AR101964A1 - Compuestos de imidazopiridazina como moduladores de pi3k - Google Patents
Compuestos de imidazopiridazina como moduladores de pi3kInfo
- Publication number
- AR101964A1 AR101964A1 ARP150103008A ARP150103008A AR101964A1 AR 101964 A1 AR101964 A1 AR 101964A1 AR P150103008 A ARP150103008 A AR P150103008A AR P150103008 A ARP150103008 A AR P150103008A AR 101964 A1 AR101964 A1 AR 101964A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heteroaryl
- haloalkyl
- halo
- optionally substituted
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
Abstract
Esta descripción provee compuestos de imidazopiridazina y sales farmacéuticamente aceptables de los mismos, composiciones farmacéuticas que los contienen, un proceso para prepararlos y su efecto práctico en la inhibición de Pl3K y su uso potencial en el tratamiento de una enfermedad que responde a la inhibición de Pl3K, por ejemplo, una enfermedad inflamatoria, una enfermedad autoinmune o cáncer. Reivindicación 1: Un compuesto de fórmula (1) y/o una sal farmacéuticamente aceptable del mismo, y/o solvatos, mezcla racémica, enantiómeros, diastereómeros y tautómeros del mismo, en donde Ar es arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido con uno o más grupos elegidos de deuterio, halo, -CN, -OH, -SH, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, -O(alquilo C₁₋₆), -(alquilo C₁₋₆)OH, -NH₂, -NH(alquilo C₁₋₆), -N(alquilo C₁₋₆)(alquilo C₁₋₆), y -S(O)₂(alquilo C₁₋₆); W es elegido de heteroarilo y -N(R³)heteroarilo, en donde dicho heteroarilo está opcionalmente sustituido con uno o más grupos elegidos de halo, -CN, -OH, -SH, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, -O(alquilo C₁₋₆), -(alquilo C₁₋₆)OH, -NH₂, -NH(alquilo C₁₋₆), -N(alquilo C₁₋₆)(alquilo C₁₋₆), -COOH, -C(O)NH₂, C(O)NH(alquilo C₁₋₆), -C(O)N(alquilo C₁₋₆)(alquilo C₁₋₆), -SO₂(alquilo C₁₋₆), fenilo, y heteroarilo de 5- ó 6- miembros; en el cual cada uno de dichos fenilo o heteroarilo de 5- ó 6- miembros como sustituyente de W está opcionalmente sustituido con uno o más grupos elegidos de halo, -CN, -OH, -SH, alquilo C₁₋₆, haloalquilo C₁₋₆, -O(alquilo C₁₋₆), -(alquilo C₁₋₆)OH, -NH₂, -NH(alquilo C₁₋₆), y -N(alquilo C₁₋₆)(alquilo C₁₋₆); R¹ es independientemente elegido de H, halo, -CN, alquilo C₁₋₆, haloalquilo C₁₋₆, -(alquilo C₁₋₆)OH, -(alquilo C₁₋₆)O(alquilo C₁₋₆), y alquinilo C₂₋₆; R² es elegido de H, alquilo C₁₋₆, y cicloalquilo C₃₋₈, cada uno de los cuales, excepto para H, está opcionalmente sustituido con uno o más grupos elegidos de halo, -CN, alquilo C₁₋₆, haloalquilo C₁₋₆, y -OH; R³ es H o alquilo C₁₋₆; m es 1 ó 2. Reivindicación 32: Un compuesto de fórmula (2) y/o una sal del mismo; y/o una mezcla racémica o enantiómero del mismo; en donde Ar y R² están definidos como en una cualquiera de las reivindicaciones 1 - 23.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410494483.5A CN105503877A (zh) | 2014-09-24 | 2014-09-24 | 咪唑并哒嗪类化合物及其用途 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR101964A1 true AR101964A1 (es) | 2017-01-25 |
Family
ID=55580324
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103008A AR101964A1 (es) | 2014-09-24 | 2015-09-18 | Compuestos de imidazopiridazina como moduladores de pi3k |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US10208066B2 (es) |
| EP (1) | EP3197898B1 (es) |
| JP (1) | JP6381792B2 (es) |
| KR (2) | KR102111570B1 (es) |
| CN (2) | CN105503877A (es) |
| AR (1) | AR101964A1 (es) |
| AU (1) | AU2015320142B2 (es) |
| BR (1) | BR112017006002B1 (es) |
| CA (1) | CA2958671C (es) |
| CL (1) | CL2017000682A1 (es) |
| CY (1) | CY1122763T1 (es) |
| DK (1) | DK3197898T3 (es) |
| EA (1) | EA032643B1 (es) |
| ES (1) | ES2765510T3 (es) |
| HR (1) | HRP20192279T1 (es) |
| HU (1) | HUE047377T2 (es) |
| IL (1) | IL250703B (es) |
| LT (1) | LT3197898T (es) |
| MX (1) | MX2017003902A (es) |
| MY (1) | MY178136A (es) |
| NZ (1) | NZ729886A (es) |
| PE (1) | PE20170936A1 (es) |
| PH (1) | PH12017500564B1 (es) |
| PL (1) | PL3197898T3 (es) |
| PT (1) | PT3197898T (es) |
| RS (1) | RS59831B1 (es) |
| SG (1) | SG11201701545YA (es) |
| SI (1) | SI3197898T1 (es) |
| TW (1) | TWI707855B (es) |
| UA (1) | UA118066C2 (es) |
| WO (1) | WO2016045591A1 (es) |
| ZA (1) | ZA201701312B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105503877A (zh) * | 2014-09-24 | 2016-04-20 | 和记黄埔医药（上海）有限公司 | 咪唑并哒嗪类化合物及其用途 |
| CN109516973A (zh) * | 2017-09-19 | 2019-03-26 | 南京圣和药业股份有限公司 | 取代嘧啶类化合物、其制备方法及用途 |
| CN110386937A (zh) | 2018-04-20 | 2019-10-29 | 和记黄埔医药（上海）有限公司 | 化合物的晶型和无定型 |
| EP3898620A1 (en) | 2018-12-20 | 2021-10-27 | Bayer Aktiengesellschaft | Heterocyclyl pyridazine as fungicidal compounds |
| CN110028502B (zh) * | 2019-05-29 | 2020-02-14 | 济南周行医药科技有限公司 | 一种激酶抑制剂类药物中间体的制备方法 |
| CA3187297A1 (en) | 2020-06-18 | 2021-12-23 | Bayer Aktiengesellschaft | Active compound combinations |
| CN114031558A (zh) * | 2021-12-14 | 2022-02-11 | 无锡捷化医药科技有限公司 | 一种1-(6-氯哒嗪-4-基）乙基-1-酮的制备方法 |
| WO2023143496A1 (zh) * | 2022-01-28 | 2023-08-03 | 和记黄埔医药（上海）有限公司 | 咪唑并[1,2-b]哒嗪类化合物的中间体的合成方法 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5773958A (en) | 1997-01-03 | 1998-06-30 | Ovonic Battery Company, Inc. | Apparatus for detecting cell reversal in rechargeable batteries |
| CA2285264A1 (en) * | 1997-04-25 | 1998-11-05 | Michiyo Gyoten | Condensed pyridazine derivatives, their production and use |
| US7932260B2 (en) | 2004-05-13 | 2011-04-26 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| KR20080104351A (ko) | 2006-03-31 | 2008-12-02 | 노파르티스 아게 | 유기 화합물 |
| CN101522682A (zh) * | 2006-10-30 | 2009-09-02 | 诺瓦提斯公司 | 作为抗炎剂的杂环化合物 |
| WO2008052733A1 (en) | 2006-10-30 | 2008-05-08 | Novartis Ag | Imidazopyridazines as pi3k lipid kinase inhibitors |
| CN101528748A (zh) * | 2006-10-30 | 2009-09-09 | 诺瓦提斯公司 | 作为pi3k脂质激酶抑制剂的咪唑并哒嗪类化合物 |
| AU2008250328A1 (en) | 2007-05-09 | 2008-11-20 | Novartis Ag | Substituted imidazopyridazines as PI3K lipid kinase inhibitors |
| US20110046127A1 (en) * | 2007-11-08 | 2011-02-24 | Paolo Pevarello | Imidazopyridazines for Use as Protein Kinase Inhibitors |
| JP5520831B2 (ja) * | 2007-12-19 | 2014-06-11 | アムジエン・インコーポレーテツド | Ｐｉ３キナーゼの阻害薬 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| WO2010007099A1 (en) | 2008-07-15 | 2010-01-21 | Cellzome Limited | 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors |
| CA2975473C (en) | 2008-11-13 | 2021-01-19 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| US9127000B2 (en) * | 2011-02-23 | 2015-09-08 | Intellikine, LLC. | Heterocyclic compounds and uses thereof |
| CN104024257A (zh) * | 2011-10-04 | 2014-09-03 | 吉利德卡利斯托加有限责任公司 | Pi3k的新的喹喔啉抑制剂 |
| US20130143902A1 (en) | 2011-12-02 | 2013-06-06 | Gilead Calistoga Llc | Compositions and methods of treating a proliferative disease with a quinazolinone derivative |
| WO2013090725A1 (en) | 2011-12-15 | 2013-06-20 | Philadelphia Health & Education Corporation | NOVEL PI3K p110 INHIBITORS AND METHODS OF USE THEREOF |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| US20140120060A1 (en) | 2012-11-01 | 2014-05-01 | Infinity Pharmaceuticals, Inc. | Treatment of rheumatoid arthritis and asthma using pi3 kinase inhibitors |
| US20140120083A1 (en) | 2012-11-01 | 2014-05-01 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| 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 |
| JP6207100B2 (ja) | 2012-12-21 | 2017-10-04 | ギリアード カリストガ エルエルシー | イソキノリノンまたはキナゾリノンホスファチジルイノシトール３−キナーゼ阻害剤 |
| CN105503877A (zh) * | 2014-09-24 | 2016-04-20 | 和记黄埔医药（上海）有限公司 | 咪唑并哒嗪类化合物及其用途 |
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2014
- 2014-09-24 CN CN201410494483.5A patent/CN105503877A/zh active Pending
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2015
- 2015-09-18 AR ARP150103008A patent/AR101964A1/es active IP Right Grant
- 2015-09-23 US US15/513,811 patent/US10208066B2/en active Active
- 2015-09-23 CN CN201580047532.3A patent/CN106715432B/zh active Active
- 2015-09-23 UA UAA201703837A patent/UA118066C2/uk unknown
- 2015-09-23 AU AU2015320142A patent/AU2015320142B2/en active Active
- 2015-09-23 JP JP2017516139A patent/JP6381792B2/ja active Active
- 2015-09-23 HU HUE15843649A patent/HUE047377T2/hu unknown
- 2015-09-23 MY MYPI2017700637A patent/MY178136A/en unknown
- 2015-09-23 KR KR1020197021644A patent/KR102111570B1/ko active IP Right Grant
- 2015-09-23 SG SG11201701545YA patent/SG11201701545YA/en unknown
- 2015-09-23 BR BR112017006002-7A patent/BR112017006002B1/pt active IP Right Grant
- 2015-09-23 MX MX2017003902A patent/MX2017003902A/es active IP Right Grant
- 2015-09-23 CA CA2958671A patent/CA2958671C/en active Active
- 2015-09-23 SI SI201531035T patent/SI3197898T1/sl unknown
- 2015-09-23 NZ NZ729886A patent/NZ729886A/en unknown
- 2015-09-23 LT LTEP15843649.3T patent/LT3197898T/lt unknown
- 2015-09-23 KR KR1020177010274A patent/KR102006670B1/ko active IP Right Grant
- 2015-09-23 PT PT158436493T patent/PT3197898T/pt unknown
- 2015-09-23 RS RS20200012A patent/RS59831B1/sr unknown
- 2015-09-23 EP EP15843649.3A patent/EP3197898B1/en active Active
- 2015-09-23 DK DK15843649.3T patent/DK3197898T3/da active
- 2015-09-23 WO PCT/CN2015/090367 patent/WO2016045591A1/en active Application Filing
- 2015-09-23 PE PE2017000461A patent/PE20170936A1/es unknown
- 2015-09-23 ES ES15843649T patent/ES2765510T3/es active Active
- 2015-09-23 PL PL15843649T patent/PL3197898T3/pl unknown
- 2015-09-23 EA EA201790276A patent/EA032643B1/ru unknown
- 2015-09-24 TW TW104131565A patent/TWI707855B/zh active
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2017
- 2017-02-21 IL IL250703A patent/IL250703B/en active IP Right Grant
- 2017-02-21 ZA ZA2017/01312A patent/ZA201701312B/en unknown
- 2017-03-22 CL CL2017000682A patent/CL2017000682A1/es unknown
- 2017-03-24 PH PH12017500564A patent/PH12017500564B1/en unknown
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2018
- 2018-12-20 US US16/227,801 patent/US10611777B2/en active Active
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2019
- 2019-12-18 HR HRP20192279TT patent/HRP20192279T1/hr unknown
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2020
- 2020-01-08 CY CY20201100013T patent/CY1122763T1/el unknown
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