JP6318156B2 - キナーゼをモジュレートするための化合物および方法、ならびにその指標 - Google Patents
キナーゼをモジュレートするための化合物および方法、ならびにその指標 Download PDFInfo
- Publication number
- JP6318156B2 JP6318156B2 JP2015531206A JP2015531206A JP6318156B2 JP 6318156 B2 JP6318156 B2 JP 6318156B2 JP 2015531206 A JP2015531206 A JP 2015531206A JP 2015531206 A JP2015531206 A JP 2015531206A JP 6318156 B2 JP6318156 B2 JP 6318156B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituents
- formula
- compound
- certain embodiments
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 C*1(C)C(C=C**2)=C2C=C1 Chemical compound C*1(C)C(C=C**2)=C2C=C1 0.000 description 12
- DDZGQYREBDXECY-UHFFFAOYSA-N c1n[nH]c2nccnc12 Chemical compound c1n[nH]c2nccnc12 DDZGQYREBDXECY-UHFFFAOYSA-N 0.000 description 2
- INFXCZTYGOHFJO-UHFFFAOYSA-N C=CNc1c(cc[nH]2)c2ncn1 Chemical compound C=CNc1c(cc[nH]2)c2ncn1 INFXCZTYGOHFJO-UHFFFAOYSA-N 0.000 description 1
- DYTCGOMSQHOVMS-UHFFFAOYSA-N CC1=[I]C=Nc2c1ccc(NCCOC)c2 Chemical compound CC1=[I]C=Nc2c1ccc(NCCOC)c2 DYTCGOMSQHOVMS-UHFFFAOYSA-N 0.000 description 1
- DNFBJBRWITZICO-WKBXPBOGSA-N CCC1OC=C/C1=N/C=C\N Chemical compound CCC1OC=C/C1=N/C=C\N DNFBJBRWITZICO-WKBXPBOGSA-N 0.000 description 1
- XKNMFSNLEDMBHK-UHFFFAOYSA-N C[N+](C(CC1)=CC=C1N)(O)[OH2+] Chemical compound C[N+](C(CC1)=CC=C1N)(O)[OH2+] XKNMFSNLEDMBHK-UHFFFAOYSA-N 0.000 description 1
- KBSRYRNFSYDEHY-UHFFFAOYSA-N Ic1c(cccc2)c2ncn1 Chemical compound Ic1c(cccc2)c2ncn1 KBSRYRNFSYDEHY-UHFFFAOYSA-N 0.000 description 1
- CSJOLXDFFYCGDZ-UHFFFAOYSA-N Ic1c(cn[nH]2)c2ncn1 Chemical compound Ic1c(cn[nH]2)c2ncn1 CSJOLXDFFYCGDZ-UHFFFAOYSA-N 0.000 description 1
- UREDQPSRDVZQFV-UHFFFAOYSA-N Ic1c2[s]ccc2ncn1 Chemical compound Ic1c2[s]ccc2ncn1 UREDQPSRDVZQFV-UHFFFAOYSA-N 0.000 description 1
- MDANCFSZYMOGEV-GUSUVPGTSA-N N/C=C\N=C1\OC=NC1=[IH] Chemical compound N/C=C\N=C1\OC=NC1=[IH] MDANCFSZYMOGEV-GUSUVPGTSA-N 0.000 description 1
- COJABJBCLBJEBG-UHFFFAOYSA-N Nc1nccnc1N=N Chemical compound Nc1nccnc1N=N COJABJBCLBJEBG-UHFFFAOYSA-N 0.000 description 1
- HFTVJMFWJUFBNO-UHFFFAOYSA-N c1c[nH]c2nccnc12 Chemical compound c1c[nH]c2nccnc12 HFTVJMFWJUFBNO-UHFFFAOYSA-N 0.000 description 1
- JJTNLWSCFYERCK-UHFFFAOYSA-N c1c[nH]c2ncncc12 Chemical compound c1c[nH]c2ncncc12 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 description 1
- YJSKZIATOGOJEB-UHFFFAOYSA-N c1c[s]c2nccnc12 Chemical compound c1c[s]c2nccnc12 YJSKZIATOGOJEB-UHFFFAOYSA-N 0.000 description 1
- DLHRAOSKUZJSEB-UHFFFAOYSA-N c1cnc2[o]nnc2n1 Chemical compound c1cnc2[o]nnc2n1 DLHRAOSKUZJSEB-UHFFFAOYSA-N 0.000 description 1
- HXTBYLZGLRCHTM-UHFFFAOYSA-N c1n[o]c2nccnc12 Chemical compound c1n[o]c2nccnc12 HXTBYLZGLRCHTM-UHFFFAOYSA-N 0.000 description 1
- ZKAMEFMDQNTDFK-UHFFFAOYSA-N c1nc2nccnc2[nH]1 Chemical compound c1nc2nccnc2[nH]1 ZKAMEFMDQNTDFK-UHFFFAOYSA-N 0.000 description 1
- PUZFXDRHCPIYCB-UHFFFAOYSA-N c1nc2nccnc2[o]1 Chemical compound c1nc2nccnc2[o]1 PUZFXDRHCPIYCB-UHFFFAOYSA-N 0.000 description 1
- HEIZPACCIHXHKV-UHFFFAOYSA-N c1nc2nccnc2[s]1 Chemical compound c1nc2nccnc2[s]1 HEIZPACCIHXHKV-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- 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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261697761P | 2012-09-06 | 2012-09-06 | |
| US61/697,761 | 2012-09-06 | ||
| US201361775347P | 2013-03-08 | 2013-03-08 | |
| US61/775,347 | 2013-03-08 | ||
| PCT/US2013/058320 WO2014039714A2 (en) | 2012-09-06 | 2013-09-05 | Compounds and methods for kinase modulation, and indications therefor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015529224A JP2015529224A (ja) | 2015-10-05 |
| JP2015529224A5 JP2015529224A5 (https=) | 2017-04-27 |
| JP6318156B2 true JP6318156B2 (ja) | 2018-04-25 |
Family
ID=50237764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015531206A Active JP6318156B2 (ja) | 2012-09-06 | 2013-09-05 | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10227357B2 (https=) |
| EP (1) | EP2892534B8 (https=) |
| JP (1) | JP6318156B2 (https=) |
| CN (1) | CN104981247A (https=) |
| AU (1) | AU2013312477B2 (https=) |
| CA (1) | CA2883894C (https=) |
| ES (1) | ES2889757T3 (https=) |
| MX (1) | MX2015002887A (https=) |
| WO (1) | WO2014039714A2 (https=) |
Families Citing this family (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US8673928B2 (en) | 2009-11-18 | 2014-03-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN102753549A (zh) | 2009-12-23 | 2012-10-24 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| EP2651417B1 (en) | 2010-12-16 | 2016-11-30 | Calchan Limited | Ask1 inhibiting pyrrolopyrimidine derivatives |
| KR101911972B1 (ko) | 2011-02-07 | 2018-10-25 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| AU2012255275B2 (en) | 2011-05-17 | 2016-01-28 | Plexxikon Inc. | Kinase modulation and indications therefor |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| EP2935248B1 (en) | 2012-12-21 | 2018-02-28 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| SG11201505999VA (en) | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| SG11201506687RA (en) | 2013-03-15 | 2015-09-29 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
| DE102013008118A1 (de) | 2013-05-11 | 2014-11-13 | Merck Patent Gmbh | Arylchinazoline |
| EP3004060B1 (en) * | 2013-05-30 | 2019-11-27 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| MX365614B (es) | 2013-10-17 | 2019-06-07 | Blueprint Medicines Corp | Composiciones utiles para tratar trastornos relacionados con kit. |
| US9334263B2 (en) | 2013-10-17 | 2016-05-10 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| MX368464B (es) * | 2013-12-05 | 2019-10-02 | Pfizer | Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo. |
| WO2015134536A1 (en) * | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| GB201410816D0 (en) * | 2014-06-17 | 2014-07-30 | Ucb Biopharma Sprl And Katholieke Universiteit Leuven | Therapeutic agents |
| CA2961356C (en) | 2014-09-15 | 2023-03-07 | Plexxikon Inc. | Heterocyclic compounds and their uses in modulating bromodomain and for treating diseases or conditions relevant thereto |
| MA41051B1 (fr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA2984899C (en) | 2015-05-06 | 2021-06-15 | Plexxikon Inc. | Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases |
| DK3292123T3 (da) | 2015-05-06 | 2020-08-17 | Plexxikon Inc | Faste former af en forbindelse, der modulerer kinaser |
| CA2986735A1 (en) | 2015-05-22 | 2016-12-01 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| US10053465B2 (en) * | 2015-08-26 | 2018-08-21 | Incyte Corporation | Pyrrolopyrimidine derivatives as TAM inhibitors |
| CN108137585B (zh) | 2015-09-21 | 2021-10-22 | 普莱希科公司 | 杂环化合物及其应用 |
| RU2018123825A (ru) | 2015-12-07 | 2020-01-15 | Плексксикон Инк. | Соединения и способы для модуляции киназ, и показания для этого |
| CN105311585A (zh) * | 2015-12-08 | 2016-02-10 | 李朝彬 | 一种治疗肝硬化的中药组合物 |
| US9630968B1 (en) | 2015-12-23 | 2017-04-25 | Arqule, Inc. | Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof |
| WO2017161045A1 (en) | 2016-03-16 | 2017-09-21 | Plexxikon Inc. | Compounds and methods for kinase modulation and indications therefore |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| CA3019380A1 (en) | 2016-03-31 | 2017-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CN105936633B (zh) * | 2016-04-27 | 2018-11-09 | 广东环境保护工程职业学院 | 5-（3-异丙基苯并异噁唑）吡嗪-2-胺及其制备方法 |
| TW201811795A (zh) * | 2016-08-24 | 2018-04-01 | 美商亞闊股份有限公司 | 胺基－吡咯并嘧啶酮化合物及其用途 |
| TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症 |
| CN109803962B (zh) | 2016-09-30 | 2022-04-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物 |
| MD3551622T2 (ro) | 2016-12-09 | 2021-03-31 | Vertex Pharma | Modulator al regulatorului conductanței transmembranare în fibroză chistică, compoziții farmaceutice, metode de tratament și procedeu pentru fabricarea modulatorului |
| AU2017382870B2 (en) * | 2016-12-22 | 2022-03-24 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
| US10703757B2 (en) | 2016-12-23 | 2020-07-07 | Plexxikon Inc. | Compounds and methods for CDK8 modulation and indications therefor |
| JP2020511467A (ja) | 2017-03-20 | 2020-04-16 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | ブロモドメインを阻害する４−（１−（１，１−ジ（ピリジン−２−イル）エチル）−６−（３，５−ジメチルイソオキサゾール−４−イル）−１Ｈ−ピロロ［３，２−ｂ］ピリジン−３−イル）安息香酸の結晶形 |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
| US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| MA49631A (fr) | 2017-07-17 | 2020-05-27 | Vertex Pharma | Méthodes de traitement de la fibrose kystique |
| BR112019028235B1 (pt) | 2017-07-25 | 2024-04-30 | Plexxikon, Inc. | Composições e seus métodos de preparação |
| JP7121794B2 (ja) | 2017-08-02 | 2022-08-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | ピロリジン化合物を調製するためのプロセス |
| CN109400610A (zh) * | 2017-08-18 | 2019-03-01 | 浙江海正药业股份有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途 |
| SI3687996T1 (sl) | 2017-09-27 | 2022-04-29 | Incyte Corporation | Soli pirolotriazinskih derivatov, ki so uporabne kot zaviralci TAM |
| JP7675519B2 (ja) | 2017-10-13 | 2025-05-13 | オプナ バイオ ソシエテ アノニム | キナーゼを調節するための化合物の固体形態 |
| WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
| WO2019084462A1 (en) | 2017-10-27 | 2019-05-02 | Plexxikon Inc. | FORMULATION OF A COMPOUND MODULATING KINASES |
| EP3720849A2 (en) | 2017-12-08 | 2020-10-14 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| AU2019239952A1 (en) | 2018-03-20 | 2020-10-08 | Plexxikon Inc. | Compounds and methods for IDO and TDO modulation, and indications therefor |
| EP3774825A1 (en) | 2018-04-13 | 2021-02-17 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| EP3782998B1 (en) | 2018-04-16 | 2023-05-10 | Shenzhen TargetRx, Inc. | Substituted pyrrolotriazine compound, pharmaceutical composition thereof and use thereof |
| WO2019243971A1 (en) * | 2018-06-17 | 2019-12-26 | Foundation For Neglected Disease Research | Novel compounds and their methods of use thereof |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| KR102833434B1 (ko) * | 2018-09-27 | 2025-07-15 | 쉔젠 칩스크린 바이오사이언스 씨오., 엘티디. | 인돌아민-2,3-디옥시게나아제 억제 활성을 갖는 퀴놀린 유도체 |
| JP7629200B2 (ja) * | 2018-11-20 | 2025-02-13 | ジョージタウン ユニバーシティ | 神経変性、筋変性及びリソソーム蓄積障害を治療するための組成物及び方法 |
| CN111410648B (zh) * | 2019-01-07 | 2024-03-29 | 浙江海正药业股份有限公司 | 一种手性c-KIT抑制剂药物关键中间体及其制备方法 |
| US11098044B2 (en) | 2019-02-22 | 2021-08-24 | 1ST Biotherapeutics, Inc. | Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders |
| KR20220018475A (ko) | 2019-04-09 | 2022-02-15 | 플렉시콘 인코퍼레이티드 | Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진 |
| US10829493B2 (en) | 2019-04-12 | 2020-11-10 | Blueprint Medicines Corporation | Compositions and methods for treating KIT- and PDGFRA-mediated diseases |
| WO2020210669A1 (en) | 2019-04-12 | 2020-10-15 | Blueprint Medicines Corporation | Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making |
| WO2021009568A1 (en) | 2019-07-17 | 2021-01-21 | 2692372 Ontario, Inc. | Benzenesulfonamide derivatives and uses thereof |
| WO2021020902A1 (ko) * | 2019-07-30 | 2021-02-04 | 주식회사 하임바이오 | 신규한 항암용 화합물, 및 이를 유효성분으로 포함하는 약학조성물 |
| KR20220122637A (ko) * | 2019-11-28 | 2022-09-02 | 바이엘 악티엔게젤샤프트 | 면역 활성화를 위한 dgk알파 억제제로서의 치환된 아미노퀴놀론 |
| US12509444B2 (en) | 2019-12-06 | 2025-12-30 | Plexxikon Inc. | Compounds and methods for CD73 modulation and indications therefor |
| LT4081305T (lt) | 2019-12-24 | 2024-11-25 | Carna Biosciences, Inc. | Diacilglicerolio kinazę moduliuojantys junginiai |
| PH12022552021A1 (en) * | 2020-02-07 | 2024-02-05 | Cytokinetics Inc | Nampt modulators |
| KR20260017503A (ko) | 2020-02-14 | 2026-02-05 | 길리애드 사이언시즈, 인코포레이티드 | Ccr8에 결합하는 항체 및 융합 단백질, 및 이의 용도 |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| CN111303155A (zh) * | 2020-03-13 | 2020-06-19 | 深圳大学 | 靶向pak1抑制剂及其在抗肿瘤治疗药物中的应用 |
| TWI908780B (zh) * | 2020-03-17 | 2025-12-21 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合二環類衍生物、其製備方法及其在醫藥上的應用 |
| CN111320634A (zh) * | 2020-04-14 | 2020-06-23 | 浙江工业大学 | 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法 |
| US11807626B2 (en) | 2020-04-23 | 2023-11-07 | Opna Bio SA | Compounds and methods for CD73 modulation and indications therefor |
| CN115605460A (zh) | 2020-04-29 | 2023-01-13 | 普莱希科公司（Us） | 杂环化合物的合成 |
| EP3915990A1 (en) * | 2020-05-26 | 2021-12-01 | Centre National de la Recherche Scientifique | 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-3,6-dihydropyridine-1-(2h)-carboxamide derivatives as limk and/or rock kinases inhibitors for use in the treatment of cancer |
| EP4199926A1 (en) | 2020-08-21 | 2023-06-28 | Plexxikon Inc. | Combinational drug anticancer therapies |
| KR102590438B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 조성물 |
| KR102590444B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물 |
| CN113831353A (zh) * | 2021-06-03 | 2021-12-24 | 四川大学 | 一种vegfr3小分子抑制剂及其在抗肿瘤药物中的应用 |
| CA3222277A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| WO2022271677A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| WO2022271659A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| CN115716840B (zh) * | 2021-08-24 | 2024-07-23 | 昆药集团股份有限公司 | 一种具有kras突变蛋白抑制作用的杂环化合物及其药物组合和用途 |
| US20230183216A1 (en) | 2021-10-28 | 2023-06-15 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
| WO2023075529A1 (ko) * | 2021-10-29 | 2023-05-04 | 보로노이바이오 주식회사 | 퀴나졸린 유도체 화합물 및 이의 용도 |
| EP4422756A1 (en) | 2021-10-29 | 2024-09-04 | Gilead Sciences, Inc. | Cd73 compounds |
| CN118488946A (zh) | 2021-12-22 | 2024-08-13 | 吉利德科学公司 | Ikaros锌指家族降解剂及其用途 |
| EP4452415B1 (en) | 2021-12-22 | 2026-02-25 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| CA3253296A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Zinc Finger Degradation Agents of the Ikaros Family and Their Uses |
| CN114573591B (zh) * | 2022-04-16 | 2023-04-25 | 成都施贝康生物医药科技有限公司 | 一种取代的吡咯并嘧啶化合物及其应用 |
| WO2023205719A1 (en) | 2022-04-21 | 2023-10-26 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| US20240116928A1 (en) | 2022-07-01 | 2024-04-11 | Gilead Sciences, Inc. | Cd73 compounds |
| EP4638436A1 (en) | 2022-12-22 | 2025-10-29 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| CN120882725A (zh) | 2023-04-11 | 2025-10-31 | 吉利德科学公司 | Kras调节化合物 |
| WO2024220917A1 (en) | 2023-04-21 | 2024-10-24 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250042922A1 (en) | 2023-06-30 | 2025-02-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| AU2024297978A1 (en) | 2023-07-26 | 2026-02-05 | Gilead Sciences, Inc. | Parp7 inhibitors |
| US20250066328A1 (en) | 2023-07-26 | 2025-02-27 | Gilead Sciences, Inc. | Parp7 inhibitors |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| WO2025054347A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| US20250376484A1 (en) | 2024-05-21 | 2025-12-11 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2026039365A1 (en) | 2024-08-12 | 2026-02-19 | Gilead Sciences, Inc. | Kras modulating compounds |
Family Cites Families (105)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3037980A (en) * | 1955-08-18 | 1962-06-05 | Burroughs Wellcome Co | Pyrrolopyrimidine vasodilators and method of making them |
| US5710158A (en) * | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| GB9323290D0 (en) | 1992-12-10 | 1994-01-05 | Zeneca Ltd | Quinazoline derivatives |
| ATE217873T1 (de) * | 1996-01-23 | 2002-06-15 | Novartis Erfind Verwalt Gmbh | Pyrrolopyrimidinen und verfahren zu deren herstellung |
| PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| EP1255536B1 (en) | 1999-12-22 | 2006-06-28 | Sugen, Inc. | Indolinone derivatives for modulation of c-kit tyrosine protein kinase |
| GB0100620D0 (en) * | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical cokpounds V |
| GB0115393D0 (en) * | 2001-06-23 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| WO2003057149A2 (en) * | 2001-12-28 | 2003-07-17 | Bayer Corporation | 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones |
| US20040171062A1 (en) | 2002-02-28 | 2004-09-02 | Plexxikon, Inc. | Methods for the design of molecular scaffolds and ligands |
| BRPI0314042B8 (pt) | 2002-09-06 | 2021-05-25 | Calando Pharmaceuticals Inc | polímeros à base de ciclodextrina para o fornecimento de agentes terapêuticos ligados a eles por covalência |
| AU2003272548A1 (en) | 2002-09-16 | 2004-04-30 | Plexxikon, Inc. | Crystal structure of pim-1 kinase |
| US20050048573A1 (en) | 2003-02-03 | 2005-03-03 | Plexxikon, Inc. | PDE5A crystal structure and uses |
| WO2004078923A2 (en) | 2003-02-28 | 2004-09-16 | Plexxikon, Inc. | Pyk2 crystal structure and uses |
| WO2004092123A2 (en) * | 2003-04-10 | 2004-10-28 | Microbia, Inc. | Inhibitors of fungal invasion |
| US7253166B2 (en) | 2003-04-22 | 2007-08-07 | Irm Llc | 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells |
| US20050079548A1 (en) | 2003-07-07 | 2005-04-14 | Plexxikon, Inc. | Ligand development using PDE4B crystal structures |
| US7348338B2 (en) | 2003-07-17 | 2008-03-25 | Plexxikon, Inc. | PPAR active compounds |
| EP1648867B1 (en) | 2003-07-17 | 2013-09-04 | Plexxikon Inc. | Ppar active compounds |
| US20050164300A1 (en) | 2003-09-15 | 2005-07-28 | Plexxikon, Inc. | Molecular scaffolds for kinase ligand development |
| CA2546754A1 (en) * | 2003-11-21 | 2005-06-09 | Array Biopharma Inc. | Akt protein kinase inhibitors |
| US7517970B2 (en) | 2003-12-19 | 2009-04-14 | Plexxikon, Inc. | Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same |
| US20070066641A1 (en) | 2003-12-19 | 2007-03-22 | Prabha Ibrahim | Compounds and methods for development of RET modulators |
| CA2550361C (en) | 2003-12-19 | 2014-04-29 | Prabha Ibrahim | Compounds and methods for development of ret modulators |
| WO2005067546A2 (en) | 2004-01-13 | 2005-07-28 | Ambit Biosciences Corporation | Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases |
| GB0403606D0 (en) * | 2004-02-18 | 2004-03-24 | Novartis Ag | Organic compounds |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| WO2006078287A2 (en) | 2004-05-06 | 2006-07-27 | Plexxikon, Inc. | Pde4b inhibitors and uses therefor |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| CA2570817A1 (en) | 2004-06-17 | 2006-01-26 | Plexxikon, Inc. | Azaindoles modulating c-kit activity and uses therefor |
| US7605168B2 (en) | 2004-09-03 | 2009-10-20 | Plexxikon, Inc. | PDE4B inhibitors |
| WO2006060535A2 (en) | 2004-11-30 | 2006-06-08 | Plexxikon, Inc. | Indole derivatives for use as ppar active compounds |
| EP1819673A2 (en) | 2004-11-30 | 2007-08-22 | Plexxikon, Inc. | Indole derivatives for use as ppar active compounds |
| US20060160135A1 (en) | 2004-12-08 | 2006-07-20 | Weiru Wang | SF-1 and LRH-1 modulator development |
| CA2590961C (en) * | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| EP1846396A2 (de) * | 2005-02-11 | 2007-10-24 | Freie Universität Berlin | Substituierte 4-(indol-3-yl)chinazoline und ihre verwendung |
| US7423043B2 (en) | 2005-02-18 | 2008-09-09 | Lexicon Pharmaceuticals, Inc. | 4-Piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidine compounds |
| AU2006272951A1 (en) | 2005-05-17 | 2007-02-01 | Plexxikon, Inc. | Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors |
| CN102206216B (zh) | 2005-06-22 | 2014-11-12 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
| KR20080042170A (ko) | 2005-09-07 | 2008-05-14 | 플렉시콘, 인코퍼레이티드 | Ｐｐａｒ 활성 화합물 |
| RU2419618C2 (ru) | 2005-09-07 | 2011-05-27 | Плекссикон, Инк. | Соединения, активные в отношении ppar (рецепторов активаторов пролиферации пероксисом) |
| AU2006287528A1 (en) | 2005-09-07 | 2007-03-15 | Plexxikon, Inc. | 1 , 4 and 1 , 5-disubstituted indole derivatives for use as PPAR active compounds |
| EA200801968A1 (ru) | 2006-03-11 | 2009-02-27 | Вернэлис (Р&Д) Лтд. | Пирролопиримидиновые производные, используемые в качестве ингибиторов hsp90 |
| US7807671B2 (en) * | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
| WO2008005368A2 (en) * | 2006-06-30 | 2008-01-10 | Abbott Laboratories | Piperazines as p2x7 antagonists |
| WO2008020302A2 (en) | 2006-08-17 | 2008-02-21 | Pfizer Products Inc. | Heteroaromatic quinoline-based compounds as phosphodiesterase (pde) inhibitors |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| AU2007336811A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20090159A1 (es) | 2007-03-08 | 2009-02-21 | Plexxikon Inc | COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs |
| RU2009137190A (ru) | 2007-03-08 | 2011-04-20 | Плексксикон, Инк. (Us) | Соединения, обладающие активностью в отношении ppar |
| EP2139869A2 (en) * | 2007-04-13 | 2010-01-06 | SuperGen, Inc. | Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders |
| UA99284C2 (ru) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
| EP2170886A1 (en) * | 2007-07-02 | 2010-04-07 | Cancer Research Technology Limited | 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors |
| JP2010533729A (ja) | 2007-07-17 | 2010-10-28 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物と方法、及びそのための適応 |
| EP2188289B1 (en) * | 2007-08-08 | 2015-10-28 | Lexicon Pharmaceuticals, Inc. | (7h-pyrrolo[2,3-d]pyrimidin-4-yl)-piperazines as kinase inhibitors for the treatment of cancer and inflammation |
| TW200924781A (en) | 2007-09-14 | 2009-06-16 | Janssen Pharmaceutica Nv | Thieno- and furo-pyrimidine modulators of the histamine H4 receptor |
| WO2009057139A2 (en) * | 2007-10-29 | 2009-05-07 | Natco Pharma Limited | Novel 4-(tetrazol-5-yl)-quinazoline derivatives as anti cancer agents |
| US20090118276A1 (en) | 2007-11-02 | 2009-05-07 | Wyeth | Thienopyrimidines, thienopyridines, and pyrrolopyrimidines as b-raf inhibitors |
| GB0725103D0 (en) | 2007-12-21 | 2008-01-30 | Glaxo Group Ltd | Novel compounds |
| US8193202B2 (en) * | 2008-04-21 | 2012-06-05 | Lexicon Pharmaceuticals, Inc. | LIMK2 inhibitors, compositions comprising them, and methods of their use |
| PE20091846A1 (es) | 2008-05-19 | 2009-12-16 | Plexxikon Inc | DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS |
| WO2009143018A2 (en) | 2008-05-19 | 2009-11-26 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US8119637B2 (en) | 2008-06-10 | 2012-02-21 | Plexxikon Inc. | Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor |
| US8110576B2 (en) | 2008-06-10 | 2012-02-07 | Plexxikon Inc. | Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications |
| WO2010036316A1 (en) * | 2008-09-24 | 2010-04-01 | Yangbo Feng | Urea and carbamate compounds and analogs as kinase inhibitors |
| US8232273B2 (en) | 2008-12-19 | 2012-07-31 | Genentech, Inc. | Heterocyclic compounds and methods of use |
| SG10201402977WA (en) | 2009-03-11 | 2014-09-26 | Plexxikon Inc | Pyrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases |
| AU2010224184A1 (en) | 2009-03-11 | 2011-09-29 | Plexxikon, Inc. | Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of Raf kinases |
| WO2010111527A1 (en) | 2009-03-26 | 2010-09-30 | Plexxikon, Inc. | Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use |
| KR101739994B1 (ko) | 2009-04-03 | 2017-05-25 | 에프. 호프만-라 로슈 아게 | 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도 |
| CA2761009A1 (en) | 2009-05-04 | 2010-11-11 | Plexxikon, Inc. | Compounds and methods for inhibition of renin, and indications therefor |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| US9346809B2 (en) * | 2009-07-08 | 2016-05-24 | Leo Pharma A/S | Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors |
| EP2473054B1 (en) * | 2009-09-04 | 2017-06-14 | The Regents of the University of Michigan | Compositions and methods for treatment of leukemia |
| NZ599866A (en) | 2009-11-06 | 2014-09-26 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| US8673928B2 (en) | 2009-11-18 | 2014-03-18 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN102753549A (zh) | 2009-12-23 | 2012-10-24 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
| TWI619713B (zh) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | 用於激酶調節的化合物和方法及其適應症 |
| EP2566866A1 (en) * | 2010-05-05 | 2013-03-13 | Vertex Pharmaceuticals Incorporated | 4 substituted pyrazolopyrimidines useful as pkc-theta inhibitors |
| US8642606B2 (en) | 2010-09-29 | 2014-02-04 | Plexxikon Inc. | ZAP-70 active compounds |
| EP2651417B1 (en) | 2010-12-16 | 2016-11-30 | Calchan Limited | Ask1 inhibiting pyrrolopyrimidine derivatives |
| US8853213B2 (en) | 2011-01-03 | 2014-10-07 | Hanmi Pharm. Co., Ltd | Bicyclic compound for modulating G protein-coupled receptors |
| KR101911972B1 (ko) | 2011-02-07 | 2018-10-25 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| AU2012255275B2 (en) | 2011-05-17 | 2016-01-28 | Plexxikon Inc. | Kinase modulation and indications therefor |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| HK1209674A1 (en) * | 2012-08-31 | 2016-04-08 | 诺瓦药品公司 | Heterocyclyl carboxamides for treating viral diseases |
| EP2935248B1 (en) | 2012-12-21 | 2018-02-28 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| SG11201506687RA (en) | 2013-03-15 | 2015-09-29 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| EP3004060B1 (en) | 2013-05-30 | 2019-11-27 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| WO2015134536A1 (en) | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA2961356C (en) | 2014-09-15 | 2023-03-07 | Plexxikon Inc. | Heterocyclic compounds and their uses in modulating bromodomain and for treating diseases or conditions relevant thereto |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA2984899C (en) | 2015-05-06 | 2021-06-15 | Plexxikon Inc. | Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases |
| DK3292123T3 (da) | 2015-05-06 | 2020-08-17 | Plexxikon Inc | Faste former af en forbindelse, der modulerer kinaser |
| CA2986735A1 (en) | 2015-05-22 | 2016-12-01 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| CN107801378A (zh) | 2015-05-22 | 2018-03-13 | 普莱希科公司 | 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904 |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN108137585B (zh) | 2015-09-21 | 2021-10-22 | 普莱希科公司 | 杂环化合物及其应用 |
| RU2018123825A (ru) | 2015-12-07 | 2020-01-15 | Плексксикон Инк. | Соединения и способы для модуляции киназ, и показания для этого |
| WO2017161045A1 (en) | 2016-03-16 | 2017-09-21 | Plexxikon Inc. | Compounds and methods for kinase modulation and indications therefore |
-
2013
- 2013-09-05 MX MX2015002887A patent/MX2015002887A/es unknown
- 2013-09-05 AU AU2013312477A patent/AU2013312477B2/en active Active
- 2013-09-05 WO PCT/US2013/058320 patent/WO2014039714A2/en not_active Ceased
- 2013-09-05 CA CA2883894A patent/CA2883894C/en active Active
- 2013-09-05 ES ES13767165T patent/ES2889757T3/es active Active
- 2013-09-05 EP EP13767165.7A patent/EP2892534B8/en active Active
- 2013-09-05 JP JP2015531206A patent/JP6318156B2/ja active Active
- 2013-09-05 CN CN201380055990.2A patent/CN104981247A/zh active Pending
- 2013-09-05 US US14/019,442 patent/US10227357B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2013312477B2 (en) | 2018-05-31 |
| US20140128390A1 (en) | 2014-05-08 |
| ES2889757T3 (es) | 2022-01-13 |
| EP2892534B1 (en) | 2021-08-04 |
| WO2014039714A3 (en) | 2014-10-02 |
| US10227357B2 (en) | 2019-03-12 |
| JP2015529224A (ja) | 2015-10-05 |
| CA2883894C (en) | 2020-08-18 |
| WO2014039714A2 (en) | 2014-03-13 |
| EP2892534B8 (en) | 2021-09-15 |
| MX2015002887A (es) | 2015-07-06 |
| AU2013312477A1 (en) | 2015-04-02 |
| CA2883894A1 (en) | 2014-03-13 |
| CN104981247A (zh) | 2015-10-14 |
| EP2892534A2 (en) | 2015-07-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6318156B2 (ja) | キナーゼをモジュレートするための化合物および方法、ならびにその指標 | |
| US10301280B2 (en) | Compounds and methods for kinase modulation, and indications therefor | |
| US9771369B2 (en) | Compounds and methods for kinase modulation, and indications therefor | |
| KR102244719B1 (ko) | 헤테로시클릭 화합물 및 그의 용도 | |
| JP2017526726A (ja) | ヘテロ環化合物およびその用途 | |
| HK1213877B (en) | Compounds and methods for kinase modulation, and indications therefor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20160218 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160830 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20160830 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170324 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20170627 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20170629 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170926 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20180306 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20180402 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6318156 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |