EA201391106A1 - Новые гетероциклические производные - Google Patents

Новые гетероциклические производные

Info

Publication number
EA201391106A1
EA201391106A1 EA201391106A EA201391106A EA201391106A1 EA 201391106 A1 EA201391106 A1 EA 201391106A1 EA 201391106 A EA201391106 A EA 201391106A EA 201391106 A EA201391106 A EA 201391106A EA 201391106 A1 EA201391106 A1 EA 201391106A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new heterocyclic
heterocyclic derivatives
new
cancer
parameters
Prior art date
Application number
EA201391106A
Other languages
English (en)
Other versions
EA025011B1 (ru
Inventor
Бранко Радетич
Бин Юй
Яни Чжу
Original Assignee
Новартис Аг
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=45607319&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201391106(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201391106A1 publication Critical patent/EA201391106A1/ru
Publication of EA025011B1 publication Critical patent/EA025011B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Изобретение относится к новым гетероциклическим соединениям формулы (I)в которой все параметры определены в описании, к их получению, к их медицинскому применению, в частности к их применению при лечении рака и нейродегенеративных расстройств, и к лекарственным средствам, содержащим их.
EA201391106A 2011-01-31 2012-01-30 ПУРИНЫ, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR КИНАЗЫ, ИХ ИСПОЛЬЗОВАНИЕ И ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ EA025011B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161437956P 2011-01-31 2011-01-31
US201161552905P 2011-10-28 2011-10-28
PCT/IB2012/050428 WO2012104776A1 (en) 2011-01-31 2012-01-30 Novel heterocyclic derivatives

Publications (2)

Publication Number Publication Date
EA201391106A1 true EA201391106A1 (ru) 2014-01-30
EA025011B1 EA025011B1 (ru) 2016-11-30

Family

ID=45607319

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391106A EA025011B1 (ru) 2011-01-31 2012-01-30 ПУРИНЫ, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR КИНАЗЫ, ИХ ИСПОЛЬЗОВАНИЕ И ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Country Status (24)

Country Link
US (2) US8987257B2 (ru)
EP (1) EP2670753B1 (ru)
JP (1) JP5963777B2 (ru)
KR (1) KR101928116B1 (ru)
CN (1) CN103476777B (ru)
AP (1) AP2013007043A0 (ru)
AR (1) AR085039A1 (ru)
AU (1) AU2012213080B2 (ru)
BR (1) BR112013019509A2 (ru)
CA (1) CA2825605C (ru)
CL (1) CL2013002177A1 (ru)
CO (1) CO6781507A2 (ru)
CR (1) CR20130369A (ru)
EA (1) EA025011B1 (ru)
ES (1) ES2611885T3 (ru)
IL (1) IL227664A0 (ru)
MX (1) MX343706B (ru)
PE (1) PE20140293A1 (ru)
PL (1) PL2670753T3 (ru)
PT (1) PT2670753T (ru)
SG (1) SG192193A1 (ru)
TW (1) TW201309700A (ru)
UY (1) UY33883A (ru)
WO (1) WO2012104776A1 (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
UY33883A (es) 2011-01-31 2012-08-31 Novartis Ag Novedosos derivados heterocíclicos
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
JP6059731B2 (ja) * 2011-10-28 2017-01-11 ノバルティス アーゲー 新規プリン誘導体および疾患の処置におけるその使用
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3056210B1 (en) * 2013-10-11 2022-05-11 National University Corporation Tokyo Medical and Dental University Drug for prevention or treatment of spinocerebellar degeneration
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
LT3122358T (lt) 2014-03-26 2021-04-12 Astex Therapeutics Ltd. Egfr ir cmet inhibitorių deriniai, skirti vėžio gydymui
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
WO2015154064A2 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US20180214452A1 (en) 2015-03-06 2018-08-02 Korea Advanced Institute Of Science And Technology COMPOSITION FOR PREVENTION OR TREATMENT OF INTRACTABLE EPILEPSY COMPRISING mTOR INHIBITOR
KR20170131444A (ko) 2015-03-30 2017-11-29 다이이찌 산쿄 가부시키가이샤 6-모르폴리닐-2-피라졸릴-9h-푸린 유도체 및 pi3k 저해제로서의 이들의 용도
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
CN108026095B (zh) 2015-09-23 2021-07-27 詹森药业有限公司 新化合物
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
US11208442B2 (en) 2016-12-02 2021-12-28 Daiichi Sankyo Company, Limited Endo-beta-N-acetylglucosaminidase
CZ308800B6 (cs) * 2019-02-12 2021-05-26 Univerzita Palackého v Olomouci Heterocyklické dusíkaté deriváty purinu, farmaceutické přípravky obsahující tyto deriváty a jejich použití při neuroprotekci
WO2021247841A1 (en) * 2020-06-03 2021-12-09 Yumanity Therapeutics, Inc. Purines and methods of their use
WO2023107552A2 (en) * 2021-12-08 2023-06-15 Kineta, Inc. Purines and methods of their use
CN115181100A (zh) * 2022-07-27 2022-10-14 广西大学 一种以嘌呤及吡咯并嘧啶母核的磺酰胺类小分子抑制剂

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB864145A (en) * 1959-06-02 1961-03-29 Thomae Gmbh Dr K Novel purines and a process for their manufacture
US3016378A (en) * 1959-07-01 1962-01-09 Thomae Gmbh Dr K Amino-substituted purine derivatives
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 １，２‐ジアミノシクロヘキサン異性体のシス白金（２）錯体
US4323581A (en) 1978-07-31 1982-04-06 Johnson & Johnson Method of treating carcinogenesis
IL73534A (en) 1983-11-18 1990-12-23 Riker Laboratories Inc 1h-imidazo(4,5-c)quinoline-4-amines,their preparation and pharmaceutical compositions containing certain such compounds
WO1988007045A1 (en) 1987-03-09 1988-09-22 Kyowa Hakko Kogyo Co., Ltd. Derivatives of physiologically active substance k-252
US4904768A (en) 1987-08-04 1990-02-27 Bristol-Myers Company Epipodophyllotoxin glucoside 4'-phosphate derivatives
EP0383919A4 (en) 1988-02-04 1992-08-05 Kyowa Hakko Kogyo Co., Ltd. Staurosporin derivatives
US5238944A (en) 1988-12-15 1993-08-24 Riker Laboratories, Inc. Topical formulations and transdermal delivery systems containing 1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
US4929624A (en) 1989-03-23 1990-05-29 Minnesota Mining And Manufacturing Company Olefinic 1H-imidazo(4,5-c)quinolin-4-amines
US5389640A (en) 1991-03-01 1995-02-14 Minnesota Mining And Manufacturing Company 1-substituted, 2-substituted 1H-imidazo[4,5-c]quinolin-4-amines
US6410010B1 (en) 1992-10-13 2002-06-25 Board Of Regents, The University Of Texas System Recombinant P53 adenovirus compositions
US5268376A (en) 1991-09-04 1993-12-07 Minnesota Mining And Manufacturing Company 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines
EP0540185A1 (en) 1991-10-10 1993-05-05 Schering Corporation 4'-(N-substituted-N-oxide)staurosporine derivatives
US5266575A (en) 1991-11-06 1993-11-30 Minnesota Mining And Manufacturing Company 2-ethyl 1H-imidazo[4,5-ciquinolin-4-amines
CA2123096A1 (en) 1991-11-08 1993-05-13 Beat J. Knusel Compositions containing k-252 compounds for potentiation of neurotrophin activity
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
US5948898A (en) 1992-03-16 1999-09-07 Isis Pharmaceuticals, Inc. Methoxyethoxy oligonucleotides for modulation of protein kinase C expression
RU2103272C1 (ru) 1992-04-03 1998-01-27 Дзе Апджон Компани Бициклические гетероциклические амины и их фармацевтически приемлемые соли, бициклические гетероциклические амины и их фармацевтически приемлемые соли в качестве ингибитора реакционноспособного кислорода
US5621100A (en) 1992-07-24 1997-04-15 Cephalon, Inc. K-252a derivatives for treatment of neurological disorders
US5756494A (en) 1992-07-24 1998-05-26 Cephalon, Inc. Protein kinase inhibitors for treatment of neurological disorders
ES2225824T3 (es) 1992-08-31 2005-03-16 Ludwig Institute For Cancer Research Nonapeptido aislado derivado del gen mage-3 y presentado por hla-a1, y sus usos.
EP0630898B1 (en) 1992-09-21 2001-11-28 Kyowa Hakko Kogyo Co., Ltd. Thrombocytopenia remedy
DE69233803D1 (de) 1992-10-28 2011-03-31 Genentech Inc Verwendung von vaskulären Endothelwachstumsfaktor-Antagonisten
US5395937A (en) 1993-01-29 1995-03-07 Minnesota Mining And Manufacturing Company Process for preparing quinoline amines
US5352784A (en) 1993-07-15 1994-10-04 Minnesota Mining And Manufacturing Company Fused cycloalkylimidazopyridines
DE69425661T2 (de) 1993-07-15 2001-04-19 Minnesota Mining & Mfg IMIDAZO [4,5-c]PYRIDIN-4-AMINE
US5478932A (en) 1993-12-02 1995-12-26 The Board Of Trustees Of The University Of Illinois Ecteinascidins
EP1449529B1 (en) 1993-12-23 2010-01-27 Eli Lilly And Company Protein Kinase C Inhibitors
US5587459A (en) 1994-08-19 1996-12-24 Regents Of The University Of Minnesota Immunoconjugates comprising tyrosine kinase inhibitors
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5482936A (en) 1995-01-12 1996-01-09 Minnesota Mining And Manufacturing Company Imidazo[4,5-C]quinoline amines
CA2216796C (en) 1995-03-30 2003-09-02 Pfizer Inc. Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
WO1997007081A2 (en) 1995-08-11 1997-02-27 Yale University Glycosylated indolocarbazole synthesis
FR2741881B1 (fr) 1995-12-01 1999-07-30 Centre Nat Rech Scient Nouveaux derives de purine possedant notamment des prorietes anti-proliferatives et leurs applications biologiques
IL123568A (en) 1995-12-08 2001-08-08 Janssen Pharmaceutica Nv History (Imidazole - 5Il) Methyl-2-quinolinone inhibitors of Prenzyl transferase, their preparation, pharmaceutical preparations containing them and their preparation and drugs containing them
KR100447918B1 (ko) 1996-07-25 2005-09-28 동아제약주식회사 대장을포함한위장관보호작용을갖는플라본및플라바논화합물
WO1998005769A2 (en) 1996-08-02 1998-02-12 Genesense Technologies, Inc. Antitumor antisense sequences directed against r1 and r2 components of ribonucleotide reductase
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6126965A (en) 1997-03-21 2000-10-03 Georgetown University School Of Medicine Liposomes containing oligonucleotides
WO1999002162A1 (en) 1997-07-12 1999-01-21 Cancer Research Campaign Technology Limited Cyclin dependent kinase inhibiting purine derivatives
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
CN1250526C (zh) 1998-05-29 2006-04-12 苏根公司 吡咯取代的2－吲哚满酮蛋白激酶抑制剂
US20030083242A1 (en) 1998-11-06 2003-05-01 Alphonse Galdes Methods and compositions for treating or preventing peripheral neuropathies
EP1189641B1 (en) 1999-06-25 2009-07-29 Genentech, Inc. HUMANIZED ANTI-ErbB2 ANTIBODIES AND TREATMENT WITH ANTI-ErbB2 ANTIBODIES
WO2001004125A1 (fr) 1999-07-13 2001-01-18 Kyowa Hakko Kogyo Co., Ltd. Derives de staurosporine
KR100881105B1 (ko) 1999-11-05 2009-02-02 아스트라제네카 아베 Ｖｅｇｆ 억제제로서의 퀴나졸린 유도체
WO2001060814A2 (en) 2000-02-15 2001-08-23 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
JP2003531148A (ja) 2000-04-12 2003-10-21 ジェネーラ・コーポレーション 保護されていない７−α−ヒドロキシ基を有する中間体を使用する、７−α−ヒドロキシ３−アミノ置換ステロイドの調製のためのプロセス
HU229624B1 (en) 2000-06-30 2014-03-28 Glaxo Group Ltd Quinazoline ditosylate salt compounds
AP1666A (en) 2000-09-11 2006-09-29 Chiron Corp Quinolinone derivatives as tyrosine kinase inhibitors.
US6677450B2 (en) 2000-10-06 2004-01-13 Bristol-Myers Squibb Company Topoisomerase inhibitors
CA2434802C (en) 2001-01-16 2013-05-28 Regeneron Pharmaceuticals, Inc. Isolating cells expressing secreted proteins
WO2002062826A1 (fr) 2001-02-07 2002-08-15 Vadim Viktorovich Novikov Procede de fabrication des peptides
US20040186172A1 (en) 2001-07-02 2004-09-23 Houssam Ibrahim Oxaliplatin active substance with a very low content of oxalic acid
KR100484504B1 (ko) 2001-09-18 2005-04-20 학교법인 포항공과대학교 쿠커비투릴 유도체를 주인 분자로서 포함하고 있는 내포화합물 및 이를 포함한 약제학적 조성물
US20030134846A1 (en) 2001-10-09 2003-07-17 Schering Corporation Treatment of trypanosoma brucei with farnesyl protein transferase inhibitors
US6927036B2 (en) 2002-02-19 2005-08-09 Xero Port, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
ES2336094T3 (es) 2002-03-29 2010-04-08 Novartis Vaccines And Diagnostics, Inc. Benzazoles sustituidos y uso de los mismos como inhibidores de quinasa raf.
US6727272B1 (en) 2002-07-15 2004-04-27 Unitech Pharmaceuticals, Inc. Leflunomide analogs for treating rheumatoid arthritis
US7148342B2 (en) 2002-07-24 2006-12-12 The Trustees Of The University Of Pennyslvania Compositions and methods for sirna inhibition of angiogenesis
US7521062B2 (en) 2002-12-27 2009-04-21 Novartis Vaccines & Diagnostics, Inc. Thiosemicarbazones as anti-virals and immunopotentiators
ES2391770T3 (es) 2003-01-21 2012-11-29 Novartis Vaccines And Diagnostics, Inc. Uso de compuestos de triptantrina para la potenciación inmune
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
ES2423800T3 (es) 2003-03-28 2013-09-24 Novartis Vaccines And Diagnostics, Inc. Uso de compuestos orgánicos para la inmunopotenciación
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2010002954A1 (en) 2008-07-02 2010-01-07 Wyeth (2-aryl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2350029A1 (en) 2008-10-15 2011-08-03 Gilead Sciences, Inc. 3-hydroquinazolin-4-one derivatives for use as stearoyl coa desaturase inhibitors
ES2539478T3 (es) * 2008-11-11 2015-07-01 Xcovery Holding Company Llc Inhibidores de PI3K/mTOR cinasa
PL2470546T3 (pl) 2009-08-28 2013-12-31 Takeda Pharmaceuticals Co Związki heksahydrooksazynopterydynowe do zastosowania jako inhibitory MTOR
CN102712642B (zh) 2009-11-12 2015-08-12 霍夫曼-拉罗奇有限公司 N-7取代的嘌呤和吡唑并嘧啶化合物、组合物和使用方法
RU2607635C2 (ru) 2009-11-12 2017-01-10 Ф.Хоффманн-Ля Рош Аг N-9-замещенные пуриновые соединения, композиции и способы применения
WO2011078795A1 (en) 2009-12-21 2011-06-30 S*Bio Pte Ltd Bridged morpholino substituted purines
AR083267A1 (es) 2010-10-04 2013-02-13 Novartis Ag Combinaciones farmaceuticas
UY33883A (es) 2011-01-31 2012-08-31 Novartis Ag Novedosos derivados heterocíclicos
TWI472781B (zh) 2011-07-22 2015-02-11 Nvidia Corp 元件分析的系統與方法
JP6059731B2 (ja) 2011-10-28 2017-01-11 ノバルティス アーゲー 新規プリン誘導体および疾患の処置におけるその使用

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MX343706B (es) 2016-11-18
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