JP2020528904A - RORγの阻害剤 - Google Patents
RORγの阻害剤 Download PDFInfo
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- JP2020528904A JP2020528904A JP2020503969A JP2020503969A JP2020528904A JP 2020528904 A JP2020528904 A JP 2020528904A JP 2020503969 A JP2020503969 A JP 2020503969A JP 2020503969 A JP2020503969 A JP 2020503969A JP 2020528904 A JP2020528904 A JP 2020528904A
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- XUYMIRYNRKXKOR-HMHJJOSWSA-N CCS(c1cnc(CNC(c2cnc([C@H](C(C)C)N(C[C@H](CC3)CC[C@@H]3C(F)(F)F)C3)c3c2)=O)cc1)(=O)=O Chemical compound CCS(c1cnc(CNC(c2cnc([C@H](C(C)C)N(C[C@H](CC3)CC[C@@H]3C(F)(F)F)C3)c3c2)=O)cc1)(=O)=O XUYMIRYNRKXKOR-HMHJJOSWSA-N 0.000 description 3
- TYMZQOUSJWNMLZ-ZFSLFXRCSA-N CC/S(/c1cnc(CNC(c2cc(CN(C[C@H](CC3)CC[C@@H]3C(F)(F)F)[C@H]3C(C)C)c3nc2)=O)cc1)=[O]\C Chemical compound CC/S(/c1cnc(CNC(c2cc(CN(C[C@H](CC3)CC[C@@H]3C(F)(F)F)[C@H]3C(C)C)c3nc2)=O)cc1)=[O]\C TYMZQOUSJWNMLZ-ZFSLFXRCSA-N 0.000 description 1
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Description
[0001]本出願は、その全内容が参照により本明細書に組み込まれる、2017年7月24日出願の米国仮特許出願第62/536,114への優先権の利益を主張する。
[0020]用語「形態D」は、単独で使用されている場合、化合物1の結晶多形体Dを指す。用語「形態D」、「化合物1の形態D」および「化合物1の結晶形態D」は、互換的に使用される。同様に、用語「形態E」は、単独で使用されている場合、化合物1の結晶多形体Eを指す。用語「形態E」、「化合物1の形態E」および「化合物1の結晶形態E」は、互換的に使用される。
[0028]化合物1の一臭化水素塩およびビス臭化水素塩を調製する方法が、本明細書において提供される。化合物1および前駆体物質を調製するための出発材料および合成方法は、例えば、その内容が参照により本明細書に組み込まれている米国特許第9,266,886号の一般手順Bに見いだすことができる。
材料/方法
示差走査熱量測定(DSC)
[0047]DSCは、TA Instruments2920示差走査熱量測定を使用して行った。温度較正は、NISTにより追跡可能なインジウム金属を使用して行った。試料をアルミニウム製のTzero圧着パン(T0C)内に置き、その重量を正確に記録した。試料用パンとして構成される秤量済みのアルミニウム製パンを、セルの参照側に置いた。各サーモグラムに関するデータアクイジションパラメーターおよびパン構成は、図中の画像に表示される。サーモグラム上の方法コードは、開始温度および終了温度、ならびに加熱速度の略称である。例えば、(−30)−250−10は、「−30℃から10℃/分で250℃まで」を意味する。
[0048]TG分析は、TA Instruments Q5000 IR熱重量分析器を使用して行った。温度較正は、ニッケルおよびAlumel(商標)を使用して行った。各試料を白金製パンに置いた。この試料を気密密閉し、蓋に穴を開けて、次に、TG炉に挿入した。炉を窒素下で加熱した。各サーモグラムに関するデータアクイジションパラメーターは、図中に表示される。サーモグラム上の方法コードは、開始温度および終了温度、ならびに加熱速度の略称である。例えば、00−350−10は、「周囲℃から10℃/分で350℃まで」を意味する。
[0049]XRPDパターンは、Optixy長高精度焦点源(Optix long,fine−focus source)を使用して発生させたCu照射線の入射ビームを使用する、PANalytical X‘Pert PRO MPD回折計を用いて収集した。楕円状傾斜多層ミラーを使用して、試験体を通して検出器表面にCu Kα X線の焦点を合わせた。分析前に、ケイ素試験体(NIST SRM 640e)を分析し、Si 111ピークの観察位置が、NISTによる認証位置と一致していることを検証した。試料の試験体を、3μmの厚みのフィルムの間に挟んで、透過幾何学で分析した。ビームストップ、短い散乱防止エクステンション(short antiscatter extension)、散乱防止ナイフエッジを使用して、空気により発生するバックグラウンドを最小限にした。入射ビームおよび回折ビームに対するソラースリットを使用して、軸発散に起因する広がりを最小限にした。回折パターンは、試験体から240nmに位置する走査型位置高感度検出器(X’Celerator)およびデータ収集ソフトウェアv.2.2bを使用して収集した。各パターンのデータアクイジションパラメーターは、ミラーの前の発散スリット(DS)を含む、この報告書のデータ項目における画像の上に表示する。
2工程形成
[0050]形態Dに到達する2工程形成が、以下のスキーム5に示される。中間体2は、その内容が参照により本明細書に組み込まれている、米国特許第9,266,886号における一般手順Bに準拠して調製した。
[0057]1工程手法が、以下のスキーム6に示される。中間体2は、米国特許第9,266,886号の一般手順Bに準拠してやはり調製した。
Claims (24)
- 組成物が、酢酸イソプロピル/水の混合物中でスラリー形成される、請求項1に記載の方法。
- 組成物が、0.25%〜2.5%v/vの水を含む酢酸イソプロピルの混合物中でスラリー形成される、請求項1または2に記載の方法。
- 組成物が、0.5%〜2.0%v/vの水を含む酢酸イソプロピルの混合物中でスラリー形成される、請求項1から3のいずれか一項に記載の方法。
- 組成物が、0.9%〜1.1%v/vの水を含む酢酸イソプロピルの混合物中でスラリー形成される、請求項1から4のいずれか一項に記載の方法。
- 組成物が、スラリー形成前に、45ppmより多い臭化メチルを含む、請求項1から5のいずれか一項に記載の方法。
- 分離後の結晶形態Dであるビス臭化水素塩が、40ppm未満の臭化メチルを含む、請求項1から6のいずれか一項に記載の方法。
- 分離後の結晶形態Dであるビス臭化水素塩が、検出レベル未満の量の臭化メチルを含む、請求項1から7のいずれか一項に記載の方法。
- 結晶形態Dであるビス臭化水素塩が、ろ過によって分離される、請求項1から8のいずれか一項に記載の方法。
- 組成物が、0.25%〜2.5%v/vの水を含む酢酸イソプロピルの混合物中でスラリー形成される、請求項10に記載の方法。
- 分離がろ過によって行われる、請求項10または11に記載の方法。
- 組成物中に存在する結晶形態E、FおよびGのうちの1つ以上の量が、90重量%より多い、請求項10から12のいずれか一項に記載の方法。
- ビス臭化水素塩が、14.24°、15.24°、15.90°、18.54°、18.82°および22.46°から選択される2θの角度における、少なくとも3本のX線粉末回折ピークを特徴とする結晶形態Dのものである、請求項1から13のいずれか一項に記載の方法。
- 溶媒としてのエタノール中で還元アミノ化を実施する工程をさらに含む、請求項15に記載の方法。
- 酸が塩酸であり、塩基が水酸化ナトリウムである、請求項15または16に記載の方法。
- イミン還元剤がトリアセトキシ水素化ホウ素ナトリウムである、請求項15から17のいずれか一項に記載の方法。
- 溶液が、工程iii)において、pH5〜7に中和される、請求項15から18のいずれか一項に記載の方法。
- アミン化合物が、アミンの酸塩形態を第三級アミン塩基で処理することによってin situで形成される、請求項15から19のいずれか一項に記載の方法。
- アミンが、アミンの二塩酸塩形態をジイソプロピルエチルアミンで処理することによってin situで形成される、請求項15から20のいずれか一項に記載の方法。
- イソプロパノール、MTBEおよび酢酸の添加をさらに含む、請求項22に記載の方法。
- 臭化水素酸の前記十分な量が、2〜3当量の40%または48%臭化水素酸を含む、請求項22または23に記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762536114P | 2017-07-24 | 2017-07-24 | |
US62/536,114 | 2017-07-24 | ||
PCT/US2018/043451 WO2019023207A1 (en) | 2017-07-24 | 2018-07-24 | INHIBITORS OF RORƳ |
Publications (1)
Publication Number | Publication Date |
---|---|
JP2020528904A true JP2020528904A (ja) | 2020-10-01 |
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ID=63143419
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2020503969A Ceased JP2020528904A (ja) | 2017-07-24 | 2018-07-24 | RORγの阻害剤 |
Country Status (19)
Country | Link |
---|---|
US (2) | US10913739B2 (ja) |
EP (1) | EP3658555A1 (ja) |
JP (1) | JP2020528904A (ja) |
KR (1) | KR20200053481A (ja) |
CN (3) | CN115650976A (ja) |
AR (1) | AR112461A1 (ja) |
AU (1) | AU2018307919B2 (ja) |
BR (1) | BR112020001246A2 (ja) |
CA (1) | CA3070611A1 (ja) |
CL (2) | CL2020000190A1 (ja) |
CO (1) | CO2020001807A2 (ja) |
IL (2) | IL298639A (ja) |
MA (1) | MA49685A (ja) |
MX (2) | MX2020000887A (ja) |
PH (1) | PH12020500129A1 (ja) |
RU (1) | RU2020107919A (ja) |
SG (1) | SG11202000621VA (ja) |
UA (1) | UA126583C2 (ja) |
WO (1) | WO2019023207A1 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX371017B (es) | 2014-02-03 | 2020-01-13 | Vitae Pharmaceuticals Llc | Inhibidores de dihidropirrolopiridina de receptor huerfano relacionado-gamma. |
MX2018006223A (es) | 2015-11-20 | 2018-12-19 | Vitae Pharmaceuticals Inc | Moduladores de ror-gamma. |
MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE ROR gamma |
WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2017505318A (ja) * | 2014-02-03 | 2017-02-16 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | Rorガンマのジヒドロピロロピリジン阻害剤 |
WO2019023216A1 (en) * | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
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KR20200053481A (ko) | 2020-05-18 |
IL272191B2 (en) | 2023-05-01 |
IL298639A (en) | 2023-01-01 |
IL272191A (en) | 2020-03-31 |
RU2020107919A (ru) | 2021-08-25 |
WO2019023207A1 (en) | 2019-01-31 |
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CN115650976A (zh) | 2023-01-31 |
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CA3070611A1 (en) | 2019-01-31 |
AR112461A1 (es) | 2019-10-30 |
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