/tr unknown
- 2013-03-05 RU RU2014140735A patent/RU2014140735A/ru not_active Application Discontinuation
- 2013-03-05 DK DK13710250.5T patent/DK2834243T3/en active
- 2013-03-05 US US13/785,355 patent/US8946415B2/en active Active
- 2013-03-05 WO PCT/US2013/029056 patent/WO2013134228A1/en active Application Filing
- 2013-03-05 PT PT137102505T patent/PT2834243T/pt unknown
- 2013-03-08 TW TW102108283A patent/TW201341386A/zh unknown
- 2013-03-11 UY UY0001034668A patent/UY34668A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100765A patent/AR090292A1/es unknown
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2014
- 2014-08-21 ZA ZA2014/06149A patent/ZA201406149B/en unknown
- 2014-09-07 IL IL234486A patent/IL234486A/en active IP Right Grant
- 2014-09-11 US US14/483,898 patent/US9403832B2/en active Active
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2015
- 2015-02-13 HK HK15101651.1A patent/HK1201257A1/xx unknown
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2016
- 2016-07-12 US US15/207,677 patent/US20170129896A1/en not_active Abandoned
Also Published As
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Publication | Publication Date | Title |
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