HRP20141034T1 - Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza - Google Patents
Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza Download PDFInfo
- Publication number
- HRP20141034T1 HRP20141034T1 HRP20141034AT HRP20141034T HRP20141034T1 HR P20141034 T1 HRP20141034 T1 HR P20141034T1 HR P20141034A T HRP20141034A T HR P20141034AT HR P20141034 T HRP20141034 T HR P20141034T HR P20141034 T1 HRP20141034 T1 HR P20141034T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- carcinoma
- compound according
- phenyl
- preparation
- Prior art date
Links
- IIRWNGPLJQXWFJ-KRWDZBQOSA-N (1s)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)phenyl]ethanol Chemical compound C1([C@](O)(CN)C=2C=CC(=CC=2)C2=CNN=C2)=CC=C(Cl)C=C1 IIRWNGPLJQXWFJ-KRWDZBQOSA-N 0.000 title claims 2
- 102000001253 Protein Kinase Human genes 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 108060006633 protein kinase Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 13
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000012458 free base Substances 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- IIRWNGPLJQXWFJ-UHFFFAOYSA-N 2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)phenyl]ethanol Chemical compound C=1C=C(C2=CNN=C2)C=CC=1C(O)(CN)C1=CC=C(Cl)C=C1 IIRWNGPLJQXWFJ-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000017897 Carcinoma of esophagus Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 206010016935 Follicular thyroid cancer Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061534 Oesophageal squamous cell carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000036765 Squamous cell carcinoma of the esophagus Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000008275 breast carcinoma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005619 esophageal carcinoma Diseases 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 208000010979 non-small cell squamous lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
- C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
- C07C215/30—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
- C07C215/32—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton containing hydroxy groups and carbon atoms of two six-membered aromatic rings bound to the same carbon atom of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C247/00—Compounds containing azido groups
- C07C247/02—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
- C07C247/08—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated
- C07C247/10—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being unsaturated and containing rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
- C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
-
- 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
- C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Claims (13)
1. Pripravak koji sadrži 2-amino-1-(4-klorlo-fenil)-1-[4-(1H-pirazol-4-il)-fenil]-etanol ili neku njegovu sol, solvat, tautomer ili N-oksid, od kojih je najmanje 90% u obliku S-enantiomera.
2. Pripravak prema zahtjevu 1 naznačen time da je najmanje 98% u obliku S-enantiomera.
3. Pripravak prema zahtjevu 1 naznačen time da je najmanje 99% u obliku S-enantiomera.
4. Pripravak prema bilo kojem od prethodnih zahtjeva naznačen time da je (S)-2-amino-1-(4-klorlo-fenil)-1-[4-(1Hpirazol-4-il)-fenil]-etanol u obliku aditivne soli neke slobodne baze ili kiseline.
5. Spoj čija je formula (I):
[image]
ili neka njegova sol, solvat, tautomer ili N-oksid, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 90%.
6. Spoj prema zahtjevu 5, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 98%.
7. Spoj prema zahtjevu 5, naznačen time da taj spoj ima enantiomernu čistoću od najmanje 99%.
8. Spoj formule (I) prema bilo kojem od zahtjeva 5 do 7, u obliku neke slobodne baze ili njene soli, solvata ili tautomera.
9. Spoj prema bilo kojem od zahtjeva 5 do 8 koji je di-sol oblikovana s klorovodičnom kiselinom.
10. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9 i neki farmaceutski prihvatljiv nosač.
11. Pripravak prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9 za primjenu u medicini.
12. Pripravak prema bilo kojem od zahtjeva 1 do 4 ili spoj prema bilo kojem od zahtjeva 5 do 9, za primjenu u profilaksi ili liječenju nekog bolesnog stanja ili bolesti iz skupine u koju spadaju karcinom mokraćnog mjehura, dojke, debelog crijeva, bubrega, epidermalni karcinom, karcinom jetre, pluća, jednjaka, žučnog mjehura, jajnika, gušterače, želuca, grlića maternice, sluznice maternice, štitnjače, prostate ili kože, hematopoetski tumor limfoidnog podrijetla, hematopoetski tumor mijeloidnog podrijetla, folikularni karcinom štitnjače, tumor mezenhimalnog podrijetla, tumor središnjeg ili perifernog živčanog sustava, melanom, seminom, teratokarcinom, osteosarkom, kseroderma pigmentosum, keratoktantom, folikularni karcinom štitnjače ili Kaposijev sarkom, karcinom dojke, karconom jajnika, karcinom debelog crijeva, karcinom jednjaka, karcinom skvamoznih stanica i nesitnostanični karcinomi pluća.
13. Uporaba pripravka prema bilo kojem od zahtjeva 1 do 4 ili spoja prema bilo kojem od zahtjeva 5 do 9 za proizvodnju nekog lijeka za profilaksu ili liječenje bilo kojeg od bolesnih stanja ili bolesti navedenih u zahtjevu 12.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89475207P | 2007-03-14 | 2007-03-14 | |
| GBGB0704932.3A GB0704932D0 (en) | 2007-03-14 | 2007-03-14 | Pharmaceutical compounds |
| PCT/GB2008/050180 WO2008110846A2 (en) | 2007-03-14 | 2008-03-14 | Compositions comprising (s)-2-amino-1-(4-chlorophenyl)-1-[4-(1h-pyrazol-4-yl)-phenyl]-ethanol as modulator of protein kinases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20141034T1 true HRP20141034T1 (hr) | 2014-12-19 |
Family
ID=38008428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20141034AT HRP20141034T1 (hr) | 2007-03-14 | 2014-10-27 | Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US20100113551A1 (hr) |
| EP (2) | EP2433632A1 (hr) |
| JP (2) | JP2010521446A (hr) |
| KR (1) | KR20100014720A (hr) |
| CN (1) | CN101686965B (hr) |
| AU (1) | AU2008224657B2 (hr) |
| BR (1) | BRPI0808802A2 (hr) |
| CA (1) | CA2679878A1 (hr) |
| CY (1) | CY1115877T1 (hr) |
| DK (1) | DK2134339T3 (hr) |
| ES (1) | ES2511817T3 (hr) |
| GB (1) | GB0704932D0 (hr) |
| HK (1) | HK1133828A1 (hr) |
| HR (1) | HRP20141034T1 (hr) |
| IL (1) | IL200822A (hr) |
| MX (1) | MX2009009874A (hr) |
| NZ (1) | NZ579341A (hr) |
| PL (1) | PL2134339T3 (hr) |
| PT (1) | PT2134339E (hr) |
| RS (1) | RS53580B1 (hr) |
| RU (1) | RU2527151C2 (hr) |
| SI (1) | SI2134339T1 (hr) |
| WO (1) | WO2008110846A2 (hr) |
| ZA (1) | ZA200906303B (hr) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2228369A1 (en) | 2003-12-23 | 2010-09-15 | Astex Therapeutics Ltd. | Pyrazole derivatives as protein kinase modulators |
| US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
| JP5345842B2 (ja) | 2005-06-23 | 2013-11-20 | アステックス・セラピューティクス・リミテッド | プロテインキナーゼモジュレーターとしてのピラゾール誘導体を含む医薬組み合わせ |
| GB0704932D0 (en) | 2007-03-14 | 2007-04-25 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| JOP20190231A1 (ar) * | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| MX2016011361A (es) * | 2014-03-06 | 2017-05-08 | Univ Southern California | Utilización de régimen de ayuno a corto plazo en combinación con inhibidores de cinasa para potenciar la eficacia y viabilidad de fármacos quimioterápicos tradicionales e invertir los efectos secundarios de cinasas en células y tejidos normales. |
| RU2657832C1 (ru) * | 2017-06-07 | 2018-06-15 | федеральное государственное автономное образовательное учреждение высшего образования "Южный федеральный университет" | Антидиабетическое средство |
| EP3424533A1 (en) * | 2017-07-05 | 2019-01-09 | Nh Theraguix | Methods for treating tumors |
| US10696638B2 (en) | 2017-12-26 | 2020-06-30 | Industrial Technology Research Institute | Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same |
| CA3169944A1 (en) * | 2020-03-25 | 2021-09-30 | Thomas Macallister | Methods of using rho kinase inhibitors to treat frontotemporal dementia |
| CN111707830B (zh) * | 2020-07-16 | 2023-08-15 | 首都医科大学附属北京朝阳医院 | Rock激酶活性在辅助诊断肺损害中的应用 |
Family Cites Families (68)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4666828A (en) | 1984-08-15 | 1987-05-19 | The General Hospital Corporation | Test for Huntington's disease |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| US4801531A (en) | 1985-04-17 | 1989-01-31 | Biotechnology Research Partners, Ltd. | Apo AI/CIII genomic polymorphisms predictive of atherosclerosis |
| US5272057A (en) | 1988-10-14 | 1993-12-21 | Georgetown University | Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase |
| CA2046628A1 (en) | 1989-02-08 | 1990-08-09 | Dee W. Brooks | 4-hydroxythiazoles as 5-lipoxygenase inhibitors |
| US5192659A (en) | 1989-08-25 | 1993-03-09 | Genetype Ag | Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes |
| US5049570A (en) | 1990-01-23 | 1991-09-17 | Du Pont Merck Pharmaceutical Company | Pyridylphenyl nitrogen heterocycle-substituted carbinols and derivatives thereof with anti-inflammatory activity |
| FR2707295A1 (fr) | 1993-06-07 | 1995-01-13 | Rhone Poulenc Agrochimie | Fongicides pyrazoles substitués en position 3 par un hétérocycle. |
| US6756388B1 (en) | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| US5532356A (en) | 1995-06-06 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Method for preparing N,N'-disubstituted cyclic ureas |
| GB9512961D0 (en) | 1995-06-26 | 1995-08-30 | Pfizer Ltd | Antifungal agents |
| US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
| CA2262403C (en) | 1995-07-31 | 2011-09-20 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
| EP0891343A1 (en) | 1996-04-03 | 1999-01-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| GB2314327B (en) | 1996-04-30 | 2000-07-12 | Kodak Ltd | Pyrazolone image dye-forming couplers |
| AR008789A1 (es) | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
| WO1998025617A1 (en) | 1996-12-13 | 1998-06-18 | Merck & Co., Inc. | Substituted aryl piperazines as modulators of chemokine receptor activity |
| US6020357A (en) | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| GB9700555D0 (en) | 1997-01-13 | 1997-03-05 | Merck Sharp & Dohme | Therapeutic agents |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| AU751139B2 (en) | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
| CA2319465C (en) | 1998-01-29 | 2013-03-19 | Viropharma Incorporated | Compounds, compositions and methods for treating or preventing pneumovirus infection and associated diseases |
| GB9804734D0 (en) | 1998-03-05 | 1998-04-29 | Pfizer Ltd | Compounds |
| JP2002522422A (ja) | 1998-08-07 | 2002-07-23 | カイロン コーポレイション | エストロゲンレセプターモジュレーターとしてのピラゾール |
| HN1999000149A (es) | 1998-09-09 | 2000-01-12 | Pfizer Prod Inc | Derivados de 4,4-biarilpiperidina |
| US6503905B1 (en) | 1998-12-29 | 2003-01-07 | Pfizer Inc | 3,3-biarylpiperidine and 2,2-biarylmorpholine derivatives |
| AU4308300A (en) | 1999-05-03 | 2000-11-17 | Dr. Reddy's Research Foundation | Pyrazoles having antiinflammatory activity |
| EP1185530A1 (en) | 1999-05-14 | 2002-03-13 | Neurocrine Biosciences, Inc. | Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists |
| US6632815B2 (en) | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| RU2002110295A (ru) | 1999-09-17 | 2003-12-10 | Милленниум Фармасьютикалс, Инк. (Us) | Ингибиторы фактора Ха |
| CZ2002961A3 (cs) | 1999-09-17 | 2002-08-14 | Millennium Pharmaceuticals, Inc. | Benzamidy a příbuzné sloučeniny pro inhibici faktoru Xa |
| US7393842B2 (en) | 2001-08-31 | 2008-07-01 | University Of Connecticut | Pyrazole analogs acting on cannabinoid receptors |
| US6455525B1 (en) | 1999-11-04 | 2002-09-24 | Cephalon, Inc. | Heterocyclic substituted pyrazolones |
| ATE311366T1 (de) | 2000-02-29 | 2005-12-15 | Millennium Pharm Inc | Benzamide und ähnliche inhibitoren vom faktor xa |
| IL136458A0 (en) | 2000-05-30 | 2001-06-14 | Peptor Ltd | Protein kinase inhibitors |
| US6511994B2 (en) | 2000-10-11 | 2003-01-28 | Merck & Co., Inc. | Modulators of CCR5 chemokine receptor activity |
| MXPA03009847A (es) | 2001-04-27 | 2004-02-12 | Vertex Pharma | Inhibidores de cinasa derivados de pirazol. |
| DE60226154T2 (de) | 2001-08-03 | 2009-05-20 | Vertex Pharmaceuticals Inc., Cambridge | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
| FR2830192B1 (fr) | 2001-09-28 | 2004-08-20 | Oreal | Composition tinctoriale comprenant une base d'oxydation du type diaminopyrazole et un coupleur pyrazolo-azole |
| WO2003048081A2 (en) | 2001-12-04 | 2003-06-12 | Bristol-Myers Squibb Company | Glycinamides as factor xa inhibitors |
| WO2003059884A1 (en) | 2001-12-21 | 2003-07-24 | X-Ceptor Therapeutics, Inc. | Modulators of lxr |
| BR0307631A (pt) | 2002-02-14 | 2004-12-21 | Pharmacia Corp | Piridinonas substituìdas como moduladores de p38 map-quinase |
| CN101172983A (zh) | 2002-03-20 | 2008-05-07 | 麦它波莱克斯股份有限公司 | 取代的苯乙酸 |
| WO2003086247A1 (en) | 2002-04-08 | 2003-10-23 | Barosense, Inc. | Satiation devices and methods |
| US20050026929A1 (en) | 2002-04-23 | 2005-02-03 | Axys Pharmaceuticals, Inc. | Novel phenyl derivatives as inducers of apoptosis |
| EP1542997B1 (en) | 2002-07-24 | 2012-02-29 | Dermira (Canada), Inc. | Pyrazolylbenzothiazole derivatives and their use as therapeutic agents |
| WO2004026819A2 (en) | 2002-09-18 | 2004-04-01 | The Curators Of The University Of Missouri | OPIATE ANALOGS SELECTIVE FOR THE delta-OPIOID RECEPTOR |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| JP4847868B2 (ja) | 2003-05-14 | 2011-12-28 | ニューロジェネティック ファーマシューティカルズ、 インコーポレイテッド | 化合物、及び、アミロイドベータの調節におけるその使用 |
| EP1644365A2 (en) | 2003-07-02 | 2006-04-12 | Biofocus Discovery Ltd | Pyrazine and pyridine derivatives as rho kinase inhibitors |
| MXPA06000794A (es) | 2003-07-22 | 2006-08-23 | Astex Therapeutics Ltd | Compuestos 1h-pirazola 3,4-disustituida y su uso como moduladores de quinasas dependientes de ciclina (cdk) y quinasa-3 de sintasa de glicogeno (gsr-3). |
| KR101163800B1 (ko) | 2003-10-15 | 2012-07-09 | 산텐 세이야꾸 가부시키가이샤 | 신규 인다졸 유도체 |
| JP2007512255A (ja) | 2003-11-13 | 2007-05-17 | アンビット バイオサイエンシス コーポレーション | キナーゼ調節因子としての尿素誘導体 |
| EP1692112A4 (en) | 2003-12-08 | 2008-09-24 | Cytokinetics Inc | COMPOUNDS, COMPOSITIONS, AND METHODS |
| RU2419612C2 (ru) * | 2003-12-23 | 2011-05-27 | Астекс Терапьютикс Лимитед | Производные пиразола в качестве модуляторов протеинкиназы |
| EP2228369A1 (en) | 2003-12-23 | 2010-09-15 | Astex Therapeutics Ltd. | Pyrazole derivatives as protein kinase modulators |
| GB0329617D0 (en) * | 2003-12-23 | 2004-01-28 | Astex Technology Ltd | Pharmaceutical compounds |
| AU2005249380C1 (en) | 2004-04-23 | 2012-09-20 | Exelixis, Inc. | Kinase modulators and methods of use |
| UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
| JP5274842B2 (ja) | 2004-12-28 | 2013-08-28 | エグゼリクシス， インコーポレイテッド | 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物 |
| WO2006091450A1 (en) | 2005-02-18 | 2006-08-31 | Lexicon Genetics Incorporated | 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds |
| AR054485A1 (es) * | 2005-06-21 | 2007-06-27 | Cancer Rec Tech Ltd | ARIL-ALQUILAMINAS Y HETEROARIL-ALQUILAMINAS COMO INHIBIDORES DE PROTEINA QUINASA A Y B, UN PROCESO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO O PROFILAXIS DE ENFERMEDADES ORIGINADAS EN EL CRECIMIENTO ANORMAL DE LA |
| WO2006136823A1 (en) | 2005-06-21 | 2006-12-28 | Astex Therapeutics Limited | Heterocyclic containing amines as kinase b inhibitors |
| GB2427406A (en) | 2005-06-21 | 2006-12-27 | Astex Technology Ltd | Silicon-containing PKB/PKA kinase inhibitors |
| JP2008543919A (ja) | 2005-06-21 | 2008-12-04 | アステックス・セラピューティクス・リミテッド | 医薬化合物 |
| US8343953B2 (en) | 2005-06-22 | 2013-01-01 | Astex Therapeutics Limited | Pharmaceutical compounds |
| JP5345842B2 (ja) * | 2005-06-23 | 2013-11-20 | アステックス・セラピューティクス・リミテッド | プロテインキナーゼモジュレーターとしてのピラゾール誘導体を含む医薬組み合わせ |
| GB0704932D0 (en) | 2007-03-14 | 2007-04-25 | Astex Therapeutics Ltd | Pharmaceutical compounds |
-
2007
- 2007-03-14 GB GBGB0704932.3A patent/GB0704932D0/en not_active Ceased
-
2008
- 2008-03-14 RU RU2009137779/04A patent/RU2527151C2/ru not_active IP Right Cessation
- 2008-03-14 CN CN200880015813.0A patent/CN101686965B/zh not_active Expired - Fee Related
- 2008-03-14 EP EP11194939A patent/EP2433632A1/en not_active Withdrawn
- 2008-03-14 SI SI200831312T patent/SI2134339T1/sl unknown
- 2008-03-14 MX MX2009009874A patent/MX2009009874A/es active IP Right Grant
- 2008-03-14 US US12/531,013 patent/US20100113551A1/en not_active Abandoned
- 2008-03-14 PL PL08719025T patent/PL2134339T3/pl unknown
- 2008-03-14 BR BRPI0808802A patent/BRPI0808802A2/pt not_active IP Right Cessation
- 2008-03-14 JP JP2009553222A patent/JP2010521446A/ja active Pending
- 2008-03-14 PT PT87190252T patent/PT2134339E/pt unknown
- 2008-03-14 RS RSP20140587 patent/RS53580B1/en unknown
- 2008-03-14 KR KR1020097020516A patent/KR20100014720A/ko not_active Application Discontinuation
- 2008-03-14 CA CA002679878A patent/CA2679878A1/en not_active Abandoned
- 2008-03-14 WO PCT/GB2008/050180 patent/WO2008110846A2/en active Application Filing
- 2008-03-14 DK DK08719025.2T patent/DK2134339T3/da active
- 2008-03-14 ES ES08719025.2T patent/ES2511817T3/es active Active
- 2008-03-14 EP EP08719025.2A patent/EP2134339B1/en active Active
- 2008-03-14 AU AU2008224657A patent/AU2008224657B2/en not_active Ceased
- 2008-03-14 NZ NZ579341A patent/NZ579341A/xx not_active IP Right Cessation
-
2009
- 2009-09-08 IL IL200822A patent/IL200822A/en not_active IP Right Cessation
- 2009-09-10 ZA ZA2009/06303A patent/ZA200906303B/en unknown
-
2010
- 2010-01-08 HK HK10100202.2A patent/HK1133828A1/xx not_active IP Right Cessation
-
2011
- 2011-07-11 US US13/180,127 patent/US8497294B2/en not_active Expired - Fee Related
-
2014
- 2014-08-25 JP JP2014170885A patent/JP2015028033A/ja active Pending
- 2014-10-27 HR HRP20141034AT patent/HRP20141034T1/hr unknown
- 2014-11-12 CY CY20141100938T patent/CY1115877T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200906303B (en) | 2015-08-26 |
| WO2008110846A2 (en) | 2008-09-18 |
| WO2008110846A3 (en) | 2009-03-05 |
| MX2009009874A (es) | 2009-09-24 |
| EP2134339B1 (en) | 2014-09-17 |
| IL200822A (en) | 2016-09-29 |
| PL2134339T3 (pl) | 2015-04-30 |
| CA2679878A1 (en) | 2008-09-18 |
| KR20100014720A (ko) | 2010-02-10 |
| PT2134339E (pt) | 2014-11-03 |
| AU2008224657B2 (en) | 2014-06-26 |
| IL200822A0 (en) | 2010-05-17 |
| EP2433632A1 (en) | 2012-03-28 |
| AU2008224657A1 (en) | 2008-09-18 |
| ES2511817T3 (es) | 2014-10-23 |
| GB0704932D0 (en) | 2007-04-25 |
| CN101686965B (zh) | 2014-09-17 |
| BRPI0808802A2 (pt) | 2017-05-02 |
| HK1133828A1 (en) | 2010-04-09 |
| US20100113551A1 (en) | 2010-05-06 |
| NZ579341A (en) | 2012-08-31 |
| US20110269808A1 (en) | 2011-11-03 |
| RS53580B1 (en) | 2015-02-27 |
| CY1115877T1 (el) | 2017-01-25 |
| JP2010521446A (ja) | 2010-06-24 |
| JP2015028033A (ja) | 2015-02-12 |
| DK2134339T3 (da) | 2014-11-03 |
| EP2134339A2 (en) | 2009-12-23 |
| CN101686965A (zh) | 2010-03-31 |
| RU2527151C2 (ru) | 2014-08-27 |
| SI2134339T1 (sl) | 2014-12-31 |
| US8497294B2 (en) | 2013-07-30 |
| RU2009137779A (ru) | 2011-05-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20141034T1 (hr) | Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza | |
| CN102816175B (zh) | 一种杂环并吡啶酮类化合物,其中间体、制备方法和用途 | |
| CN101675053B (zh) | 磷酸肌醇3-激酶抑制剂化合物及使用方法 | |
| CN104039798B (zh) | 具有蛋白激酶抑制活性的噻吩并[3，2-d]嘧啶衍生物 | |
| CN103402519B (zh) | 肿瘤治疗剂 | |
| PH12018550049A1 (en) | Protein kinase inhibitor, preparation method and medical use thereof | |
| JP2011126896A5 (hr) | ||
| JP2010528026A5 (hr) | ||
| US20130281397A1 (en) | Treatment of diseases by epigenetic regulation | |
| CN101932587A (zh) | 噻唑并嘧啶pi3k抑制剂化合物及使用方法 | |
| JP2015529229A5 (hr) | ||
| HRP20220864T1 (hr) | Derivati n-piridinil acetamida kao inhibitori signalnog puta wnt | |
| JP2010518110A5 (hr) | ||
| JP2015524450A5 (hr) | ||
| JP2015529234A5 (hr) | ||
| HRP20171783T1 (hr) | Derivati imidazopirazinona | |
| HRP20160044T1 (hr) | Novi spojevi fenilamino izonikotinamida | |
| HRP20201681T1 (hr) | Inhibitor aurora a kinaze | |
| JP2015511609A5 (hr) | ||
| CN111484482B (zh) | 炔基嘧啶或炔基吡啶类化合物、及其组合物与应用 | |
| JP2014509653A5 (hr) | ||
| CN103140484A (zh) | 环状胺氮杂杂环甲酰胺 | |
| TR201815685T4 (tr) | Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları. | |
| US10745433B2 (en) | Compounds for inhibiting cancer and virus | |
| EP3052504B1 (en) | Conformationally restricted pi3k and mtor inhibitors |