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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
| Country | Link |
|---|---|
| US (2) | US20120232087A1 (enExample) |
| EP (1) | EP2501370A1 (enExample) |
| JP (1) | JP2013511526A (enExample) |
| KR (1) | KR20120107962A (enExample) |
| CN (2) | CN104224791A (enExample) |
| AU (1) | AU2010322114B2 (enExample) |
| BR (1) | BR112012011823A2 (enExample) |
| CA (1) | CA2781210A1 (enExample) |
| CL (1) | CL2012001271A1 (enExample) |
| IL (1) | IL219636A0 (enExample) |
| MA (1) | MA33739B1 (enExample) |
| MX (1) | MX2012005695A (enExample) |
| NZ (1) | NZ599964A (enExample) |
| PH (1) | PH12012500911A1 (enExample) |
| RU (1) | RU2012125152A (enExample) |
| TN (1) | TN2012000205A1 (enExample) |
| WO (1) | WO2011062939A1 (enExample) |
| ZA (1) | ZA201203325B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013511541A (ja) | 2009-11-18 | 2013-04-04 | 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および方法、ならびにその適応 |
| US20140094461A1 (en) * | 2011-06-02 | 2014-04-03 | 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 |
| KR20150105302A (ko) | 2012-11-05 | 2015-09-16 | 난트 홀딩스 아이피, 엘엘씨 | 헤지 호그 신호 경로의 억제제로서 환상 술폰아미드 함유 유도체 |
| 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 |
| AU2018205253B2 (en) | 2017-01-06 | 2022-01-13 | Palvella Therapeutics, Inc. | Anhydrous compositions of mTOR inhibitors and methods of use |
| FI3700902T3 (fi) | 2017-10-27 | 2023-05-25 | Boehringer Ingelheim Int | TRPC6:n inhibiittoreita |
| EP3817743A4 (en) * | 2018-07-02 | 2022-07-06 | Palvella Therapeutics, Inc. | ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE |
| WO2020061584A1 (en) * | 2018-09-21 | 2020-03-26 | 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 |
| PT2057156T (pt) | 2006-08-23 | 2017-05-04 | Kudos Pharm Ltd | Derivados de 2-metilmorfolina pirido-, pirazo- e pirimidopirimidina como inibidores de mtor |
| EP2137162B1 (en) * | 2007-03-15 | 2018-08-01 | Novartis AG | Organic compounds and their uses |
| ES2569941T3 (es) * | 2007-06-07 | 2016-05-13 | Novartis Ag | Derivados de bifenilcarboxamida como moduladores de la ruta de hedgehog |
| ES2505091T3 (es) * | 2007-06-25 | 2014-10-09 | Amgen Inc. | Compuestos, composiciones y métodos de uso de ftalazina |
| EP2249844A1 (en) * | 2008-03-12 | 2010-11-17 | Ludwig-Maximilians-Universität München | Active substance combination with gemcitabine for the treatment of epithelial cancer |
| US7981892B2 (en) * | 2008-04-29 | 2011-07-19 | Eli Lilly And Company | Disubstituted phthalazine hedgehog pathway antagonists |
| US20100041663A1 (en) * | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
-
2010
- 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 AU AU2010322114A patent/AU2010322114B2/en not_active Ceased
- 2010-11-17 JP JP2012539987A patent/JP2013511526A/ja not_active Ceased
- 2010-11-17 EP EP10782767A patent/EP2501370A1/en not_active Withdrawn
- 2010-11-17 CA CA2781210A patent/CA2781210A1/en not_active Abandoned
- 2010-11-17 WO PCT/US2010/056942 patent/WO2011062939A1/en not_active Ceased
- 2010-11-17 PH PH1/2012/500911A patent/PH12012500911A1/en unknown
- 2010-11-17 US US13/509,857 patent/US20120232087A1/en not_active Abandoned
- 2010-11-17 MX MX2012005695A patent/MX2012005695A/es not_active Application Discontinuation
- 2010-11-17 CN CN201410410334.6A patent/CN104224791A/zh active Pending
- 2010-11-17 NZ NZ599964A patent/NZ599964A/en not_active IP Right Cessation
- 2010-11-17 CN CN2010800517592A patent/CN102665700A/zh active Pending
- 2010-11-17 RU RU2012125152/15A patent/RU2012125152A/ru unknown
-
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 |
|---|---|
| IL219636A0 (en) | 2012-07-31 |
| BR112012011823A2 (pt) | 2019-09-24 |
| WO2011062939A1 (en) | 2011-05-26 |
| PH12012500911A1 (en) | 2012-11-26 |
| AU2010322114A1 (en) | 2012-05-31 |
| TN2012000205A1 (en) | 2013-12-12 |
| CA2781210A1 (en) | 2011-05-26 |
| KR20120107962A (ko) | 2012-10-04 |
| AU2010322114B2 (en) | 2014-07-31 |
| CN104224791A (zh) | 2014-12-24 |
| US20120232087A1 (en) | 2012-09-13 |
| NZ599964A (en) | 2014-08-29 |
| MA33739B1 (fr) | 2012-11-01 |
| ZA201203325B (en) | 2013-01-30 |
| CN102665700A (zh) | 2012-09-12 |
| US20150025074A1 (en) | 2015-01-22 |
| EP2501370A1 (en) | 2012-09-26 |
| MX2012005695A (es) | 2012-06-13 |
| CL2012001271A1 (es) | 2012-10-12 |
| JP2013511526A (ja) | 2013-04-04 |
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