HUP0300497A2 - Humán foszfatidilinozit-3-kináz-delta inhibitorok és alkalmazásuk - Google Patents
Humán foszfatidilinozit-3-kináz-delta inhibitorok és alkalmazásukInfo
- Publication number
- HUP0300497A2 HUP0300497A2 HU0300497A HUP0300497A HUP0300497A2 HU P0300497 A2 HUP0300497 A2 HU P0300497A2 HU 0300497 A HU0300497 A HU 0300497A HU P0300497 A HUP0300497 A HU P0300497A HU P0300497 A2 HUP0300497 A2 HU P0300497A2
- Authority
- HU
- Hungary
- Prior art keywords
- pi3kd
- activity
- aryl
- heteroaryl
- alkyl
- Prior art date
Links
- 108091007960 PI3Ks Proteins 0.000 title 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000000694 effects Effects 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 210000004027 cell Anatomy 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000006386 Bone Resorption Diseases 0.000 abstract 1
- 108010044467 Isoenzymes Proteins 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004450 alkenylene group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000005275 alkylenearyl group Chemical group 0.000 abstract 1
- -1 alkylenecycloalkyl Chemical group 0.000 abstract 1
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 abstract 1
- 230000024279 bone resorption Effects 0.000 abstract 1
- 101150068479 chrb gene Proteins 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 208000026278 immune system disease Diseases 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 210000000265 leukocyte Anatomy 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 210000002997 osteoclast Anatomy 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- 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
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- 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
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
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- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
- C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- C07D473/36—Sulfur atom
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- 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
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Abstract
A találmány (I) általános képletű vegyületekre, gyógyászatilagelfogadható sóikra és szolvátjaikra vonatkozik, ahol a képletben ahelyettesítők jellemző jelentése a többek között: A jelentése legalábbkét nitrogénatomot tartalmazó monociklusos vagy biciklusosgyűrűrendszer; X jelentése CHRb, CH2CHRb vagy CH=C(Rb) csoport; aholRb jelentése hidrogénatom, alkil-, aril-, heteroaril-, arilalkil-,heteroarilalkil-, alkilénaril vagy alkilénheteroaril-csoport; Y nincsjelen vagy jelentése kénatom, SO, SO2, NH, oxigénatom, C(=O), OC(=O),C(=O)O vagy NHC(=O)CH2S csoport; R1 és R2 jelentése egymástólfüggetlenül hidrogénatom, alkil-, aril-, heteroarilcsoport,halogénatom, vagy R1 és R2 együtt alkilén vagy alkenilénláncot alkot,amely egy gyűrű része; R3 jelentése hidrogénatom; vagy adott esetbenszubsztituált alkil-, cikloalkil-, heterocikloalkil-,alkiléncikloalkil-, alkenil-, alkilén-aril-, arilalkil-, aril-,heteroaril-csoport. A találmány szerinti vegyületek szelektívengátolják a PI3Kd izoenzim aktivitását sejtekben, különösenleukocitákban, oszteoklasztokban és rákos sejtekben. Így a találmánytárgyát képezik in vitro és ex vivo eljárások a PI3Kd aktivitásánakgátlására, valamint az (I) általános képletű vegyületek alkalmazásaolyan gyógyászati készítmények előállítására, amelyek szelektívengátolják PI3Kd aktivitását, így alkalmasak PI3Kd aktivitás általmediált betegségek, például immunrendszeri és gyulladásos betegségek,csontreszorpciós rendellenesség és rák kezelésére. Ó
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19965500P | 2000-04-25 | 2000-04-25 | |
| US60/199,655 | 2000-04-25 | ||
| US23805700P | 2000-10-05 | 2000-10-05 | |
| US60/238,057 | 2000-10-05 | ||
| PCT/US2001/013315 WO2001081346A2 (en) | 2000-04-25 | 2001-04-24 | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| HUP0300497A2 true HUP0300497A2 (hu) | 2003-06-28 |
| HUP0300497A3 HUP0300497A3 (en) | 2004-10-28 |
| HU230554B1 HU230554B1 (hu) | 2016-12-28 |
Family
ID=26894992
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0300497A HU230554B1 (hu) | 2000-04-25 | 2001-04-24 | Humán foszfatidilinozit-3-kináz-delta inhibitorok és alkalmazásuk |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US6518277B1 (hu) |
| EP (3) | EP1278748B1 (hu) |
| JP (1) | JP4642309B2 (hu) |
| KR (1) | KR100785363B1 (hu) |
| CN (1) | CN1440408B (hu) |
| AT (1) | ATE502941T1 (hu) |
| AU (2) | AU2001255667C1 (hu) |
| BR (1) | BRPI0110371B8 (hu) |
| CA (1) | CA2406278C (hu) |
| CY (1) | CY1117672T1 (hu) |
| DE (1) | DE60144277D1 (hu) |
| DK (3) | DK2223922T3 (hu) |
| EA (1) | EA008241B1 (hu) |
| ES (3) | ES2567260T3 (hu) |
| GE (1) | GEP20084317B (hu) |
| HK (1) | HK1053308A1 (hu) |
| HR (1) | HRP20020838A2 (hu) |
| HU (1) | HU230554B1 (hu) |
| IL (3) | IL152275A0 (hu) |
| IS (1) | IS2822B (hu) |
| MX (1) | MXPA02010618A (hu) |
| NO (2) | NO329136B1 (hu) |
| NZ (1) | NZ522076A (hu) |
| PT (3) | PT1939203E (hu) |
| RS (1) | RS51458B (hu) |
| SI (2) | SI3029041T1 (hu) |
| WO (1) | WO2001081346A2 (hu) |
Families Citing this family (213)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6545004B1 (en) | 1999-10-27 | 2003-04-08 | Cytokinetics, Inc. | Methods and compositions utilizing quinazolinones |
| US7230000B1 (en) * | 1999-10-27 | 2007-06-12 | Cytokinetics, Incorporated | Methods and compositions utilizing quinazolinones |
| US7671200B2 (en) * | 1999-10-27 | 2010-03-02 | Cytokinetics, Inc. | Quinazolinone KSP inhibitors |
| US6667300B2 (en) * | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| US6608053B2 (en) | 2000-04-27 | 2003-08-19 | Yamanouchi Pharmaceutical Co., Ltd. | Fused heteroaryl derivatives |
| US6403588B1 (en) | 2000-04-27 | 2002-06-11 | Yamanouchi Pharmaceutical Co., Ltd. | Imidazopyridine derivatives |
| US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
| US20030133939A1 (en) | 2001-01-17 | 2003-07-17 | Genecraft, Inc. | Binding domain-immunoglobulin fusion proteins |
| US7829084B2 (en) * | 2001-01-17 | 2010-11-09 | Trubion Pharmaceuticals, Inc. | Binding constructs and methods for use thereof |
| NZ518726A (en) * | 2001-05-09 | 2004-06-25 | Warner Lambert Co | Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor |
| US6689782B2 (en) * | 2001-07-16 | 2004-02-10 | Essential Therapeutics, Inc. | Fungal efflux pump inhibitors |
| AU2002364889A1 (en) * | 2001-09-24 | 2003-06-10 | University Of Aarhus | Methods for diagnosis and treatment of diseases associated with altered expression of nrf2 |
| AU2002346882A1 (en) * | 2001-10-26 | 2003-05-06 | Novartis Ag | Methods for the treatment of osteoarthritis and compositions thereof |
| EP1444209A4 (en) * | 2001-11-07 | 2005-02-16 | Merck & Co Inc | INHIBITORS OF MITOTIC KINESIN |
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