AR080863A1 - Derivados del acido1-amino-2-ciclopropiletilboronico, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer. - Google Patents
Derivados del acido1-amino-2-ciclopropiletilboronico, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer.Info
- Publication number
- AR080863A1 AR080863A1 ARP110101066A ARP110101066A AR080863A1 AR 080863 A1 AR080863 A1 AR 080863A1 AR P110101066 A ARP110101066 A AR P110101066A AR P110101066 A ARP110101066 A AR P110101066A AR 080863 A1 AR080863 A1 AR 080863A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- substituted
- unsubstituted
- aliphatic
- aryl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title 1
- 201000011510 cancer Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000001931 aliphatic group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 230000000903 blocking effect Effects 0.000 abstract 1
- 239000008139 complexing agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicacion 1: Compuesto de la formula (1) o una sal farmacéuticamente aceptable o anhídrido de ácido boronico del mismo, caracterizado porque: A es 0, 1 o 2; P es hidrogeno o un radical de bloqueo de grupo amino; cada Ra2 independientemente hidrogeno, alifático C1-6, fluoroalifático C1-6, (CH2)m-CH2-Rb, (CH2)m-CH2-NHC(=NR4)NH-Y, (CH2)m-CH2-CON(R4)2, -(CH2)m-CH2-N(R4)CON(R4)2, -(CH2)m-CH(R6)N(R4)2, -(CH2)m-CH(R5) OR5 o -(CH2)m-CH(R5)-SR5 cada Y es independientemente hidrogeno, -CN, -NO2 o -S(O)2-R10; cada RB es independientemente un sistema de anillo mono o bicíclico sustituido o insustituido; cada R4 es independientemente hidrogeno o un grupo arilo, heteroarilo o heterociclilo alifático sustituido o insustituido; o dos R4 en el mismo átomo de nitrogeno, tomados juntos con el átomo de nitrogeno, forman un anillo heterociclilo sustituido o insustituido de 4 a 8 miembros que tiene, además del átomo de nitrogeno, 0-2 heteroátomos de anillo seleccionados independientemente de N, O y S; cada R5 es independientemente hidrogeno o un grupo alifático arilo, heteroarilo o heterociclilo sustituido o insustituido; cada R6 es independientemente un grupo arilo o heteroarilo alifático sustituido o insustituido; cada R10 es independientemente alifático C1-6, arilo C1-10 o -N(R4)2; m es 0, 1 o 2; Z1 y Z2 son cada uno independientemente hidroxi, alcoxi, ariloxi; o aralcoxi; o Z1 y Z2 forman juntos un radical derivado de un agente de acomplejamiento de ácido boronico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31946410P | 2010-03-31 | 2010-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080863A1 true AR080863A1 (es) | 2012-05-16 |
Family
ID=44710349
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101066A AR080863A1 (es) | 2010-03-31 | 2011-03-30 | Derivados del acido1-amino-2-ciclopropiletilboronico, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer. |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US8513218B2 (es) |
| EP (1) | EP2552216B1 (es) |
| JP (1) | JP5933523B2 (es) |
| KR (1) | KR20130036228A (es) |
| CN (3) | CN106008570A (es) |
| AR (1) | AR080863A1 (es) |
| AU (1) | AU2011235227B2 (es) |
| CA (1) | CA2794334C (es) |
| CL (1) | CL2012002733A1 (es) |
| CO (1) | CO6630162A2 (es) |
| CR (1) | CR20120529A (es) |
| DO (1) | DOP2012000257A (es) |
| EA (1) | EA029521B1 (es) |
| EC (1) | ECSP12012249A (es) |
| MA (1) | MA34169B1 (es) |
| MX (1) | MX2012011298A (es) |
| NZ (1) | NZ602622A (es) |
| PE (1) | PE20130383A1 (es) |
| PH (1) | PH12012501943A1 (es) |
| RU (1) | RU2012146101A (es) |
| SG (1) | SG184222A1 (es) |
| TN (1) | TN2012000465A1 (es) |
| UA (1) | UA110612C2 (es) |
| UY (1) | UY33314A (es) |
| WO (1) | WO2011123502A1 (es) |
| ZA (2) | ZA201207406B (es) |
Families Citing this family (37)
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| ES2628620T3 (es) | 2005-11-09 | 2017-08-03 | Onyx Therapeutics, Inc. | Compuesto para inhibición de enzimas |
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| KR20100088664A (ko) | 2007-10-04 | 2010-08-10 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| EA030685B1 (ru) | 2008-06-17 | 2018-09-28 | Милленниум Фармасьютикалз, Инк. | Способ получения соединения боронатного эфира |
| AR075090A1 (es) * | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. |
| US20110236428A1 (en) | 2008-10-21 | 2011-09-29 | Onyx Therapeutics, Inc. | Combination therapy with peptide epoxyketones |
| AR075899A1 (es) | 2009-03-20 | 2011-05-04 | Onyx Therapeutics Inc | Tripeptidos epoxicetonas cristalinos inhibidores de proteasa |
| WO2011060179A1 (en) | 2009-11-13 | 2011-05-19 | Onyx Therapeutics, Inc | Use of peptide epoxyketones for metastasis suppression |
| MX2012010017A (es) | 2010-03-01 | 2012-10-01 | Onyx Therapeutics Inc | Compuestos de para la inhibicion de inmunoproteasomas. |
| US8513218B2 (en) | 2010-03-31 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
| SG187757A1 (en) | 2010-08-10 | 2013-03-28 | Rempex Pharmaceuticals Inc | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| JP6286358B2 (ja) | 2011-11-11 | 2018-02-28 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | プロテアソーム阻害剤に応答するバイオマーカー |
| WO2013071142A1 (en) | 2011-11-11 | 2013-05-16 | Millennium Pharmaceuticals, Inc. | Biomarkers of response to proteasome inhibitors |
| JP6129203B2 (ja) * | 2011-12-22 | 2017-05-17 | アレス トレーディング ソシエテ アノニム | α−アミノボロン酸誘導体、選択性免疫プロテアソーム阻害剤 |
| EP2810066B1 (en) | 2012-01-24 | 2019-07-31 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
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| CN109096370B (zh) * | 2012-07-26 | 2022-03-18 | 圣特莱国际公司 | 多肽环氧酮化合物 |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP2941246A4 (en) | 2013-01-04 | 2016-12-21 | Rempex Pharmaceuticals Inc | BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USES |
| MX2016003979A (es) | 2013-10-03 | 2016-06-15 | Millennium Pharm Inc | Metodo para profilaxis o tratamiento de lupus eritematoso sistemico y/o nefritis lupica. |
| USRE49816E1 (en) | 2014-01-10 | 2024-01-30 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| LT3140310T (lt) | 2014-05-05 | 2019-11-25 | Rempex Pharmaceuticals Inc | Boronato druskų sintezė ir jų panaudojimas |
| KR20170007448A (ko) | 2014-05-19 | 2017-01-18 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
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| CA2952968A1 (en) | 2014-07-01 | 2016-01-07 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP3177292B1 (en) | 2014-08-07 | 2020-11-25 | Mayo Foundation for Medical Education and Research | Compounds and methods for treating cancer |
| CN114796207A (zh) | 2014-08-18 | 2022-07-29 | 康奈尔大学 | 作为人免疫蛋白酶体的抑制剂的二肽模拟物 |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2016149393A1 (en) | 2015-03-17 | 2016-09-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR102764027B1 (ko) | 2015-10-15 | 2025-02-07 | 코넬 유니버시티 | 프로테아좀 억제제 및 이의 용도 |
| EP3478693B1 (en) | 2016-06-30 | 2021-07-21 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| WO2018160717A1 (en) | 2017-02-28 | 2018-09-07 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
| EP3694605A4 (en) | 2017-10-11 | 2021-10-27 | Cornell University | PEPTIDOMIMETIC PROTEASOME INHIBITORS |
| BR112020007138B1 (pt) | 2017-10-11 | 2023-03-21 | Qpex Biopharma, Inc | Derivados de ácido borônico, métodos de síntese, composição farmacêutica e uso dos mesmos |
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| CA3097127A1 (en) | 2018-04-20 | 2019-10-24 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
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| WO2009006473A2 (en) | 2007-07-05 | 2009-01-08 | Trustees Of Tufts College | Pro-soft polypeptide proteasome inhibitors, and methods of use thereof |
| KR20140042933A (ko) | 2007-08-06 | 2014-04-07 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 프로테아좀 억제제 |
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| EA030685B1 (ru) | 2008-06-17 | 2018-09-28 | Милленниум Фармасьютикалз, Инк. | Способ получения соединения боронатного эфира |
| AR075090A1 (es) | 2008-09-29 | 2011-03-09 | Millennium Pharm Inc | Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. |
| US8513218B2 (en) | 2010-03-31 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
-
2011
- 2011-03-30 US US13/075,306 patent/US8513218B2/en not_active Expired - Fee Related
- 2011-03-30 PE PE2012001810A patent/PE20130383A1/es not_active Application Discontinuation
- 2011-03-30 CA CA2794334A patent/CA2794334C/en not_active Expired - Fee Related
- 2011-03-30 MA MA35323A patent/MA34169B1/fr unknown
- 2011-03-30 PH PH1/2012/501943A patent/PH12012501943A1/en unknown
- 2011-03-30 EA EA201290980A patent/EA029521B1/ru not_active IP Right Cessation
- 2011-03-30 CN CN201610326909.5A patent/CN106008570A/zh active Pending
- 2011-03-30 JP JP2013502789A patent/JP5933523B2/ja not_active Expired - Fee Related
- 2011-03-30 CN CN2011800240565A patent/CN102892291A/zh active Pending
- 2011-03-30 SG SG2012070595A patent/SG184222A1/en unknown
- 2011-03-30 RU RU2012146101/04A patent/RU2012146101A/ru not_active Application Discontinuation
- 2011-03-30 CN CN201710639537.6A patent/CN107266485A/zh active Pending
- 2011-03-30 WO PCT/US2011/030455 patent/WO2011123502A1/en not_active Ceased
- 2011-03-30 MX MX2012011298A patent/MX2012011298A/es unknown
- 2011-03-30 EP EP11763354.5A patent/EP2552216B1/en active Active
- 2011-03-30 UA UAA201212379A patent/UA110612C2/uk unknown
- 2011-03-30 AU AU2011235227A patent/AU2011235227B2/en not_active Ceased
- 2011-03-30 AR ARP110101066A patent/AR080863A1/es unknown
- 2011-03-30 NZ NZ602622A patent/NZ602622A/en not_active IP Right Cessation
- 2011-03-30 KR KR1020127028506A patent/KR20130036228A/ko not_active Ceased
- 2011-03-31 UY UY0001033314A patent/UY33314A/es not_active Application Discontinuation
-
2012
- 2012-09-26 TN TNP2012000465A patent/TN2012000465A1/en unknown
- 2012-09-28 CL CL2012002733A patent/CL2012002733A1/es unknown
- 2012-09-28 DO DO2012000257A patent/DOP2012000257A/es unknown
- 2012-10-03 ZA ZA2012/07406A patent/ZA201207406B/en unknown
- 2012-10-11 EC ECSP12012249 patent/ECSP12012249A/es unknown
- 2012-10-17 CR CR20120529A patent/CR20120529A/es unknown
- 2012-10-30 CO CO12195461A patent/CO6630162A2/es active IP Right Grant
-
2013
- 2013-07-03 US US13/934,989 patent/US8703743B2/en not_active Expired - Fee Related
- 2013-10-30 ZA ZA2013/08086A patent/ZA201308086B/en unknown
-
2014
- 2014-02-25 US US14/189,303 patent/US9023832B2/en active Active
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