HUP0302669A2 - Pirazolszármazékok és ezeket tartalmazó gyógyszerkészítmények abnormális sejtnövekedés és központi idegrendszeri betegségek kezelésére - Google Patents
Pirazolszármazékok és ezeket tartalmazó gyógyszerkészítmények abnormális sejtnövekedés és központi idegrendszeri betegségek kezeléséreInfo
- Publication number
- HUP0302669A2 HUP0302669A2 HU0302669A HUP0302669A HUP0302669A2 HU P0302669 A2 HUP0302669 A2 HU P0302669A2 HU 0302669 A HU0302669 A HU 0302669A HU P0302669 A HUP0302669 A HU P0302669A HU P0302669 A2 HUP0302669 A2 HU P0302669A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- carbon
- carbon atoms
- members
- general formula
- Prior art date
Links
- 230000002159 abnormal effect Effects 0.000 title abstract 2
- 230000010261 cell growth Effects 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000003217 pyrazoles Chemical class 0.000 title abstract 2
- 230000004770 neurodegeneration Effects 0.000 title 1
- 208000015122 neurodegenerative disease Diseases 0.000 title 1
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000003903 Cyclin-dependent kinases Human genes 0.000 abstract 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 2
- 108090000790 Enzymes Proteins 0.000 abstract 2
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 abstract 2
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 101150053721 Cdk5 gene Proteins 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 101150073031 cdk2 gene Proteins 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic 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
- C07D417/02—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 two hetero rings
- C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Communicable Diseases (AREA)
- Pregnancy & Childbirth (AREA)
- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
A találmány pirazolszármazékokra, ilyen származékokat tartalmazógyógyszerkészítményre, valamint olyan eljárásra vonatkozik, amelyszerint a találmány szerinti származékokat abnormális sejtnövekedés ésbizonyos, a központi idegrendszerrel kapcsolatos betegségek kezelésérelehet alkalmazni. A találmány szerinti vegyületek a cdk5 (ciklinfüggőprotein kináz5) és a cdk2 (ciklinfüggő protein kináz2) enzimekinhibitoraiként hatnak. A találmány szerinti vegyületek inhibitoraiezen kívül a GSK-3 (glikogén szintáz kináz-3) enzimnek. A találmánytárgya (I) általános képletű vegyületek, ahol a képletben R1 jelentése- többek között - adott esetben helyettesített 1-8 szénatomosalkilcsoport, 2-8 szénatomos alkenilcsoport, 2-8 szénatomosalkinilcsoport, 3-8 szénatomos cikloalkilcsoport, 3-8 tagúheterocikloalkilcsoport, 5-11 szénatomos bicikloalkilcsoport, vagy 5-11-tagú heterobicikloalkilcsoport, R2 jelentése hidrogénatom,fluoratom, -CH3, -CN vagy -C(=O)OR7 általános képletű csoport; R3jelentése -C(=O)NR9, -C(=O)O-, -C(=O)(CR10R11)n- vagy -(CR10R11)n-általános képletű csoport, R4 jelentése - többek között - adottesetben helyettesített 3-8 szénatomos cikloalkilcsoport, 4-8szénatomos cikloalkenilcsoport, 3-8 tagú heterocikloalkilcsoport, 5-11szénatomos bicikloalkilcsoport, 7-11 szénatomos bicikloalkenilcsoportvagy 5-11-tagú heterobicikloalkilcsoport, 6-14 szénatomos arilcsoportvagy 5-14-tagú heteroarilcsoport, n értéke 0, 1, 2 vagy 3; vagy ezekgyógyászatilag elfogadható sói. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22941500P | 2000-08-31 | 2000-08-31 | |
| PCT/IB2001/001540 WO2002018346A1 (en) | 2000-08-31 | 2001-08-24 | Pyrazole derivatives and their use as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0302669A2 true HUP0302669A2 (hu) | 2003-12-29 |
| HUP0302669A3 HUP0302669A3 (en) | 2004-03-29 |
Family
ID=22861151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0302669A HUP0302669A3 (en) | 2000-08-31 | 2001-08-24 | Pyrazole derivatives and pharmaceutical compositions containing them for treating diseases comprising abnormal cell growth and neurodegenerative diseases |
Country Status (38)
| Country | Link |
|---|---|
| EP (1) | EP1313710A1 (hu) |
| JP (1) | JP2004507526A (hu) |
| KR (1) | KR20030027093A (hu) |
| CN (1) | CN1518543A (hu) |
| AP (1) | AP2001002266A0 (hu) |
| AR (1) | AR035345A1 (hu) |
| AU (1) | AU2001280009A1 (hu) |
| BG (1) | BG107455A (hu) |
| BR (1) | BR0113574A (hu) |
| CA (1) | CA2420363A1 (hu) |
| CR (1) | CR6881A (hu) |
| CZ (1) | CZ2003468A3 (hu) |
| DO (1) | DOP2001000243A (hu) |
| DZ (1) | DZ3398A1 (hu) |
| EA (1) | EA200300205A1 (hu) |
| EC (1) | ECSP034480A (hu) |
| EE (1) | EE200300085A (hu) |
| GT (1) | GT200100179A (hu) |
| HN (1) | HN2001000192A (hu) |
| HR (1) | HRP20030140A2 (hu) |
| HU (1) | HUP0302669A3 (hu) |
| IL (1) | IL154016A0 (hu) |
| IS (1) | IS6687A (hu) |
| MA (1) | MA26946A1 (hu) |
| MX (1) | MXPA03001785A (hu) |
| NO (1) | NO20030958L (hu) |
| NZ (1) | NZ523656A (hu) |
| OA (1) | OA12368A (hu) |
| PA (1) | PA8528101A1 (hu) |
| PE (1) | PE20020470A1 (hu) |
| PL (1) | PL360742A1 (hu) |
| SK (1) | SK2002003A3 (hu) |
| SV (1) | SV2002000618A (hu) |
| TN (1) | TNSN01132A1 (hu) |
| UY (1) | UY26909A1 (hu) |
| WO (1) | WO2002018346A1 (hu) |
| YU (1) | YU14703A (hu) |
| ZA (1) | ZA200301064B (hu) |
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| EP2298311B1 (en) | 1999-01-13 | 2012-05-09 | Bayer HealthCare LLC | w-Carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors |
| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1317448B2 (en) | 2000-09-15 | 2011-05-04 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| JP4160395B2 (ja) | 2000-12-21 | 2008-10-01 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼインヒビターとして有用なピラゾール化合物 |
| WO2003026649A1 (en) * | 2001-09-27 | 2003-04-03 | Applied Research Systems Ars Holding N.V. | Methods of increasing endogenous testosterone levels |
| US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
| SI1478358T1 (sl) | 2002-02-11 | 2013-09-30 | Bayer Healthcare Llc | Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi |
| CA2492673A1 (en) * | 2002-07-17 | 2004-01-22 | Pharmacia Italia S.P.A. | Heterobicyclic pyrazole derivatives as kinase inhibitors |
| JP2006504725A (ja) | 2002-10-09 | 2006-02-09 | ファイザー・プロダクツ・インク | 神経変性障害治療用ピラゾール化合物 |
| US7582630B2 (en) * | 2002-10-15 | 2009-09-01 | Smithkline Beecham Corporation | Pyradazine compounds as GSK-3 inhibitors |
| WO2004076414A2 (en) * | 2003-02-27 | 2004-09-10 | Smithkline Beecham Corporation | Novel compounds |
| JP2007511203A (ja) | 2003-05-20 | 2007-05-10 | バイエル、ファーマシューテイカルズ、コーポレイション | キナーゼ阻害活性を有するジアリール尿素 |
| US7759382B2 (en) * | 2003-06-05 | 2010-07-20 | Elan Pharmaceuticals, Inc. | Acylated amino acid amidyl pyrazoles and related compounds |
| WO2005012256A1 (en) | 2003-07-22 | 2005-02-10 | Astex Therapeutics Limited | 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators |
| SI1663978T1 (sl) | 2003-07-23 | 2008-02-29 | Bayer Pharmaceuticals Corp | Fluoro substituirana omega-karboksiaril difenil secnina za zdravljenje ali preprecevanje bolezni instanj |
| BRPI0412820A (pt) * | 2003-07-25 | 2006-09-26 | Pfizer | compostos de aminopirazol e utilização como inibidores de chk1 |
| DK1689721T3 (da) * | 2003-11-26 | 2010-09-20 | Pfizer Prod Inc | Aminopyrazolderivater som GSK-3-ihibitorer |
| US7244757B2 (en) | 2004-04-01 | 2007-07-17 | Pfizer Inc | Pyrazole-amine compounds for the treatment of neurodegenerative disorders |
| WO2005103010A2 (en) * | 2004-04-21 | 2005-11-03 | Astrazeneca Ab | Pyrazole derivatives useful for the treatment of cancer |
| WO2005110994A2 (en) | 2004-04-30 | 2005-11-24 | Bayer Pharmaceuticals Corporation | Substituted pyrazolyl urea derivatives useful in the treatment of cancer |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| US7521560B2 (en) | 2004-06-29 | 2009-04-21 | Rigel Pharmaceuticals, Inc. | 2-substituted quinoline compounds and their uses |
| US7491720B2 (en) | 2004-10-29 | 2009-02-17 | Banyu Pharmaceutical Co., Ltd. | Aminopyridine derivatives having Aurora A selective inhibitory action |
| RU2007122485A (ru) | 2004-11-17 | 2008-12-27 | Мийкана Терапьютикс | Ингибиторы киназы |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| PT1846394E (pt) | 2005-02-04 | 2012-01-05 | Astrazeneca Ab | Derivados de pirazolilaminopiridina úteis como inibidores da quinase |
| US20090156582A1 (en) * | 2005-02-09 | 2009-06-18 | Tetsuya Tsukamoto | Pyrazole Compound |
| BRPI0607455A2 (pt) | 2005-02-16 | 2009-09-01 | Astrazeneca Ab | composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica |
| EP1899323A2 (en) | 2005-05-16 | 2008-03-19 | AstraZeneca AB | Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors |
| EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
| CA2620333A1 (en) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP2258358A3 (en) | 2005-08-26 | 2011-09-07 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| KR20140025610A (ko) | 2005-09-30 | 2014-03-04 | 미카나 테라퓨틱스, 인크. | 치환된 피라졸 화합물 |
| EP1940389A2 (en) | 2005-10-21 | 2008-07-09 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| PT1945631E (pt) | 2005-10-28 | 2012-10-15 | Astrazeneca Ab | Derivados de 4-(3-aminopirazole)pirimidina para utilização como inibidores da tirosina-cinase no tratamento do cancro |
| WO2007053596A1 (en) | 2005-10-31 | 2007-05-10 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| JP5249771B2 (ja) | 2005-11-03 | 2013-07-31 | バーテックス ファーマシューティカルズ インコーポレイテッド | キナーゼインヒビターとして有用なアミノピリミジン |
| US7572809B2 (en) * | 2005-12-19 | 2009-08-11 | Hoffmann-La Roche Inc. | Isoquinoline aminopyrazole derivatives |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| CA2651813A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| EP2086642B1 (en) | 2006-10-18 | 2014-06-25 | Periness Ltd. | Dnase for the treatment of male sub-fertility |
| CN101573352A (zh) | 2006-10-21 | 2009-11-04 | 艾博特股份有限两合公司 | 杂环化合物和其作为糖原合酶激酶3抑制剂的用途 |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| US7737149B2 (en) * | 2006-12-21 | 2010-06-15 | Astrazeneca Ab | N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof |
| US8093268B2 (en) | 2007-01-24 | 2012-01-10 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-) |
| MX2010000617A (es) | 2007-07-17 | 2010-05-17 | Plexxikon Inc | Compuestos y metodos para modulacion de cinasa, e indicaciones de estos. |
| WO2009017453A1 (en) * | 2007-07-30 | 2009-02-05 | Astrazeneca Ab | New therapeutic combination of an antipsychotic and a gsk3 inhibitor 958 |
| EP3078662A1 (en) | 2007-09-21 | 2016-10-12 | Array Biopharma, Inc. | Pyridin-2-yl-amino-1,2,4-thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus |
| JPWO2009130900A1 (ja) * | 2008-04-24 | 2011-08-11 | 日本曹達株式会社 | オキシム誘導体、中間体化合物および植物病害防除剤 |
| US20100216805A1 (en) | 2009-02-25 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| SG173178A1 (en) | 2009-04-03 | 2011-09-29 | Hoffmann La Roche | Propane- i-sulfonic acid {3- [5- (4 -chloro-phenyl) -1h-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof |
| US20110081316A1 (en) * | 2009-10-02 | 2011-04-07 | Vertex Pharmaceuticals Incorporated | Pyrazole inhibitors of phosphatidylinositol 3-kinase |
| JP2013510166A (ja) | 2009-11-06 | 2013-03-21 | プレキシコン インコーポレーテッド | キナーゼ調節のための化合物、方法およびその適用 |
| US9266855B2 (en) | 2010-09-27 | 2016-02-23 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| RS58455B1 (sr) | 2011-02-07 | 2019-04-30 | Plexxikon Inc | Jedinjenja i postupci za modulaciju kinaze, i indikacije za njih |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| EP3033339B1 (en) | 2013-08-16 | 2018-02-28 | Merck Patent GmbH | 3-substituted cyclopentylamine derivatives |
| CN106580986B (zh) * | 2016-11-28 | 2017-09-15 | 王保亮 | 一种治疗少弱精子症的药物组合物 |
| US11084825B2 (en) | 2018-12-31 | 2021-08-10 | Biomea Fusion, Llc | Substituted pyridines as irreversible inhibitors of menin-MLL interaction |
| EP3906029A4 (en) | 2018-12-31 | 2022-09-21 | Biomea Fusion, LLC | INHIBITORS OF MENIN-MLL INTERACTION |
| JP7094456B2 (ja) * | 2019-01-31 | 2022-07-01 | ファイザー・インク | Ｃｄｋ２阻害剤 |
| TW202229268A (zh) * | 2020-12-22 | 2022-08-01 | 大陸商上海拓界生物醫藥科技有限公司 | Ｃｄｋ２抑制劑及其製備方法 |
| MX2023013173A (es) | 2021-05-07 | 2023-11-30 | Kymera Therapeutics Inc | Degradadores de cinasa 2 dependiente de ciclina (cdk2) y sus usos. |
| US11932648B2 (en) | 2021-06-28 | 2024-03-19 | Blueprint Medicines Corporation | CDK2 inhibitors |
| TW202317564A (zh) * | 2021-07-01 | 2023-05-01 | 大陸商上海拓界生物醫藥科技有限公司 | Cdk2抑制劑及其製備方法和用途 |
| MX2024002189A (es) | 2021-08-20 | 2024-06-11 | Biomea Fusion Inc | Forma cristalina de n-[4-[4-(4-morfolinil)-7h-pirrolo[2,3-d]pirimi din-6-il]fenil]-4-[[3(r)-[(1-oxo)-2-propen-1-il)amino]-1-piperidi nil]metil]-2-piridinacarboxamida, un inhibidor irreversible de menina-mll para el tratamiento del cancer. |
| TW202325280A (zh) * | 2021-11-09 | 2023-07-01 | 大陸商上海拓界生物醫藥科技有限公司 | 一種胺基吡唑衍生物及其製備方法和用途 |
| WO2023092088A1 (en) * | 2021-11-19 | 2023-05-25 | Blueprint Medicines Corporation | Cdk2 inhibitors and methods of making and using same |
| WO2023239629A1 (en) * | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Compounds and pharmaceutical compositions that degrade cdk2 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100571588B1 (ko) * | 1997-12-22 | 2006-04-17 | 바이엘 코포레이션 | 치환 헤테로시클릭 우레아를 이용한 ｒａｆ 키나제의 억제 |
| KR100579792B1 (ko) * | 1998-05-13 | 2006-05-12 | 동화약품공업주식회사 | 신규 2,5-피리딘디카복실산 유도체 |
| GB9811427D0 (en) * | 1998-05-29 | 1998-07-22 | Zeneca Ltd | Chemical compounds |
| EP1199306B1 (en) * | 1999-07-26 | 2005-12-07 | Banyu Pharmaceutical Co., Ltd. | Biarylurea derivatives |
| US6387900B1 (en) * | 1999-08-12 | 2002-05-14 | Pharmacia & Upjohn S.P.A. | 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents |
| EA005373B1 (ru) * | 1999-08-12 | 2005-02-24 | Фармация Италия С.П.А. | Производные 3(5)-аминопиразола, способ их получения и их применение в качестве противоопухолевых средств |
| CN1402720A (zh) * | 1999-11-30 | 2003-03-12 | 辉瑞产品公司 | 用作免疫抑制剂的2,4－二氨基嘧啶化合物 |
| MXPA02010222A (es) * | 2000-04-18 | 2003-05-23 | Agouron Pharma | Pirazoles para inhibir proteina cinasa. |
-
2001
- 2001-08-24 JP JP2002523464A patent/JP2004507526A/ja active Pending
- 2001-08-24 NZ NZ523656A patent/NZ523656A/en unknown
- 2001-08-24 KR KR10-2003-7002894A patent/KR20030027093A/ko not_active Application Discontinuation
- 2001-08-24 OA OA1200300050A patent/OA12368A/en unknown
- 2001-08-24 AP APAP/P/2001/002266A patent/AP2001002266A0/en unknown
- 2001-08-24 MX MXPA03001785A patent/MXPA03001785A/es not_active Application Discontinuation
- 2001-08-24 AU AU2001280009A patent/AU2001280009A1/en not_active Abandoned
- 2001-08-24 DZ DZ013398A patent/DZ3398A1/xx active
- 2001-08-24 WO PCT/IB2001/001540 patent/WO2002018346A1/en not_active Application Discontinuation
- 2001-08-24 IL IL15401601A patent/IL154016A0/xx unknown
- 2001-08-24 EE EEP200300085A patent/EE200300085A/xx unknown
- 2001-08-24 SK SK200-2003A patent/SK2002003A3/sk not_active Application Discontinuation
- 2001-08-24 CA CA002420363A patent/CA2420363A1/en not_active Abandoned
- 2001-08-24 YU YU14703A patent/YU14703A/sh unknown
- 2001-08-24 EA EA200300205A patent/EA200300205A1/ru unknown
- 2001-08-24 CZ CZ2003468A patent/CZ2003468A3/cs unknown
- 2001-08-24 CN CNA018147615A patent/CN1518543A/zh active Pending
- 2001-08-24 BR BR0113574-0A patent/BR0113574A/pt not_active IP Right Cessation
- 2001-08-24 PL PL36074201A patent/PL360742A1/xx not_active Application Discontinuation
- 2001-08-24 EP EP01958287A patent/EP1313710A1/en not_active Withdrawn
- 2001-08-24 HU HU0302669A patent/HUP0302669A3/hu unknown
- 2001-08-27 UY UY26909A patent/UY26909A1/es not_active Application Discontinuation
- 2001-08-28 HN HN2001000192A patent/HN2001000192A/es unknown
- 2001-08-29 PE PE2001000872A patent/PE20020470A1/es not_active Application Discontinuation
- 2001-08-29 AR ARP010104115A patent/AR035345A1/es unknown
- 2001-08-29 DO DO2001000243A patent/DOP2001000243A/es unknown
- 2001-08-30 GT GT200100179A patent/GT200100179A/es unknown
- 2001-08-30 TN TNTNSN01132A patent/TNSN01132A1/fr unknown
- 2001-08-30 SV SV2001000618A patent/SV2002000618A/es unknown
- 2001-08-31 PA PA20018528101A patent/PA8528101A1/es unknown
-
2003
- 2003-01-13 BG BG107455A patent/BG107455A/xx unknown
- 2003-01-15 CR CR6881A patent/CR6881A/es not_active Application Discontinuation
- 2003-01-16 IS IS6687A patent/IS6687A/is unknown
- 2003-02-07 ZA ZA200301064A patent/ZA200301064B/en unknown
- 2003-02-17 EC EC2003004480A patent/ECSP034480A/es unknown
- 2003-02-21 MA MA27050A patent/MA26946A1/fr unknown
- 2003-02-26 HR HR20030140A patent/HRP20030140A2/hr not_active Application Discontinuation
- 2003-02-28 NO NO20030958A patent/NO20030958L/no not_active Application Discontinuation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HUP0302669A2 (hu) | Pirazolszármazékok és ezeket tartalmazó gyógyszerkészítmények abnormális sejtnövekedés és központi idegrendszeri betegségek kezelésére | |
| WO2002092573A3 (en) | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases | |
| HUP0303069A2 (hu) | Imidazolszármazékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk | |
| TW200728305A (en) | Spiropiperidine beta-sectetase inhibitors for the treatment of alzheimer's disease | |
| TW200716531A (en) | Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia | |
| MXPA03011652A (es) | 5-(2-aminopirimidin-4-il) benzioxazoles como inhibidores de proteinas cinasa. | |
| TNSN07279A1 (en) | Pyrazole derivatives for the inhibition of cdk's and gsk's | |
| HUP9802224A1 (hu) | Pirazolszármazékok, eljárás előállításukra, és gyógyszerként történő alkalmazásuk | |
| MXPA05008172A (es) | Derivados de malonamida como inhibidores gamma-secretasa. | |
| SI1678166T1 (sl) | Inhibitorji proteinske kinaze | |
| HUP0401987A2 (hu) | A triazolil-imidazopiridin és a triazolilpurin vegyületek adenozin-a2A-receptorligandumként használható származékai és gyógyszerként történő alkalmazásuk | |
| MX2009013213A (es) | Indazoles 5-sustituidos 5-heteroarilo como inhibidores de cinasa. | |
| HUP0302487A2 (hu) | Új mandulasavszármazékok és felhasználásuk trombin inhibitorokként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
| WO2008030412A3 (en) | Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease | |
| NO20062726L (no) | Nye pyridazin-3(2H)-on derivater | |
| HU230344B1 (hu) | Pirrolopirimidinon-származékok, a vegyületek előállítása és alkalmazása | |
| JO2293B1 (en) | Derivatives of 3-indoleil 4-phenyl-1H-birol-5.2 -Dayon as inhibitors of glycogen synthacinase-3b | |
| WO2005065195A3 (en) | Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease | |
| WO2006044497A3 (en) | Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer’s disease | |
| EP1841426A4 (en) | TERTIARY CARBINAMINES INCLUDING SUBSTITUTED HETEROCYCLES AS BETA SECRETASE INHIBITORS AND FOR THE TREATMENT OF ALZHEIMER'S DISEASE | |
| NO20053748L (no) | Pyrrolopyridazinderivater. | |
| EP2091328A4 (en) | SPIROPIPERIDININHIBITORS OF BETA-SECRETASE FOR THE TREATMENT OF ALZHEIMER DISEASE | |
| ATE512147T1 (de) | Makrozyklische aminiopyridyl-beta-sekretase- hemmer zur behandlung von morbus alzheimer | |
| DE602008001725D1 (de) | 1-(1-benzylpiperidin-4-yl)benzimidazol-5-carbonsäurederivate zur behandlung von diabetes mellitus | |
| PL1685142T3 (pl) | Pochodne kwasu fosfinowego, inhibitory beta-sekterazy do leczenia choroby Alzheimera |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |