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 (25)
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) |
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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DK2623113T3 (en) | 2005-11-09 | 2017-07-17 | Onyx Therapeutics Inc | Enzyme inhibition compound |
US7691852B2 (en) | 2006-06-19 | 2010-04-06 | Onyx Therapeutics, Inc. | Compounds for enzyme inhibition |
DK2207791T4 (da) | 2007-10-04 | 2019-10-07 | Onyx Therapeutics Inc | Krystallinske peptidepoxyketon-proteasehæmmere og syntese af aminosyreketoepoxider |
SG194349A1 (en) | 2008-06-17 | 2013-11-29 | Millennium Pharm Inc | Boronate ester compounds and pharmaceutical compositions thereof |
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. |
ES2617560T3 (es) | 2008-10-21 | 2017-06-19 | Onyx Therapeutics, Inc. | Combinación del inhibidor del proteasoma de epoxicetona peptídica carfilzomib con melfalán para su uso en el tratamiento del mieloma múltiple |
TWI504598B (zh) | 2009-03-20 | 2015-10-21 | Onyx Therapeutics Inc | 結晶性三肽環氧酮蛋白酶抑制劑 |
EP2498793B1 (en) | 2009-11-13 | 2019-07-10 | Onyx Therapeutics, Inc. | Oprozomib for use in metastasis suppression |
MA34133B1 (fr) | 2010-03-01 | 2013-04-03 | Onyx Therapeutics Inc | Composes pour inhibiteurs de l'immunoproteasome |
NZ602622A (en) | 2010-03-31 | 2015-01-30 | Millennium Pharm Inc | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
ES2691468T3 (es) | 2010-08-10 | 2018-11-27 | Rempex Pharmaceuticals, Inc. | Derivados de éster del ácido borónico cíclicos y usos terapéuticos de los mismos |
EP2776586B1 (en) | 2011-11-11 | 2018-03-07 | 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 |
SG10201605152SA (en) * | 2011-12-22 | 2016-08-30 | Ares Trading Sa | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors |
WO2013112601A1 (en) | 2012-01-24 | 2013-08-01 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
EP2869820A4 (en) | 2012-07-09 | 2016-02-17 | Onyx Therapeutics Inc | PRODRUGS OF PEPTIDEPOXIDE 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 |
JP2016509594A (ja) | 2013-01-04 | 2016-03-31 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | ボロン酸誘導体及びその治療的使用 |
CN105705149A (zh) | 2013-10-03 | 2016-06-22 | 米伦纽姆医药公司 | 用于预防或治疗系统性红斑狼疮和/或狼疮性肾炎的方法 |
USRE49816E1 (en) | 2014-01-10 | 2024-01-30 | Cornell University | Dipeptides as inhibitors of human immunoproteasomes |
EP3139930A4 (en) | 2014-05-05 | 2018-01-17 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
DK3140310T3 (da) | 2014-05-05 | 2019-10-21 | Rempex Pharmaceuticals Inc | Syntese af boronatsalte og brug deraf |
EP3145936B1 (en) | 2014-05-19 | 2020-09-30 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
JP2017524652A (ja) | 2014-05-20 | 2017-08-31 | 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. | 一次癌療法後に使用するためのホウ素含有プロテアソーム阻害剤 |
EP3164406A4 (en) * | 2014-07-01 | 2018-04-04 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
EP4180041A1 (en) | 2014-08-07 | 2023-05-17 | 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 |
EP3362754B1 (en) | 2015-10-15 | 2021-12-22 | Cornell University | Proteasome inhibitors and uses thereof |
ES2894251T3 (es) | 2016-06-30 | 2022-02-14 | Qpex Biopharma Inc | Derivados de ácido borónico y usos terapéuticos de los mismos |
EP3589659A4 (en) | 2017-02-28 | 2021-03-24 | Mayo Foundation for Medical Education and Research | CANCER TREATMENT COMPOUNDS AND METHODS |
JP7377545B2 (ja) | 2017-10-11 | 2023-11-10 | キューペックス バイオファーマ, インコーポレイテッド | ボロン酸誘導体およびその合成 |
WO2019075252A1 (en) | 2017-10-11 | 2019-04-18 | Cornell University | PEPTIDOMIMETIC INHIBITORS OF PROTEASOME |
US11243207B2 (en) | 2018-03-29 | 2022-02-08 | Mayo Foundation For Medical Education And Research | Assessing and treating cancer |
CN112424209A (zh) | 2018-04-20 | 2021-02-26 | Qpex生物制药有限公司 | 硼酸衍生物及其治疗用途 |
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SG194349A1 (en) * | 2008-06-17 | 2013-11-29 | Millennium Pharm Inc | Boronate ester compounds and pharmaceutical compositions thereof |
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. |
NZ602622A (en) | 2010-03-31 | 2015-01-30 | Millennium Pharm Inc | Derivatives of 1-amino-2-cyclopropylethylboronic acid |
-
2011
- 2011-03-30 NZ NZ602622A patent/NZ602622A/en not_active IP Right Cessation
- 2011-03-30 SG SG2012070595A patent/SG184222A1/en unknown
- 2011-03-30 CA CA2794334A patent/CA2794334C/en not_active Expired - Fee Related
- 2011-03-30 PE PE2012001810A patent/PE20130383A1/es not_active Application Discontinuation
- 2011-03-30 WO PCT/US2011/030455 patent/WO2011123502A1/en active Application Filing
- 2011-03-30 UA UAA201212379A patent/UA110612C2/uk unknown
- 2011-03-30 JP JP2013502789A patent/JP5933523B2/ja not_active Expired - Fee Related
- 2011-03-30 KR KR1020127028506A patent/KR20130036228A/ko not_active Application Discontinuation
- 2011-03-30 MA MA35323A patent/MA34169B1/fr unknown
- 2011-03-30 US US13/075,306 patent/US8513218B2/en not_active Expired - Fee Related
- 2011-03-30 MX MX2012011298A patent/MX2012011298A/es unknown
- 2011-03-30 EP EP11763354.5A patent/EP2552216B1/en active Active
- 2011-03-30 CN CN201610326909.5A patent/CN106008570A/zh active Pending
- 2011-03-30 EA EA201290980A patent/EA029521B1/ru not_active IP Right Cessation
- 2011-03-30 AU AU2011235227A patent/AU2011235227B2/en not_active Ceased
- 2011-03-30 CN CN2011800240565A patent/CN102892291A/zh active Pending
- 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 AR ARP110101066A patent/AR080863A1/es 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 DO DO2012000257A patent/DOP2012000257A/es unknown
- 2012-09-28 CL CL2012002733A patent/CL2012002733A1/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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