CA2093203A1 - Pyrimidine derivatives and processes for the preparation thereof - Google Patents

Pyrimidine derivatives and processes for the preparation thereof

Info

Publication number
CA2093203A1
CA2093203A1 CA002093203A CA2093203A CA2093203A1 CA 2093203 A1 CA2093203 A1 CA 2093203A1 CA 002093203 A CA002093203 A CA 002093203A CA 2093203 A CA2093203 A CA 2093203A CA 2093203 A1 CA2093203 A1 CA 2093203A1
Authority
CA
Canada
Prior art keywords
lower alkyl
free
amino
substituted
aliphatic
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002093203A
Other languages
French (fr)
Other versions
CA2093203C (en
Inventor
Jurg Zimmermann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Ciba Geigy AG
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=4202064&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2093203(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ciba Geigy AG filed Critical Ciba Geigy AG
Publication of CA2093203A1 publication Critical patent/CA2093203A1/en
Application granted granted Critical
Publication of CA2093203C publication Critical patent/CA2093203C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Macromonomer-Based Addition Polymer (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Paints Or Removers (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

There are described N-phenyl-2-pyrimidine-amine derivatives of formula I
wherein R1 is pyrazinyl, 1-methyl-1H pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each cast is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstitut ed or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2 and R3 are each independently of the other hydrogen or lower alkyl, one or two of the radicals R4, R5, R6, R7 and R8 are each nitro, fluoro-substituted lower alkoxy or a radical of formula II
-N(R9)-C(=X)-(Y)n-R10 (II), wherein R9 is hydrogen or lower alkyl, -X is oxo, thio, imino, N-lower alkyl-imino, hydroximino or O-lower alkyl-hydrox-imino, Y is oxygen or the group NH, n is a or 1 and R10 is an aliphatic radical having at least 5 carbon atoms, or an aromatic, aromatic-aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or heterocyclic-aliphatic radical, and the remaining radicals R4, R5, R6, R7 and R8 are each independently of the others hydrogen, lower alkyl that is unsubstituted or substituted by free or alkylated amino, piperazinyl, piperidinyl, pyrrolidinyl or by morpholinyl, or lower alkanoyl, trifluoro-methyl, free, etherified or esterifed hydroxy, free, alkylated or acylated amino or free or esterified carboxy.
These compounds can be used, for example, in the therapy of tumoral diseases.
CA002093203A 1992-04-03 1993-04-01 Pyrimidine derivatives and processes for the preparation thereof Expired - Lifetime CA2093203C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH1083/92-1 1992-04-03
CH108392 1992-04-03

Publications (2)

Publication Number Publication Date
CA2093203A1 true CA2093203A1 (en) 1993-10-04
CA2093203C CA2093203C (en) 2002-11-26

Family

ID=4202064

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002093203A Expired - Lifetime CA2093203C (en) 1992-04-03 1993-04-01 Pyrimidine derivatives and processes for the preparation thereof

Country Status (29)

Country Link
EP (1) EP0564409B1 (en)
JP (1) JP2706682B2 (en)
KR (1) KR100261366B1 (en)
CN (1) CN1043531C (en)
AT (1) ATE188964T1 (en)
AU (1) AU666709B2 (en)
BR (1) BR1100739A (en)
CA (1) CA2093203C (en)
CY (2) CY2229B1 (en)
CZ (1) CZ283944B6 (en)
DE (2) DE10299016I2 (en)
DK (1) DK0564409T3 (en)
ES (1) ES2142857T3 (en)
FI (1) FI109534B (en)
GR (1) GR3032927T3 (en)
HU (2) HU227080B1 (en)
IL (1) IL105264A (en)
LU (1) LU90908I2 (en)
MX (1) MX9301929A (en)
NL (1) NL300086I2 (en)
NO (2) NO302473B1 (en)
NZ (1) NZ247299A (en)
PT (1) PT564409E (en)
RU (1) RU2125992C1 (en)
SA (1) SA93140441B1 (en)
SG (1) SG43859A1 (en)
SK (1) SK280620B6 (en)
TW (1) TW225528B (en)
ZA (1) ZA932397B (en)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
WO2003090720A1 (en) 2002-04-23 2003-11-06 Novartis Ag High drug load tablet
WO2012116666A1 (en) 2011-02-28 2012-09-07 USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, v.v.i. Pyrimidine compounds inhibiting the formation of nitric oxide and prostaglandin e2, method of production thereof and use thereof
US9018205B2 (en) 2007-09-04 2015-04-28 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
US10000469B2 (en) 2014-03-25 2018-06-19 Duke University Heat shock protein 70 (hsp-70) receptor ligands
US10442806B2 (en) 2012-08-06 2019-10-15 Duke University Substituted heterocycles for targeting HSP90
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90

Families Citing this family (344)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9212673D0 (en) * 1992-06-15 1992-07-29 Celltech Ltd Chemical compounds
US6171786B1 (en) 1992-09-17 2001-01-09 Board Of Trustees Of University Of Illinois Methods for preventing multidrug resistance in cancer cells
US5972598A (en) * 1992-09-17 1999-10-26 Board Of Trustess Of The University Of Illinois Methods for preventing multidrug resistance in cancer cells
GB9222253D0 (en) * 1992-10-23 1992-12-09 Celltech Ltd Chemical compounds
GB9304920D0 (en) * 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
GB9304919D0 (en) * 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
HU228172B1 (en) * 1993-10-01 2013-01-28 Novartis Ag Pharmacologically active pyridine derivatives and their preparation
WO1995009851A1 (en) * 1993-10-01 1995-04-13 Ciba-Geigy Ag Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
US5543520A (en) * 1993-10-01 1996-08-06 Ciba-Geigy Corporation Pyrimidine derivatives
JPH08503971A (en) * 1993-10-01 1996-04-30 チバ−ガイギー アクチェンゲゼルシャフト Pyrimidineamine derivatives and methods for their preparation
GB9325217D0 (en) * 1993-12-09 1994-02-09 Zeneca Ltd Pyrimidine derivatives
WO1995017399A1 (en) * 1993-12-22 1995-06-29 Celltech Therapeutics Limited Trisubstituted phenyl derivatives, processes for their preparation and their use as phosphodiesterase (type iv) inhibitors
GB9326600D0 (en) * 1993-12-22 1994-03-02 Celltech Ltd Chemical compounds
US5786354A (en) * 1994-06-21 1998-07-28 Celltech Therapeutics, Limited Tri-substituted phenyl derivatives and processes for their preparation
US6245774B1 (en) 1994-06-21 2001-06-12 Celltech Therapeutics Limited Tri-substituted phenyl or pyridine derivatives
GB9412571D0 (en) * 1994-06-22 1994-08-10 Celltech Ltd Chemical compounds
GB9412573D0 (en) 1994-06-22 1994-08-10 Celltech Ltd Chemical compounds
GB9412672D0 (en) * 1994-06-23 1994-08-10 Celltech Ltd Chemical compounds
US5756527A (en) * 1995-06-07 1998-05-26 Ontogen Corporation Imidazole derivatives useful as modulators of multi drug resistances
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9526246D0 (en) * 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
GB9526245D0 (en) * 1995-12-21 1996-02-21 Celltech Therapeutics Ltd Chemical compounds
GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
EP0812829A1 (en) * 1996-06-14 1997-12-17 Ontogen Corporation Substituted imidazoles as modulators of multi-drug resistance
EP0812830A1 (en) * 1996-06-14 1997-12-17 Ontogen Corporation Modulators of multi-drug resistances
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
GB9625184D0 (en) * 1996-12-04 1997-01-22 Celltech Therapeutics Ltd Chemical compounds
US6057329A (en) * 1996-12-23 2000-05-02 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives
GB9705361D0 (en) * 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
GB9713087D0 (en) * 1997-06-20 1997-08-27 Celltech Therapeutics Ltd Chemical compounds
CO4940418A1 (en) * 1997-07-18 2000-07-24 Novartis Ag MODIFICATION OF A CRYSTAL OF A DERIVATIVE OF N-PHENYL-2-PIRIMIDINAMINE, PROCESSES FOR ITS MANUFACTURE AND USE
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
EP1194152A4 (en) 1999-06-30 2002-11-06 Merck & Co Inc Src kinase inhibitor compounds
AU6605200A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
ATE253915T1 (en) 1999-06-30 2003-11-15 Merck & Co Inc SRC KINASE INHIBITING COMPOUNDS
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
AU779908B2 (en) 1999-09-10 2005-02-17 Merck & Co., Inc. Tyrosine kinase inhibitors
GB9924862D0 (en) 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
MXPA02007957A (en) * 2000-02-17 2002-11-29 Amgen Inc Kinase inhibitors.
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
US7030219B2 (en) 2000-04-28 2006-04-18 Johns Hopkins University B7-DC, Dendritic cell co-stimulatory molecules
EP1315715B1 (en) 2000-08-18 2008-07-23 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as kinase inhibitors
GB0022438D0 (en) 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
IL155029A0 (en) * 2000-10-27 2003-10-31 Novartis Ag Treatment of gastrointestinal stromal tumors
DE60144284D1 (en) 2000-11-01 2011-05-05 Millennium Pharm Inc NITROGENIC HETEROCYCLIC COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF
GB0103926D0 (en) * 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
PT3345602T (en) 2001-02-19 2022-07-04 Novartis Pharma Ag RAPAMICIN DERIVATIVE FOR TREATMENT OF SOLID TUMORS
SE0100569D0 (en) * 2001-02-20 2001-02-20 Astrazeneca Ab New compounds
IL157466A0 (en) * 2001-02-27 2004-03-28 Novartis Ag Novartis Ag Combination comprising a signal transduction inhibitor and an epothilone derivative
AU2002342335B2 (en) 2001-05-16 2006-02-02 Novartis Ag Combination comprising N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent
EP1395261B1 (en) * 2001-05-16 2006-06-28 GPC Biotech AG Pyridylpyrimidine derivatives as effective compounds against prion diseases
DE60232370D1 (en) 2001-06-14 2009-06-25 Univ California MUTATIONS IN RESISTANCE TO STI-
WO2003000186A2 (en) 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
ES2255621T3 (en) 2001-06-22 2006-07-01 MERCK & CO., INC. THYROSINE KINASE INHIBITORS.
ES2274075T3 (en) 2001-06-29 2007-05-16 Ab Science USE OF C-KIT INHIBITORS TO TREAT INTESTINAL INFLAMMATORY DISEASES (IBD).
ATE345839T1 (en) 2001-06-29 2006-12-15 Ab Science THE USE OF TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF ALLERGY DISEASES
WO2003003006A2 (en) * 2001-06-29 2003-01-09 Ab Science New potent, selective and non toxic c-kit inhibitors
US20040266797A1 (en) * 2001-06-29 2004-12-30 Alain Moussy Use of potent,selective and non toxic c-kit inhibitors for treating tumor angiogensis
WO2003002108A2 (en) 2001-06-29 2003-01-09 Ab Science Use of tyrosine kinase inhibitors for treating inflammatory diseases
WO2003039550A1 (en) * 2001-09-20 2003-05-15 Ab Science Use of tyrosine kinase inhibitors for whitening human skin and treating melanocyte dysfunction associated diseases
WO2003040141A1 (en) * 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
US20050202519A1 (en) 2001-10-05 2005-09-15 Christophe Barthe Mutated abl kinase domains
GB0201508D0 (en) 2002-01-23 2002-03-13 Novartis Ag Organic compounds
AU2007203463B2 (en) * 2002-02-07 2010-12-23 Novartis Pharma Ag N-phenyl-2-pyrimidine-amine derivatives
GB0202874D0 (en) * 2002-02-07 2002-03-27 Novartis Ag Organic compounds
GB0202873D0 (en) 2002-02-07 2002-03-27 Novartis Ag Organic compounds
DE60305460D1 (en) * 2002-02-22 2006-06-29 Us Government USE OF 4- (4-METHYLPIPERAZINE-1-YLMETHYL) -N 4-METHYL-3- (4-PYRIDIN-3-YL) PYRIMIDIN-2-YLAMINO) PHENYL BENZAMIDE FOR THE TREATMENT OF SEMINOMES
AU2003209933A1 (en) * 2002-02-27 2003-09-09 Ab Science Use of tyrosine kinase inhibitors for treating substance use disorders
PT1478380E (en) * 2002-02-27 2006-12-29 Ab Science Use of tyrosine kinase inhibitors for treating cns disorders
EP1480688A1 (en) * 2002-02-28 2004-12-01 Novartis AG N-(5- 4-(4-methyl-piperazino-methyl)-benzoylamido)-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine coated stents
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
AU2003231231A1 (en) * 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
EP1505959B1 (en) 2002-05-16 2008-10-29 Novartis AG Use of edg receptor binding agents in cancer
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
US20060052387A1 (en) * 2002-06-26 2006-03-09 Marsh Clay B Organic compounds
DE60329918D1 (en) * 2002-06-28 2009-12-17 Nippon Shinyaku Co Ltd amide derivative
GB0215676D0 (en) * 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US6872724B2 (en) 2002-07-24 2005-03-29 Merck & Co., Inc. Polymorphs with tyrosine kinase activity
WO2004014903A1 (en) * 2002-08-02 2004-02-19 Ab Science 2-(3-aminoaryl)amino-4-aryl-thiazoles and their use as c-kit inhibitors
GB0222514D0 (en) * 2002-09-27 2002-11-06 Novartis Ag Organic compounds
JP2006504721A (en) * 2002-10-11 2006-02-09 ノバルティス　アクチエンゲゼルシャフト Use of Imatinib (Gleevec, STI-571) to inhibit breast cancer resistance protein (BCRP) -mediated resistance to therapeutic agents
GB0224455D0 (en) * 2002-10-21 2002-11-27 Novartis Ag Organic compounds
US7094785B1 (en) 2002-12-18 2006-08-22 Cornell Research Foundation, Inc. Method of treating polycythemia vera
US7144911B2 (en) * 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
GB2398565A (en) * 2003-02-18 2004-08-25 Cipla Ltd Imatinib preparation and salts
JP2006513791A (en) * 2003-04-04 2006-04-27 ベイコ テック リミテッド Vascular stent
AU2003232650A1 (en) 2003-05-06 2004-11-26 Il Yang Pharm Co., Ltd. N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
JP4944613B2 (en) 2003-05-19 2012-06-06 アイアールエム・リミテッド・ライアビリティ・カンパニー Immunosuppressive compounds and compositions
PL1631291T3 (en) * 2003-05-27 2010-04-30 Haegerkvist Robert P Use of tyrosine kinase inhibitors to treat diabetes
PT1635835E (en) * 2003-06-13 2010-03-17 Novartis Ag 2-aminopyrimidine derivatives as raf kinase inhibitors
DK1660057T3 (en) 2003-08-27 2012-08-20 Ophthotech Corp Combination therapy for the treatment of neovascular eye disorders
JP4762150B2 (en) 2003-11-18 2011-08-31 ノバルティス アーゲー KIT mutant inhibitors
AU2004309248B2 (en) * 2003-12-25 2009-11-05 Nippon Shinyaku Co., Ltd. Amide derivative and medicine
WO2005072826A2 (en) 2004-01-21 2005-08-11 Emory University Compositions and use of tyrosine kinase inhibitors to treat pathogenic infection
PE20051096A1 (en) 2004-02-04 2006-01-23 Novartis Ag SALT FORMS OF 4- (4-METHYLPIPERAZIN-1-ILMETHYL) -N- [4-METHYL-3- (4-PYRIDIN-3-IL) PYRIMIDIN-2-ILAMINO) PHENYL] -BENZAMIDE
HUE028884T2 (en) 2004-02-11 2017-01-30 Natco Pharma Ltd Novel polymorphic form of imatinib mesylate and a process for its preparation
CN1309719C (en) * 2004-02-18 2007-04-11 陈国庆 Derivative of phenylamide pyrimidine and application thereof
CN1964970B (en) 2004-04-07 2011-08-03 诺瓦提斯公司 Inhibitors of IAP
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
CA2578122A1 (en) * 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
TR200701870T1 (en) 2004-09-02 2007-05-21 Cipla Limited The stable crystalline form of imatinib mesylate and the process for its preparation.
US8735415B2 (en) 2004-09-09 2014-05-27 Natco Pharma Limited Acid addition salts of (3,5-Bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide
EA013328B1 (en) 2004-09-09 2010-04-30 Натко Фарма Лимитед Novel phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase
US7939541B2 (en) 2004-09-09 2011-05-10 Natco Pharma Limited Intermediates and a process employing the intermediates for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide
WO2006054314A1 (en) * 2004-11-17 2006-05-26 Natco Pharma Limited Polymorphic forms of imatinib mesylate
PL1833815T3 (en) * 2004-12-30 2011-03-31 Inst Farmaceutyczny A process for preparation of imatinib base
CN1972917B (en) * 2004-12-31 2010-08-25 孙飘扬 Aminopyrimidine compounds and their salts, process for preparation and pharmaceutical use thereof
CN1939910A (en) * 2004-12-31 2007-04-04 孙飘扬 Amino-metadiazine compound and its salt, its preparation and pharmaceutical use
AU2006207321B2 (en) 2005-01-21 2012-09-06 Astex Therapeutics Limited Pharmaceutical compounds
AU2006242311B2 (en) 2005-05-02 2010-03-04 Novartis Ag Use of pyrimidylamimobenzamide derivatives for the treatment of systematic mastocytosis
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
UA96139C2 (en) 2005-11-08 2011-10-10 Дженентек, Інк. Anti-neuropilin-1 (nrp1) antibody
PT2275103E (en) 2005-11-21 2014-07-24 Novartis Ag Mtor inhibitors in the treatment of endocrine tumors
UY29964A1 (en) 2005-11-25 2007-06-29 Novartis Ag CRYSTAL FORMS F, G, H, I, AND K OF THE IMATINIB MESILATE
GB0605120D0 (en) 2006-03-14 2006-04-26 Novartis Ag Organic Compounds
CN101415409B (en) 2006-04-05 2012-12-05 诺瓦提斯公司 Combinations of therapeutic agents for treating cancer
WO2007115289A2 (en) 2006-04-05 2007-10-11 Novartis Ag Combinations comprising bcr-abl/c-kit/pdgf-r tk inhibitors for treating cancer
PE20080251A1 (en) 2006-05-04 2008-04-25 Boehringer Ingelheim Int USES OF DPP IV INHIBITORS
BRPI0711385A2 (en) 2006-05-09 2011-11-08 Novartis Ag combination comprising an iron chelator and an antineoplastic agent and its use
US20060223817A1 (en) * 2006-05-15 2006-10-05 Chemagis Ltd. Crystalline imatinib base and production process therefor
AU2006345660A1 (en) 2006-06-01 2007-12-06 Japan As Represented By Director General Of Agency Of National Cancer Center Tumor suppressor
JP2010504933A (en) 2006-09-29 2010-02-18 ノバルティス アーゲー Pyrazolopyrimidines as PI3K lipid kinase inhibitors
JP5528806B2 (en) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド Compound drug
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
KR20090061055A (en) * 2006-10-26 2009-06-15 시코르, 인크. Crystalline and amorphous imatinib bases, imatinib mesylate and methods for their preparation
RU2480461C2 (en) * 2006-11-16 2013-04-27 Ф.И.С. Фаббрика Итальяна Синтетичи С.П.А. Method of producing imatinib and intermediate compounds thereof
CN101245061B (en) * 2007-02-13 2012-09-19 天津天士力集团有限公司 N-(5-amido-2-methyl phenyl)-4-(3-pyridinyl)-2-aminopyrimidine nitric oxide donating derivant, production method and uses thereof
MX2009008584A (en) 2007-02-15 2009-08-18 Novartis Ag Combinations of therapeutic agents for treating cancer.
RU2329260C1 (en) * 2007-02-20 2008-07-20 Юрий Иосифович Копырин Method of obtaining 2-anilinopyrimidines or their salts (options)
KR20090128396A (en) * 2007-03-12 2009-12-15 닥터 레디스 레보러터리즈 리미티드 Imatinib mesylate
WO2008117298A1 (en) * 2007-03-26 2008-10-02 Natco Pharma Limited A novel method of preparation of imatinib
US7550591B2 (en) 2007-05-02 2009-06-23 Chemagis Ltd. Imatinib production process
WO2008136010A1 (en) * 2007-05-07 2008-11-13 Natco Pharma Limited A process for the preparation of highly pure imatinib base
WO2008153959A1 (en) 2007-06-07 2008-12-18 Intra-Cellular Therapies, Inc. Novel heterocycle compounds and uses thereof
ES2607794T3 (en) 2007-06-07 2017-04-04 Intra-Cellular Therapies, Inc. Novel heterocyclic compounds and uses thereof
WO2009060463A1 (en) * 2007-11-05 2009-05-14 Natco Pharma Limited An environmentally friendly process for the preparation of imatinib base
EP2062885A1 (en) * 2007-11-21 2009-05-27 Eczacibasi-Zentiva Kimyasal Ürünler Sanayi ve Ticaret A.S. Acid addition salts of imatinib and formulations comprising the same
ES2459297T3 (en) * 2008-02-01 2014-05-08 Akinion Pharmaceuticals Ab Pyrazine derivatives and their use as protein kinase inhibitors
CN102036953B (en) 2008-03-24 2015-05-06 诺华股份有限公司 Arylsulfonamide-based matrix metalloprotease inhibitors
BRPI0909159A2 (en) 2008-03-26 2015-11-24 Novartis Ag deacetylase b hydroxamate based inhibitors
SI2300013T2 (en) 2008-05-21 2025-05-30 Takeda Pharmaceutical Company Limited Phosphorus derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
CN101584696A (en) 2008-05-21 2009-11-25 上海艾力斯医药科技有限公司 Composition containing quinazoline derivatives, preparation method and use
PL215042B1 (en) * 2008-08-01 2013-10-31 Temapharm Spolka Z Ograniczona Odpowiedzialnoscia Method of imatinib manufacturing
UY32030A (en) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "TREATMENT FOR DIABETES IN INAPPROPRIATE PATIENTS FOR THERAPY WITH METFORMIN"
PE20110297A1 (en) 2008-08-15 2011-05-26 Boehringer Ingelheim Int DPP-4 INHIBITORS FOR WOUND HEALING
EA201500417A1 (en) 2008-08-25 2015-11-30 Эмплиммьюн, Инк. ANTAGONIST COMPOSITIONS PD-1 AND APPLICATIONS
ES2704986T3 (en) 2008-10-16 2019-03-21 Celator Pharmaceuticals Inc Combinations of a water-soluble liposomal camptothecin with cetuximab or bevacizumab
EP2186514B1 (en) 2008-11-14 2016-06-29 Kinki University Treatment of Malignant Peripheral Nerve Sheath Tumors
PL2676953T3 (en) 2008-12-18 2017-09-29 Novartis Ag Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3 -trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid for use in the treatment of lymphocyte mediated diseases
CN102256942B (en) 2008-12-18 2013-07-24 诺瓦提斯公司 New polymorphic form of 1- (4- { l- [ (e) -4-cyclohexyl--3-trifluoromethyl-benzyloxyimino] -ethyl) -2-ethyl-benzyl) -azetidine-3-formic acid
MX2011006622A (en) 2008-12-18 2011-07-12 Novartis Ag New salts.
EP2382216A1 (en) 2008-12-23 2011-11-02 Boehringer Ingelheim International GmbH Salt forms of organic compound
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
WO2010083617A1 (en) 2009-01-21 2010-07-29 Oncalis Ag Pyrazolopyrimidines as protein kinase inhibitors
AR075204A1 (en) 2009-01-29 2011-03-16 Boehringer Ingelheim Int DPP-4 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USEFUL TO TREAT METABOLIC DISEASES IN PEDIATRIC PATIENTS, PARTICULARLY MELLITUS DIABETES TYPE 2
PT2391366E (en) 2009-01-29 2013-02-05 Novartis Ag Substituted benzimidazoles for the treatment of astrocytomas
KR20110115582A (en) 2009-02-13 2011-10-21 베링거 인겔하임 인터내셔날 게엠베하 Antidiabetic agents comprising a DPP-4 inhibitor (linagliptin), optionally in combination with other antidiabetics
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
JP2012519281A (en) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー Methods for identifying mesenchymal tumor cells or agents that inhibit their production
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
EP2401613A2 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
UA103918C2 (en) 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
TW201102068A (en) 2009-06-02 2011-01-16 Novartis Ag Treatment of ophthalmologic disorders mediated by alpha-carbonic anhydrase isoforms
PT2445903E (en) 2009-06-26 2014-07-08 Novartis Ag 1,3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
WO2011014520A2 (en) 2009-07-29 2011-02-03 Irm Llc Compounds and compositions as modulators of gpr119 activity
US8389526B2 (en) 2009-08-07 2013-03-05 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives
MX2012001838A (en) 2009-08-12 2012-02-29 Novartis Ag Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation.
SG10201404886PA (en) 2009-08-17 2014-10-30 Intellikine Llc Heterocyclic compounds and uses thereof
JP5775871B2 (en) 2009-08-20 2015-09-09 ノバルティス アーゲー Heterocyclic oxime compounds
AU2010288534A1 (en) 2009-08-26 2012-03-15 Novartis Ag Tetra-substituted heteroaryl compounds and their use as MDM2 and/or MDM4 modulators
KR20120093867A (en) 2009-09-10 2012-08-23 아이알엠 엘엘씨 Ether derivatives of bicyclic heteroaryls
PT2482812T (en) 2009-10-02 2023-01-24 Boehringer Ingelheim Int Therapeutic uses of pharmaceutical compositions
MX2012004078A (en) 2009-10-09 2012-07-25 Irm Llc Compounds and compositions as modulators of gpr119 activity.
PL389357A1 (en) 2009-10-22 2011-04-26 Tomasz Koźluk Tartaric acids derivatives imatinib salts and process for the preparation thereof
NZ599565A (en) 2009-11-04 2013-05-31 Novartis Ag Heterocyclic sulfonamide derivatives useful as mek inhibitors
JP6220126B2 (en) 2009-11-23 2017-10-25 セルリアン・ファーマ・インコーポレイテッド Polymers based on cyclodextrins for therapeutic delivery
WO2011064211A1 (en) 2009-11-25 2011-06-03 Novartis Ag Benzene-fused 6-membered oxygen-containing heterocyclic derivatives of bicyclic heteroaryls
KR20120107080A (en) 2009-11-27 2012-09-28 베링거 인겔하임 인터내셔날 게엠베하 Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
US8394858B2 (en) 2009-12-03 2013-03-12 Novartis Ag Cyclohexane derivatives and uses thereof
EP2509964B1 (en) 2009-12-08 2014-04-30 Novartis AG Heterocyclic sulfonamide derivatives
EP2509973A1 (en) 2009-12-10 2012-10-17 Arch Pharmalabs Limited Process for the preparation of imatinib and salts thereof
US8440693B2 (en) 2009-12-22 2013-05-14 Novartis Ag Substituted isoquinolinones and quinazolinones
CU24130B1 (en) 2009-12-22 2015-09-29 Novartis Ag ISOQUINOLINONES AND REPLACED QUINAZOLINONES
WO2011090940A1 (en) 2010-01-19 2011-07-28 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
JP2013519665A (en) 2010-02-15 2013-05-30 リライアンス ライフ サイエンシズ ピーヴィーティー リミティッド Process for producing α form of imatinib mesylate
PL390611A1 (en) 2010-03-04 2011-09-12 Tomasz Koźluk Process for the preparation of polymorphic alpha form and new polymorphic form of imatinib mesylate
WO2011114337A1 (en) 2010-03-15 2011-09-22 Natco Pharma Limited Process for the preparation of highly pure crystalline imatinib base
EP2547339A1 (en) 2010-03-18 2013-01-23 Boehringer Ingelheim International GmbH Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
US20110237686A1 (en) 2010-03-26 2011-09-29 Cerulean Pharma Inc Formulations and methods of use
WO2011130918A1 (en) * 2010-04-23 2011-10-27 上海百灵医药科技有限公司 Process for synthesizing imatinib
EP2382976A1 (en) 2010-04-30 2011-11-02 Hiroshima University Use of pdgf-r inhibitors for the treatment of lymph node metastasis of gastric cancer
EA033415B1 (en) 2010-05-05 2019-10-31 Boehringer Ingelheim Int Methods for treating obesity, use of dpp-4 inhibitor in these methods and method for treating patients suffering from type 2 diabetes mellitus
CN102947275A (en) 2010-06-17 2013-02-27 诺瓦提斯公司 Piperidinyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
US20130090342A1 (en) 2010-06-17 2013-04-11 Novartis Ag Biphenyl substituted 1,3-dihydro-benzoimidazol-2-ylideneamine derivatives
SI2582689T1 (en) 2010-06-18 2017-05-31 Krka, D.D., Novo Mesto New polymorphic form of imatinib base and preparation of salts thereof
EP2582362A1 (en) 2010-06-21 2013-04-24 Zaklady Farmaceutyczne "Polpharma" S.A. Pharmaceutical compositions comprising imatinib or pharmaceutically acceptable salt thereof and processes for the manufacture thereof
KR20130093012A (en) 2010-06-24 2013-08-21 베링거 인겔하임 인터내셔날 게엠베하 Diabetes therapy
UA112517C2 (en) 2010-07-06 2016-09-26 Новартіс Аг TETRAHYDROPYRIDOPYRIMIDINE DERIVATIVES
CA2803792A1 (en) 2010-07-09 2012-01-12 Genentech, Inc. Anti-neuropilin antibodies and methods of use
US8697739B2 (en) 2010-07-29 2014-04-15 Novartis Ag Bicyclic acetyl-CoA carboxylase inhibitors and uses thereof
EP2603288A1 (en) 2010-08-11 2013-06-19 Synthon BV Pharmaceutical granulate comprising imatinib mesylate
TR201007005A2 (en) 2010-08-23 2011-09-21 Mustafa Nevzat İlaç Sanayi̇i̇ A.Ş. Imatinib base production method
EP2627648A1 (en) 2010-09-16 2013-08-21 Novartis AG 17aHYDROXYLASE/C17,20-LYASE INHIBITORS
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
TR201010618A2 (en) 2010-12-20 2012-07-23 Bi̇lgi̇ç Mahmut An oral dosage form comprising imatinib and the manufacture of an oral dosage form
AU2011346567A1 (en) 2010-12-21 2013-07-25 Novartis Ag Bi-heteroaryl compounds as Vps34 inhibitors
WO2012090221A1 (en) 2010-12-29 2012-07-05 Cadila Healthcare Limited Novel salts of imatinib
JP2014505088A (en) 2011-02-10 2014-02-27 ノバルティス アーゲー [1,2,4] Triazolo [4,3-b] pyridazine compounds as C-MET tyrosine kinase inhibitors
CN106619647A (en) 2011-02-23 2017-05-10 因特利凯有限责任公司 Combinations of kinase inhibitors and uses thereof
US9127000B2 (en) 2011-02-23 2015-09-08 Intellikine, LLC. Heterocyclic compounds and uses thereof
JP2014507465A (en) 2011-03-08 2014-03-27 ノバルティス アーゲー Fluorophenyl bicyclic heteroaryl compounds
PL394169A1 (en) 2011-03-09 2012-09-10 Adamed Spółka Z Ograniczoną Odpowiedzialnością The pharmaceutical composition of imatinib mesylate for filling unit dosage forms and the method for its preparation
EP2508525A1 (en) 2011-04-05 2012-10-10 Bayer Pharma Aktiengesellschaft Substituted 2,3-dihydroimidazo[1,2-c]quinazoline salts
EP2702173A1 (en) 2011-04-25 2014-03-05 OSI Pharmaceuticals, LLC Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment
JP6002210B2 (en) 2011-04-28 2016-10-05 ノバルティス アーゲー 17α-hydroxylase / C17,20-lyase inhibitor
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN102796110B (en) * 2011-05-23 2016-03-30 复旦大学 Aniline pyrimidine compound and its production and use
EA201391820A1 (en) 2011-06-09 2014-12-30 Новартис Аг HETEROCYCLIC SULPHONAMIDE DERIVATIVES
EP2721008B1 (en) 2011-06-20 2015-04-29 Novartis AG Hydroxy substituted isoquinolinone derivatives as p53 (mdm2 or mdm4) inhibitors
EP2721007B1 (en) 2011-06-20 2015-04-29 Novartis AG Cyclohexyl isoquinolinone compounds
US9750700B2 (en) 2011-06-22 2017-09-05 Natco Pharma Limited Imatinib mesylate oral pharmaceutical composition and process for preparation thereof
MX2013015001A (en) 2011-06-27 2014-03-31 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives.
ITMI20111309A1 (en) 2011-07-14 2013-01-15 Italiana Sint Spa PREPARATION PROCEDURE OF IMATINIB MESILATO
PL3517539T3 (en) 2011-07-15 2023-04-24 Boehringer Ingelheim International Gmbh Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes
WO2013035102A1 (en) 2011-09-05 2013-03-14 Natco Pharma Limited Processes for the preparation of imatinib base and intermediates thereof
MX339302B (en) 2011-09-15 2016-05-19 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase.
CN104039324B (en) 2011-11-01 2017-03-15 莫德基因有限责任公司 Reduce the compositionss and method of amyloid beta load
RU2486180C1 (en) * 2011-11-02 2013-06-27 Общество с ограниченной ответственностью "ТехноХим" (ООО "ТехноХим") Method for preparing 2-arylamino-4-hetarylpyrimidines
WO2013080141A1 (en) 2011-11-29 2013-06-06 Novartis Ag Pyrazolopyrrolidine compounds
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CN103159739A (en) * 2011-12-09 2013-06-19 天津市国际生物医药联合研究院有限公司 1, 4-disubstituted-1, 2, 3-triazole compounds and preparation method thereof
CN104011045B (en) 2011-12-22 2016-08-24 诺华股份有限公司 Dihydrobenzoxazine and dihydropyridoxazine derivatives
WO2013093850A1 (en) 2011-12-22 2013-06-27 Novartis Ag Quinoline derivatives
CA2859876A1 (en) 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
US20130178520A1 (en) 2011-12-23 2013-07-11 Duke University Methods of treatment using arylcyclopropylamine compounds
MX2014007729A (en) 2011-12-23 2015-01-12 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners.
JP2015503517A (en) 2011-12-23 2015-02-02 ノバルティス アーゲー Compound for inhibiting interaction between BCL2 and binding partner
EP2794589A1 (en) 2011-12-23 2014-10-29 Novartis AG Compounds for inhibiting the interaction of bcl2 with binding partners
KR20140104047A (en) 2011-12-23 2014-08-27 노파르티스 아게 Compounds for inhibiting the interaction of bcl2 with binding partners
US20130172244A1 (en) 2011-12-29 2013-07-04 Thomas Klein Subcutaneous therapeutic use of dpp-4 inhibitor
PL226174B1 (en) 2011-12-30 2017-06-30 Inst Farm Combination therapy of non-small-cell lung carcinoma
UY34591A (en) 2012-01-26 2013-09-02 Novartis Ag IMIDAZOPIRROLIDINONA COMPOUNDS
WO2013120852A1 (en) 2012-02-13 2013-08-22 Grindeks, A Joint Stock Company Intermediates for a novel process of preparing imatinib and related tyrosine kinase inhibitors
WO2013136141A1 (en) 2012-03-13 2013-09-19 Fresenius Kabi Oncology Ltd. An improved process for the preparation of alpha form of imatinib mesylate
EP3964513A1 (en) 2012-04-03 2022-03-09 Novartis AG Combination products with tyrosine kinase inhibitors and their use
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
TW201348187A (en) 2012-04-24 2013-12-01 Chugai Pharmaceutical Co Ltd Benzamide derivative
CN104379568A (en) 2012-04-24 2015-02-25 中外制药株式会社 Quinazolinedione derivative
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
US20130303462A1 (en) 2012-05-14 2013-11-14 Boehringer Ingelheim International Gmbh Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome
EP2849754B1 (en) 2012-05-14 2022-09-14 Boehringer Ingelheim International GmbH Linagliptin, a xanthine derivative as dpp-4 inhibitor, for use in the treatment of sirs and/or sepsis
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
WO2013174768A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of autoimmune diabetes, particularly lada
US9365576B2 (en) 2012-05-24 2016-06-14 Novartis Ag Pyrrolopyrrolidinone compounds
JP6427097B2 (en) 2012-06-15 2018-11-21 ザ ブリガム アンド ウィメンズ ホスピタル インコーポレイテッドＴｈｅ Ｂｒｉｇｈａｍ ａｎｄ Ｗｏｍｅｎ’ｓ Ｈｏｓｐｉｔａｌ， Ｉｎｃ． Compositions for treating cancer and methods for producing said compositions
WO2014016848A2 (en) 2012-07-24 2014-01-30 Laurus Labs Private Limited Solid forms of tyrosine kinase inhibitors, process for the preparation and their pharmaceutical composition thereof
WO2014041551A1 (en) 2012-09-14 2014-03-20 Natco Pharma Limited Formulation comprising imatinib as oral solution
CN103664787B (en) 2012-09-17 2015-09-09 南京圣和药业股份有限公司 Alkynes heteroaromatic ring compounds and application thereof
WO2014052619A1 (en) 2012-09-27 2014-04-03 Irm Llc Piperidine derivatives and compositions as modulators of gpr119 activity
US20150238488A1 (en) 2012-09-28 2015-08-27 Hangzhou Bensheng Pharmaceutical Co., Ltd. Drug composition for treating tumors and application thereof
EP2903979B1 (en) * 2012-10-04 2020-08-19 Inhibikase Therapeutics, Inc. Novel compounds, their preparation and their uses
EP2914278B1 (en) 2012-11-05 2021-06-02 Dana-Farber Cancer Institute, Inc. Xbp1, cd138, and cs1 peptides, pharmaceutical compositions that include the peptides, and methods of using such peptides and compositions
TW201422625A (en) 2012-11-26 2014-06-16 Novartis Ag Solid form of dihydro-pyrido-oxazine derivative
CN103848812B (en) * 2012-12-04 2016-08-03 北大方正集团有限公司 The method of refined imatinib
CN103044394A (en) * 2012-12-20 2013-04-17 北京理工大学 Phenyl aminopyrimidine derivant and preparation method and application thereof
EP2749271A1 (en) 2012-12-31 2014-07-02 Deva Holding Anonim Sirketi Optimized manufacturing method and pharmaceutical formulation of imatinib
US9556180B2 (en) 2013-01-22 2017-01-31 Novartis Ag Pyrazolo[3,4-d]pyrimidinone compounds as inhibitors of the P53/MDM2 interaction
EP2948451B1 (en) 2013-01-22 2017-07-12 Novartis AG Substituted purinone compounds
WO2014124860A1 (en) 2013-02-14 2014-08-21 Boehringer Ingelheim International Gmbh Specific pde4b-inhibitors for the treatment of diabetes mellitus
PL2958943T3 (en) 2013-02-20 2020-04-30 The Trustees Of The University Of Pennsylvania Treatment of malignant neoplasm with a humanized chimeric anti-egfrviii antigen receptor
WO2014128612A1 (en) 2013-02-20 2014-08-28 Novartis Ag Quinazolin-4-one derivatives
BR112015020209A2 (en) 2013-03-15 2017-07-18 Boehringer Ingelheim Int use of linagliptin in antidiabetic therapy of cardiac and renal protection
HK1219421A1 (en) 2013-03-15 2017-04-07 因特利凯有限责任公司 Combination of kinase inhibitors and uses thereof
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
ES2683361T3 (en) 2013-05-14 2018-09-26 Hetero Research Foundation Imatinib compositions
US20150018376A1 (en) 2013-05-17 2015-01-15 Novartis Ag Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof
UY35675A (en) 2013-07-24 2015-02-27 Novartis Ag SUBSTITUTED DERIVATIVES OF QUINAZOLIN-4-ONA
WO2015022664A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
WO2015022663A1 (en) 2013-08-14 2015-02-19 Novartis Ag Compounds and compositions as inhibitors of mek
AU2014321419B2 (en) 2013-09-22 2017-06-15 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
JP6445573B2 (en) 2013-10-17 2018-12-26 サルタル セラピューティクス エルティーディＳａｒｔａｒ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｌｔｄ Compositions containing phosphodiesterase inhibitors for use in the treatment of solid tumors in human patients
JP6307088B2 (en) 2013-10-23 2018-04-04 中外製薬株式会社 Quinazolinone and isoquinolinone derivatives
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
WO2015145388A2 (en) 2014-03-27 2015-10-01 Novartis Ag Methods of treating colorectal cancers harboring upstream wnt pathway mutations
CA2943979A1 (en) 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
WO2015153345A1 (en) 2014-04-03 2015-10-08 Invictus Oncology Pvt. Ltd. Supramolecular combinatorial therapeutics
US9630944B2 (en) 2014-04-04 2017-04-25 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Process for preparing Imatinib and salts thereof, free of genotoxic impurity F
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2016011658A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
JP6526789B2 (en) 2014-07-31 2019-06-05 ノバルティス アーゲー Combination therapy
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
CN105585556A (en) * 2014-11-13 2016-05-18 连云港杰瑞药业有限公司 Synthetic method of imatinib
JP2018527362A (en) 2015-09-11 2018-09-20 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． Substituted heteroaryl compounds and methods of use
WO2017129624A1 (en) 2016-01-25 2017-08-03 Krka, D.D., Novo Mesto Fast dispersible pharmaceutical composition comprising tyrosine-kinase inhibitor
NZ745778A (en) 2016-03-25 2022-07-01 Ab Science Use of masitinib for treatment of an amyotrophic lateral sclerosis patient subpopulation
AU2017276758A1 (en) 2016-06-10 2018-11-08 Boehringer Ingelheim International Gmbh Combinations of Linagliptin and metformin
EP3257499A1 (en) 2016-06-17 2017-12-20 Vipharm S.A. Process for preparation of imatinib methanesulfonate capsules
CN107652269A (en) * 2016-07-26 2018-02-02 江苏豪森药业集团有限公司 Methanesulfonic acid fluorine imatinib purification of intermediate method
WO2018039203A1 (en) 2016-08-23 2018-03-01 Oncopep, Inc. Peptide vaccines and durvalumab for treating multiple myeloma
CA3034666A1 (en) 2016-08-23 2018-03-01 Oncopep, Inc. Peptide vaccines and durvalumab for treating breast cancer
CN107805240A (en) * 2016-09-08 2018-03-16 中国科学院合肥物质科学研究院 A kind of new PDGFR kinase inhibitors and application thereof
CA3035080A1 (en) 2016-09-27 2018-04-05 Cero Therapeutics, Inc. Chimeric engulfment receptor molecules
US10207998B2 (en) 2016-09-29 2019-02-19 Duke University Substituted benzimidazole and substituted benzothiazole inhibitors of transforming growth factor-β kinase and methods of use thereof
US10927083B2 (en) 2016-09-29 2021-02-23 Duke University Substituted benzimidazoles as inhibitors of transforming growth factor-β kinase
EP3333162A1 (en) 2016-12-12 2018-06-13 Silesian Catalysts sp. z o.o. Metod for preparing n-(2-methyl-5-nitrophenyl)-4-(pyridin-3-yl)pyrimidin-2-amine
CN107089969B (en) * 2017-04-26 2020-04-24 黑龙江鑫创生物科技开发有限公司 Method for synthesizing imatinib intermediate
WO2019067328A1 (en) 2017-09-26 2019-04-04 Cero Therapeutics, Inc. Chimeric engulfment receptor molecules and methods of use
US12059463B2 (en) 2017-10-24 2024-08-13 Oncopep, Inc. Peptide vaccines and pembrolizumab for treating breast cancer
WO2019083960A1 (en) 2017-10-24 2019-05-02 Oncopep, Inc. Peptide vaccines and hdac inhibitors for treating multiple myeloma
EP3710006A4 (en) 2017-11-19 2021-09-01 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
WO2019119486A1 (en) 2017-12-21 2019-06-27 中国科学院合肥物质科学研究院 Class of pyrimidine derivative kinase inhibitors
KR102737185B1 (en) 2018-01-20 2024-12-05 선샤인 레이크 파르마 컴퍼니 리미티드 Substituted aminopyrimidine compounds and methods of use thereof
EP3774906A1 (en) 2018-03-28 2021-02-17 Cero Therapeutics, Inc. Chimeric tim4 receptors and uses thereof
CN112218886A (en) 2018-03-28 2021-01-12 森罗治疗公司 Chimeric phagocytosis receptor expression vector, genetically modified host cell and use thereof
AU2019243154A1 (en) 2018-03-28 2020-10-01 Cero Therapeutics, Inc. Cellular immunotherapy compositions and uses thereof
EP3823625A1 (en) 2018-07-17 2021-05-26 Boehringer Ingelheim International GmbH Cardio- and renosafe antidiabetic therapy
CA3103992A1 (en) 2018-07-17 2020-01-23 Boehringer Ingelheim International Gmbh Cardiosafe antidiabetic therapy
US12220423B2 (en) 2018-07-24 2025-02-11 Hygia Pharmaceuticals, Llc Compounds, derivatives, and analogs for cancer
BR112022000571A2 (en) 2019-07-15 2022-03-15 Intas Pharmaceuticals Ltd Pharmaceutical composition and process for preparing a pharmaceutical composition comprising imatinib or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients in powder form
US20240058446A1 (en) 2019-10-03 2024-02-22 Cero Therapeutics, Inc. Chimeric tim4 receptors and uses thereof
WO2021097256A1 (en) 2019-11-14 2021-05-20 Cohbar, Inc. Cxcr4 antagonist peptides
WO2021185844A1 (en) 2020-03-16 2021-09-23 Pvac Medical Technologies Ltd Use of substance and pharmaceutical composition thereof, and medical treatments or uses thereof
WO2021233534A1 (en) 2020-05-20 2021-11-25 Pvac Medical Technologies Ltd Use of substance and pharmaceutical composition thereof, and medical treatments or uses thereof
CN115768890A (en) 2020-04-15 2023-03-07 加州理工学院 Thermal control of T cell immunotherapy by molecular and physical initiation
WO2021228983A1 (en) 2020-05-13 2021-11-18 INSERM (Institut National de la Santé et de la Recherche Médicale) A pharmaceutical composition comprising an arsenic compound, an inductor of type-1 ifn and a protein kinase inhibitor for treating cancer
US20230285576A1 (en) 2020-08-05 2023-09-14 Ellipses Pharma Ltd Treatment of cancer using a cyclodextrin-containing polymer-topoisomerase inhibitor conjugate and a parp inhibitor
WO2022036265A1 (en) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Chimeric tim receptors and uses thereof
WO2022036287A1 (en) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Anti-cd72 chimeric receptors and uses thereof
WO2022036285A1 (en) 2020-08-14 2022-02-17 Cero Therapeutics, Inc. Compositions and methods for treating cancer with chimeric tim receptors in combination with inhibitors of poly (adp-ribose) polymerase
WO2022047259A1 (en) 2020-08-28 2022-03-03 California Institute Of Technology Synthetic mammalian signaling circuits for robust cell population control
TW202237638A (en) 2020-12-09 2022-10-01 日商武田藥品工業股份有限公司 Compositions of guanylyl cyclase c (gcc) antigen binding agents and methods of use thereof
CN117203223A (en) 2021-02-26 2023-12-08 凯洛尼亚疗法有限公司 Lymphocyte targeting lentiviral vectors
US20250127896A1 (en) 2021-07-28 2025-04-24 Cero Therapeutics Holdings, Inc. Chimeric tim4 receptors and uses thereof
CN119816589A (en) 2022-08-02 2025-04-11 国立大学法人北海道大学 Methods to improve cell therapy using organelle complexes

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU523746B2 (en) * 1977-04-05 1982-08-12 Taiho Pharmaceutical Co., Ltd. Anticancer composition
DE3751742T3 (en) * 1986-01-13 2002-11-21 American Cyanamid Co., Wayne 4,5,6-substituted 2-pyrimidinamines

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
WO2003090720A1 (en) 2002-04-23 2003-11-06 Novartis Ag High drug load tablet
EP1501485A1 (en) 2002-04-23 2005-02-02 Novartis AG High drug load tablet
US9011911B2 (en) 2002-04-23 2015-04-21 Novartis Ag High drug load tablet
US9018205B2 (en) 2007-09-04 2015-04-28 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
WO2012116666A1 (en) 2011-02-28 2012-09-07 USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, v.v.i. Pyrimidine compounds inhibiting the formation of nitric oxide and prostaglandin e2, method of production thereof and use thereof
EP3195867A1 (en) 2011-02-28 2017-07-26 Ustav Organicke Chemie A Biochemie Akademie Ved Cr, v.v.i. Pyrimidine compounds inhibiting the formation of nitric oxide and prostaglandin e2, method of production thereof and use thereof
US10442806B2 (en) 2012-08-06 2019-10-15 Duke University Substituted heterocycles for targeting HSP90
US10000469B2 (en) 2014-03-25 2018-06-19 Duke University Heat shock protein 70 (hsp-70) receptor ligands
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90

Also Published As

Publication number Publication date
JP2706682B2 (en) 1998-01-28
FI931458A0 (en) 1993-03-31
SK28093A3 (en) 1994-04-06
JPH0687834A (en) 1994-03-29
SA93140441B1 (en) 2005-12-14
CY2003003I1 (en) 2010-07-28
DK0564409T3 (en) 2000-06-19
ATE188964T1 (en) 2000-02-15
ZA932397B (en) 1993-10-04
CN1077713A (en) 1993-10-27
PT564409E (en) 2000-06-30
KR930021624A (en) 1993-11-22
NL300086I1 (en) 2002-05-01
EP0564409A1 (en) 1993-10-06
NL300086I2 (en) 2002-06-03
SK280620B6 (en) 2000-05-16
CY2229B1 (en) 2003-04-18
NO302473B1 (en) 1998-03-09
DE10299016I1 (en) 2002-08-29
NO2002001I2 (en) 2007-01-29
DE10299016I2 (en) 2006-08-24
HU226488B1 (en) 2009-03-02
HU9300982D0 (en) 1993-06-28
HU227080B1 (en) 2010-06-28
NO931283L (en) 1993-10-04
CZ283944B6 (en) 1998-07-15
ES2142857T3 (en) 2000-05-01
HUT64050A (en) 1993-11-29
CA2093203C (en) 2002-11-26
FI109534B (en) 2002-08-30
CN1043531C (en) 1999-06-02
AU3569493A (en) 1993-10-07
DE59309931D1 (en) 2000-02-24
FI931458A7 (en) 1993-10-04
MX9301929A (en) 1994-07-29
SG43859A1 (en) 1997-11-14
LU90908I2 (en) 2003-04-30
TW225528B (en) 1994-06-21
NZ247299A (en) 1995-07-26
IL105264A0 (en) 1993-08-18
RU2125992C1 (en) 1999-02-10
IL105264A (en) 1999-04-11
AU666709B2 (en) 1996-02-22
CZ56093A3 (en) 1994-02-16
BR1100739A (en) 2000-06-06
KR100261366B1 (en) 2002-07-18
NO931283D0 (en) 1993-04-02
GR3032927T3 (en) 2000-07-31
EP0564409B1 (en) 2000-01-19

Similar Documents

Publication Publication Date Title
CA2093203A1 (en) Pyrimidine derivatives and processes for the preparation thereof
RU93005357A (en) Pyrimidine derivatives and method of their manufacture
IL89119A0 (en) Pt(iv)complexes
ES2000481A6 (en) Derivatives of 2,3-dihydro-benzofurane, processes for their preparation and pharmaceutical compositions containing them.
EP0218541A3 (en) 3-vinyl and 3-ethinyl-beta-carboline derivatives, their preparation and their use as medicaments
BG101601A (en) PHARMACEUTICAL PIPERAZINE DERIVATIVES
AU645799B2 (en) Hydrazones
ES8507503A1 (en) Substituted anthra(1,9-cd)pyrazol-6(2H)-ones.
RU94046379A (en) New derivatives of piperazinyl-bis-(alkylamino)-pyrimidines
MX9706014A (en) Tricyclic dione derivatives.
KR960702463A (en) DC-89 derivative [DC-89 DERIVATIVE]
MY100938A (en) Arylkylimidazole derivatives.
ES2001102A6 (en) Indene compounds.
TW282458B (en)
ES2019228A6 (en) New Azaspyro not 4.5 decane-7,9-dione derivatives
KR870006898A (en) Nephritis Drugs

Legal Events

Date Code Title Description
EEER Examination request