RU2012125152A - Способы и композиции, предназначенные для лечения солидных опухолей и других злокачественных новообразований - Google Patents
Способы и композиции, предназначенные для лечения солидных опухолей и других злокачественных новообразований Download PDFInfo
- Publication number
- RU2012125152A RU2012125152A RU2012125152/15A RU2012125152A RU2012125152A RU 2012125152 A RU2012125152 A RU 2012125152A RU 2012125152/15 A RU2012125152/15 A RU 2012125152/15A RU 2012125152 A RU2012125152 A RU 2012125152A RU 2012125152 A RU2012125152 A RU 2012125152A
- Authority
- RU
- Russia
- Prior art keywords
- agent
- combination
- inhibitor
- mtor
- everolimus
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims abstract 5
- 230000003211 malignant effect Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 239000007787 solid Substances 0.000 title 1
- 239000003795 chemical substances by application Substances 0.000 claims abstract 24
- 229940124302 mTOR inhibitor Drugs 0.000 claims abstract 10
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims abstract 10
- BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims abstract 8
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 claims abstract 8
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 claims abstract 8
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims abstract 7
- 229960005167 everolimus Drugs 0.000 claims abstract 7
- KVLFRAWTRWDEDF-IRXDYDNUSA-N AZD-8055 Chemical compound C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3[C@H](COCC3)C)N3[C@H](COCC3)C)C2=N1 KVLFRAWTRWDEDF-IRXDYDNUSA-N 0.000 claims abstract 4
- RFSMUFRPPYDYRD-CALCHBBNSA-N Ku-0063794 Chemical compound C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3C[C@@H](C)O[C@@H](C)C3)N3CCOCC3)C2=N1 RFSMUFRPPYDYRD-CALCHBBNSA-N 0.000 claims abstract 4
- 208000000172 Medulloblastoma Diseases 0.000 claims abstract 4
- 102000013380 Smoothened Receptor Human genes 0.000 claims abstract 4
- 108010090739 Smoothened Receptor Proteins 0.000 claims abstract 4
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims abstract 4
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims abstract 4
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims abstract 4
- 230000003281 allosteric effect Effects 0.000 claims abstract 4
- 201000011510 cancer Diseases 0.000 claims abstract 4
- JROFGZPOBKIAEW-HAQNSBGRSA-N chembl3120215 Chemical compound N1C=2C(OC)=CC=CC=2C=C1C(=C1C(N)=NC=NN11)N=C1[C@H]1CC[C@H](C(O)=O)CC1 JROFGZPOBKIAEW-HAQNSBGRSA-N 0.000 claims abstract 4
- 239000003112 inhibitor Substances 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims abstract 4
- 229960002930 sirolimus Drugs 0.000 claims abstract 4
- 229960000235 temsirolimus Drugs 0.000 claims abstract 4
- -1 6-benzyl-4,5-dimethylpyridazin-3-yl Chemical group 0.000 claims abstract 2
- 241000027355 Ferocactus setispinus Species 0.000 claims abstract 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000012268 protein inhibitor Substances 0.000 claims abstract 2
- 229940121649 protein inhibitor Drugs 0.000 claims abstract 2
- 230000019491 signal transduction Effects 0.000 claims abstract 2
- QLHHRYZMBGPBJG-UHFFFAOYSA-N 1-[4-[1-(1,4-dioxaspiro[4.5]decan-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-6-pyrazolo[3,4-d]pyrimidinyl]phenyl]-3-methylurea Chemical compound C1=CC(NC(=O)NC)=CC=C1C1=NC(N2CC3CCC(O3)C2)=C(C=NN2C3CCC4(CC3)OCCO4)C2=N1 QLHHRYZMBGPBJG-UHFFFAOYSA-N 0.000 claims 2
- 102000009308 Mechanistic Target of Rapamycin Complex 2 Human genes 0.000 claims 2
- 108010034057 Mechanistic Target of Rapamycin Complex 2 Proteins 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000001747 exhibiting effect Effects 0.000 claims 2
- LNRROOUNLXDADK-UHFFFAOYSA-N 2-methyl-3-[4-(trifluoromethoxy)phenyl]benzoic acid Chemical compound CC1=C(C(O)=O)C=CC=C1C1=CC=C(OC(F)(F)F)C=C1 LNRROOUNLXDADK-UHFFFAOYSA-N 0.000 claims 1
- VLPBNQMPKNGOJC-DTORHVGOSA-N 6-[(2r,6s)-2,6-dimethylmorpholin-4-yl]pyridin-3-amine Chemical group C1[C@@H](C)O[C@@H](C)CN1C1=CC=C(N)C=N1 VLPBNQMPKNGOJC-DTORHVGOSA-N 0.000 claims 1
- GMJDSLPKJHTIQL-UHFFFAOYSA-N 5-phenyl-2-(trifluoromethoxy)benzamide Chemical compound FC(OC1=C(C=C(C=C1)C1=CC=CC=C1)C(=O)N)(F)F GMJDSLPKJHTIQL-UHFFFAOYSA-N 0.000 abstract 1
- JRLTTZUODKEYDH-UHFFFAOYSA-N 8-methylquinoline Chemical group C1=CN=C2C(C)=CC=CC2=C1 JRLTTZUODKEYDH-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- 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
- A61K31/436—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 oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26234209P | 2009-11-18 | 2009-11-18 | |
| US61/262,342 | 2009-11-18 | ||
| US29203210P | 2010-01-04 | 2010-01-04 | |
| US61/292,032 | 2010-01-04 | ||
| PCT/US2010/056942 WO2011062939A1 (en) | 2009-11-18 | 2010-11-17 | Methods and compositions for treating solid tumors and other malignancies |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012125152A true RU2012125152A (ru) | 2013-12-27 |
Family
ID=43384585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012125152/15A RU2012125152A (ru) | 2009-11-18 | 2010-11-17 | Способы и композиции, предназначенные для лечения солидных опухолей и других злокачественных новообразований |
Country Status (18)
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2501236B1 (en) | 2009-11-18 | 2017-03-29 | Plexxikon Inc. | N-[2-fluoro-3-(4-amino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-phenyl]-4-benzenesulfonamide derivatives as Raf protein kinase modulators for the treatment of cancer |
| EP2715366B1 (en) * | 2011-06-02 | 2017-07-19 | Novartis AG | Biomarkers for hedgehog inhibitor therapy |
| WO2013106812A1 (en) * | 2012-01-12 | 2013-07-18 | Board Of Regents, The University Of Texas System | Personalized medicine for the prediction of therapy targeting the hedgehog pathway |
| JP6293770B2 (ja) * | 2012-11-05 | 2018-03-14 | ナント ホールディングス アイピー，エルエルシー | ヘッジホッグシグナル伝達経路阻害剤としての環状スルホンアミド含有誘導体 |
| CN103524535B (zh) * | 2013-10-16 | 2016-07-13 | 苏州云轩医药科技有限公司 | 具有刺猬通路拮抗剂活性的胺基噻唑-吡啶杂环化合物 |
| WO2018129364A1 (en) | 2017-01-06 | 2018-07-12 | Palvella Therapeutics Llc | Anhydrous compositions of mtor inhibitors and methods of use |
| KR20200125758A (ko) | 2017-10-27 | 2020-11-04 | 베링거 인겔하임 인터내셔날 게엠베하 | 피리딘 카보닐 유도체 및 trpc6 억제제로서 이의 치료학적 용도 |
| EP3817743A4 (en) * | 2018-07-02 | 2022-07-06 | Palvella Therapeutics, Inc. | ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE |
| US20210346385A1 (en) * | 2018-09-21 | 2021-11-11 | MSB Holdings, Inc | Taste-masked dosage forms |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| KR101464384B1 (ko) | 2005-11-22 | 2014-11-21 | 쿠도스 파마슈티칼스 리미티드 | ｍＴＯＲ 억제제로서 피리도피리미딘, 피라조피리미딘 및피리미도피리미딘 유도체 |
| UA93548C2 (uk) * | 2006-05-05 | 2011-02-25 | Айерем Елелсі | Сполуки та композиції як модулятори хеджхогівського сигнального шляху |
| JP5227321B2 (ja) | 2006-08-23 | 2013-07-03 | クドス ファーマシューティカルズ リミテッド | Ｍｔｏｒ阻害剤としての２−メチルモルホリンピリド−、ピラゾ−及びピリミド−ピリミジン誘導体 |
| US8536168B2 (en) * | 2007-03-15 | 2013-09-17 | Novartis Ag | Benzyl and pyridinyl derivatives as modulators of the hedgehog signaling pathway |
| ES2569941T3 (es) * | 2007-06-07 | 2016-05-13 | Novartis Ag | Derivados de bifenilcarboxamida como moduladores de la ruta de hedgehog |
| US8153633B2 (en) * | 2007-06-25 | 2012-04-10 | Amgen Inc. | Phthalazine compounds, compositions and methods of use |
| WO2009112266A1 (en) * | 2008-03-12 | 2009-09-17 | Ludwig-Maximilians-Universität | Active substance combination with gemcitabine for the treatment of epithelial cancer |
| CN102066353B (zh) * | 2008-04-29 | 2013-12-11 | 伊莱利利公司 | 二取代的酞嗪Hedgehog通路拮抗剂 |
| US20100041663A1 (en) * | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
-
2010
- 2010-11-17 JP JP2012539987A patent/JP2013511526A/ja not_active Ceased
- 2010-11-17 CN CN2010800517592A patent/CN102665700A/zh active Pending
- 2010-11-17 PH PH1/2012/500911A patent/PH12012500911A1/en unknown
- 2010-11-17 CA CA2781210A patent/CA2781210A1/en not_active Abandoned
- 2010-11-17 CN CN201410410334.6A patent/CN104224791A/zh active Pending
- 2010-11-17 RU RU2012125152/15A patent/RU2012125152A/ru unknown
- 2010-11-17 AU AU2010322114A patent/AU2010322114B2/en not_active Ceased
- 2010-11-17 MX MX2012005695A patent/MX2012005695A/es not_active Application Discontinuation
- 2010-11-17 KR KR1020127015545A patent/KR20120107962A/ko not_active Withdrawn
- 2010-11-17 BR BR112012011823A patent/BR112012011823A2/pt not_active IP Right Cessation
- 2010-11-17 WO PCT/US2010/056942 patent/WO2011062939A1/en not_active Ceased
- 2010-11-17 NZ NZ599964A patent/NZ599964A/en not_active IP Right Cessation
- 2010-11-17 EP EP10782767A patent/EP2501370A1/en not_active Withdrawn
- 2010-11-17 US US13/509,857 patent/US20120232087A1/en not_active Abandoned
-
2012
- 2012-05-07 ZA ZA2012/03325A patent/ZA201203325B/en unknown
- 2012-05-07 IL IL219636A patent/IL219636A0/en unknown
- 2012-05-07 TN TNP2012000205A patent/TN2012000205A1/en unknown
- 2012-05-11 MA MA34856A patent/MA33739B1/fr unknown
- 2012-05-16 CL CL2012001271A patent/CL2012001271A1/es unknown
-
2014
- 2014-10-09 US US14/510,713 patent/US20150025074A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2501370A1 (en) | 2012-09-26 |
| KR20120107962A (ko) | 2012-10-04 |
| JP2013511526A (ja) | 2013-04-04 |
| WO2011062939A1 (en) | 2011-05-26 |
| PH12012500911A1 (en) | 2012-11-26 |
| MX2012005695A (es) | 2012-06-13 |
| AU2010322114A1 (en) | 2012-05-31 |
| MA33739B1 (fr) | 2012-11-01 |
| CA2781210A1 (en) | 2011-05-26 |
| NZ599964A (en) | 2014-08-29 |
| ZA201203325B (en) | 2013-01-30 |
| CN102665700A (zh) | 2012-09-12 |
| AU2010322114B2 (en) | 2014-07-31 |
| CN104224791A (zh) | 2014-12-24 |
| US20120232087A1 (en) | 2012-09-13 |
| CL2012001271A1 (es) | 2012-10-12 |
| IL219636A0 (en) | 2012-07-31 |
| BR112012011823A2 (pt) | 2019-09-24 |
| US20150025074A1 (en) | 2015-01-22 |
| TN2012000205A1 (en) | 2013-12-12 |
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