PE20130383A1 - Derivados del acido 1-amino-2-ciclopropiletilboronico - Google Patents
Derivados del acido 1-amino-2-ciclopropiletilboronicoInfo
- Publication number
- PE20130383A1 PE20130383A1 PE2012001810A PE2012001810A PE20130383A1 PE 20130383 A1 PE20130383 A1 PE 20130383A1 PE 2012001810 A PE2012001810 A PE 2012001810A PE 2012001810 A PE2012001810 A PE 2012001810A PE 20130383 A1 PE20130383 A1 PE 20130383A1
- Authority
- PE
- Peru
- Prior art keywords
- amino
- acid
- cyclopropylethylboronic
- cyclopropyl
- phenyl
- Prior art date
Links
- MRSJTEYJBNWEFR-UHFFFAOYSA-N (1-amino-2-cyclopropylethyl)boronic acid Chemical class OB(O)C(N)CC1CC1 MRSJTEYJBNWEFR-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000003254 radicals Chemical class 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 229940079156 Proteasome inhibitor Drugs 0.000 abstract 1
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000003207 proteasome inhibitor Substances 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
-
- 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
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (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
SE REFIERE A UN COMPUESTO DERIVADO DEL ACIDO 1-AMINO-2-CICLOPROPILETILBORONICO .DE FORMULA (I) DONDE: A ES UN ENTERO ENTRE 0 Y 2; P ES H O UN RADICAL DE BLOQUEO DE GRUPO; Ra2 ES HIDROGENO, ALIFATICO C1-C6, FLUOROALIFATICO C1-C6 ENTRE OTROS; Z 1 Y Z2 SON HIDROXI, ALCOXI, ARILOXI, ARALCOXI O FORMAN JUNTOS UN RADICAL DERIVADO DE AGENTE DE ACOMPLEJAMIENTO DE ACIDO BORONICO. SON COMPUESTOS PREFERIDOS: ACIDO((1R)-2-CICLOPROPIL-1-{[(2S)-3-FENIL-2-({[4-(PIRIDIN-2-ILOXI)FENIL]SULFONIL}AMINO)PROPANOIL]AMINO}ETIL)BORONICO, ACIDO{(1R)-2-CICLOPROPIL-1-[((2S)-2-{[(6-FENOXIPIRIDIN-3-IL)SULFONIL]AMINO}-3-FENILPROPANOIL)AMINO]ETIL}BORONICO; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE PROTEASOMA UTIL EN EL TRATAMIENTO DEL CANCER.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31946410P | 2010-03-31 | 2010-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20130383A1 true PE20130383A1 (es) | 2013-04-24 |
Family
ID=44710349
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012001810A PE20130383A1 (es) | 2010-03-31 | 2011-03-30 | Derivados del acido 1-amino-2-ciclopropiletilboronico |
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) |
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| MX2008006090A (es) | 2005-11-09 | 2008-10-23 | Proteolix Inc | Compuestos para inhibicion de la enzima. |
| RU2450016C2 (ru) | 2006-06-19 | 2012-05-10 | Протеоликс, Инк. | Пептидные эпоксикетоны для ингибирования протеасомы |
| KR20160086980A (ko) | 2007-10-04 | 2016-07-20 | 오닉스 세라퓨틱스, 인크. | 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성 |
| KR101691093B1 (ko) | 2008-06-17 | 2016-12-29 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | 보로네이트 에스테르 화합물 및 이의 제약학적 조성물 |
| 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. |
| MX2011004225A (es) | 2008-10-21 | 2011-06-21 | Onyx Therapeutics Inc | Terapia de combinacion con epoxicetonas peptidicas. |
| 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 |
| BR112012022060A2 (pt) | 2010-03-01 | 2018-05-08 | Onyx Therapeutics Inc | composto para a inibição de imunoproteassoma |
| MX2012011298A (es) | 2010-03-31 | 2012-11-06 | Millennium Pharm Inc | Derivados del acido 1-amino-2-ciclopropiletilboronico. |
| MY188960A (en) | 2010-08-10 | 2022-01-14 | Melinta Therapeutics Llc | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US20150184246A1 (en) | 2011-11-11 | 2015-07-02 | Millennium Pharmaceuticals, Inc. | Biomarkers of response to proteasome inhibitors |
| CA2855356A1 (en) | 2011-11-11 | 2013-05-16 | Millennium Pharmaceuticals, Inc. | Biomarkers of response to proteasome inhibitors |
| KR20140114391A (ko) * | 2011-12-22 | 2014-09-26 | 아레스 트레이딩 에스.에이. | 알파-아미노 보론산 유도체, 선택적 면역프로테아좀 저해인자 |
| WO2013112601A1 (en) | 2012-01-24 | 2013-08-01 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
| WO2014011695A2 (en) | 2012-07-09 | 2014-01-16 | Onyx Therapeutics, Inc. | Prodrugs of peptide epoxy ketone protease inhibitors |
| 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 |
| MX2015008628A (es) | 2013-01-04 | 2015-09-23 | Rempex Pharmaceuticals Inc | Derivados de acido boronico y usos terapeuticos de los mismos. |
| US20160250238A1 (en) | 2013-10-03 | 2016-09-01 | Millennium Pharmaceuticals, Inc. | Method for the Prophylaxis or Treatment of Systemic Lupus Erythematosus and/or Lupus Nephritis |
| WO2015106200A2 (en) | 2014-01-10 | 2015-07-16 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
| ES2985626T3 (es) | 2014-05-05 | 2024-11-06 | Melinta Therapeutics Inc | Sales y polimorfos de derivados cíclicos de éster de ácido borónico y usos terapéuticos de los mismos |
| RS59488B1 (sr) | 2014-05-05 | 2019-12-31 | Rempex Pharmaceuticals Inc | Sinteza boronatnih soli i njihove upotrebe |
| EA201691988A1 (ru) | 2014-05-19 | 2017-06-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
| WO2015179443A1 (en) | 2014-05-20 | 2015-11-26 | Millennium Pharmaceuticals. Inc. | Boron-containing proteasome inhibitors for use after primary cancer therapy |
| CA2952968A1 (en) | 2014-07-01 | 2016-01-07 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP3808349B1 (en) | 2014-08-07 | 2022-10-05 | Mayo Foundation for Medical Education and Research | Compounds and methods for treating cancer |
| JP6758282B2 (ja) | 2014-08-18 | 2020-09-23 | コーネル・ユニバーシティーCornell University | ヒト免疫プロテアソーム阻害剤としてのジペプチド模倣薬 |
| US10662205B2 (en) | 2014-11-18 | 2020-05-26 | Qpex Biopharma, 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 |
| ES2905008T3 (es) | 2015-10-15 | 2022-04-06 | Univ Cornell | Inhibidores de proteasomas y usos de los mismos |
| PL3478693T3 (pl) | 2016-06-30 | 2021-12-13 | Qpex Biopharma, Inc. | Pochodne kwasu boronowego i ich zastosowania terapeutyczne |
| WO2018160717A1 (en) | 2017-02-28 | 2018-09-07 | Mayo Foundation For Medical Education And Research | Compounds and methods for treating cancer |
| WO2019075084A1 (en) | 2017-10-11 | 2019-04-18 | Qpex Biopharma, Inc. | BORONIC ACID DERIVATIVES AND SYNTHESIS THEREOF |
| US11203613B2 (en) | 2017-10-11 | 2021-12-21 | Cornell University | Peptidomimetic proteasome inhibitors |
| US11243207B2 (en) | 2018-03-29 | 2022-02-08 | Mayo Foundation For Medical Education And Research | Assessing and treating cancer |
| AU2019256351B2 (en) | 2018-04-20 | 2024-02-29 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
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| 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. |
| MX2012011298A (es) | 2010-03-31 | 2012-11-06 | Millennium Pharm Inc | Derivados del acido 1-amino-2-ciclopropiletilboronico. |
-
2011
- 2011-03-30 MX MX2012011298A patent/MX2012011298A/es unknown
- 2011-03-30 CN CN201610326909.5A patent/CN106008570A/zh active Pending
- 2011-03-30 AR ARP110101066A patent/AR080863A1/es unknown
- 2011-03-30 PH PH1/2012/501943A patent/PH12012501943A1/en unknown
- 2011-03-30 AU AU2011235227A patent/AU2011235227B2/en not_active Ceased
- 2011-03-30 RU RU2012146101/04A patent/RU2012146101A/ru not_active Application Discontinuation
- 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 KR KR1020127028506A patent/KR20130036228A/ko not_active Ceased
- 2011-03-30 EA EA201290980A patent/EA029521B1/ru not_active IP Right Cessation
- 2011-03-30 SG SG2012070595A patent/SG184222A1/en unknown
- 2011-03-30 CN CN2011800240565A patent/CN102892291A/zh active Pending
- 2011-03-30 UA UAA201212379A patent/UA110612C2/uk unknown
- 2011-03-30 WO PCT/US2011/030455 patent/WO2011123502A1/en not_active Ceased
- 2011-03-30 EP EP11763354.5A patent/EP2552216B1/en active Active
- 2011-03-30 JP JP2013502789A patent/JP5933523B2/ja not_active Expired - Fee Related
- 2011-03-30 CA CA2794334A patent/CA2794334C/en not_active Expired - Fee Related
- 2011-03-30 NZ NZ602622A patent/NZ602622A/en not_active IP Right Cessation
- 2011-03-30 CN CN201710639537.6A patent/CN107266485A/zh active Pending
- 2011-03-30 MA MA35323A patent/MA34169B1/fr unknown
- 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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