JP5599784B2 - ジアザカルバゾール類と使用方法 - Google Patents
ジアザカルバゾール類と使用方法 Download PDFInfo
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- JP5599784B2 JP5599784B2 JP2011513498A JP2011513498A JP5599784B2 JP 5599784 B2 JP5599784 B2 JP 5599784B2 JP 2011513498 A JP2011513498 A JP 2011513498A JP 2011513498 A JP2011513498 A JP 2011513498A JP 5599784 B2 JP5599784 B2 JP 5599784B2
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- GBMLHAJYZHFQQN-UHFFFAOYSA-N N#Cc(ncc1c2c3cc(Br)cnc3[nH]1)c2N1CCN(CC(F)(F)F)CC1 Chemical compound N#Cc(ncc1c2c3cc(Br)cnc3[nH]1)c2N1CCN(CC(F)(F)F)CC1 GBMLHAJYZHFQQN-UHFFFAOYSA-N 0.000 description 1
- VRBOCWBONSGDTI-UHFFFAOYSA-N N#Cc1ncc2[nH]c3nccc(NC4CCNCC4)c3c2c1 Chemical compound N#Cc1ncc2[nH]c3nccc(NC4CCNCC4)c3c2c1 VRBOCWBONSGDTI-UHFFFAOYSA-N 0.000 description 1
- CASUGPAELXXROV-UHFFFAOYSA-N NC(C1)N=Cc([nH]2)c1c1c2ncc(-c2ccccc2CO)c1 Chemical compound NC(C1)N=Cc([nH]2)c1c1c2ncc(-c2ccccc2CO)c1 CASUGPAELXXROV-UHFFFAOYSA-N 0.000 description 1
- KBPIERJXKUICOW-UHFFFAOYSA-N NC(c(nc1)cc(c2c3)c1[nH]c2ncc3Br)=O Chemical compound NC(c(nc1)cc(c2c3)c1[nH]c2ncc3Br)=O KBPIERJXKUICOW-UHFFFAOYSA-N 0.000 description 1
- SZCHTCMDYFBODB-UHFFFAOYSA-N NNC(c(cc1c2c3)ncc1[nH]c2ncc3-c1ccc(CN2CCCCC2)cc1)=O Chemical compound NNC(c(cc1c2c3)ncc1[nH]c2ncc3-c1ccc(CN2CCCCC2)cc1)=O SZCHTCMDYFBODB-UHFFFAOYSA-N 0.000 description 1
- DRIDSHDBMUCZDX-UHFFFAOYSA-N Nc(c(I)c1)cnc1Br Chemical compound Nc(c(I)c1)cnc1Br DRIDSHDBMUCZDX-UHFFFAOYSA-N 0.000 description 1
- YDEFRKQAFYKZOZ-UHFFFAOYSA-N Nc(cn1)c(-c(cc(cn2)-c3ccc(CN4CCCCC4)cc3)c2F)c(Br)c1Cl Chemical compound Nc(cn1)c(-c(cc(cn2)-c3ccc(CN4CCCCC4)cc3)c2F)c(Br)c1Cl YDEFRKQAFYKZOZ-UHFFFAOYSA-N 0.000 description 1
- PMBMWAUXJPACJZ-UHFFFAOYSA-N Nc(nc1)cc2c1[nH]c(nc1)c2cc1-c1ccc(CN2CCCCC2)cc1 Chemical compound Nc(nc1)cc2c1[nH]c(nc1)c2cc1-c1ccc(CN2CCCCC2)cc1 PMBMWAUXJPACJZ-UHFFFAOYSA-N 0.000 description 1
- FCQLKAWVWVURRM-UHFFFAOYSA-N O=C(C=C1c2c3)NC=C1Nc2ncc3-c1ccc(CN2CCCCC2)cc1 Chemical compound O=C(C=C1c2c3)NC=C1Nc2ncc3-c1ccc(CN2CCCCC2)cc1 FCQLKAWVWVURRM-UHFFFAOYSA-N 0.000 description 1
- YAYAZDVNZQCMIW-UHFFFAOYSA-N O=C(c(nc1)cc(c2c3)c1[nH]c2ncc3Br)N1CCCC1 Chemical compound O=C(c(nc1)cc(c2c3)c1[nH]c2ncc3Br)N1CCCC1 YAYAZDVNZQCMIW-UHFFFAOYSA-N 0.000 description 1
- ILOLVIRUGHWYBI-UHFFFAOYSA-N OC(c1ncc2[nH]c(ncc(-c3cccc(C(F)(F)F)c3)c3)c3c2c1)=O Chemical compound OC(c1ncc2[nH]c(ncc(-c3cccc(C(F)(F)F)c3)c3)c3c2c1)=O ILOLVIRUGHWYBI-UHFFFAOYSA-N 0.000 description 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
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- 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
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- 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
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- 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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (5)
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| US6074608P | 2008-06-11 | 2008-06-11 | |
| US61/060,746 | 2008-06-11 | ||
| US14800109P | 2009-01-28 | 2009-01-28 | |
| US61/148,001 | 2009-01-28 | ||
| PCT/US2009/003492 WO2009151598A1 (en) | 2008-06-11 | 2009-06-10 | Diazacarbazoles and methods of use |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2015028027A (ja) * | 2008-06-11 | 2015-02-12 | ジェネンテック, インコーポレイテッド | ジアザカルバゾール類と使用方法 |
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| SI1896040T1 (sl) | 2005-06-29 | 2012-12-31 | Threshold Pharmaceuticals, Inc. | Fosforamidatna alkilatorska predzdravila |
| AR072084A1 (es) * | 2008-06-12 | 2010-08-04 | Sanofi Aventis | Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim |
| UY32275A (es) * | 2009-03-24 | 2010-06-30 | Sanofi Aventis | DERIVADOS DE AZACARBOLINAS 9H-PIRROLO[2,3-b:5,4-c'] DIPIRIDINA, SU PREPARACION Y SU UTILIZACIÓN TERAPÉUTICA. |
| FR2950891B1 (fr) * | 2009-10-06 | 2012-11-09 | Sanofi Aventis | Derives d'azacarbolines 9h-pyrrolo[2,3-b:5,4-c']dipyridine, leur preparation et leur utilisation therapeutique |
| US20110183938A1 (en) * | 2009-12-16 | 2011-07-28 | Genentech, Inc. | 1,7-diazacarbazoles and methods of use |
| WO2012074754A1 (en) | 2010-11-16 | 2012-06-07 | Array Biopharma Inc. | Combination of checkpoint kinase 1 inhibitors and wee 1 kinase inhibitors |
| CN102503959B (zh) * | 2011-10-25 | 2015-04-08 | 南方医科大学 | 一种稠三环类化合物及其制备方法、以及含该类化合物的药物组合物及其应用 |
| EP2776417B1 (en) * | 2011-11-09 | 2018-10-31 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| JP2015500885A (ja) * | 2011-12-22 | 2015-01-08 | スレッショルド ファーマシューティカルズ,インコーポレイテッド | 癌を治療するためのchk1阻害剤と組み合わせた低酸素活性化プロドラッグの投与 |
| JP6182593B2 (ja) | 2012-04-20 | 2017-08-16 | アドヴィーナス セラピューティクス リミテッド | 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途 |
| EP2671881A1 (en) | 2012-06-07 | 2013-12-11 | Syngenta Participations AG. | Pesticidally active pyridyl- and pyrimidyl- substituted thiazole derivatives |
| KR20160104612A (ko) | 2013-07-26 | 2016-09-05 | 업데이트 파마 인코포레이트 | 비산트렌의 치료 효과 개선용 조성물 |
| US10071109B2 (en) | 2013-11-06 | 2018-09-11 | Molecular Templates, Inc. | Predictive biomarker for hypoxia-activated prodrug therapy |
| AU2015240465B2 (en) | 2014-04-04 | 2020-02-27 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| CN107118207B (zh) * | 2017-05-22 | 2020-10-02 | 苏州东南药业股份有限公司 | 一类cdk抑制剂的制备方法 |
| EP3788046B1 (en) | 2018-05-04 | 2025-12-10 | Incyte Corporation | Salts of an fgfr inhibitor |
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| SE0401655D0 (sv) | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | New compounds |
| JP2008542433A (ja) * | 2005-06-09 | 2008-11-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | CDK−1インヒビターとしてのα−カルボリン |
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| WO2010015589A1 (en) | 2008-08-05 | 2010-02-11 | Nycomed Gmbh | Benzyl-substituted tetracyclic heterocyclic compounds as pde5 inhibitors |
| UY32275A (es) * | 2009-03-24 | 2010-06-30 | Sanofi Aventis | DERIVADOS DE AZACARBOLINAS 9H-PIRROLO[2,3-b:5,4-c'] DIPIRIDINA, SU PREPARACION Y SU UTILIZACIÓN TERAPÉUTICA. |
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| JP2015028027A (ja) * | 2008-06-11 | 2015-02-12 | ジェネンテック, インコーポレイテッド | ジアザカルバゾール類と使用方法 |
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