PE20160113A1 - Procesos de fabricacion y formas cristalinas de un inhibidor de mdm2 - Google Patents

Procesos de fabricacion y formas cristalinas de un inhibidor de mdm2

Info

Publication number
PE20160113A1
PE20160113A1 PE2015002561A PE2015002561A PE20160113A1 PE 20160113 A1 PE20160113 A1 PE 20160113A1 PE 2015002561 A PE2015002561 A PE 2015002561A PE 2015002561 A PE2015002561 A PE 2015002561A PE 20160113 A1 PE20160113 A1 PE 20160113A1
Authority
PE
Peru
Prior art keywords
manufacturing processes
crystal forms
mdm2 inhibitor
chlorophenyl
intermediates
Prior art date
Application number
PE2015002561A
Other languages
English (en)
Inventor
Matthew Bio
Sebastien Caille
Brian Cochran
Yuanqing Fang
Sarah Wortman
Brian S Lucas
Lawrence R Mcgee
Filisaty Vounatsos
Sean Wiedemann
Brian M Fox
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51063849&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20160113(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of PE20160113A1 publication Critical patent/PE20160113A1/es

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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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/45—Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/25—Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C313/00—Sulfinic acids; Sulfenic acids; Halides, esters or anhydrides thereof; Amides of sulfinic or sulfenic acids, i.e. compounds having singly-bound oxygen atoms of sulfinic or sulfenic groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C313/02—Sulfinic acids; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Epoxy Compounds (AREA)

Abstract

La presente invencion proporciona procesos para fabricar acido 2-((3R, 5R, 6S)-5-(3-clorofenil)-6-(4-clorofenil)-1-((S)-1-(isipropilsulfonil)-3-metilbutan-2-il)-3-metil-2-oxopiperidin-3-il) acetico de formula (I), asi como intermediarios y procesos para fabricar los intermediarios. Tambien se proporcionan formas cristalinas del compuesto y los intermediarios. Conocido tambien como: {(3R, 5R, 6S)-5-(3-clorofenil)-6-(4-clorofenil)-1-[(2S)-1-(isopropilsulfonil)-3-metil-2-butani]-3-metil-2-oxo-3-piperidinil} acetico acido
PE2015002561A 2013-06-10 2014-06-09 Procesos de fabricacion y formas cristalinas de un inhibidor de mdm2 PE20160113A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361833196P 2013-06-10 2013-06-10

Publications (1)

Publication Number Publication Date
PE20160113A1 true PE20160113A1 (es) 2016-03-03

Family

ID=51063849

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PE2015002561A PE20160113A1 (es) 2013-06-10 2014-06-09 Procesos de fabricacion y formas cristalinas de un inhibidor de mdm2
PE2020000392A PE20210153A1 (es) 2013-06-10 2014-06-09 Procesos de fabricacion y formas cristalinas de un inhibidor de mdm2

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Country Status (37)

Country Link
US (10) US9376386B2 (es)
EP (2) EP3805232A1 (es)
JP (4) JP6998655B2 (es)
KR (3) KR20160018576A (es)
CN (3) CN105358530A (es)
AP (1) AP2015008891A0 (es)
AR (2) AR096582A1 (es)
AU (4) AU2014278428B2 (es)
BR (2) BR122020003153B1 (es)
CA (4) CA3200532A1 (es)
CL (3) CL2015003589A1 (es)
CR (2) CR20210290A (es)
CY (1) CY1123661T1 (es)
DK (1) DK3008039T3 (es)
EA (3) EA202091612A1 (es)
ES (1) ES2851023T3 (es)
HR (1) HRP20202065T1 (es)
HU (1) HUE053047T2 (es)
IL (4) IL297860A (es)
JO (2) JOP20200296A1 (es)
LT (1) LT3008039T (es)
MA (3) MA53572A1 (es)
MX (2) MX2015016856A (es)
MY (1) MY194848A (es)
NZ (1) NZ714821A (es)
PE (2) PE20160113A1 (es)
PH (1) PH12015502705B1 (es)
PL (1) PL3008039T3 (es)
PT (1) PT3008039T (es)
RS (1) RS61192B1 (es)
SG (2) SG11201509896VA (es)
SI (1) SI3008039T1 (es)
TN (1) TN2015000521A1 (es)
TW (3) TWI649306B (es)
UA (1) UA121301C2 (es)
UY (1) UY35605A (es)
WO (1) WO2014200937A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
CA2850166C (en) 2011-09-27 2019-12-03 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
WO2014151863A1 (en) 2013-03-14 2014-09-25 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
DK3068393T5 (da) 2013-11-11 2022-08-22 Amgen Inc Kombinationsterapi som inkluderer en mdm2-inhibitor og et eller flere yderligere farmaceutisk aktive midler til behandlingen af kræftformer
PL3458101T3 (pl) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Koniugaty PROTAC-przeciwciało i sposoby ich stosowania
CA3098606A1 (en) * 2018-04-30 2019-11-07 Kartos Therapeutics, Inc. Methods of treating cancer
WO2019224803A2 (en) * 2018-05-25 2019-11-28 Kartos Therapeutics, Inc. Methods of treating myeloproliferative neoplasms
SG11202101886VA (en) * 2018-08-31 2021-03-30 Amgen Inc Processes for preparing a mdm2 inhibitor
CN110963958A (zh) * 2018-09-30 2020-04-07 上海长森药业有限公司 一种mdm2抑制剂，及其制备方法、药物组合物和应用
GB201919219D0 (en) 2019-12-23 2020-02-05 Otsuka Pharma Co Ltd Cancer biomarkers
US20230272001A1 (en) * 2020-05-22 2023-08-31 Merck Sharp & Dohme Llc Novel processes for preparing conjugates of the il-2 protein
EP4204812A2 (en) 2020-08-27 2023-07-05 Otsuka Pharmaceutical Co., Ltd. Biomarkers for cancer therapy using mdm2 antagonists
GB202103080D0 (en) 2021-03-04 2021-04-21 Otsuka Pharma Co Ltd Cancer biomarkers
CA3227793A1 (en) * 2021-08-05 2023-02-09 Yong Moon Choi Phenylcarbamate crystalline form and method for manufacturing the same
WO2023039161A1 (en) * 2021-09-09 2023-03-16 Kartos Therapeutics Methods of treating cancer dependent on myc gene expresssion
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483213A (en) * 1947-06-14 1949-09-27 American Cyanamid Co Alpha naphthalene sulfonic anhydride
GB1016828A (en) 1961-11-13 1966-01-12 Mcneilab Inc Substituted morpholines and process for preparing same
US3518236A (en) * 1967-07-20 1970-06-30 Uniroyal Inc Acceleration of sulfur-vulcanization of rubber with sulfinic acids and derivatives
DE3246148A1 (de) 1982-12-14 1984-06-14 Troponwerke GmbH & Co KG, 5000 Köln Pyrazolo(4.3-b)(1.4)oxazine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
JP2604472B2 (ja) 1989-07-12 1997-04-30 株式会社クラレ 重合性組成物
WO1995023135A1 (en) 1991-03-07 1995-08-31 Fisons Corporation Diphenyl-2-piperidinone and -2-pyrrolidinone derivatives having anti-convulsant and neuroprotective activity
US5334720A (en) 1991-03-07 1994-08-02 Fisons Corporation Diphenyl-1-(aminoalkyl)-2-piperidinone and -2-pyrrolidinone derivatives having anticonvulsant properties
WO1996006095A1 (en) 1994-08-19 1996-02-29 Abbott Laboratories Endothelin antagonists
NZ330818A (en) 1996-02-13 2000-05-26 Abbott Lab Benzo-1, 3-dioxolyl- and benzofuranyl substituted pyrrolidine derivatives as endothelin antagonists
US6159990A (en) 1997-06-18 2000-12-12 Synaptic Pharmaceutical Corporation Oxazolidinones as α1A receptor antagonists
EP1003740A2 (en) 1997-08-04 2000-05-31 Abbott Laboratories Pyrrolidine-3-carboxylic acid derivatives and their use as endothelin antagoists
AU1910299A (en) 1997-12-18 1999-07-05 Eli Lilly And Company Peptidomimetic template-based combinatorial libraries
US6770658B2 (en) 1998-09-09 2004-08-03 Inflazyme Pharmaceuticals Ltd. Substituted γ-phenyl-Δ-lactams and uses related thereto
US7214540B2 (en) * 1999-04-06 2007-05-08 Uab Research Foundation Method for screening crystallization conditions in solution crystal growth
US6630006B2 (en) * 1999-06-18 2003-10-07 The Regents Of The University Of California Method for screening microcrystallizations for crystal formation
US7052545B2 (en) * 2001-04-06 2006-05-30 California Institute Of Technology High throughput screening of crystallization of materials
US7195670B2 (en) * 2000-06-27 2007-03-27 California Institute Of Technology High throughput screening of crystallization of materials
DE19951418A1 (de) * 1999-10-26 2001-05-03 Merck Patent Gmbh Verfahren zur Herstellung von N-(4,5-Bismethansulfonyl-2-methyl-benzoyl) -guanidin, Hydrochlorid
WO2002017912A1 (en) 2000-08-31 2002-03-07 Abbott Laboratories Endothelin antagonists
US7229500B2 (en) * 2000-11-20 2007-06-12 Parallel Synthesis Technologies, Inc. Methods and devices for high throughput crystallization
CA2436774A1 (en) 2001-01-30 2002-08-08 R. Michael Lawrence Sulfonamide lactam inhibitors of factor xa
AU2002305450A1 (en) 2001-05-08 2002-11-18 Yale University Proteomimetic compounds and methods
EP1395560A1 (en) 2001-05-23 2004-03-10 Ucb, S.A. 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivativ es for the treatment of epilepsy and other neurological disorders
JP4477351B2 (ja) 2001-12-18 2010-06-09 エフ．ホフマン−ラ ロシュ アーゲー シス−２，４，５−トリフェニル−イミダゾリン類及び腫瘍の処理へのそれらの使用
US6860940B2 (en) * 2002-02-11 2005-03-01 The Regents Of The University Of California Automated macromolecular crystallization screening
US6916833B2 (en) * 2003-03-13 2005-07-12 Hoffmann-La Roche Inc. Substituted piperidines
US7425638B2 (en) 2003-06-17 2008-09-16 Hoffmann-La Roche Inc. Cis-imidazolines
ATE414693T1 (de) 2004-05-18 2008-12-15 Hoffmann La Roche Neuartige cis-imidazoline
US7893278B2 (en) 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines
JP2007297283A (ja) * 2004-07-28 2007-11-15 Santen Pharmaceut Co Ltd 新規桂皮酸関連化合物
US7354944B2 (en) 2004-10-18 2008-04-08 Amgen Inc. Thiadiazole compounds and methods of use
EP2602259A3 (en) 2005-02-18 2014-09-10 Mitsubishi Tanabe Pharma Corporation Salt of proline derivative, solvate thereof, and production method thereof
MX2007011151A (es) 2005-03-16 2007-10-17 Hoffmann La Roche Cis-2,4,5-triaril-imidazolinas y su uso como medicamentos anticancer.
RS51822B (en) 2005-04-04 2012-02-29 Eisai R. &D. Management Co. Ltd. DIHYDROPYRIDINE COMPOUNDS FOR TREATMENT OF NEURODEGENERATIVE DISEASES AND Dementia
MX2007015511A (es) * 2005-06-07 2008-03-06 Univ Ramot Sales novedosas de farmacos sicotropicos conjugados y procesos para prepararlas.
WO2007015929A2 (en) * 2005-07-27 2007-02-08 University Of Toledo Epothilone analogues
EP2130822A1 (en) 2005-12-01 2009-12-09 F. Hoffmann-La Roche AG 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between p53 and mdm2 proteins for use as anticancer agents
CA2636077C (en) 2006-01-18 2012-01-03 Amgen Inc. Thiazole compounds as protein kinase b (pkb) inhibitors
US20070213341A1 (en) 2006-03-13 2007-09-13 Li Chen Spiroindolinone derivatives
CN101595107A (zh) 2006-06-30 2009-12-02 先灵公司 能提高p53活性的有取代哌啶及其用途
MX2009000661A (es) 2006-07-19 2009-03-27 Univ Georgia Res Found Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion.
WO2008021338A2 (en) 2006-08-15 2008-02-21 Wyeth Tricyclic oxazolidone derivatives useful as pr modulators
WO2008021339A2 (en) 2006-08-15 2008-02-21 Wyeth Pyrrolidine and related derivatives useful as pr modulators
TW200831080A (en) 2006-12-15 2008-08-01 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
GB0722769D0 (en) 2007-11-21 2008-01-02 Biolipox Ab New compounds
ES2446417T3 (es) 2007-03-23 2014-03-07 Amgen Inc. Derivados de quinolina o quinoxalina sustituidos en 3 y su uso como inhibidores de fosfatidilinositol 3-cinasa (PI3K)
MX2009009968A (es) 2007-03-23 2009-10-08 Amgen Inc Compuestos heterociclicos y sus usos.
WO2008118454A2 (en) 2007-03-23 2008-10-02 Amgen Inc. Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer
US7625895B2 (en) 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
WO2008130614A2 (en) 2007-04-20 2008-10-30 University Of Pittsburg-Of The Commonwealth System Of Higher Education Selective and dual-action p53/mdm2/mdm4 antagonists
US7834179B2 (en) 2007-05-23 2010-11-16 Hoffmann-La Roche Inc. Spiroindolinone derivatives
WO2009004430A1 (en) 2007-06-29 2009-01-08 Pfizer Inc. N-benzyl oxazolidinones and related heterocycleic compounds as potentiators of glutamate receptors
BRPI0814688A2 (pt) 2007-07-09 2017-06-06 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito antiproliferativo em um animal de sangue quente, e para tratar doenças, e, composição farmacêutica
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
WO2009011871A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
TW200911798A (en) 2007-08-02 2009-03-16 Amgen Inc PI3 kinase modulators and methods of use
CN104710408A (zh) 2007-10-09 2015-06-17 霍夫曼-拉罗奇有限公司 手性顺式-咪唑啉类
US7776875B2 (en) 2007-12-19 2010-08-17 Hoffman-La Roche Inc. Spiroindolinone derivatives
JP5520831B2 (ja) 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
JP2011507799A (ja) 2007-12-26 2011-03-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 癲癇のためのａｍｐａ受容体アンタゴニストおよびゾニサミド
CA2718959A1 (en) 2008-03-21 2009-09-24 Chlorion Pharma, Inc. Substituted pyrrolidine and piperidine compounds, derivatives thereof, and methods for treating pain
JP5599783B2 (ja) 2008-05-30 2014-10-01 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
WO2010030704A2 (en) * 2008-09-10 2010-03-18 Achaogen, Inc. Antibacterial aminoglycoside analogs
TW201011009A (en) 2008-09-15 2010-03-16 Priaxon Ag Novel pyrrolidin-2-ones
KR101380013B1 (ko) 2008-09-18 2014-04-10 에프. 호프만-라 로슈 아게 치환 피롤리딘-2-카르복사미드
WO2010083246A1 (en) 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
AU2010216239B2 (en) 2009-02-18 2012-06-14 Amgen Inc. Indole/benzimidazole compounds as mTOR kinase inhibitors
WO2010108074A2 (en) 2009-03-20 2010-09-23 Amgen Inc. Inhibitors of pi3 kinase
US8076482B2 (en) 2009-04-23 2011-12-13 Hoffmann-La Roche Inc. 3,3′-spiroindolinone derivatives
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
MX2011012037A (es) 2009-05-13 2012-02-28 Amgen Inc Compuestos de heteroarilo como inhibidores de pikk.
EP2445902A2 (en) 2009-06-25 2012-05-02 Amgen, Inc Heterocyclic compounds and their uses as inhibitors of pi3k activity
WO2010151740A2 (en) 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
BR112012000660A2 (pt) 2009-06-25 2016-11-16 Amgen Inc compostos heterociclos e seus usos
JP2012531435A (ja) 2009-06-25 2012-12-10 アムジエン・インコーポレーテツド ＰＩ３Ｋ阻害剤としての４Ｈ−ピリド［１，２−ａ］ピリミジン−４−オン誘導体
US20120149661A1 (en) 2009-08-26 2012-06-14 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
CN102596981A (zh) * 2009-10-09 2012-07-18 尔察祯有限公司 抗菌氨基糖苷类类似物
US8088815B2 (en) 2009-12-02 2012-01-03 Hoffman-La Roche Inc. Spiroindolinone pyrrolidines
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
JP2013519980A (ja) * 2010-02-10 2013-05-30 モチイ，インコーポレイテッド（ディービーエー ヴォクサ） 収差補正暗視野電子顕微鏡
IT1399923B1 (it) * 2010-05-11 2013-05-09 Cbb Net S A Procedimento di preparazione di sali dell'acido (r) alfa-lipoico loro formulazione ed uso nelle composizioni farmaceutiche in forma di compresse che li contengono
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
CN103648499B (zh) * 2011-01-10 2017-02-15 无限药品股份有限公司 用于制备异喹啉酮的方法及异喹啉酮的固体形式
CN102153557B (zh) 2011-01-21 2013-03-20 中国科学院上海有机化学研究所 具有乙二胺骨架的多手性中心氮杂环卡宾前体盐、合成方法及用途
TW201311938A (zh) * 2011-04-28 2013-03-16 Otsuka Chemical Co Ltd 偶氮二甲醯胺之新穎製造法
TW201309651A (zh) * 2011-06-29 2013-03-01 Otsuka Pharma Co Ltd 阿立哌唑（ａｒｉｐｉｐｒａｚｏｌｅ）無水物Ｂ形結晶微粒子之製造方法
CA2850166C (en) 2011-09-27 2019-12-03 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
CN103373951B (zh) * 2012-04-28 2016-03-09 上海医药工业研究院 一种拉帕替尼中间体的制备方法
MX362896B (es) 2013-02-19 2019-02-22 Amgen Inc Cis-morfolinona y otros compuestos como inhibidores de mdm2 para el tratamiento del cáncer.
MX368703B (es) 2013-02-28 2019-10-11 Amgen Inc Un inhibidor de mdm2 derivado de acido benzoico para el tratamiento del cancer.
WO2014151863A1 (en) 2013-03-14 2014-09-25 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط

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