HRP20131139T1 - Novi supstituirani imidazokinolini - Google Patents
Novi supstituirani imidazokinolini Download PDFInfo
- Publication number
- HRP20131139T1 HRP20131139T1 HRP20131139AT HRP20131139T HRP20131139T1 HR P20131139 T1 HRP20131139 T1 HR P20131139T1 HR P20131139A T HRP20131139A T HR P20131139AT HR P20131139 T HRP20131139 T HR P20131139T HR P20131139 T1 HRP20131139 T1 HR P20131139T1
- Authority
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- Croatia
- Prior art keywords
- alkyl
- aryl
- compound
- group
- heterocyclyl
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- RHKWIGHJGOEUSM-UHFFFAOYSA-N 3h-imidazo[4,5-h]quinoline Chemical class C1=CN=C2C(N=CN3)=C3C=CC2=C1 RHKWIGHJGOEUSM-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- -1 -N3 Chemical group 0.000 claims 2
- 208000009458 Carcinoma in Situ Diseases 0.000 claims 2
- 208000009889 Herpes Simplex Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000031888 Mycoses Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 206010052428 Wound Diseases 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- 201000010153 skin papilloma Diseases 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010059313 Anogenital warts Diseases 0.000 claims 1
- 241000228212 Aspergillus Species 0.000 claims 1
- 208000012657 Atopic disease Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000013165 Bowen disease Diseases 0.000 claims 1
- 208000019337 Bowen disease of the skin Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 241000222122 Candida albicans Species 0.000 claims 1
- 206010007134 Candida infections Diseases 0.000 claims 1
- 241000606161 Chlamydia Species 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000000907 Condylomata Acuminata Diseases 0.000 claims 1
- 208000006081 Cryptococcal meningitis Diseases 0.000 claims 1
- 208000008953 Cryptosporidiosis Diseases 0.000 claims 1
- 206010011502 Cryptosporidiosis infection Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010014950 Eosinophilia Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 201000002563 Histoplasmosis Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000004554 Leishmaniasis Diseases 0.000 claims 1
- 206010024229 Leprosy Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010073245 Meningitis aspergillus Diseases 0.000 claims 1
- 206010027209 Meningitis cryptococcal Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 241000237852 Mollusca Species 0.000 claims 1
- 241000186367 Mycobacterium avium Species 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 241000233872 Pneumocystis carinii Species 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 201000005485 Toxoplasmosis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000000260 Warts Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 208000025009 anogenital human papillomavirus infection Diseases 0.000 claims 1
- 201000004201 anogenital venereal wart Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 206010006060 bowenoid papulosis Diseases 0.000 claims 1
- 210000000133 brain stem Anatomy 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000003984 candidiasis Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000007969 cellular immunity Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000003372 endocrine gland Anatomy 0.000 claims 1
- 210000004696 endometrium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 210000003026 hypopharynx Anatomy 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000003292 kidney cell Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 230000036210 malignancy Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000005962 mycosis fungoides Diseases 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- PHGJRFUIUALFTQ-UHFFFAOYSA-N n-[4-(4-amino-2-ethylimidazo[4,5-c]quinolin-1-yl)butyl]-n-(1,1-dioxothiolan-3-yl)acetamide Chemical compound CCC1=NC2=C(N)N=C3C=CC=CC3=C2N1CCCCN(C(C)=O)C1CCS(=O)(=O)C1 PHGJRFUIUALFTQ-UHFFFAOYSA-N 0.000 claims 1
- COGVUYGQNCAAOQ-UHFFFAOYSA-N n-[4-(4-amino-2-ethylimidazo[4,5-c]quinolin-1-yl)butyl]-n-(1-benzyl-2-methyl-1-oxidopyrrolidin-1-ium-3-yl)acetamide Chemical compound CCC1=NC2=C(N)N=C3C=CC=CC3=C2N1CCCCN(C(C)=O)C(C1C)CC[N+]1([O-])CC1=CC=CC=C1 COGVUYGQNCAAOQ-UHFFFAOYSA-N 0.000 claims 1
- YIOXEHCKXWZYNV-UHFFFAOYSA-N n-[4-(4-amino-2-ethylimidazo[4,5-c]quinolin-1-yl)butyl]-n-(1-methyl-1-oxidopiperidin-1-ium-4-yl)acetamide Chemical compound CCC1=NC2=C(N)N=C3C=CC=CC3=C2N1CCCCN(C(C)=O)C1CC[N+](C)([O-])CC1 YIOXEHCKXWZYNV-UHFFFAOYSA-N 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 208000012111 paraneoplastic syndrome Diseases 0.000 claims 1
- 201000001245 periodontitis Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 208000010626 plasma cell neoplasm Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 210000004872 soft tissue Anatomy 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 230000004936 stimulating effect Effects 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 238000012360 testing method Methods 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 210000003708 urethra Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 229960005486 vaccine Drugs 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 210000003905 vulva Anatomy 0.000 claims 1
Classifications
-
- 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
-
- 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
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- 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
- A61P31/10—Antimycotics
-
- 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
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- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/08—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis for Pneumocystis carinii
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- C07D453/04—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems having a quinolyl-4, a substituted quinolyl-4 or a alkylenedioxy-quinolyl-4 radical linked through only one carbon atom, attached in position 2, e.g. quinine
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biotechnology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- AIDS & HIV (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Otolaryngology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (14)
1. Spoj formule I:
[image]
,
naznačen time što
R1 se bira iz skupine koju čine:
-H, alkil, alkinil, aril, alkoksi, heterociklil i heteroaril,
gdje alkil, alkinil, aril, alkoksi, heterociklil ili heteroaril mogu biti nesupstituirani ili supstituirani s jednim ili više supstituenata, koje se bira iz skupine koju čine: -H, -OH, halogen, -CO-N(R4)2, -N(R4)2, -CO-C1-10 alkil, -CO-O-C1-10 alkil, -N3, aril i heterociklil, gdje se svakog R4 neovisno bira iz skupine koju čine -H, -C1-10 alkil, -C1-10 alkil-aril ili aril,
A je C1-C6 alkil;
B je -N(R2)(R3);
R2 je -(CO)-R5,
R5 se bira iz skupine koju čine:
alkil, uključujući skupine s nerazgranatim i razgranatim lancem i prstenaste skupine, alkinil, aril, heterociklil i heteroaril,
od kojih svaki može biti nesupstituiran ili supstituiran s jednim ili više supstituenata, koje se bira iz skupine koju čine: -H, -OH, halogen, -CN, -NO2, -COOH, -SH, -CO-C1-6 alkil, -CO-O-C1-6 alkil, -N3, aril, heterociklil, -CO-aril i -CO-heterociklil,
R3 se bira iz skupine koju čine:
alkenil, heteroaril, cikloalkil i heterociklil,
gdje alkenil, heteroarili, cikloalkil ili heterociklil mogu biti nesupstituirani ili supstituirani s jednim ili više supstituenata, koje se bira iz skupine koju čine: -H, alkil, alkenil, alkoksi, halogen, -OH, -N3,
triflurometil, -alkil-aril, -O-alkil-aril, -CO-aril, aril, heterociklil, heteroaril,-CO-heteroaril, -CO-O-alkil, -CO-N-alkil, -CO-N-aril,
ili njegovi farmaceutski prihvatljivi solvati, soli, N-oksidi ili stereoizomeri, ili njihove kombinacije.
2. Spoj formule I u skladu s patentnim zahtjevom 1, naznačen time što je R1 alkinil ili alkoksi.
3. Spoj formule I u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je R3 heterociklil, koji može biti nesupstituiran ili supstituiran s jednim ili više supstituenata, koji se biraju iz skupine koju čine: -H, alkil, alkenil, halogen i -OH.
4. Spoj formule I u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što se R3 bira iz skupine koju čine: dioksotetrahidrotiofenil, piperidinil, tetrahidrofuranil, piridin, tetrahidropiranil i azabiciklooktanil, od kojih svaki može biti izborno supstituirani s jednom ili više skupina, koji se biraju iz skupine koju čine halogen, hidroksil, aril, alkil, alkoksi, trifluormetil, ili njihove kombinacije.
5. Spoj formule I u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time što je R1 alkil, po mogućnosti etil.
6. Spoj formule I u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je R5 alkil, po mogućnosti metil.
7. Spoj u slkadu s patentnim zahtjevom 1, naznačen time što je:
N-[4-(4-amino-2-etil-1H-imidazo[4,5-c]kinolin-1-il)butil]-N-(1,1-dioksidotetrahidro-3-tienil)acetamid,
N-[4-(4-amino-2-etil-1H-imidazo[4,5-c]kinolin-1-il)butil]-N-(1-metil-1-oksidopiperidin-4-il)acetamid,
3-{acetil[4-(4-amino-2-etil-1H-imidazo[4,5-c]kinolin-1-il)butil]amino}-2,5-anhidro-1,3,4-trideoksipentitol,
N-[4-(4-amino-2-etil-1H-imidazo[4,5-c]kinolin-1-il)butil]-N-(1-benzil-2-metil-1-oksidopirolidin-3-il)acetamid,
ili njihovi farmaceutski prihvatljivi solvati, soli, N-oksidi ili stereoizomeri, ili njihove kombinacije.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je namijenjen upotrebi kao medikament.
9. Farmaceutski pripravak, naznačen time što sadrži terapijski djelotvornu količinu spoja formule I u skladu s bilo kojim od patentnih zahtjeva 1 do 7, u kombinaciji s farmaceutski prihvatljivom podlogom.
10. Farmaceutski pripravak u skladu s patentnim zahtjevom 9, naznačen time što sadrži količinu spoja formule I, ili njegovih farmaceutski prihvatljivih solvata, soli, N-oksida ili stereoizomera, ili njihovih kombinacija, dovoljnu da osigura dozu od otprilike 100 ng/kg do otprilike 50 mg/kg, po mogućnosti otprilike 10 µg/kg do otprilike 5 mg/kg spoja za subjekta.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili farmaceutski pripravak u skladu s patentnim zahtjevom 9 ili 10, naznačen time što je namijenjen upotrebi u liječenju virusne ili neoplastične bolesti.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili farmaceutski pripravak u skladu s patentnim zahtjevom 9 ili 10, naznačen time što je namijenjen upotrebi u liječenju raka, koji se biraju iz skupine koju čine rak dojke, mokraćnog mjehura, kostiju, mozga, središnjeg i perifernog živčanog sustava, debelog crijeva, endokrinih žlijezda, jednjaka, endometrija, germinativnih stanica, glave i vrata, bubrega, jetre, pluća, grkljana i hipofarinksa, mezoteliom, sarkom, rak jajnika, gušterače, prostate, rektuma, bubrežnih stanica, tankog crijeva, mekih tkiva, testisa, želuca, kože, mokraćovoda, vagine i vulve; nasljedni oblici raka, retinomblastom i Wilmsov tumor; leukemija, limfom, ne-Hodgkinova bolest, kronična i akutna mijeloidna leukaemija, akutna limfoblastična leukemija, Hodgkinova bolest, multipli mijelom i T-stanični limfom; mijelodisplastični sindrom, plazmacitne novotvorine, paraneoplastični sindromi, rak nepoznatog primarnog sijela i malignomi povezani s AIDS-om.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili farmaceutski pripravak u skladu s patentnim zahtjevom 9 ili 10, naznačen time što je namijenjen upotrebi u liječenju medicinskog stanja koje se bira iz skupine koju čine genitalne bradavice; obične bradavice; bradavice na stopalima; hepatitis B; hepatitis C; herpes simpleks tip I i tip II;mollusca contagiosum; HIV; CMV; VZV; intraepitelne novotvorine, uključujući intraepitelne novotvorine na vratu maternice, ljudski papilomavirus (HPV) i s njim povezne novotvorine; gljivične bolesti, uključujući kandidijazu, asperglozu i kriptokokni meningitis; neoplastične bolesti, uključujući karcinom bazalnih stanica, leukemiju vlasastih stanica, Kaposijev sarkom, karcinom bubrežnih stanica, karcinom pločastih stanica, mijelogenu leukemiju, multipli mijelom, melanom, ne-Hodgkinov limfom, kutani T-stanični limfom i druge oblike raka; parazitarne bolesti, uključujući Pneumocistis carinii, kriptosporidiozu, histoplasmozu, toksoplasmozu, tripanosomnu infekciju i lišmenijazu; bakterijske infekcije uključujući tuberkulozu i Mycobacterium avium; egzem; eozinofilija; esencijalna trombocitemija; lepra; multipla skleroza; Ommenov sindrom; discoid lupus; Bowenova bolest; Bowenoidna papuloza; atopične bolesti, uključujući atopični dermatitis; astma; alergija; alergijski rinitis; sistemni eritematozni lupus; recidivi gljivičnih bolesti, periodontitis i klamidije; ili što je namijenjen upotrebi kao adjuvans za cjepiva, za poticanje stanične imunosti; ili što je namijenjen upotrebi kod poboljšavanja ili stimuliranja zacjeljivanja rana, uključujući kronične rane.
14. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačena time što je spoj namijenjen upotrebi u proizvodnji medikamenta.
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| IN614MU2008 | 2008-03-24 | ||
| PCT/EP2009/053399 WO2009118296A2 (en) | 2008-03-24 | 2009-03-23 | Novel substituted imidazoquinolines |
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| HRP20131139T1 true HRP20131139T1 (hr) | 2014-01-03 |
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| JP (3) | JP5670876B2 (hr) |
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| AU (2) | AU2009228769C1 (hr) |
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| ES (2) | ES2436540T3 (hr) |
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| SI (1) | SI2276486T1 (hr) |
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