AR082945A1 - Derivados de imidazo[1,2-b]piridazina como inhibidores de la trk - Google Patents
Derivados de imidazo[1,2-b]piridazina como inhibidores de la trkInfo
- Publication number
- AR082945A1 AR082945A1 ARP110103293A ARP110103293A AR082945A1 AR 082945 A1 AR082945 A1 AR 082945A1 AR P110103293 A ARP110103293 A AR P110103293A AR P110103293 A ARP110103293 A AR P110103293A AR 082945 A1 AR082945 A1 AR 082945A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently selected
- substituted
- halo
- heteroatoms
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 12
- 125000005843 halogen group Chemical group 0.000 abstract 9
- 125000005842 heteroatom Chemical group 0.000 abstract 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 125000002947 alkylene group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 108020004021 3-ketosteroid receptors Proteins 0.000 abstract 2
- 108020000002 NR3 subfamily Proteins 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) 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
- -1 -OR4 Chemical group 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 1
- 230000002159 abnormal effect Effects 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 230000002074 deregulated effect Effects 0.000 abstract 1
- 229910052805 deuterium Inorganic materials 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P25/04—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
- 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
- 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
-
- 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
-
- 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
-
- 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
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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Composiciones farmacéuticas que comprenden dichos compuestos y métodos de uso de tales compuestos para tratar o prevenir enfermedades o trastornos asociados con actividad anormal o desregulada de la quinasa TRK.Reivindicación 1: Un compuesto de la fórmula (1) en donde RA es un resto del grupo de fórmulas (2); X es C(R3)2, S o NR3; RB es halo, -CN, -C(O)NH2, -L1R2, -L2R7, -C(O)NHOR3, -C(O)NR3OR8, -C(O)NHNH2, -C(O)NR3C(O)OR3, -C(O)NR3C(O)N(R3)2, -NR3C(O)NR3R5, un resto de fórmula (3) o -SO2NR3R3; L1 es -C(O)NR3-, -C(O)NR3(CR4R4)q-, -C(O)-, -C(O)NR3O(CR4R4)q, -C(O)O-, -C(O)-alquileno C1-8 o -C(O)-alquenileno C2-8; L2 es -NR3C(O)(CR4R4)q-; cada L3 se selecciona independientemente de un alquileno C1-8 y alquileno C1-8 sustituido con 1 a 3 sustituyentes independientemente seleccionados de alquilo C1-6; R2 se selecciona de R9, -N(R3)2, alquilo C1-6, fenilo, arilo C6-10, arilo C1-4, cicloalquilo C3-8, heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados entre N, O y S, un heteroarilo de 5, 6, 9 ó 10 miembros que contiene de 1 a 3 heteroátomos N y alquilo C1-8 sustituido con 1 a 6 grupos seleccionados independientemente entre halo, alquilo C1-4 y R6; o R2 se selecciona de fenilo, arilo C10, arilo C14, cicloalquilo C3-8, heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados entre N, O y S, y un heteroarilo de 5, 6, 9 ó 10 miembros que contiene de 1 a 3 heteroátomos N, cada uno de los cuales está sustituido con 1 a 3 sustituyentes seleccionados independientemente entre halo, alquilo C1-6, alquilo C1-6 sustituido con 1 a 4 grupos hidroxilo, heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados entre N, O y S, CN, -R8, -OR4, -C(O)R4-, -C(O)OR4, -C(O)L3R6, -S(O)2R4, y -S(O)2NR4R4; cada R3 es independientemente seleccionado a partir de H, alquilo C1-6; cada R4 es independientemente seleccionado a partir de H, alquilo C1-6, y alquilo C1-6 sustituido por 1 a 4 grupos hidroxilo; R5 es haloalquilo C1-4 u -OR3; R6 es seleccionado a partir de -OC(O)R4, -NHC(O)OR4, -NR3R3, -C(O)N(R3R3), -S(O)2R4, -S(O)2NR4R4, -C(O)OR4 y -OR4; R7 es halo, -OC(O)R12, -OR12, -CN, -NHC(O)OR12, -NHC(O)R12 o -NR3R3; R8 es un heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados a partir de N, O y S o heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados a partir de N, O y S sustituido por 1 a 4 sustituyentes independientemente seleccionados a partir de halo, -OR4, alquilo C1-6 y haloalquilo C1-6; R9 es ciclohexilo que tiene un puente alquilo C1-6, o un resto del grupo de fórmulas (4), en donde cada uno es opcionalmente sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de halo, -CN, alquilo C1-6, -R8, y -OR3; cada R10 es independientemente seleccionado a partir de halo, alquilo C1-6, haloalquilo C1-6, -C=NOR3, -CN, -(CR4R4)qCN, -NR3R3, -C(O)OR4, -C(O)NR3R3, -(CR4R4)qR6, -NR3C(O)NR3R3, -NR3S(O)2R4, - NR3S(O)2NR4R4, -S(O)2NR4R4, -S(O)2R4, -OR4, heterocicloalquilo de 4 - 6 miembros que contiene 1 a 2 heteroátomos seleccionados a partir de N, O y S y un heteroarilo de 5 miembros que contiene 1 a 4 heteroátomos N; cada R11 es independientemente seleccionado a partir de halo, -OR3, deuterio, alquilo C1-6, alquilo C1-6hidroxil-sustituido, haloalquilo C1-6; R12 es H, alquilo C1-6, fenilo o fenilo sustituido por 1 a 3 grupos independientemente seleccionados a partir de halo, alquilo C1-4, y -R6; R20 es seleccionado a partir de los restos del grupo de fórmulas (5), cada uno sustituido por 1 a 3 sustituyentes independientemente seleccionados a partir de R10, o R20 es seleccionado a partir de los restos del grupo de fórmulas (6), cada uno opcionalmente sustituido por 1 a 3 sustituyentes Independientemente seleccionados a partir de R10; n es 0, 1, 2, 3, 4, 5, 6 ó 7; p es 1 ó 2; y q es 1, 2, 3, 4, 5 ó 6; o una sal farmacéuticamente aceptable de la misma.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38137310P | 2010-09-09 | 2010-09-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR082945A1 true AR082945A1 (es) | 2013-01-23 |
Family
ID=44653602
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103293A AR082945A1 (es) | 2010-09-09 | 2011-09-09 | Derivados de imidazo[1,2-b]piridazina como inhibidores de la trk |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8637516B2 (es) |
| EP (1) | EP2614062A1 (es) |
| JP (1) | JP2013537199A (es) |
| AR (1) | AR082945A1 (es) |
| AU (1) | AU2011299026A1 (es) |
| CA (1) | CA2810858A1 (es) |
| TW (1) | TW201211050A (es) |
| UY (1) | UY33597A (es) |
| WO (1) | WO2012034091A1 (es) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2952692C (en) | 2008-09-22 | 2020-04-28 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds |
| PT3372605T (pt) | 2008-10-22 | 2021-12-09 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]pirimidina substituídos como inibidores de quinase trk |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| SMT201900203T1 (it) | 2010-05-20 | 2019-05-10 | Array Biopharma Inc | Composti macrociclici come inibitori di trk chinasi |
| BR112013021638A2 (pt) * | 2011-02-25 | 2016-08-02 | Irm Llc | "compostos inibidores de trk, seu uso e composições que os compreendem" |
| TWI574962B (zh) | 2012-11-14 | 2017-03-21 | 加拓科學公司 | 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途 |
| EP3800183A1 (en) * | 2013-02-19 | 2021-04-07 | ONO Pharmaceutical Co., Ltd. | Urea derivatives as trk-inhibiting compounds |
| WO2014138692A1 (en) | 2013-03-07 | 2014-09-12 | Califia Bio, Inc. | Mixed lineage kinase inhibitors and method of treatments |
| US10407509B2 (en) | 2013-07-30 | 2019-09-10 | Blueprint Medicines Corporation | NTRK2 fusions |
| PL3097107T3 (pl) | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| CN103864786A (zh) * | 2014-03-13 | 2014-06-18 | 定陶县友帮化工有限公司 | 一种6-氟咪唑并[1,2-a]吡啶-3-甲酸的合成方法 |
| CN103880843A (zh) * | 2014-04-03 | 2014-06-25 | 定陶县友帮化工有限公司 | 6-溴咪唑并[1,2-a]吡啶-3-甲腈的合成方法 |
| CN103896941A (zh) * | 2014-04-03 | 2014-07-02 | 定陶县友帮化工有限公司 | 6-氯咪唑并[1,2-a]吡啶-3-甲腈的合成方法 |
| WO2015183837A1 (en) * | 2014-05-27 | 2015-12-03 | Brian Haynes | Compositions, methods, and uses related to ntrk2-tert fusions |
| CA2967951C (en) | 2014-11-16 | 2023-11-07 | Array Biopharma, Inc. | Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| KR20180021745A (ko) | 2015-06-01 | 2018-03-05 | 록쏘 온콜로지, 인코포레이티드 | 암을 진단하고 치료하는 방법 |
| EP3317285B1 (en) * | 2015-07-02 | 2021-01-27 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| RS65593B1 (sr) | 2015-07-06 | 2024-06-28 | Turning Point Therapeutics Inc | Polimorf diaril makrocikla |
| SI3322706T1 (sl) | 2015-07-16 | 2021-04-30 | Array Biopharma, Inc. | Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze |
| PL3733187T3 (pl) | 2015-07-21 | 2025-01-07 | Turning Point Therapeutics, Inc. | Chiralny makrocykl diarylowy i jego zastosowanie w leczeniu raka |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| CA3003153A1 (en) | 2015-10-26 | 2017-05-04 | Loxo Oncology, Inc. | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| SG11201803920TA (en) | 2015-11-19 | 2018-06-28 | Blueprint Medicines Corp | Compounds and compositions useful for treating disorders related to ntrk |
| JP7057343B2 (ja) | 2016-04-04 | 2022-04-19 | ロクソ オンコロジー， インコーポレイテッド | 小児癌の処置方法 |
| PH12018502124B1 (en) | 2016-04-04 | 2024-04-12 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| PT3458456T (pt) | 2016-05-18 | 2020-12-07 | Array Biopharma Inc | Preparação de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidino-1-carboxamida |
| CA3031100A1 (en) | 2016-07-28 | 2018-02-01 | Tp Therapeutics, Inc. | Macrocycle kinase inhibitors |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| CN106632353A (zh) * | 2016-11-18 | 2017-05-10 | 山东友帮生化科技有限公司 | 3‑硝基‑6‑氯咪唑并[1,2‑b]哒嗪的合成方法 |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret 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 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| PL3658148T3 (pl) | 2017-07-28 | 2024-10-07 | Turning Point Therapeutics, Inc. | Związki makrocykliczne i ich zastosowania |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| US20190247398A1 (en) | 2017-10-26 | 2019-08-15 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| AU2018392332B2 (en) | 2017-12-19 | 2023-08-03 | Turning Point Therapeutics, Inc. | Macrocyclic compounds for treating disease |
| JP6997876B2 (ja) | 2018-01-18 | 2022-02-04 | アレイ バイオファーマ インコーポレイテッド | Ｒｅｔキナーゼ阻害剤としての置換ピラゾリル［４，３－ｃ］ピリジン化合物 |
| US11524963B2 (en) | 2018-01-18 | 2022-12-13 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| EP3765462B1 (en) * | 2018-03-14 | 2023-10-18 | Fochon Biosciences, Ltd. | Substituted (2-azabicyclo [3.1.0] hexan-2-yl) pyrazolo [1, 5-a] pyrimidine and imidazo [1, 2-b] pyridazine compounds as trk kinases inhibitors |
| CA3095366A1 (en) | 2018-03-29 | 2019-10-03 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN110294761B (zh) * | 2018-06-08 | 2020-09-08 | 南京雷正医药科技有限公司 | 作为Trk激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| GB201811825D0 (en) * | 2018-07-19 | 2018-09-05 | Benevolentai Bio Ltd | Organic compounds |
| US12109193B2 (en) | 2018-07-31 | 2024-10-08 | Loxo Oncology Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide |
| GB201813791D0 (en) | 2018-08-23 | 2018-10-10 | Benevolental Bio Ltd | Organic compounds |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| CN111171019A (zh) * | 2018-11-13 | 2020-05-19 | 上海轶诺药业有限公司 | 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途 |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| CA3126034A1 (en) * | 2019-01-23 | 2020-07-30 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| MX2021013576A (es) * | 2019-05-08 | 2021-12-15 | Tyk Medicines Inc | Compuesto utilizado como inhibidor de la quinasa y aplicación del mismo. |
| WO2021047584A1 (en) * | 2019-09-11 | 2021-03-18 | Fochon Pharmaceuticals, Ltd. | SUBSTITUTED (2-AZABICYCLO [3.1.0] HEXAN-2-YL) PYRAZOLO [1, 5-a] PYRIMIDINE AND IMIDAZO [1, 2-b] PYRIDAZINE COMPOUNDS AS TRK KINASES INHIBITORS |
| CN110804059B (zh) * | 2019-09-30 | 2024-03-12 | 郑州泰基鸿诺医药股份有限公司 | 氨基甲酸酯类化合物、药物组合物及其应用 |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| CN112812118A (zh) * | 2019-11-18 | 2021-05-18 | 上海轶诺药业有限公司 | 一类蛋白受体激酶抑制剂的制备和应用 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| JP2023511172A (ja) | 2020-01-22 | 2023-03-16 | ベネボレントエーアイ バイオ リミティド | 医薬組成物及びその使用 |
| JP2023511170A (ja) * | 2020-01-22 | 2023-03-16 | ベネボレントエーアイ バイオ リミティド | 医薬組成物及びその使用 |
| KR102874188B1 (ko) * | 2020-05-15 | 2025-10-21 | 씨에스피씨 종콰이 팔마씨우티컬 테크놀로지 (스자좡) 컴퍼니 리미티드 | 융합된 아자 헤테로 시클릭 아미드계 화합물 및 이의 용도 |
| AU2021290168A1 (en) | 2020-06-10 | 2023-01-05 | Epics Therapeutics | Synthesis of (2S,5R)-5-(2-chlorophenyl)-1-(2'-methoxy-[1,1'-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid |
| CN112321592B (zh) * | 2020-11-12 | 2022-03-04 | 山东省科学院菏泽分院 | 一种6-氯咪唑并[1,2-b]哒嗪-3-甲腈的合成方法 |
| KR20230170938A (ko) * | 2021-04-13 | 2023-12-19 | 선전 뉴델 바이오텍 씨오., 엘티디. | 알키닐페닐벤즈아미드계 화합물 및 이의 응용 |
| WO2022234287A1 (en) | 2021-05-06 | 2022-11-10 | Benevolentai Bio Limited | Imidazopyridazine derivatives useful as trk inhibitors |
| EP4357347B1 (en) * | 2021-06-21 | 2024-12-11 | Henan Medinno Pharmaceutical Technology Co., Ltd. | Trk kinase inhibitor compound and use thereof |
| CN114989176B (zh) * | 2022-07-08 | 2024-08-27 | 深圳市新樾生物科技有限公司 | 咪唑并哒嗪类衍生物及其应用 |
| CN117417340B (zh) * | 2023-10-12 | 2025-08-26 | 山东省科学院菏泽分院 | 一种6-氯咪唑并[1,2-b]哒嗪-3-甲腈的制备方法 |
Family Cites Families (204)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1219606A (en) | 1968-07-15 | 1971-01-20 | Rech S Et D Applic Scient Soge | Quinuclidinol derivatives and preparation thereof |
| GB8334494D0 (en) | 1983-12-24 | 1984-02-01 | Tanabe Seiyaku Co | Carbostyril derivatives |
| JPS6235216A (ja) | 1985-08-09 | 1987-02-16 | Noritoshi Nakabachi | 不均質物質層の層厚非破壊測定方法および装置 |
| GB8916480D0 (en) | 1989-07-19 | 1989-09-06 | Glaxo Group Ltd | Chemical process |
| GB8923590D0 (en) | 1989-10-19 | 1989-12-06 | Pfizer Ltd | Antimuscarinic bronchodilators |
| PT100441A (pt) | 1991-05-02 | 1993-09-30 | Smithkline Beecham Corp | Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso |
| US5451700A (en) | 1991-06-11 | 1995-09-19 | Ciba-Geigy Corporation | Amidino compounds, their manufacture and methods of treatment |
| WO1993018007A1 (fr) | 1992-03-13 | 1993-09-16 | Tokyo Tanabe Company Limited | Nouveau derive de carbostyrile |
| WO1993019750A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating allergic or inflammatory diseases |
| HU225869B1 (en) | 1992-04-02 | 2007-11-28 | Smithkline Beecham Corp | Compounds with antiallergic and antiinflammatory activity and pharmaceutical compns. contg. them |
| JP3251587B2 (ja) | 1992-04-02 | 2002-01-28 | スミスクライン・ビーチャム・コーポレイション | 炎症疾患の治療および腫瘍壊死因子の産生阻害に有用な化合物 |
| GB9301000D0 (en) | 1993-01-20 | 1993-03-10 | Glaxo Group Ltd | Chemical compounds |
| GB9414193D0 (en) | 1994-07-14 | 1994-08-31 | Glaxo Group Ltd | Compounds |
| GB9414208D0 (en) | 1994-07-14 | 1994-08-31 | Glaxo Group Ltd | Compounds |
| GB9622386D0 (en) | 1996-10-28 | 1997-01-08 | Sandoz Ltd | Organic compounds |
| TW528755B (en) | 1996-12-24 | 2003-04-21 | Glaxo Group Ltd | 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives |
| AU9281298A (en) | 1997-10-01 | 1999-04-23 | Kyowa Hakko Kogyo Co. Ltd. | Benzodioxole derivatives |
| GB9723589D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB9723590D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB9723566D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| YU44900A (sh) | 1998-01-31 | 2003-01-31 | Glaxo Group Limited | Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola |
| PE20000270A1 (es) | 1998-02-14 | 2000-05-20 | Glaxo Group Ltd | Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol |
| US6541669B1 (en) | 1998-06-08 | 2003-04-01 | Theravance, Inc. | β2-adrenergic receptor agonists |
| GB9813540D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| CN1313861A (zh) | 1998-06-23 | 2001-09-19 | 葛兰素集团有限公司 | 2－(嘌呤－9－基)－四氢呋喃－3,4－二醇衍生物 |
| GB9813535D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| GB9813565D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| CA2335094C (en) | 1998-06-30 | 2008-12-23 | The Dow Chemical Company | Polymer polyols and a process for the production thereof |
| AU5879299A (en) | 1998-10-16 | 2000-05-08 | Monaghan, Sandra Marina | Adenine derivatives |
| GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| YU25500A (sh) | 1999-05-11 | 2003-08-29 | Pfizer Products Inc. | Postupak za sintezu analoga nukleozida |
| US6683115B2 (en) | 1999-06-02 | 2004-01-27 | Theravance, Inc. | β2-adrenergic receptor agonists |
| GB9913932D0 (en) | 1999-06-15 | 1999-08-18 | Pfizer Ltd | Purine derivatives |
| US6322771B1 (en) | 1999-06-18 | 2001-11-27 | University Of Virginia Patent Foundation | Induction of pharmacological stress with adenosine receptor agonists |
| CA2383546A1 (en) | 1999-06-30 | 2001-01-04 | William H. Parsons | Src kinase inhibitor compounds |
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| AU777012B2 (en) | 1999-08-21 | 2004-09-30 | Takeda Gmbh | Synergistic combination of PDE inhibitors and beta 2 adrenoceptor agonist |
| CO5180581A1 (es) | 1999-09-30 | 2002-07-30 | Pfizer Prod Inc | Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia |
| GB9924363D0 (en) | 1999-10-14 | 1999-12-15 | Pfizer Central Res | Purine derivatives |
| GB9924361D0 (en) | 1999-10-14 | 1999-12-15 | Pfizer Ltd | Purine derivatives |
| OA11558A (en) | 1999-12-08 | 2004-06-03 | Advanced Medicine Inc | Beta 2-adrenergic receptor agonists. |
| WO2003000840A2 (en) | 2001-06-21 | 2003-01-03 | Diversa Corporation | Nitrilases |
| GB0003960D0 (en) | 2000-02-18 | 2000-04-12 | Pfizer Ltd | Purine derivatives |
| WO2001083462A1 (de) | 2000-04-27 | 2001-11-08 | Boehringer Ingelheim Pharma Kg | Neue, langwirksame betamimetika, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| TWI227240B (en) | 2000-06-06 | 2005-02-01 | Pfizer | 2-aminocarbonyl-9H-purine derivatives |
| GB0015727D0 (en) | 2000-06-27 | 2000-08-16 | Pfizer Ltd | Purine derivatives |
| DK1300407T4 (da) | 2000-06-27 | 2011-09-05 | S A L V A T Lab Sa | Carbamater afledt af arylalkylaminer |
| GB0015876D0 (en) | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| DE10038639A1 (de) | 2000-07-28 | 2002-02-21 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| KR100889426B1 (ko) | 2000-08-05 | 2009-03-23 | 글락소 그룹 리미티드 | 항염증제로서의 6.알파.,9.알파.-디플루오로-17.알파.-'(2-푸라닐카르복실)옥시-11.베타.-히드록시-16.알파.-메틸-3-옥소-안드로스트-1,4-디엔-17-카르보티오산 ｓ-플루오로메틸 에스테르 |
| GB0022695D0 (en) | 2000-09-15 | 2000-11-01 | Pfizer Ltd | Purine Derivatives |
| GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
| ATE305468T1 (de) | 2000-12-22 | 2005-10-15 | Almirall Prodesfarma Ag | Chinuclidincarbamat derivate und deren verwendung als m3 antagonisten |
| SI1353919T1 (sl) | 2000-12-28 | 2006-12-31 | Almirall Prodesfarma Ag | Novi derivati kinuklidina in medicinske zmesi, kijih vsebujejo. |
| GB0103630D0 (en) | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
| JP2004526720A (ja) | 2001-03-08 | 2004-09-02 | グラクソ グループ リミテッド | βアドレナリン受容体のアゴニスト |
| EP1241176A1 (en) | 2001-03-16 | 2002-09-18 | Pfizer Products Inc. | Purine derivatives for the treatment of ischemia |
| ATE381537T1 (de) | 2001-03-22 | 2008-01-15 | Glaxo Group Ltd | Formanilid-derivative als beta2-adrenorezeptor- agonisten |
| AU2002253342B2 (en) | 2001-04-30 | 2007-01-04 | Glaxo Group Limited | Novel anti-inflammatory androstane derivatives |
| BR0209986A (pt) | 2001-05-25 | 2004-04-06 | Pfizer | Agonista de a2a em combinação com um agente anticolinérgico, para o tratamento de doenças obstrutivas das vias respiratórias |
| JP2005500290A (ja) | 2001-06-12 | 2005-01-06 | グラクソ グループ リミテッド | 抗炎症性の、１７β−カルボチオアートアンドロスタン誘導体である１７α複素環エステル |
| AU2002326026B2 (en) | 2001-09-14 | 2005-04-28 | Glaxo Group Limited | Phenethanolamine derivatives for treatment of respiratory diseases |
| CA2462980A1 (en) | 2001-10-17 | 2003-04-24 | Ucb, S.A. | Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors |
| GB0125259D0 (en) | 2001-10-20 | 2001-12-12 | Glaxo Group Ltd | Novel compounds |
| AR037517A1 (es) | 2001-11-05 | 2004-11-17 | Novartis Ag | Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria |
| HU229504B1 (hu) | 2001-11-09 | 2014-01-28 | Gilead Sciences | A2B-adenozinreceptor-antagonisták |
| WO2003042160A1 (en) | 2001-11-13 | 2003-05-22 | Theravance, Inc. | Aryl aniline beta-2 adrenergic receptor agonists |
| TWI249515B (en) | 2001-11-13 | 2006-02-21 | Theravance Inc | Aryl aniline beta2 adrenergic receptor agonists |
| AU2002356759A1 (en) | 2001-12-01 | 2003-06-17 | Glaxo Group Limited | 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents |
| PL211250B1 (pl) | 2001-12-20 | 2012-04-30 | Chiesi Farma Spa | Pochodne karbaminianu 1-alkilo-1-azoniabicyklo [2.2.2] oktanu, jej zastosowania, kompozycja farmaceutyczna zawierająca ten związek oraz związek pośredni |
| WO2003072592A1 (en) | 2002-01-15 | 2003-09-04 | Glaxo Group Limited | 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents |
| WO2003062259A2 (en) | 2002-01-21 | 2003-07-31 | Glaxo Group Limited | Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents |
| GB0202216D0 (en) | 2002-01-31 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
| GB0204719D0 (en) | 2002-02-28 | 2002-04-17 | Glaxo Group Ltd | Medicinal compounds |
| US7268152B2 (en) | 2002-03-26 | 2007-09-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| KR101022977B1 (ko) | 2002-03-26 | 2011-03-18 | 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 | 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도 |
| DE60318192T2 (de) | 2002-04-10 | 2008-04-30 | The University Of Virginia Patent Foundation | Verwendung von a2a adenosin rezeptor agonisten und anti-pathogene mittel enthaltenden kombinationen zur behandlung von entzündungskrankheiten |
| US7282591B2 (en) | 2002-04-11 | 2007-10-16 | Merck & Co., Inc. | 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators |
| ES2206021B1 (es) | 2002-04-16 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de pirrolidinio. |
| ATE381535T1 (de) | 2002-04-25 | 2008-01-15 | Glaxo Group Ltd | Phenethanolaminderivate |
| EP1507754A1 (en) | 2002-05-28 | 2005-02-23 | Theravance, Inc. | Alkoxy aryl beta-2 adrenergic receptor agonists |
| ES2201907B1 (es) | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
| US7186864B2 (en) | 2002-05-29 | 2007-03-06 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| DE10224888A1 (de) | 2002-06-05 | 2003-12-24 | Merck Patent Gmbh | Pyridazinderivate |
| US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| DE10225574A1 (de) | 2002-06-10 | 2003-12-18 | Merck Patent Gmbh | Aryloxime |
| DE10227269A1 (de) | 2002-06-19 | 2004-01-08 | Merck Patent Gmbh | Thiazolderivate |
| US7153968B2 (en) | 2002-06-25 | 2006-12-26 | Merck Frosst Canada, Ltd. | 8-(biaryl)quinoline PDE4 inhibitors |
| CA2490097A1 (en) | 2002-07-02 | 2004-01-15 | Merck Frosst Canada & Co. | Di-aryl-substituted-ethane pyridone pde4 inhibitors |
| ES2204295B1 (es) | 2002-07-02 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de quinuclidina-amida. |
| BR0312575A (pt) | 2002-07-08 | 2005-05-03 | Pfizer Prod Inc | Moduladores do receptor de glicocorticóides |
| GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
| PE20050130A1 (es) | 2002-08-09 | 2005-03-29 | Novartis Ag | Compuestos organicos |
| EP1556369A1 (en) | 2002-08-10 | 2005-07-27 | ALTANA Pharma AG | Pyridazinone-derivatives as pde4 inhibitors |
| PL373597A1 (en) | 2002-08-10 | 2005-09-05 | Altana Pharma Ag | Piperidine-n-oxide-derivatives |
| AU2003255376A1 (en) | 2002-08-10 | 2004-03-11 | Altana Pharma Ag | Piperidine-derivatives as pde4 inhibitors |
| ATE360627T1 (de) | 2002-08-10 | 2007-05-15 | Altana Pharma Ag | Pyrrolidindion-substituierte piperidin- phthalazone als pde4-inhibitoren |
| EP1537086A2 (en) | 2002-08-17 | 2005-06-08 | ALTANA Pharma AG | Novel phenanthridines |
| WO2004018465A2 (en) | 2002-08-17 | 2004-03-04 | Altana Pharma Ag | Benzonaphthyridines with pde 3/4 inhibiting activity |
| DE60322713D1 (de) | 2002-08-21 | 2008-09-18 | Boehringer Ingelheim Pharma | Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung |
| EP1534675B1 (en) | 2002-08-23 | 2009-02-25 | Ranbaxy Laboratories, Ltd. | Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo¬3.1.0 hexane derivatives as muscarinic receptor antagonists |
| DE60333371D1 (de) | 2002-08-29 | 2010-08-26 | Boehringer Ingelheim Pharma | 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen |
| EP1539164B1 (en) | 2002-08-29 | 2006-12-20 | ALTANA Pharma AG | 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
| EP1536798B1 (en) | 2002-08-29 | 2007-02-07 | ALTANA Pharma AG | 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
| GB0220730D0 (en) | 2002-09-06 | 2002-10-16 | Glaxo Group Ltd | Medicinal compounds |
| JP2006096662A (ja) | 2002-09-18 | 2006-04-13 | Sumitomo Pharmaceut Co Ltd | 新規６−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| JP4520309B2 (ja) | 2002-09-20 | 2010-08-04 | メルク・シャープ・エンド・ドーム・コーポレイション | 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−２−Ｈ−ナフト［１，２−ｆ］インドール−４−カルボキサミド誘導体 |
| JP2004107299A (ja) | 2002-09-20 | 2004-04-08 | Japan Energy Corp | 新規１−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| DE10246374A1 (de) | 2002-10-04 | 2004-04-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| EP1440966A1 (en) | 2003-01-10 | 2004-07-28 | Pfizer Limited | Indole derivatives useful for the treatment of diseases |
| ES2302938T3 (es) | 2002-10-11 | 2008-08-01 | Pfizer Inc. | Derivados de indol como agonistas beta-2. |
| JP2006506373A (ja) | 2002-10-22 | 2006-02-23 | グラクソ グループ リミテッド | 医薬アリールエタノールアミン化合物 |
| PL376769A1 (pl) | 2002-10-23 | 2006-01-09 | Glenmark Pharmaceuticals Ltd. | Nowe związki tricykliczne użyteczne w leczeniu chorób zapalnych i alergicznych, sposób ich wytwarzania i kompozycje farmaceutyczne je zawierające |
| AU2003286143A1 (en) | 2002-10-28 | 2004-05-13 | Glaxo Group Limited | Phenethanolamine derivative for the treatment of respiratory diseases |
| GB0225030D0 (en) | 2002-10-28 | 2002-12-04 | Glaxo Group Ltd | Medicinal compounds |
| GB0225287D0 (en) | 2002-10-30 | 2002-12-11 | Glaxo Group Ltd | Novel compounds |
| GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| DE10253282A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung |
| DE10253220A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE10253426B4 (de) | 2002-11-15 | 2005-09-22 | Elbion Ag | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
| DE10261874A1 (de) | 2002-12-20 | 2004-07-08 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| DK1581535T5 (da) | 2003-01-09 | 2009-12-21 | Astellas Pharma Inc | Pyrrolopyridazinderivater |
| JP4606408B2 (ja) | 2003-01-21 | 2011-01-05 | メルク・シャープ・エンド・ドーム・コーポレイション | 選択的グルココルチコイド受容体調節物質としての１７−カルバモイルオキシコルチゾル誘導体 |
| PE20040950A1 (es) | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
| EP1460064A1 (en) | 2003-03-14 | 2004-09-22 | Pfizer Limited | Indole-2-carboxamide derivatives useful as beta-2 agonists |
| EP1615881A2 (en) | 2003-04-01 | 2006-01-18 | Theravance, Inc. | Diarylmethyl and related compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity |
| ATE421322T1 (de) | 2003-04-04 | 2009-02-15 | Novartis Pharma Gmbh | Chinolin-2-on-derivate zur behandlung von erkankungen der atemwege |
| AR044134A1 (es) | 2003-05-02 | 2005-08-24 | Novartis Ag | Derivados de quinuclidina, metodo de preparacion y composiciones farmaceuticas. |
| US7268147B2 (en) | 2003-05-15 | 2007-09-11 | Pfizer Inc | Compounds useful for the treatment of diseases |
| EP1477167A1 (en) | 2003-05-15 | 2004-11-17 | Pfizer Limited | [(2-hydroxy-2-(4-hydroxy-3-hydroxymethylphenyl)-ethylamino)-propyl] phenyl derivatives as beta2 agonists |
| TWI328009B (en) | 2003-05-21 | 2010-08-01 | Glaxo Group Ltd | Quinoline derivatives as phosphodiesterase inhibitors |
| JP4616264B2 (ja) | 2003-05-28 | 2011-01-19 | セラヴァンス， インコーポレーテッド | ムスカリン性レセプターアンタゴニストとしてのアザビシクロアルカン化合物 |
| GB0312832D0 (en) | 2003-06-04 | 2003-07-09 | Pfizer Ltd | 2-amino-pyridine derivatives useful for the treatment of diseases |
| EP1633714B1 (en) | 2003-06-04 | 2008-01-23 | Pfizer Limited | 2-amino-pyridine derivatives as beta-2 adrenoreceptor agonists |
| AU2004245146B2 (en) | 2003-06-11 | 2010-01-21 | Merck Frosst Canada Ltd | 7-(1,3-thiazol-2-yl)thio-coumarin derivatives and their use as leukotriene biosynthesis inhibitors |
| WO2004111044A1 (en) | 2003-06-17 | 2004-12-23 | Glenmark Pharmaceuticals Ltd. | Tricyclic compounds useful for the treatment of inflammatory and allergic disorders:process for their preparation |
| GB0316290D0 (en) | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
| ITMI20031451A1 (it) | 2003-07-16 | 2005-01-17 | Zambon Spa | Derivati diidro-ftalazinici inibitori della fosfodiesterasi 4 |
| JP2007500685A (ja) | 2003-07-31 | 2007-01-18 | アルタナ ファルマ アクチエンゲゼルシャフト | 新規の６−フェニルフェナントリジン |
| US20060189641A1 (en) | 2003-07-31 | 2006-08-24 | Beate Schmidt | Novel 6-phenlyphenanthridines |
| GB0322726D0 (en) | 2003-09-27 | 2003-10-29 | Glaxo Group Ltd | Compounds |
| GB0322722D0 (en) | 2003-09-27 | 2003-10-29 | Glaxo Group Ltd | Compounds |
| WO2005033121A2 (en) | 2003-10-03 | 2005-04-14 | King Pharmaceuticals Research & Development, Inc. | Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs |
| GB0323701D0 (en) | 2003-10-09 | 2003-11-12 | Glaxo Group Ltd | Formulations |
| GB0324654D0 (en) | 2003-10-22 | 2003-11-26 | Glaxo Group Ltd | Medicinal compounds |
| GB0324886D0 (en) | 2003-10-24 | 2003-11-26 | Glaxo Group Ltd | Medicinal compounds |
| TWI288306B (en) | 2003-11-05 | 2007-10-11 | Asml Netherlands Bv | Lithographic apparatus and method for manufacturing a lithographic device |
| GB0329182D0 (en) | 2003-12-17 | 2004-01-21 | Glaxo Group Ltd | Chemical compounds |
| US8070937B2 (en) | 2003-12-19 | 2011-12-06 | Shell Oil Company | Systems, methods, and catalysts for producing a crude product |
| JP2005187357A (ja) | 2003-12-25 | 2005-07-14 | Nippon Suisan Kaisha Ltd | 選択的なβ２受容体アゴニスト活性を有するベンゾチアゾロン誘導体の製造方法 |
| DE102004001413A1 (de) | 2004-01-09 | 2005-08-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Hydroxymethyl-4-Hydroxy-Phenyl-Derivate zur Behandlung von chronisch obstruktiver Lungenerkrankung |
| WO2005080313A2 (en) | 2004-01-22 | 2005-09-01 | Pfizer Limited | Sulfonamide derivatives for the treatment of diseases |
| GEP20084452B (en) | 2004-01-22 | 2008-08-10 | Pfizer | Sulfonamide derivatives for the treatment of diseases |
| DE102004003428A1 (de) | 2004-01-23 | 2005-08-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue langwirksame Beta-2-Agonisten, und deren Verwendung als Arzneimittel |
| GB0402797D0 (en) | 2004-02-09 | 2004-03-10 | Novartis Ag | Organic compounds |
| WO2005080375A1 (en) | 2004-02-13 | 2005-09-01 | Theravance, Inc. | Crystalline form of a biphenyl compound |
| ATE479433T1 (de) | 2004-02-14 | 2010-09-15 | Boehringer Ingelheim Int | Neue langwirksame beta-2-agonisten, und deren verwendung als arzneimittel |
| BRPI0508481A (pt) | 2004-03-10 | 2007-07-31 | Altana Pharma Ag | hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4 |
| WO2005087744A1 (en) | 2004-03-10 | 2005-09-22 | Altana Pharma Ag | Novel thio-containing hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors |
| EP1574501A1 (en) | 2004-03-11 | 2005-09-14 | Pfizer Limited | Quinolinone derivatives, pharmaceutical compositions containing them and their use |
| WO2005087749A1 (ja) | 2004-03-15 | 2005-09-22 | Kyowa Hakko Kogyo Co., Ltd. | ２−アミノキナゾリン誘導体 |
| US7244728B2 (en) | 2004-03-17 | 2007-07-17 | Boehringer Ingelheim International Gmbh | Long acting betamimetics for the treatment of respiratory diseases |
| CA2559200A1 (en) | 2004-03-17 | 2005-09-29 | Altana Pharma Ag | Novel n- (alkoxyalkyl) carbamoyl - substituted 6-phenyl-benzonaphthyridine derivatives and their use as pde3/4 inhibitors |
| AU2005223488A1 (en) | 2004-03-17 | 2005-09-29 | Pfizer Inc. | Phenylethanolamine derivatives as Beta-2 agonists |
| EP1577292A1 (en) | 2004-03-17 | 2005-09-21 | Pfizer Limited | Phenylaminoethanol derivatives as beta2 receptor agonists |
| WO2005092840A1 (en) | 2004-03-23 | 2005-10-06 | Pfizer Limited | Formamide derivatives useful as adrenoceptor |
| WO2005092860A1 (en) | 2004-03-23 | 2005-10-06 | Pfizer Limited | Compounds for the treatment of diseases |
| US20050215542A1 (en) | 2004-03-23 | 2005-09-29 | Pfizer Inc | Compounds for the treatment of diseases |
| ATE432278T1 (de) | 2004-03-23 | 2009-06-15 | Pfizer | Verbindungen zur behandlung von krankheiten |
| US7306631B2 (en) | 2004-03-30 | 2007-12-11 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| AU2005227733A1 (en) | 2004-04-02 | 2005-10-13 | Glaxo Group Limited | Chemical process and new crystalline form |
| DE102004019539A1 (de) | 2004-04-22 | 2005-11-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittel zur Behandlung von Atemwegserkrankungen |
| US20050239778A1 (en) | 2004-04-22 | 2005-10-27 | Boehringer Ingelheim International Gmbh | Novel medicament combinations for the treatment of respiratory diseases |
| US7307076B2 (en) | 2004-05-13 | 2007-12-11 | Boehringer Ingelheim International Gmbh | Beta agonists for the treatment of respiratory diseases |
| US7745621B2 (en) | 2004-05-14 | 2010-06-29 | Boehringer Ingelheim International Gmbh | Long acting bronchodilators for the treatment of respiratory diseases |
| US20050256115A1 (en) | 2004-05-14 | 2005-11-17 | Boehringer Ingelheim International Gmbh | Aerosol formulation for the inhalation of beta-agonists |
| EP1751086A2 (en) | 2004-06-03 | 2007-02-14 | Theravance, Inc. | DIAMINE ß2 ADRENERGIC RECEPTOR AGONISTS |
| US7317023B2 (en) | 2004-07-21 | 2008-01-08 | Theravance, Inc. | Diaryl ether β2 adrenergic receptor agonists |
| GB0416397D0 (en) | 2004-07-22 | 2004-08-25 | Glaxo Group Ltd | Pharmaceutical formulations |
| US7569586B2 (en) | 2004-08-16 | 2009-08-04 | Theravance, Inc. | Compounds having β2 adrenergic receptor agonist and muscarinic receptor antagonist activity |
| US7838597B2 (en) | 2004-08-20 | 2010-11-23 | Sekisui Specialty Chemicals America, Llc | Fluid loss concentrate for hydraulic cement |
| US7566785B2 (en) | 2004-09-10 | 2009-07-28 | Theravance, Inc. | Amidine substituted aryl aniline compounds |
| GB0424284D0 (en) | 2004-11-02 | 2004-12-01 | Novartis Ag | Organic compounds |
| GB0426164D0 (en) | 2004-11-29 | 2004-12-29 | Novartis Ag | Organic compounds |
| EP1846374A1 (en) | 2005-01-11 | 2007-10-24 | Glaxo Group Limited | Cinnamate salts of a beta-2 adrenergic agonist |
| JP2009502734A (ja) | 2005-07-29 | 2009-01-29 | アステラス製薬株式会社 | Ｌｃｋ阻害剤としての縮合複素環 |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| US7750000B2 (en) | 2005-09-02 | 2010-07-06 | Bayer Schering Pharma Ag | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| US7723336B2 (en) | 2005-09-22 | 2010-05-25 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| EP1873157A1 (en) | 2006-06-21 | 2008-01-02 | Bayer Schering Pharma Aktiengesellschaft | Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
| AR064420A1 (es) | 2006-12-21 | 2009-04-01 | Alcon Mfg Ltd | Composiciones farmaceuticas oftalmicas que comprenden una cantidad efectiva de analogos de 6-aminoimidazo[1,2b]piridazinas, utiles para el tratamiento del glaucoma y/o controlar la presion intraocular normal o elevada(iop). |
| AR067326A1 (es) | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| FR2918061B1 (fr) | 2007-06-28 | 2010-10-22 | Sanofi Aventis | Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique. |
| WO2009017954A1 (en) | 2007-08-01 | 2009-02-05 | Phenomix Corporation | Inhibitors of jak2 kinase |
| EP2217601A1 (en) | 2007-11-08 | 2010-08-18 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyridazines for use as protein kinase inhibitors |
| AU2009218459A1 (en) | 2008-02-28 | 2009-09-03 | Novartis Ag | Imidazo [1,2-B] pyridazine derivatives for the treatment of C-Met tyrosine kinase mediated disease |
| AU2009246687B2 (en) | 2008-05-13 | 2012-08-09 | Irm Llc | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
| CA2952692C (en) | 2008-09-22 | 2020-04-28 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds |
| PT3372605T (pt) | 2008-10-22 | 2021-12-09 | Array Biopharma Inc | Compostos de pirazolo[1,5-a]pirimidina substituídos como inibidores de quinase trk |
| EP2962566A1 (en) | 2008-10-31 | 2016-01-06 | Genentech, Inc. | Pyrazolopyrimidine jak inhibitor compounds and methods |
| US8927545B2 (en) | 2009-03-30 | 2015-01-06 | Duke University | Inhibiting Eph B-3 kinase |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
-
2011
- 2011-09-08 UY UY0001033597A patent/UY33597A/es unknown
- 2011-09-08 US US13/227,957 patent/US8637516B2/en not_active Expired - Fee Related
- 2011-09-09 TW TW100132702A patent/TW201211050A/zh unknown
- 2011-09-09 EP EP11758063.9A patent/EP2614062A1/en not_active Withdrawn
- 2011-09-09 JP JP2013528357A patent/JP2013537199A/ja not_active Withdrawn
- 2011-09-09 CA CA2810858A patent/CA2810858A1/en not_active Abandoned
- 2011-09-09 AR ARP110103293A patent/AR082945A1/es not_active Application Discontinuation
- 2011-09-09 AU AU2011299026A patent/AU2011299026A1/en not_active Abandoned
- 2011-09-09 WO PCT/US2011/051108 patent/WO2012034091A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2012034091A1 (en) | 2012-03-15 |
| CA2810858A1 (en) | 2012-03-15 |
| US20120065184A1 (en) | 2012-03-15 |
| US8637516B2 (en) | 2014-01-28 |
| UY33597A (es) | 2012-04-30 |
| EP2614062A1 (en) | 2013-07-17 |
| JP2013537199A (ja) | 2013-09-30 |
| AU2011299026A1 (en) | 2013-03-21 |
| TW201211050A (en) | 2012-03-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR082945A1 (es) | Derivados de imidazo[1,2-b]piridazina como inhibidores de la trk | |
| AR086019A1 (es) | COMPUESTOS DE PIRROLO SULFONAMIDA PARA MODULACION DE LA ACTIVIDAD DEL RECEPTOR HUERFANO g RELACIONADO AL RECEPTOR NUCLEAR HUERFANO RAR (RORg, NR1F3) Y PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y AUTOINMUNES CRONICAS | |
| AR052887A1 (es) | Derivados de tiazol, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para tratar enfermedades mediadas por la inhibicion de la protein quinasa | |
| AR087760A1 (es) | Heterociclilaminas como inhibidores de pi3k | |
| AR084849A1 (es) | Derivados de oxazina y su uso en el tratamiento de trastornos neurologicos | |
| AR077507A1 (es) | Derivados de naftiridina-1-ona y composiciones farmaceuticas que los comprenden como inhibidores de cinasa syk | |
| AR085316A1 (es) | Derivados de pirrolo[2,3-b]piridina, utiles para la modulacion de quinasas | |
| AR087752A1 (es) | Compuestos y composiciones como inhibidores de la quinasa c-kit | |
| AR097008A1 (es) | Derivados fosfatos, su procedimiento de preparación y las composiciones farmacéuticas que los contienen | |
| AR092108A1 (es) | Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn | |
| ES2630079T3 (es) | Moduladores de la ruta del complemento y usos de los mismos | |
| AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
| ECSP055988A (es) | Compuestos de aminoheteroarilo como inhibidores de las proteinquinasas | |
| CO6160296A2 (es) | Derivados de acido benzoazepin-oxi-acetico como agonistas de receptores activados por proliferador de peroxisona delta usados para incrementar la lipoproteina de alta densidad-colesterol-colesterol reducir la lipoproteina de baja densidad-colesterol | |
| AR110139A1 (es) | COMPUESTOS MONO Y ESPIROCÍCLICOS QUE CONTIENEN CICLOBUTANO Y AZETIDINA COMO INHIBIDORES DE LA INTEGRINA aV | |
| AR089568A1 (es) | Compuestos heterociclicos y sus metodos de usos | |
| AR037907A1 (es) | Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6 | |
| AR082886A1 (es) | Compuestos y composiciones farmaceuticas que los contienen | |
| AR045510A1 (es) | Derivados de 1,3 diazoles | |
| AR083199A1 (es) | Compuestos de n-heteroarilo con unidad de puente ciclico | |
| AR062680A1 (es) | Sintesis de 2-(piridin-2-ilamino) pirido [2,3-d] pirimidin-7-onas | |
| AR047682A1 (es) | Derivados tetrahidroisoquinolinilo de quinazolina e isoquinolina | |
| AR080596A1 (es) | Compuestos alquilamido y composiciones farmaceuticas | |
| AR074021A1 (es) | Compuestos heterociclicos fusionados como moduladores del canal ionico | |
| AR049521A1 (es) | Derivados de pirrazol - pirimidina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |