HUP0001698A2 - Substituted pyrimidine compounds and their use - Google Patents

Substituted pyrimidine compounds and their use

Info

Publication number
HUP0001698A2
HUP0001698A2 HU0001698A HUP0001698A HUP0001698A2 HU P0001698 A2 HUP0001698 A2 HU P0001698A2 HU 0001698 A HU0001698 A HU 0001698A HU P0001698 A HUP0001698 A HU P0001698A HU P0001698 A2 HUP0001698 A2 HU P0001698A2
Authority
HU
Hungary
Prior art keywords
groups
hiv
substituents
disease
diseases
Prior art date
Application number
HU0001698A
Other languages
Hungarian (hu)
Inventor
Michael J. Malone
Nathan B. Mantlo
Ulrike D. Spohr
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
Application filed by Amgen Inc. filed Critical Amgen Inc.
Priority claimed from PCT/US1997/022390 external-priority patent/WO1998024782A2/en
Publication of HUP0001698A2 publication Critical patent/HUP0001698A2/en
Publication of HUP0001698A3 publication Critical patent/HUP0001698A3/en

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C07D213/643—2-Phenoxypyridines; Derivatives thereof
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

A találmány tárgyát az (I) általános képletű vegyületek vagy ezekgyógyászatilag megfelelő sói, valamint e vegyületeket tartalmazógyógyászati készítmények képezik. A találmány szerinti vegyületekeredményesen alkalmazhatók számos betegség kezelésére vagymegelőzésére, mint a gyulladásos betegségek, így reumaszerű ízületigyulladás, Paget-kór, oszteoporózis, myeloma multiplex, uveagyulladás,akut vagy krónikus csontvelő-leukémia, hasnyálmirigy b-sejtekpusztulása, csontízületi gyulladás, a reumaszerű csigolyagyulladás,köszvényes ízület igyulladás, gyulladásos bélbetegségek, felnőttkorilégzésnehézség tünetegyüttese (ARDS), psoriasis, Crohn-féle kór,szénanátha, fekélyes vastagbélgyulladás, anaphylaxis, érintkezésselterjedő bőrgyulladás, asztma, izomsorvadás, cachexia, Reiter-féletünetegyüttes, I. típusú diabétesz, II. típusú diabétesz,csontreszorpciós betegségek, átültetésnél fellépő születési reakciók,Alzheimer-kór, szélütés, szívizominfarktus, ischémiás reperfúzióssérülés, atherosclerosis, agyi traumák, sclerosis multiplex, agyimalária, szepszis, szeptikus sokk, toxikus sokk tünetegyüttese, láz, aHIV-1, HIV-2, HIV-3, citomegalovírus (CMV), influenza, adenovírus,herpeszvírus vagy herpesz zoster fertőzések nyomán fellépőizomfájdalom. Az (I) általános képletben a szubsztituensek jelentéseigen sokféle, így R1 és R2 jelentése egymástól függeltenül -Z-Y, ahol Z jelentése egy vegyértékkötés, alkil-, alkenil-, alkinil-,heterociklusos csoport, aril- vagy heteroarilcsoport, amely csoportokmindegyike igen sokféle szubsztituenst hordozhat; Y többek között hidrogénatom, halogénatom vagy nitrocsoport, -C(O)-R20vagy -C(NR5)-NR5R21 általános képletű csoport, -OR21, -O-C(O)-R21 vagy-O-C(O)-NR5R21 vagy -O-C(O)-NR22-S(O)2-R20 általános képletű csoport; R11 és R12 jelentése adott esetben szubsztituált aril- vagyheteroarilcsoport. A fenti csoportokban szereplő R5, R20, R21 és R22csoportok igen sokféle szubsztituenst jelenthetnek. ÓThe subject of the invention is the compounds of general formula (I) or their pharmaceutically acceptable salts, as well as pharmaceutical preparations containing these compounds. The compounds according to the invention can be effectively used for the treatment or prevention of many diseases, such as inflammatory diseases, such as rheumatoid arthritis, Paget's disease, osteoporosis, multiple myeloma, uveitis, acute or chronic bone marrow leukemia, b-cell destruction of the pancreas, osteoarthritis, rheumatoid spondylitis, gout arthritis, inflammatory bowel diseases, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, hay fever, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle atrophy, cachexia, Reiter's syndrome, type I diabetes, II. type 2 diabetes, bone resorption diseases, birth reactions occurring during transplantation, Alzheimer's disease, stroke, myocardial infarction, ischemic reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, HIV-1, HIV-2 , HIV-3, cytomegalovirus (CMV), influenza, adenovirus, herpes virus or herpes zoster infections, muscle pain. The meanings of the substituents in the general formula (I) are very diverse, so that R1 and R2 independently mean -Z-Y, where Z means a valence bond, alkyl-, alkenyl-, alkynyl-, heterocyclic group, aryl or heteroaryl group, each of which groups can carry a wide variety of substituents ; Y includes hydrogen, halogen or nitro, -C(O)-R20 or -C(NR5)-NR5R21, -OR21, -O-C(O)-R21 or -O-C(O)-NR5R21 or -O-C(O )-NR22-S(O)2-R20 group; R11 and R12 are optionally substituted aryl or heteroaryl groups. The R5, R20, R21 and R22 groups in the above groups can represent a wide variety of substituents. HE

HU0001698A 1996-12-05 1997-12-04 Substituted pyrimidine compounds and their use HUP0001698A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US3212896P 1996-12-05 1996-12-05
US5095097P 1997-06-13 1997-06-13
US97605497A 1997-11-21 1997-11-21
PCT/US1997/022390 WO1998024782A2 (en) 1996-12-05 1997-12-04 Substituted pyrimidine compounds and their use

Publications (2)

Publication Number Publication Date
HUP0001698A2 true HUP0001698A2 (en) 2001-04-28
HUP0001698A3 HUP0001698A3 (en) 2002-07-29

Family

ID=27364030

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0001698A HUP0001698A3 (en) 1996-12-05 1997-12-04 Substituted pyrimidine compounds and their use

Country Status (11)

Country Link
EP (1) EP0948497A2 (en)
CN (1) CN1246858A (en)
AR (1) AR048564A1 (en)
AU (1) AU733877C (en)
BG (1) BG65128B1 (en)
BR (1) BR9713850A (en)
CA (1) CA2274063C (en)
CZ (1) CZ296911B6 (en)
HU (1) HUP0001698A3 (en)
IL (1) IL130180A0 (en)
NZ (1) NZ335997A (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7427615B2 (en) 2001-09-21 2008-09-23 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
US7504411B2 (en) 2003-03-26 2009-03-17 Mitsubishi Tanabe Pharma Corporation 2,3,6-Trisubstituted-4-pyrimidone derivatives
US7572793B2 (en) 2001-09-21 2009-08-11 Mitsubishi Tanabe Pharma Corporation 3-Substituted-4-pyrimidone derivatives
US7683069B2 (en) 2002-12-16 2010-03-23 Mitsubishi Tanabe Pharma Corporation 3-substituted-4-pyrimidone derivatives

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001295026B2 (en) * 2000-09-06 2008-04-03 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3
TWI330183B (en) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
EP1340759A1 (en) * 2002-02-28 2003-09-03 Sanofi-Synthelabo 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-(pyrimidin-4-yl)-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
PT2629776T (en) * 2010-10-18 2017-11-15 Cerenis Therapeutics Holding Sa Compounds, compositions and methods useful for cholesterol mobilisation
TWI651310B (en) * 2014-02-20 2019-02-21 日商日本煙草產業股份有限公司 Triterpenoids and their medical use
CA3002632C (en) * 2015-10-29 2023-08-29 Aska Pharmaceutical Co., Ltd. Pyrimidine derivative

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE759176A (en) * 1969-11-20 1971-05-19 Sandoz Sa PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND MEDICINAL PRODUCTS CONTAINING THESE DERIVES
US4438117A (en) * 1980-09-03 1984-03-20 E. I. Du Pont De Nemours And Company 2-Substituted thio-4,5-diarylpyrimidines
DE3319843A1 (en) * 1983-06-01 1984-12-06 Ali-Akbar Dipl.-Chem. Dr. 4300 Mülheim Pourzal Process for the preparation of pyrimidines from nitrile and alkynes
US4500533A (en) * 1983-06-22 1985-02-19 Eli Lilly And Company 2,4,5-Triaryl pyrimidines and a method of treating pain, fever, thrombosis, inflammation and arthritis
US5077142A (en) * 1989-04-20 1991-12-31 Ricoh Company, Ltd. Electroluminescent devices
US5620999A (en) * 1994-07-28 1997-04-15 Weier; Richard M. Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7427615B2 (en) 2001-09-21 2008-09-23 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
US7572793B2 (en) 2001-09-21 2009-08-11 Mitsubishi Tanabe Pharma Corporation 3-Substituted-4-pyrimidone derivatives
US7683069B2 (en) 2002-12-16 2010-03-23 Mitsubishi Tanabe Pharma Corporation 3-substituted-4-pyrimidone derivatives
US7504411B2 (en) 2003-03-26 2009-03-17 Mitsubishi Tanabe Pharma Corporation 2,3,6-Trisubstituted-4-pyrimidone derivatives

Also Published As

Publication number Publication date
BG103512A (en) 2000-07-31
IL130180A0 (en) 2000-06-01
BR9713850A (en) 2000-02-29
AU733877C (en) 2003-05-08
AU733877B2 (en) 2001-05-31
AU6012098A (en) 1998-06-29
CA2274063A1 (en) 1998-06-11
EP0948497A2 (en) 1999-10-13
CN1246858A (en) 2000-03-08
CZ9902015A3 (en) 1999-11-17
HUP0001698A3 (en) 2002-07-29
CZ296911B6 (en) 2006-07-12
BG65128B1 (en) 2007-03-30
AR048564A1 (en) 2006-05-10
CA2274063C (en) 2007-09-04
NZ335997A (en) 2001-08-31

Similar Documents

Publication Publication Date Title
HUP0101099A2 (en) Substituted pyridine and pyridazine compounds and their pharmaceutical use
Van Aerschot et al. 3'-Fluoro-2', 3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'-and 3'-fluorinated 2', 3'-dideoxynucleoside analogs
KR102030305B1 (en) Indole carboxamide compounds useful as kinase inhibitors
EP0392791B1 (en) Antiviral compounds
HUP0001698A2 (en) Substituted pyrimidine compounds and their use
KR100589935B1 (en) Novel Pyrazine Derivatives or Salts Thereof, and Pharmaceutical Composition Containing the Same
Tanaka et al. Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) as potent and selective anti-HIV-1 agents
IL123330A (en) Nucleosides having 2'-ether group their preparation their use in the production of oligonucleotides and pharmaceutical compositions containing them
DK0481214T3 (en) Prophylactic drugs of phosphonates
ZA921804B (en) Cyclic urea derivatives, pharmaceutical compositions containing these compounds and processes for preparing them.
AR039842A1 (en) REPLACED HETEROCICLICAL COMPOUNDS AND EMPLOYMENT METHODS
PE20060837A1 (en) 3H-OXAZOLE AND 3H-THIAZOLE [4,5-d] PYRIMIDIN-2-ONA 3,5-DISUSTITUIDE AND 3,5,7-TRISUSTITUIDE COMPOUNDS AND PROPHARMACES OF THE SAME
IL84810A (en) Pharmaceutical antiviral compositions containing 1-beta-d-arabinofuranosyl-5-(1-alkynyl)cytosine and uracil derivatives thereof,some new such compounds and their preparation
JP2002506878A5 (en)
JP2002526501A5 (en)
WO2002069903A3 (en) Nucleosides, preparation thereof and use as inhibitors of rna viral polymerases
JP2683297B2 (en) Pyrimidine acyclonucleoside derivative
MY141472A (en) Substituted phenyl phenol leukotriene antagonists
AU7320100A (en) Hydroxamic acid derivatives, process for the production thereof and drugs containing the same as the active ingredient
Goudgaon et al. 1-(Ethoxymethyl)-6-(phenylselenenyl) pyrimidines with activity against human immunodeficiency virus types 1 and 2
FI92491B (en) Process for the preparation of pharmacologically active nucleoside derivatives
HUP0101230A2 (en) Chemical process for the production of sulphinyl derivatives by oxidation of the corresponding co-derivatives with perborates
ATE393157T1 (en) SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF APPLICATION
JP4076114B2 (en) 4'-C-ethynylpurine nucleoside compounds
DE60312342D1 (en) 1,4,5-SUBSTITUTED 1,2-DIHYDRO-PYRAZOL-3-ONE AND 3-ALKOXY-1H-PYRAZOLE DERIVATIVES AS TNF-ALPHA AND INTERLEUKIN-SUBSTANCING ACTIVITIES FOR THE TREATMENT OF INFLAMMATION

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees