AR039564A1 - Derivados de carbonilamino como inhibidores de desacetilasa de histona, composiciones farmaceuticas y procesos de preparacion del compuesto y de las composiciones que lo contienen - Google Patents
Derivados de carbonilamino como inhibidores de desacetilasa de histona, composiciones farmaceuticas y procesos de preparacion del compuesto y de las composiciones que lo contienenInfo
- Publication number
- AR039564A1 AR039564A1 ARP030100852A ARP030100852A AR039564A1 AR 039564 A1 AR039564 A1 AR 039564A1 AR P030100852 A ARP030100852 A AR P030100852A AR P030100852 A ARP030100852 A AR P030100852A AR 039564 A1 AR039564 A1 AR 039564A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- alkyloxy
- aminoalkyl
- aminoc
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 238000002360 preparation method Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title abstract 2
- 108010033040 Histones Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 57
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 32
- -1 methylimidazolyl Chemical group 0.000 abstract 23
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 16
- 125000003545 alkoxy group Chemical group 0.000 abstract 15
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000003118 aryl group Chemical group 0.000 abstract 7
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 6
- 125000003282 alkyl amino group Chemical group 0.000 abstract 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 5
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 4
- 125000002541 furyl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 3
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 abstract 3
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 3
- 229910052799 carbon Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000002971 oxazolyl group Chemical group 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000001544 thienyl group Chemical group 0.000 abstract 2
- 125000004385 trihaloalkyl group Chemical group 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000006642 (C1-C6) cyanoalkyl group Chemical group 0.000 abstract 1
- NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical compound C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 abstract 1
- 102000003964 Histone deacetylase Human genes 0.000 abstract 1
- 108090000353 Histone deacetylase Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 1
- 125000006398 alkylpyrazinyl group Chemical group 0.000 abstract 1
- 125000005001 aminoaryl group Chemical group 0.000 abstract 1
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 abstract 1
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 abstract 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000006542 morpholinylalkyl group Chemical group 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003831 tetrazolyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 239000011701 zinc Substances 0.000 abstract 1
- 229910052725 zinc Inorganic materials 0.000 abstract 1
Classifications
-
- 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
- C07D413/12—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 chain containing hetero atoms as chain links
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/402—1-aryl substituted, e.g. piretanide
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
-
- 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
-
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P17/10—Anti-acne agents
-
- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- 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
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
- C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
- C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
- C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
- C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- 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
- 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
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/06—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 linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
- C07D409/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/573—Immunoassay; Biospecific binding assay; Materials therefor for enzymes or isoenzymes
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/914—Hydrolases (3)
- G01N2333/978—Hydrolases (3) acting on carbon to nitrogen bonds other than peptide bonds (3.5)
- G01N2333/98—Hydrolases (3) acting on carbon to nitrogen bonds other than peptide bonds (3.5) acting on amide bonds in linear amides (3.5.1)
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Wood Science & Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Biotechnology (AREA)
- Neurology (AREA)
- Physics & Mathematics (AREA)
- Hematology (AREA)
- Analytical Chemistry (AREA)
- Dermatology (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- Cardiology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- General Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Endocrinology (AREA)
Abstract
Compuestos de la fórmula (1) que poseen actividad enzimática de inhibición de desacetilasa de histona; su proceso de preparación, composiciones que los contienen y una combinación de agentes anticancerosos. Estos compuestos pueden utilizarse como una medicina para inhibir condiciones proliferativas tales como cáncer y psoriasis. Reivindicación 1: Un compuesto de fórmula (1), las formas N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isoméricas de los mismos, en la cual n es 0,1, 2 o 3 y cuando n es 0 entonces se quiere significar un enlace directo; m es 0 o 1 y cuando m es 0 entonces se quiere significar un enlace directo; t es 0, 1, 2, 3 o 4 y cuando t es 0 entonces se quiere significar un enlace directo; cada Q es nitrógeno o carbono; cada X es nitrógeno o carbono; cada Y es nitrógeno o carbono; R1 es -C(O)NR8R9, -NHC(O)R10, -C(O)-C1-6alcanodiiloSR10, -NR11C(O)N(OH)R10, -NR11C(O)C1-6alcanodiiloSR10, -NR11C(O)C=N (OH)R10 u otro grupo quelante de cinc, en donde R8 y R9 se seleccionan cada uno independientemente de hidrógeno, hidroxi, alquilo C1-6, hidroxialquilo C1-6, aminoalquilo C1-6 o aminoarilo; R10 es hidrógeno, alquilo C1-6, alquil C1-6-carbonilo, arilalquilo C1-6, alquil C1-6-pirazinilo, piridinona, pirrolidinona o metilimidazolilo; R11 es hidrógeno o alquilo C1-6 ;R2 es hidrógeno, halo, hidroxi, amino, nitro, alquilo C1-6, alquiloxilo C1-6, trifluorometilo, di(alquil C1-6)-amino, hidroxiamino o naftalenilsulfonilpirazinilo; -L- es un enlace directo o un radical bivalente seleccionado de alcanodiilo C1-6, alcanodiiloxi C1-6, amino, carbonilo o aminocarbonilo; cada R3 representa independientemente un átomo de hidrógeno y un átomo de hidrógeno puede ser reemplazado por un substituyente seleccionado de arilo; R4 es hidrógeno, hidroxilo, amino, hidroxialquilo C1-6, alquilo C1-6, alquiloxilo C1-6, arilalquilo C1-6, aminocarbonilo, hidroxicarbonilo, aminoalquilo C1-6, aminocarbonilalquilo C1-6, hidroxicarbonilalquilo C1-6, hidroxiaminocarbonilo, alquiloxi C1-6-carbonilo, alquil C1-6-aminoalquilo C1-6 o di(alquil C1-6)aminoalquilo C1-6; R5 es hidrógeno, alquilo C1-6, cicloalquilo C3-10, hidroxialquilo C1-6, alquiloxi C1-6-alquilo C1-6, di(alquil C1-6)aminoalquilo C1-6 o arilo; la parte cíclica A es un radical seleccionado entre los restos de fórmula (a-1) a (a-51) en los cuales cada s es independientemente 0, 1, 2, 3, 4 o 5; cada R6 y R7 son independientemente seleccionados de hidrógeno; halo; hidroxilo; amino; nitro; trihaloalquilo C1-6; trihaloalquiloxilo C1-6; alquilo C1-6; alquilo C1-6 substituido con arilo y cicloalquilo C3-10; alquiloxilo C1-6; alquiloxi C1-6-alquiloxilo C1-6; alquil C1-6-carbonilo; alquiloxi C1-6-carbonilo; alquil C1-6-sulfonilo; cianoalquilo C1-6; hidroxialquilo C1-6 ; hidroxialquiloxilo C1-6; hidroxialquil C1-6-amino; aminoalquiloxilo C1-6; di(alquil C1-6)aminocarbonilo; di(hidroxialquil C1-6) amino; (aril)(alquil C1-6)amino; di(alquil C1-6)aminoalquiloxilo C1-6; di(alquil C1-6)aminoalquil C1-6amino; di(alquil C1-6)aminoalquil C1-6-aminoalquilo C1-6; arilsulfonilo; arilsulfonilamino; ariloxilo; ariloxialquilo C1-6 ;arilalquenodiilo C2-6; di(alquil C1-6)amino; di(alquil C1-6)aminoalquilo C1-6; di(alquil C1-6)amino(alquil C1-6)amino; di(alquil C1-6)amino(alquil C1-6)aminoalquilo C1-6; di(alquil C1-6)aminoalquilo C1-6(alquil C1-6)amino; di(alquil C1-6)aminoalquil C1-6(alquil C1-6)aminoalquilo C1-6; aminosulfonilamino(alquil C1-6)amino; aminosulfonilamino(alquil C1-6)aminoalquilo C1-6; di(alquil C1-6)aminosulfonilamino(alquil C1-6)amino; di(alquil C1-6)aminosulfonilamino(alquil C1-6)aminoalquilo C1-6; ciano; tiofenilo; tiofenilo substituido con di(alquil C1-6)aminoalquil C1-6(alquil C1-6)aminoalquilo C1-6, di(alquil C1-6)aminoalquilo C1-6, alquil C1-6-piperazinilalquilo C1-6, hidroxialquil C1-6-piperazinilalquilo C1-6, hidroxialquiloxi C1-6-alquil C1-6-piperazinilalquilo C1-6, di(alquil C1-6)aminosulfonilpiperazinilalquilo C1-6, alquiloxi C1-6-piperidinilo, alquiloxi C1-6-piperidinilalquilo C1-6, morfolinilalquilo C1-6, hidroxialquil C1-6(alquil C1-6)aminoalquilo C1-6, o di(hidroxialquil C1-6)aminoalquilo C1-6; furanilo; furanilo substituido con hidroxialquilo C1-6; benzofuranilo; imidazolilo; oxazolilo; oxazolilo substituido con arilo y alquilo C1-6 ; alquil C1-6-triazolilo; tetrazolilo; pirrolidinilo; pirrolilo; piperidinilalquiloxilo C1-6 ; morfolinilo; alquil C1-6-morfolinilo; morfolinilalquiloxilo C1-6; morfolinilalquilo C1-6; morfolinilalquil C1-6-amino; morfolinil C1-6-alquilaminoalquilo C1-6; piperazinilo; alquil C1-6-piperazinilo; alquil C1-6-piperazinilalquiloxilo C1-6; piperazinilalquilo C1-6; naftalenilsulfonilpiperazinilo; naftalenilsulfonilpiperidinilo; naftalenilsulfonilo; alquil C1-6-piperazinilalquilo C1-6; alquil C1-6-piperazinilalquil C1-6-amino; alquil C1-6-piperazinilalquil C1-6-aminoalquilo C1-6; alquil C1-6-piperazinilsulfonilo; aminosulfonilpiperazinilalquiloxilo C1-6; aminosulfonilpiperazinilo; aminosulfonilpiperazinilalquilo C1-6; di(alquilo C1-6)aminosulfonilpiperazinilo; di(alquil C1-6)aminosulfonilpiperazinilalquilo C1-6; hidroxialquil C1-6-piperazinilo; hidroxialquil C1-6-piperazinilalquilo C1-6; alquiloxi C1-6-piperidinilo; alquiloxi C1-6-piperidinilalquilo C1-6; piperidinilaminoalquil C1-6-amino; piperdinilaminoalquil C1-6-aminoalquilo C1-6; (alquil C1-6piperdinil)(hidroxialquil C1-6)aminoalquil C1-6-amino; (alquil C1-6-piperidinil)(hidroxialquil C1-6)aminoalquil C1-6-aminoalquilo C1-6; hidroxialquiloxi C1-6-alquil C1-6-piperazinilo; hidroxialquiloxi C1-6-alquil C1-6-piperazinilalquilo C1-6; (hidroxialquil C1-6)(alquil C1-6)amino; (hidroxialquil C1-6)(alquil C1-6)-aminoalquilo C1-6; hidroxialquil C1-6-aminoalquilo C1-6; di(hidroxialquil C1-6)aminoalquilo C1-6; pirrolidinilalquilo C1-6; pirrolidinilalquiloxilo C1-6; pirazolilo; tiopirazolilo; pirazolilo substituido con dos substituyentes seleccionados de alquilo C1-6 o trihaloalquilo C1-6; piridinilo; piridinilo substituido con alquiloxilo C1-6, ariloxilo o arilo; pirimidinilo; tetrahidropirimidinilpiperazinilo; tetrahidropirimidinilpiperazinilalquilo C1-6; quinolinilo; indol; fenilo; o fenilo substituido con uno, dos o tres substituyentes independientemente seleccionados de halo, amino, nitro, alquilo C1-6, alquiloxilo C1-6, hidroxialquilo C1-4, trifluorometilo, trifluorometiloxilo, hidroxialquiloxilo C1-4, alquil C1-4-sulfonilo, alquiloxi C1-4-alquiloxilo C1-4, alquiloxi C1-4-carbonilo, aminoalquiloxilo C1-4, di(alquil C1-4)-aminoalquiloxilo C1-4, di(alquil C1-4)amino, di(alquil C1-4)aminocarbonilo, di(alquil C1-4)aminoalquilo C1-4, di(alquil C1-4)aminoalquil C1-4-aminoalquilo C1-4, di(alquil C1-4)amino(alquil C1-4)amino, di(alquil C1-4)amino(alquil C1-4)aminoalquilo C1-4, di(alquil C1-4)aminoalquil C1-4(alquil C1-4)amino, di(alquil C1-4)aminoalquil C1-4(alquil C1-4)aminoalquilo C1-4, aminosulfonilamino(alquil C1-4)amino, aminosulfonilamino(alquil C1-4)aminoalquilo C1-4, di(alquil C1-4)aminosulfonilamino(alquil C1-4)amino, di(alquil C1-4)aminosulfonilamino(alquil C1-4)aminoalquilo C1-6, ciano, piperidinilalquiloxilo C1-4, pirrolidinilalquiloxilo C1-4, aminosulfonilpiperazinilo, aminosulfonilpiperazinilalquilo C1-4, di(alquil C1-4)aminosulfonilpiperazinilo, di(alquil C1-4)aminosulfonilpiperazinilalquilo C1-4, hidroxialquil C1-4-piperazinilo, hidroxialquil C1-4-piperazinilalquilo C1-4, alquiloxi C1-4-piperidinilo, alquiloxi C1-4-piperidinilalquilo C1-4, hidroxialquiloxi C1-4-alquil C1-4-piperazinilo, hidroxialquiloxi C1-4-alquil C1-4-piperaziniloalquilo C1-4, (hidroxialquil C1-4)(alquil C1-4)amino, (hidroxialquil C1-4)(alquil C1-4)aminoalquilo C1-4, di(hidroxialquil C1-4)amino, di(hidroxialquil C1-4)aminoalquilo C1-4, furanilo, furanilo substituido con -CH=CH-CH=CH-, pirrolidinilalquilo C1-4, pirrolidiniloalquiloxi C1-4, morfolinilo, morfolinilalquiloxilo C1-4, morfolinilalquilo C1-4, morfolinilalquil C1-4-amino, morfolinilalquil C1-4-aminoalquilo C1-4, piperazinilo, alquil C1-4-piperazinilo, alquil C1-4-piperazinilalquiloxilo C1-4, piperazinilalquilo C1-4, alquil C1-4-piperazinilalquilo C1-4, alquil C1-4-piperazinilalquil C1-4-amino, alquil C1-4-piperazinilalquil C1-4-aminoalquilo C1-6, tetrahidropirimidinilpiperazinilo, tetrahidropirimidinilpiperaziniloalquilo C1-4, piperidinilaminoalquil C1-4-amino, piperidinilaminoalquil C1-4-amino-C1-4alquilo, (alquil C1-4-piperidinilo)(hidroxialquil C1-4)aminoalquil C1-4-amino, (alquil C1-4-piperidinil)(hidroxialquil C1-4)aminoalquil C1-4-aminoalquil C1-4piridinilalquiloxilo C1-4, hidroxialquil C1-4-amino, hidroxialquil C1-4-aminoalquilo C1-4, di(alquil C1-4)aminoalquil C1-4-amino, aminotiadiazolilo, aminosulfonilpiperazinilalquiloxilo C1-4, o tiofenilalquil C1-4-amino; pudiendo cada R6 y R7 estar ubicado sobre el nitrógeno en reemplazo del hidrógeno; arilo en la anterior es fenilo, o fenilo substituido con uno o más substituyentes seleccionados cada uno independientemente de halo, alquilo C1-6, alquiloxi C1-6, trifluorometilo, ciano o hidroxicarbonilo. Reivindicación 11: Un procedimiento para la preparación de un compuesto de acuerdo con la reivindicación 1, caracterizado porque se hace reaccionar un intermediario de la fórmula (2) con un ácido apropiado, tal como por ejemplo, ácido trifluoroacético (CF3COOH), produciendo un ácido hidroxámico de la fórmula (3), en la cual R1 es -C(O)NH(OH).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US36379902P | 2002-03-13 | 2002-03-13 | |
EP0214074 | 2002-12-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR039564A1 true AR039564A1 (es) | 2005-02-23 |
Family
ID=27806439
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030100852A AR039564A1 (es) | 2002-03-13 | 2003-03-12 | Derivados de carbonilamino como inhibidores de desacetilasa de histona, composiciones farmaceuticas y procesos de preparacion del compuesto y de las composiciones que lo contienen |
Country Status (22)
Country | Link |
---|---|
US (3) | US7446109B2 (es) |
EP (1) | EP1485348B1 (es) |
JP (1) | JP4648628B2 (es) |
KR (1) | KR20040090981A (es) |
CN (1) | CN100503599C (es) |
AR (1) | AR039564A1 (es) |
AT (1) | ATE398105T1 (es) |
AU (1) | AU2003212336B2 (es) |
BR (1) | BR0307607A (es) |
CA (1) | CA2476067C (es) |
DE (1) | DE60321548D1 (es) |
DK (1) | DK1485348T3 (es) |
EA (1) | EA007908B1 (es) |
ES (1) | ES2306858T3 (es) |
HR (1) | HRP20040805A2 (es) |
MX (1) | MXPA04008796A (es) |
NO (1) | NO20044146L (es) |
NZ (1) | NZ534831A (es) |
OA (1) | OA12789A (es) |
PL (1) | PL205531B1 (es) |
TW (1) | TW200404794A (es) |
WO (1) | WO2003076395A1 (es) |
Families Citing this family (75)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7868204B2 (en) | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
WO2003024448A2 (en) | 2001-09-14 | 2003-03-27 | Methylgene, Inc. | Inhibitors of histone deacetylase |
US6897220B2 (en) | 2001-09-14 | 2005-05-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
CN100519527C (zh) * | 2002-03-13 | 2009-07-29 | 詹森药业有限公司 | 组织蛋白去乙酰酶抑制剂 |
JP4674045B2 (ja) | 2002-03-13 | 2011-04-20 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒストンデアセチラーゼの新規な阻害剤としてのピペラジニル−、ピペリジニル−およびモルホリニル−誘導体 |
DE60321548D1 (de) * | 2002-03-13 | 2008-07-24 | Janssen Pharmaceutica Nv | Carbonylamino- derivativate als neue inhibitoren von histone deacetylase |
AU2003209727B2 (en) | 2002-03-13 | 2008-10-16 | Janssen Pharmaceutica N.V. | Sulfonylamino-derivatives as novel inhibitors of histone deacetylase |
TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
US8163764B2 (en) * | 2002-04-26 | 2012-04-24 | Asan Laboratories Company (Cayman) Limited | Skincare methods |
CA2510322A1 (en) * | 2002-12-17 | 2004-07-01 | Pfizer Inc. | 2-pyridyl and 2-pyrimidyl cycloalkylene amide compounds as nr2b receptor antagonists |
WO2005030704A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
US7253204B2 (en) | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
CA2566515A1 (en) | 2004-06-14 | 2005-12-22 | F. Hoffmann-La Roche Ag | Thiophene hydroxamic acid derivatives and their use as hdac inhibitors |
JP2008502627A (ja) | 2004-06-14 | 2008-01-31 | エフ.ホフマン−ラ ロシュ アーゲー | ヒドロキサム酸塩、その製造、および薬剤としての使用 |
EP1778683A1 (en) | 2004-06-14 | 2007-05-02 | F.Hoffmann-La Roche Ag | Thiophene derivatives, their manufacture and use as pharmaceutical agents |
PL1781639T3 (pl) | 2004-07-28 | 2012-07-31 | Janssen Pharmaceutica Nv | Podstawione pochodne indolilo-alkiloaminowe jako nowe inhibitory deacetylazy histonowej |
SI1781639T1 (sl) * | 2004-07-28 | 2012-06-29 | Janssen Pharmaceutica Nv | Substituirani indolil alkil amino derivati kot novi inhibitorji histon deacetilaze |
RS51189B (sr) * | 2004-07-28 | 2010-10-31 | Janssen Pharmaceutica N.V. | Supstituisani derivati propenil piperazina kao novi inhibitori histonske deacetilaze |
CN101083992A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 抑制人硬脂酰CoA去饱和酶的哒嗪衍生物 |
US7919496B2 (en) | 2004-09-20 | 2011-04-05 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes |
JP5043668B2 (ja) | 2004-09-20 | 2012-10-10 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | 複素環誘導体および治療薬としてのそれらの使用 |
BRPI0515489A (pt) | 2004-09-20 | 2008-07-29 | Xenon Pharmaceuticals Inc | derivados heterocìclicos e sua utilização como inibidores de estearoil-coa desaturase |
EP1807085B1 (en) | 2004-09-20 | 2013-08-21 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
JP5094398B2 (ja) | 2004-09-20 | 2012-12-12 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | 複素環式誘導体およびステアロイル−CoAデサチュラーゼのメディエータとしてのそれらの使用 |
CA2580857A1 (en) | 2004-09-20 | 2006-09-28 | Xenon Pharmaceuticals Inc. | Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors |
US7772245B2 (en) | 2005-02-14 | 2010-08-10 | Miikana Therapeutics, Inc. | Inhibitors of histone deacetylase |
US20090253671A1 (en) * | 2005-03-04 | 2009-10-08 | Astrazeneca Ab | Tricyclic derivatives of azetidine and pyrrole with antibacterial activity |
JP2008536924A (ja) | 2005-04-20 | 2008-09-11 | メルク エンド カムパニー インコーポレーテッド | ベンゾチオフェンヒドロキサミン酸のカーバメート、ウレア、アミドおよびスルホンアミド置換誘導体 |
WO2006115845A1 (en) | 2005-04-20 | 2006-11-02 | Merck & Co., Inc. | Benzothiophene derivatives |
US7772238B2 (en) | 2005-04-20 | 2010-08-10 | Merck Sharp & Dohme Corp. | Benzothiophene hydroxamic acid derivatives |
GB0509223D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
GB0509225D0 (en) | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Inhibitors of enzymatic activity |
AU2006248938B2 (en) | 2005-05-18 | 2011-09-29 | Janssen Pharmaceutica N.V. | Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase |
WO2007130075A1 (en) | 2005-06-03 | 2007-11-15 | Xenon Pharmaceuticals Inc. | Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors |
JP2008546793A (ja) | 2005-06-24 | 2008-12-25 | メルク エンド カムパニー インコーポレーテッド | 修飾マロン酸誘導体 |
ZA200800901B (en) | 2005-07-14 | 2010-05-26 | Takeda San Diego Inc | Histone deacetylase inhibitors |
EP1910352A1 (en) * | 2005-07-20 | 2008-04-16 | Merck Frosst Canada Ltd. | Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
ATE509920T1 (de) | 2005-10-27 | 2011-06-15 | Janssen Pharmaceutica Nv | Quadratsäurederivate als inhibitoren von histondeacetylase |
KR100696139B1 (ko) * | 2005-11-01 | 2007-03-20 | 한국화학연구원 | 히스톤 디아세틸라제 저해활성을 갖는 알킬카바모일나프탈렌일옥시 옥테노일 하이드록시아마이드 유도체 및그의 제조방법 |
AR057579A1 (es) | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
WO2007082878A1 (en) * | 2006-01-19 | 2007-07-26 | Janssen Pharmaceutica N.V. | Aminophenyl derivatives as novel inhibitors of histone deacetylase |
EP1981871B1 (en) | 2006-01-19 | 2011-12-28 | Janssen Pharmaceutica N.V. | Heterocyclylalkyl derivatives as novel inhibitors of histone deacetylase |
US7834025B2 (en) * | 2006-01-19 | 2010-11-16 | Janssen Pharmaceutica N.V. | Substituted indolyl-alkyl-amino-derivatives as inhibitors of histone deacetylase |
DK1979328T3 (da) | 2006-01-19 | 2013-03-25 | Janssen Pharmaceutica Nv | Pyridin- og pyrimidinderivater i deres egenskab af histondeacetylasehæmmere |
EP1979326B1 (en) | 2006-01-19 | 2012-10-03 | Janssen Pharmaceutica N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
EP1979327A1 (en) | 2006-01-19 | 2008-10-15 | Janssen Pharmaceutica, N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
AU2007221207A1 (en) | 2006-02-28 | 2007-09-07 | Merck Sharp & Dohme Corp. | Inhibitors of histone deacetylase |
KR101495611B1 (ko) | 2006-04-07 | 2015-02-25 | 메틸진 인코포레이티드 | 히스톤 데아세틸라아제의 억제제 |
AU2007243519A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Corp. | Disubstituted aniline compounds |
CA2651681A1 (en) | 2006-05-18 | 2007-11-29 | Merck & Co., Inc. | Aryl-fused spirocyclic compounds |
EP2049124A4 (en) | 2006-07-20 | 2010-02-10 | Merck & Co Inc | PHOSPHOR DERIVATIVES AS HISTONDEACETYLASE HEMMER |
GB0619753D0 (en) | 2006-10-06 | 2006-11-15 | Chroma Therapeutics Ltd | Enzyme inhibitors |
CA2668070A1 (en) * | 2006-10-30 | 2008-05-08 | Chroma Therapeutics Ltd. | Hydroxamates as inhibitors of histone deacetylase |
EP2913322A3 (en) | 2006-11-03 | 2015-11-11 | Korea Research Institute Of Chemical Technology | Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same |
US8030344B2 (en) | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
US8389553B2 (en) | 2007-06-27 | 2013-03-05 | Merck Sharp & Dohme Corp. | 4-carboxybenzylamino derivatives as histone deacetylase inhibitors |
CN101808518A (zh) | 2007-06-27 | 2010-08-18 | 默沙东公司 | 作为组蛋白脱乙酰酶抑制剂的吡啶基和嘧啶基衍生物 |
DK2274301T3 (da) | 2008-03-27 | 2013-01-02 | Janssen Pharmaceutica Nv | Azabicyclohexylsubstituerede indolylalkylaminoderivater som hidtil ukendte inhibitorer af histondeacetylase |
EP2303275A4 (en) * | 2008-06-17 | 2012-05-09 | Univ Duke | STANDARD RECEPTOR MODULATORS |
DK2385832T3 (en) | 2009-01-08 | 2015-09-21 | Curis Inc | Phosphoinositid-3-kinase-inhibitorer med en zink-bindingsdel |
GB0903480D0 (en) | 2009-02-27 | 2009-04-08 | Chroma Therapeutics Ltd | Enzyme Inhibitors |
CA2765678A1 (en) * | 2009-06-22 | 2010-12-29 | Christopher Blackburn | Substituted hydroxamic acids and uses thereof |
WO2010151317A1 (en) | 2009-06-22 | 2010-12-29 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2011106632A1 (en) * | 2010-02-26 | 2011-09-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
US8546588B2 (en) * | 2010-02-26 | 2013-10-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2011130163A1 (en) | 2010-04-12 | 2011-10-20 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2012027564A1 (en) * | 2010-08-26 | 2012-03-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2012054332A1 (en) | 2010-10-18 | 2012-04-26 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2012088015A2 (en) | 2010-12-22 | 2012-06-28 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
DK2683371T3 (da) | 2011-03-09 | 2021-01-18 | Cereno Scient Ab | Forbindelser og fremgangsmåder til forbedring af forringet endogen fibrinolyse ved anvendelse af histondeacetylasehæmmere |
SI3111938T1 (sl) | 2011-04-01 | 2019-08-30 | Curis, Inc. | Fosfoinozitid 3-kinazni inhibitor z delom, ki veže cink |
US20130303509A1 (en) | 2012-05-11 | 2013-11-14 | Abbvie Inc. | Nampt inhibitors |
EP3297992B1 (en) | 2015-05-22 | 2020-02-05 | Chong Kun Dang Pharmaceutical Corp. | Heterocyclicalkyl derivative compounds as selective histone deacetylase inhibitors and pharmaceutical compositions comprising the same |
AU2017279027A1 (en) | 2016-06-08 | 2018-12-20 | Glaxosmithkline Intellectual Property Development Limited | Chemical Compounds |
WO2020055840A1 (en) | 2018-09-11 | 2020-03-19 | Curis Inc. | Combination therapy with a phosphoinositide 3-kinase inhibitor with a zinc binding moiety |
Family Cites Families (86)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB901749A (en) | 1957-12-06 | 1962-07-25 | Ciba Ltd | New 2-substituted pyrimidines |
BE637271A (es) * | 1963-04-04 | 1900-01-01 | ||
US3966743A (en) * | 1968-07-23 | 1976-06-29 | Boehringer Mannheim G.M.B.H. | Ortho fused cycloalkano-4-quinolone-3-carboxylic acid derivatives |
US4049811A (en) * | 1968-07-23 | 1977-09-20 | Boehringer Mannheim G.M.B.H. | Compositions using cycloalkano-quinolone derivatives and their method of use |
GB1345872A (en) * | 1970-09-03 | 1974-02-06 | Wyeth John & Brother Ltd | Amino-and acylamino-pyridine and hydropyridine derivatives |
DE2939292A1 (de) * | 1979-09-28 | 1981-04-09 | Boehringer Mannheim Gmbh, 6800 Mannheim | N-phenoxyalkylpiperidin-derivate, verfahrenn zu deren herstellung sowie diese verbindungen enthaltende arzneimittel |
PH17194A (en) * | 1980-03-06 | 1984-06-19 | Otsuka Pharma Co Ltd | Novel carbostyril derivatives,and pharmaceutical composition containing the same |
US4962115A (en) * | 1981-10-01 | 1990-10-09 | Janssen Pharmaceutica N.V. | Novel N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
CA1183847A (en) * | 1981-10-01 | 1985-03-12 | Georges Van Daele | N-(3-hydroxy-4-piperidinyl)benzamide derivatives |
US4734418A (en) | 1984-12-14 | 1988-03-29 | Mitsui Petrochemical Industries, Ltd. | Quinazoline compounds and antihypertensives |
HU206337B (en) * | 1988-12-29 | 1992-10-28 | Mitsui Petrochemical Ind | Process for producing pyrimidine derivatives and pharmaceutical compositions |
JP2664238B2 (ja) * | 1989-03-01 | 1997-10-15 | 日清製粉株式会社 | ニコチン酸またはそのエステル誘導体 |
US5342846A (en) * | 1990-12-05 | 1994-08-30 | Synphar Laboratories, Inc. | 7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid compounds and 7-(substituted triazolyl pyrrolidin-1-yl) 4-oxoquinoline-3-carboxylic acid derivatives useful as antibacterial agents |
DE4228792A1 (de) | 1992-08-29 | 1994-03-03 | Hoechst Ag | Pyridylaminopiperidine, Verfahren zu ihrer Herstellung, sie enthaltende Mittel und deren Verwendung als Fungizide |
US5338738A (en) * | 1993-04-19 | 1994-08-16 | Bristol-Myers Squibb Company | Cerebral function enhancers: acyclic amide derivatives of pyrimidinylpiperidines |
US5459151A (en) | 1993-04-30 | 1995-10-17 | American Home Products Corporation | N-acyl substituted phenyl piperidines as bronchodilators and antiinflammatory agents |
US5446222A (en) * | 1994-06-17 | 1995-08-29 | Mobil Oil Corporation | Oligomers of cyclopentadiene and process for making them |
FR2722788B1 (fr) * | 1994-07-20 | 1996-10-04 | Pf Medicament | Nouvelles piperazides derivees d'aryl piperazine, leurs procedes de preparation, leur utilisation a titre de medicament et les compositions pharmaceutiques les comprenant |
US6083903A (en) * | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
ES2104509B1 (es) | 1995-06-13 | 1998-07-01 | Ferrer Int | Nuevos compuestos derivados de 2-(3,4-disustituido-1-piperazinil)-5-fluoropirimidina. |
ZA9610745B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists |
US5952349A (en) * | 1996-07-10 | 1999-09-14 | Schering Corporation | Muscarinic antagonists for treating memory loss |
EP0827742A1 (en) | 1996-09-04 | 1998-03-11 | Vrije Universiteit Brussel | Use of histone deacetylase inhibitors for treating fribosis or cirrhosis |
AUPO721997A0 (en) | 1997-06-06 | 1997-07-03 | Queensland Institute Of Medical Research, The | Anticancer compounds |
GB9823873D0 (en) | 1998-10-30 | 1998-12-30 | Pharmacia & Upjohn Spa | 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents |
TW526202B (en) * | 1998-11-27 | 2003-04-01 | Shionogi & Amp Co | Broad spectrum cephem having benzo[4,5-b]pyridium methyl group of antibiotic activity |
WO2000035855A1 (en) | 1998-12-14 | 2000-06-22 | American Home Products Corporation | 3,4-diamino-3-cyclobutene-1,2-dione derivatives which inhibit leukocyte adhesion mediated by vla-4 |
CN100354271C (zh) | 1999-03-03 | 2007-12-12 | 三进制药株式会社 | 哌嗪衍生物及其制备方法 |
DK1041068T3 (da) * | 1999-04-01 | 2004-05-10 | Pfizer Prod Inc | Compounds for treating and preventing diabetic complications |
CA2374788A1 (en) | 1999-05-24 | 2000-11-30 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
US6518283B1 (en) | 1999-05-28 | 2003-02-11 | Celltech R&D Limited | Squaric acid derivatives |
US6635894B1 (en) | 1999-11-22 | 2003-10-21 | Renishaw Plc | Optical measuring apparatus for measuring objects on machines |
CA2391952C (en) | 1999-11-23 | 2012-01-31 | Methylgene Inc. | Inhibitors of histone deacetylase |
US6608052B2 (en) * | 2000-02-16 | 2003-08-19 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compounds useful as anti-inflammatory agents |
JP2003528074A (ja) | 2000-03-24 | 2003-09-24 | メチルジーン インコーポレイテッド | ヒストン脱アセチル化酵素の阻害剤 |
WO2002000651A2 (en) | 2000-06-27 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Factor xa inhibitors |
WO2002018335A1 (fr) | 2000-08-28 | 2002-03-07 | Yamanouchi Pharmaceutical Co., Ltd. | Derives d'amine cyclique |
JO2409B1 (en) | 2000-11-21 | 2007-06-17 | شركة جانسين فارماسوتيكا ان. في | Second-phenyl carboxy amides are useful as lipid-lowering agents |
US6784173B2 (en) | 2001-06-15 | 2004-08-31 | Hoffmann-La Roche Inc. | Aromatic dicarboxylic acid derivatives |
DE10130374A1 (de) | 2001-06-23 | 2003-01-02 | Boehringer Ingelheim Pharma | Substituierte N-Acyl-anilinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
US6897220B2 (en) | 2001-09-14 | 2005-05-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
US7129034B2 (en) | 2001-10-25 | 2006-10-31 | Cedars-Sinai Medical Center | Differentiation of whole bone marrow |
GB0127929D0 (en) * | 2001-11-21 | 2002-01-16 | Celltech R&D Ltd | Chemical compounds |
GB0229931D0 (en) | 2002-12-21 | 2003-01-29 | Astrazeneca Ab | Therapeutic agents |
JP4674045B2 (ja) * | 2002-03-13 | 2011-04-20 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒストンデアセチラーゼの新規な阻害剤としてのピペラジニル−、ピペリジニル−およびモルホリニル−誘導体 |
CN100519527C (zh) | 2002-03-13 | 2009-07-29 | 詹森药业有限公司 | 组织蛋白去乙酰酶抑制剂 |
BR0307575A (pt) * | 2002-03-13 | 2004-12-21 | Janssen Pharmaceutica Nv | Derivados de sulfonila como inibidores de histona desacetilase |
AU2003209727B2 (en) | 2002-03-13 | 2008-10-16 | Janssen Pharmaceutica N.V. | Sulfonylamino-derivatives as novel inhibitors of histone deacetylase |
DE60321548D1 (de) * | 2002-03-13 | 2008-07-24 | Janssen Pharmaceutica Nv | Carbonylamino- derivativate als neue inhibitoren von histone deacetylase |
EP1485378B1 (en) | 2002-03-13 | 2008-06-18 | Janssen Pharmaceutica N.V. | Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase |
NZ536116A (en) | 2002-04-03 | 2007-01-26 | Topotarget Uk Ltd | Carbamic acid compounds comprising a piperazine linkage as HDAC inhibitors |
GB0209715D0 (en) | 2002-04-27 | 2002-06-05 | Astrazeneca Ab | Chemical compounds |
DE10233412A1 (de) | 2002-07-23 | 2004-02-12 | 4Sc Ag | Neue Verbindungen als Histondeacetylase-Inhibitoren |
PL374970A1 (en) | 2002-08-02 | 2005-11-14 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors |
ITMI20030025A1 (it) | 2003-01-10 | 2004-07-11 | Italfarmaco Spa | Derivati dell'acido idrossammico ad attivita' antinfiammatoria. |
TW200418806A (en) | 2003-01-13 | 2004-10-01 | Fujisawa Pharmaceutical Co | HDAC inhibitor |
JP4612621B2 (ja) | 2003-01-17 | 2011-01-12 | トポターゲット ユーケー リミテッド | Hdac阻害剤としてのエステル又はケトン結合を含むカルバミン酸化合物 |
TW200424174A (en) | 2003-02-06 | 2004-11-16 | Hoffmann La Roche | New TP diamide |
AU2003900608A0 (en) | 2003-02-11 | 2003-02-27 | Fujisawa Pharmaceutical Co., Ltd. | Hdac inhibitor |
US7244751B2 (en) | 2003-02-14 | 2007-07-17 | Shenzhen Chipscreen Biosciences Ltd. | Histone deacetylase inhibitors of novel benzamide derivatives with potent differentiation and anti-proliferation activity |
US7375228B2 (en) | 2003-03-17 | 2008-05-20 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
TW200424187A (en) | 2003-04-04 | 2004-11-16 | Hoffmann La Roche | New oxime derivatives and their use as pharmaceutically active agents |
NZ542445A (en) | 2003-04-07 | 2008-03-28 | Pharmacyclics Inc | Hydroxamates as therapeutic agents |
ATE553092T1 (de) | 2003-07-30 | 2012-04-15 | Kyowa Hakko Kirin Co Ltd | Indazolderivate |
KR101127201B1 (ko) | 2003-09-22 | 2012-04-12 | 에스*바이오 피티이 리미티드 | 벤즈이미다졸 유도체와 그의 제조방법 및 약학적 적용 |
PL1673349T3 (pl) | 2003-09-22 | 2010-11-30 | Mei Pharma Inc | Pochodne benzimidazolu: wytwarzanie i zastosowania farmaceutyczne |
WO2005030704A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
US20070167499A1 (en) | 2003-10-27 | 2007-07-19 | A*Bio Pte Ltd. | Biaryl linked hydroxamates: preparation and pharmaceutical applications |
MXPA06004735A (es) | 2003-10-27 | 2006-12-14 | S Bio Pte Ltd | Hidroxamatos conectados a acilurea y a sulfonilurea. |
GB0402496D0 (en) | 2004-02-04 | 2004-03-10 | Argenta Discovery Ltd | Novel compounds |
US20050197336A1 (en) * | 2004-03-08 | 2005-09-08 | Miikana Therapeutics Corporation | Inhibitors of histone deacetylase |
WO2005092899A1 (en) | 2004-03-26 | 2005-10-06 | Methylgene Inc. | Inhibitors of histone deacetylase |
PL1781639T3 (pl) | 2004-07-28 | 2012-07-31 | Janssen Pharmaceutica Nv | Podstawione pochodne indolilo-alkiloaminowe jako nowe inhibitory deacetylazy histonowej |
RS51189B (sr) * | 2004-07-28 | 2010-10-31 | Janssen Pharmaceutica N.V. | Supstituisani derivati propenil piperazina kao novi inhibitori histonske deacetilaze |
AU2006248938B2 (en) | 2005-05-18 | 2011-09-29 | Janssen Pharmaceutica N.V. | Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase |
WO2006136553A1 (en) * | 2005-06-23 | 2006-12-28 | Janssen Pharmaceutica N.V. | Imidazolinone and hydantoine derivatives as novel inhibitors of histone deacetylase |
WO2007016532A2 (en) | 2005-08-02 | 2007-02-08 | Novartis Ag | Mutations and polymorphisms of hdac4 |
ATE509920T1 (de) * | 2005-10-27 | 2011-06-15 | Janssen Pharmaceutica Nv | Quadratsäurederivate als inhibitoren von histondeacetylase |
EP1979327A1 (en) * | 2006-01-19 | 2008-10-15 | Janssen Pharmaceutica, N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
WO2007082878A1 (en) * | 2006-01-19 | 2007-07-26 | Janssen Pharmaceutica N.V. | Aminophenyl derivatives as novel inhibitors of histone deacetylase |
DK1979328T3 (da) * | 2006-01-19 | 2013-03-25 | Janssen Pharmaceutica Nv | Pyridin- og pyrimidinderivater i deres egenskab af histondeacetylasehæmmere |
EP1981871B1 (en) * | 2006-01-19 | 2011-12-28 | Janssen Pharmaceutica N.V. | Heterocyclylalkyl derivatives as novel inhibitors of histone deacetylase |
US7834025B2 (en) * | 2006-01-19 | 2010-11-16 | Janssen Pharmaceutica N.V. | Substituted indolyl-alkyl-amino-derivatives as inhibitors of histone deacetylase |
EP1979326B1 (en) * | 2006-01-19 | 2012-10-03 | Janssen Pharmaceutica N.V. | Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase |
AU2007296259A1 (en) * | 2006-09-15 | 2008-03-20 | Janssen Pharmaceutica Nv | Combinations of class-I specific histone deacetylase inhibitors with proteasome inhibitors |
GB0901749D0 (en) | 2009-02-03 | 2009-03-11 | Oxford Nanopore Tech Ltd | Adaptor method |
-
2003
- 2003-03-11 DE DE60321548T patent/DE60321548D1/de not_active Expired - Lifetime
- 2003-03-11 DK DK03708215T patent/DK1485348T3/da active
- 2003-03-11 NZ NZ534831A patent/NZ534831A/en unknown
- 2003-03-11 CN CNB038058847A patent/CN100503599C/zh not_active Expired - Lifetime
- 2003-03-11 BR BR0307607-5A patent/BR0307607A/pt not_active IP Right Cessation
- 2003-03-11 AU AU2003212336A patent/AU2003212336B2/en not_active Ceased
- 2003-03-11 WO PCT/EP2003/002512 patent/WO2003076395A1/en active IP Right Grant
- 2003-03-11 EP EP03708215A patent/EP1485348B1/en not_active Expired - Lifetime
- 2003-03-11 KR KR10-2004-7011327A patent/KR20040090981A/ko not_active Application Discontinuation
- 2003-03-11 JP JP2003574617A patent/JP4648628B2/ja not_active Expired - Lifetime
- 2003-03-11 AT AT03708215T patent/ATE398105T1/de not_active IP Right Cessation
- 2003-03-11 US US10/507,788 patent/US7446109B2/en active Active
- 2003-03-11 EA EA200401200A patent/EA007908B1/ru not_active IP Right Cessation
- 2003-03-11 MX MXPA04008796A patent/MXPA04008796A/es active IP Right Grant
- 2003-03-11 PL PL370982A patent/PL205531B1/pl unknown
- 2003-03-11 ES ES03708215T patent/ES2306858T3/es not_active Expired - Lifetime
- 2003-03-11 CA CA2476067A patent/CA2476067C/en not_active Expired - Lifetime
- 2003-03-11 OA OA1200400243A patent/OA12789A/en unknown
- 2003-03-12 TW TW092105281A patent/TW200404794A/zh unknown
- 2003-03-12 AR ARP030100852A patent/AR039564A1/es not_active Application Discontinuation
-
2004
- 2004-09-03 HR HR20040805A patent/HRP20040805A2/hr not_active Application Discontinuation
- 2004-09-30 NO NO20044146A patent/NO20044146L/no not_active Application Discontinuation
-
2008
- 2008-09-19 US US12/233,977 patent/US8071615B2/en not_active Expired - Fee Related
-
2011
- 2011-10-24 US US13/280,207 patent/US8394831B2/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
CN1642907A (zh) | 2005-07-20 |
MXPA04008796A (es) | 2004-11-26 |
CA2476067C (en) | 2011-09-20 |
US8071615B2 (en) | 2011-12-06 |
BR0307607A (pt) | 2004-12-21 |
ES2306858T3 (es) | 2008-11-16 |
US8394831B2 (en) | 2013-03-12 |
NZ534831A (en) | 2007-01-26 |
AU2003212336A1 (en) | 2003-09-22 |
JP4648628B2 (ja) | 2011-03-09 |
TW200404794A (en) | 2004-04-01 |
AU2003212336B2 (en) | 2008-12-18 |
OA12789A (en) | 2006-07-10 |
CA2476067A1 (en) | 2003-09-18 |
ATE398105T1 (de) | 2008-07-15 |
DK1485348T3 (da) | 2008-09-29 |
JP2005519950A (ja) | 2005-07-07 |
NO20044146L (no) | 2004-09-30 |
EA007908B1 (ru) | 2007-02-27 |
DE60321548D1 (de) | 2008-07-24 |
US20090042920A1 (en) | 2009-02-12 |
US20120041001A1 (en) | 2012-02-16 |
PL205531B1 (pl) | 2010-04-30 |
EP1485348B1 (en) | 2008-06-11 |
EA200401200A1 (ru) | 2005-02-24 |
KR20040090981A (ko) | 2004-10-27 |
US7446109B2 (en) | 2008-11-04 |
PL370982A1 (en) | 2005-06-13 |
CN100503599C (zh) | 2009-06-24 |
HRP20040805A2 (en) | 2005-04-30 |
US20050148613A1 (en) | 2005-07-07 |
WO2003076395A1 (en) | 2003-09-18 |
EP1485348A1 (en) | 2004-12-15 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR039564A1 (es) | Derivados de carbonilamino como inhibidores de desacetilasa de histona, composiciones farmaceuticas y procesos de preparacion del compuesto y de las composiciones que lo contienen | |
AR039565A1 (es) | Derivados de piperazinilo, piperidinilo y morfolinilo como inhibidores de desacetilasa de histona, composicion farmaceutica que los contiene y procedimiento de preparacion de ambos | |
AR039567A1 (es) | Derivados de sulfonilamino como nuevos inhibidores de histona deacetilasa, composicion farmaceutica y procedimiento de preparacion del compuesto | |
AR039566A1 (es) | Inhibidores de la histona deacetilasa, composicion farmaceutica que los contiene y sus procesos de preparacion | |
AR039568A1 (es) | Derivados de sulfonilo como novedosos inhibidores de la histona desacetilasa, composicion farmaceutica y procedimiento de preparacion del compuesto | |
CR20220230A (es) | Inhibidores de pequeñas moléculas de mutante g12c de kras | |
PH12020552004A1 (en) | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof | |
AR046711A1 (es) | 5-7-diaminopirazolo[4,3d]pirimidinas como inhibidores de la pde-5,composiciones farmaceuticas que las contienen y usos en el tratamiento de hipertensiones | |
TW200526658A (en) | Heterocyclic inhibitors of MEK and methods of use thereof | |
MY138906A (en) | Phenyl derivatives as ppar agonists | |
DK0591528T3 (da) | Pyrazolo[1,5-a]pyrimidinderivat og antiinflammatorisk middel, der indeholder dette | |
AR088808A2 (es) | Derivados de 2h-piridazin-3-ona, composiciones farmaceuticas que los contienen y un proceso para la preparacion de dichos derivados y el uso de dichos derivados para la preparacion de una composicion farmaceutica | |
AR067599A1 (es) | Derivados de indazol sustituido activos como inhibidores de quinasa | |
CO5640136A2 (es) | Derivados de hexahidropiridoisoquinolinas inhibidores de dpp-iv y composiciones farmaceuticas que los contienen | |
MY156407A (en) | 5-phenylthiazole derivatives and use as p13 kinase inhibitors | |
BRPI0408068A (pt) | derivados de 5-feniltiazol e seus usos como inibidores de pi3 cinase | |
AR037485A1 (es) | Uso de un compuesto derivado de pirazol-triazina en la fabricacion de un medicamento, medicamento que comprende un compuesto derivado de pirazol-triazina, producto industrial y composicion farmaceutica | |
EA200601178A1 (ru) | Морфолинилсодержащие бензимидазолы в качестве ингибиторов репликации респираторно-синцитиального вируса | |
ECSP034904A (es) | Derivados de índole naftil sustituido como inhibidores del activador plasminogen del inhibidor tipo-1 (pai-1) | |
NO20014529D0 (no) | Tetrahydropyranderivater og deres anvendelse som terapautiske midler | |
AR045155A1 (es) | Derivados de 6-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos | |
AR054272A1 (es) | Derivados de 3- aminopirrilidinas tri, tetra - sustituidos | |
MX2007011698A (es) | Derivados de oxindol sustituido, medicamentos que contienen dichos derivados y uso de los mismos. | |
TW200508207A (en) | New benzimidazole derivatives | |
GB1088973A (en) | Indazole derivatives |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Abandonment or withdrawal |