AR083353A1 - Co-cristales y sales de inhibidores de ccr3 - Google Patents
Co-cristales y sales de inhibidores de ccr3Info
- Publication number
- AR083353A1 AR083353A1 ARP110103717A ARP110103717A AR083353A1 AR 083353 A1 AR083353 A1 AR 083353A1 AR P110103717 A ARP110103717 A AR P110103717A AR P110103717 A ARP110103717 A AR P110103717A AR 083353 A1 AR083353 A1 AR 083353A1
- Authority
- AR
- Argentina
- Prior art keywords
- acid
- alkyl
- haloalkyl
- compounds
- crystals
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 4
- 102100024167 C-C chemokine receptor type 3 Human genes 0.000 title 1
- 101710149862 C-C chemokine receptor type 3 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 abstract 2
- QIAFMBKCNZACKA-UHFFFAOYSA-N N-benzoylglycine Chemical compound OC(=O)CNC(=O)C1=CC=CC=C1 QIAFMBKCNZACKA-UHFFFAOYSA-N 0.000 abstract 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 abstract 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- OCQAXYHNMWVLRH-UHFFFAOYSA-N 2,3-dibenzoyl-2,3-dihydroxybutanedioic acid Chemical compound C=1C=CC=CC=1C(=O)C(O)(C(O)=O)C(O)(C(=O)O)C(=O)C1=CC=CC=C1 OCQAXYHNMWVLRH-UHFFFAOYSA-N 0.000 abstract 1
- CIWBSHSKHKDKBQ-SZSCBOSDSA-N 2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one Chemical compound OC[C@H](O)C1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-SZSCBOSDSA-N 0.000 abstract 1
- ODHCTXKNWHHXJC-GSVOUGTGSA-N 5-oxo-D-proline Chemical compound OC(=O)[C@H]1CCC(=O)N1 ODHCTXKNWHHXJC-GSVOUGTGSA-N 0.000 abstract 1
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical compound OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 abstract 1
- 208000004998 Abdominal Pain Diseases 0.000 abstract 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 abstract 1
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Natural products OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 abstract 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 abstract 1
- 102000004499 CCR3 Receptors Human genes 0.000 abstract 1
- 108010017316 CCR3 Receptors Proteins 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 abstract 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 abstract 1
- 208000002881 Colic Diseases 0.000 abstract 1
- KZSNJWFQEVHDMF-SCSAIBSYSA-N D-valine Chemical compound CC(C)[C@@H](N)C(O)=O KZSNJWFQEVHDMF-SCSAIBSYSA-N 0.000 abstract 1
- 229930182831 D-valine Natural products 0.000 abstract 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 abstract 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 1
- DSLZVSRJTYRBFB-UHFFFAOYSA-N Galactaric acid Natural products OC(=O)C(O)C(O)C(O)C(O)C(O)=O DSLZVSRJTYRBFB-UHFFFAOYSA-N 0.000 abstract 1
- 239000004471 Glycine Substances 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 abstract 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 abstract 1
- 235000000069 L-ascorbic acid Nutrition 0.000 abstract 1
- 239000002211 L-ascorbic acid Substances 0.000 abstract 1
- 229930182821 L-proline Natural products 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 229910002651 NO3 Inorganic materials 0.000 abstract 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 abstract 1
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 abstract 1
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- 235000021355 Stearic acid Nutrition 0.000 abstract 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract 1
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 abstract 1
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 150000001450 anions Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- SNCZNSNPXMPCGN-UHFFFAOYSA-N butanediamide Chemical compound NC(=O)CCC(N)=O SNCZNSNPXMPCGN-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 abstract 1
- 229960003964 deoxycholic acid Drugs 0.000 abstract 1
- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- DSLZVSRJTYRBFB-DUHBMQHGSA-N galactaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)C(O)=O DSLZVSRJTYRBFB-DUHBMQHGSA-N 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 abstract 1
- 230000004957 immunoregulator effect Effects 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 230000002458 infectious effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- VFQXVTODMYMSMJ-UHFFFAOYSA-N isonicotinamide Chemical compound NC(=O)C1=CC=NC=C1 VFQXVTODMYMSMJ-UHFFFAOYSA-N 0.000 abstract 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 1
- 235000001968 nicotinic acid Nutrition 0.000 abstract 1
- 239000011664 nicotinic acid Substances 0.000 abstract 1
- 229960003512 nicotinic acid Drugs 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 abstract 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 abstract 1
- 239000010452 phosphate Substances 0.000 abstract 1
- 229960005141 piperazine Drugs 0.000 abstract 1
- 229960002429 proline Drugs 0.000 abstract 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 abstract 1
- 229940081974 saccharin Drugs 0.000 abstract 1
- 235000019204 saccharin Nutrition 0.000 abstract 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 abstract 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 abstract 1
- 229960001860 salicylate Drugs 0.000 abstract 1
- 239000008117 stearic acid Substances 0.000 abstract 1
- WPLOVIFNBMNBPD-ATHMIXSHSA-N subtilin Chemical compound CC1SCC(NC2=O)C(=O)NC(CC(N)=O)C(=O)NC(C(=O)NC(CCCCN)C(=O)NC(C(C)CC)C(=O)NC(=C)C(=O)NC(CCCCN)C(O)=O)CSC(C)C2NC(=O)C(CC(C)C)NC(=O)C1NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C1NC(=O)C(=C/C)/NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C2NC(=O)CNC(=O)C3CCCN3C(=O)C(NC(=O)C3NC(=O)C(CC(C)C)NC(=O)C(=C)NC(=O)C(CCC(O)=O)NC(=O)C(NC(=O)C(CCCCN)NC(=O)C(N)CC=4C5=CC=CC=C5NC=4)CSC3)C(C)SC2)C(C)C)C(C)SC1)CC1=CC=CC=C1 WPLOVIFNBMNBPD-ATHMIXSHSA-N 0.000 abstract 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 abstract 1
- 229940095064 tartrate Drugs 0.000 abstract 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 abstract 1
- 229940035893 uracil Drugs 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- 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
- 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
- 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
- A61P31/12—Antivirals
-
- 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
- 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
- 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
- C07D213/81—Amides; Imides
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Virology (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos y composiciones farmacéuticas que los contienen. Los compuestos son útiles para el tratamiento y/o prevención de enfermedades relacionadas con el receptor CCR3, tales como enfermedades inflamatorias, infecciosas e inmunorreguladoras (incluyendo asma y alergias).Reivindicación 1: Co-cristales caracterizados porque son co-cristales de compuestos de fórmula (1) en la que R1 es alquilo C1-6, haloalquilo C1-6, O-haloalquilo C1-6, halógeno; m es 1, 2 ó 3; cada uno de R2a y R2b se selecciona independientemente entre H, alquilo C1-6, alquenilo C1-6, alquinilo C1-6, cicloalquilo C3-6, COO-alquilo C1-6, O-alquilo C1-6, CONR2b1R2b2, halógeno; R2b1 es H, alquilo C1-6, alquil C0-4-cicloalquilo C3-6, haloalquilo C1-6; R2b2 es H, alquilo C1-6; o R2b1 y R2b2 juntos son un grupo alquileno C3-6 que forma con el átomo de nitrógeno un anillo heterocíclico, donde opcionalmente un átomo de carbono o el anillo está reemplazado por un átomo de oxígeno; R3 es H o alquilo C1-6; X es un anión seleccionado entre el grupo que consiste en cloruro, bromuro, yoduro, sulfato, fosfato, metanosulfonato, nitrato, maleato, acetato, benzoato, citrato, salicilato, fumarato, tartrato, dibenzoiltartrato, oxalato, succinato, benzoato y p-toluenosulfonato; j es 0, 0,5, 1, 1,5 ó 2; con un agente de formación de co-cristales seleccionado entre el grupo que consiste en ácido prótico, ácido hipúrico, ácido L-piroglutámico, ácido D-piroglutámico, ácido nicotínico, ácido L-(+)-ascórbico, sacarina, piperazina, ácido 3-hidroxi-2-naftoico, ácido múcico (galactárico), ácido pamoico (embónico), ácido esteárico, ácido cólico, ácido desoxicólico, nicotinamida, isonicotinamida, succinamida, uracilo, L-lisina, L-prolina, D-valina, L-arginina, glicina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10186901 | 2010-10-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083353A1 true AR083353A1 (es) | 2013-02-21 |
Family
ID=44741339
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110103717A AR083353A1 (es) | 2010-10-07 | 2011-10-06 | Co-cristales y sales de inhibidores de ccr3 |
Country Status (37)
| Country | Link |
|---|---|
| US (3) | US8742115B2 (es) |
| EP (1) | EP2625174B1 (es) |
| JP (1) | JP5794713B2 (es) |
| KR (3) | KR102163874B1 (es) |
| CN (1) | CN103140486B (es) |
| AP (1) | AP3268A (es) |
| AR (1) | AR083353A1 (es) |
| AU (1) | AU2011311530B2 (es) |
| BR (2) | BR122021010665B1 (es) |
| CA (1) | CA2807255C (es) |
| CL (1) | CL2013000488A1 (es) |
| CO (1) | CO6710910A2 (es) |
| CY (1) | CY1116168T1 (es) |
| DK (1) | DK2625174T3 (es) |
| EA (1) | EA029097B1 (es) |
| EC (1) | ECSP13012600A (es) |
| ES (1) | ES2535264T3 (es) |
| GE (1) | GEP20166488B (es) |
| HR (1) | HRP20150419T1 (es) |
| HU (1) | HUE024540T2 (es) |
| IL (1) | IL224269A (es) |
| MA (1) | MA34545B1 (es) |
| ME (1) | ME02040B (es) |
| MX (1) | MX2013003785A (es) |
| MY (1) | MY167898A (es) |
| NZ (1) | NZ605827A (es) |
| PE (1) | PE20140188A1 (es) |
| PH (1) | PH12013500644A1 (es) |
| PL (1) | PL2625174T3 (es) |
| PT (1) | PT2625174E (es) |
| RS (1) | RS53858B1 (es) |
| SG (1) | SG188949A1 (es) |
| SI (1) | SI2625174T1 (es) |
| TW (1) | TWI546294B (es) |
| UA (1) | UA109290C2 (es) |
| UY (1) | UY33655A (es) |
| WO (1) | WO2012045803A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8278302B2 (en) | 2009-04-08 | 2012-10-02 | Boehringer Ingelheim International Gmbh | Substituted piperidines as CCR3 antagonists |
| UA109290C2 (uk) | 2010-10-07 | 2015-08-10 | Спільні кристали і солі інгібіторів ccr3 | |
| AR090566A1 (es) * | 2012-04-02 | 2014-11-19 | Boehringer Ingelheim Int | Proceso para la produccion de inhibidores de crr |
| US20130261153A1 (en) * | 2012-04-03 | 2013-10-03 | Boehringer Ingelheim International Gmbh | Use of ccr3-inhibitors |
| US10213421B2 (en) * | 2012-04-04 | 2019-02-26 | Alkahest, Inc. | Pharmaceutical formulations comprising CCR3 antagonists |
| US11382907B2 (en) * | 2017-04-05 | 2022-07-12 | Alkahest, Inc. | Methods and compositions for treating aging-associated impairments using CCR3-inhibitors |
| US20200054622A1 (en) * | 2017-04-05 | 2020-02-20 | Alkahest, Inc. | Methods and Compositions for Treating Aging-Associated Impairments Using CCR3-Inhibitors |
| MX394915B (es) | 2017-04-05 | 2025-03-24 | Alkahest Inc | Metodos y composiciones para tratar enfermedades asociadas a la retina mediante inhibidores de ccr3 |
| CN111343983A (zh) * | 2017-10-13 | 2020-06-26 | 万能溶剂有限公司 | 使用ccr3抑制剂治疗瘙痒、干燥症和相关疾病的方法和组合物 |
| CA3097083A1 (en) | 2018-05-15 | 2019-11-21 | Alkahest, Inc. | Treatment of aging-associated disease with modulators of leukotriene a4 hydrolase |
| JP7528065B2 (ja) * | 2018-09-26 | 2024-08-05 | アルカヘスト，インコーポレイテッド | Ｃｃｒ３阻害剤を用いて、加齢性機能障害を治療するための方法および組成物 |
| AU2021287906B2 (en) * | 2020-06-11 | 2025-09-11 | Alkahest Inc. | Methods of improving retina-associated disease outcome using CCR3-inhibitors |
| CA3221177A1 (en) | 2021-11-01 | 2023-05-04 | Meghan Kerrisk Campbell | Benzodioxane modulators of leukotriene a4 hydrolase (lta4h) for prevention and treatment of aging-associated diseases |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| SE7907121L (sv) | 1979-08-27 | 1981-02-28 | Astra Laekemedel Ab | Ftalimidinderivat |
| JP2807577B2 (ja) | 1990-06-15 | 1998-10-08 | エーザイ株式会社 | 環状アミド誘導体 |
| AU2335699A (en) | 1998-01-21 | 1999-08-09 | Kyowa Hakko Kogyo Co. Ltd. | Chemokine receptor antagonists and methods of use therefor |
| US6140349A (en) | 1998-02-02 | 2000-10-31 | Merck & Co., Inc. | Cyclic amine modulators of chemokine receptor activity |
| AU2654399A (en) | 1998-02-02 | 1999-08-16 | Merck & Co., Inc. | Cyclic amine modulators of chemokine receptor activity |
| WO2003066593A2 (en) * | 2001-11-29 | 2003-08-14 | Schering Corporation | Preparation of pharmaceutical salts of 4 ( (z) - (4-bromophenyl) (ethoxyimino) methyl )-1'-( (2,4-dimethyl-1-oxido-3-pyridinyl) carbonyl) -4'-methyl-1,4' bipiperidine as ccr5-antagonists for the treatment of aids and related hiv infections |
| US7452555B2 (en) | 2003-01-21 | 2008-11-18 | S.S.C.I., Inc. | Cocrystallization |
| AU2004283842A1 (en) | 2003-10-24 | 2005-05-06 | F. Hoffmann-La Roche Ag | CCR3 receptor antagonists |
| ES2324224T3 (es) | 2004-02-05 | 2009-08-03 | Schering Corporation | Derivados de piperidina que se pueden utilizar como antagonistas ccr3. |
| EP1765379A4 (en) | 2004-06-17 | 2009-05-27 | Transform Pharmaceuticals Inc | PHARMACEUTICAL CO-CRYSTAL COMPOSITIONS AND RELEVANT USE METHOD |
| JP2006137718A (ja) | 2004-11-12 | 2006-06-01 | Astellas Pharma Inc | インドール若しくはインダゾール誘導体 |
| WO2006083390A2 (en) | 2004-12-07 | 2006-08-10 | Children's Hospital Medical Center | Eotaxin-3 in eosinophilic esophagitis |
| DOP2006000051A (es) | 2005-02-24 | 2006-08-31 | Lilly Co Eli | Inhibidores de vegf-r2 y métodos |
| JP3701964B1 (ja) | 2005-03-08 | 2005-10-05 | アステラス製薬株式会社 | キヌクリジン誘導体の新規な塩 |
| EP2059515A2 (en) * | 2006-04-12 | 2009-05-20 | Pfizer Limited | Pyrrolidine derivatives as modulators of chemokine ccr5 receptors |
| KR101176697B1 (ko) | 2006-04-20 | 2012-08-23 | 에프. 호프만-라 로슈 아게 | 케모카인 수용체의 다이아제판 유도체 조절자 |
| GB0701992D0 (en) | 2007-02-02 | 2007-03-14 | 7Tm Pharma As | Grehlin Receptor Modulators |
| US8008092B2 (en) | 2007-10-09 | 2011-08-30 | University Of Kentucky Research Foundation | CCR3 inhibition for ocular angiogenesis and macular degeneration |
| TW201000446A (en) | 2008-05-30 | 2010-01-01 | Astrazeneca Ab | New compounds useful in pain therapy |
| US8278302B2 (en) | 2009-04-08 | 2012-10-02 | Boehringer Ingelheim International Gmbh | Substituted piperidines as CCR3 antagonists |
| UA109290C2 (uk) | 2010-10-07 | 2015-08-10 | Спільні кристали і солі інгібіторів ccr3 | |
| AR090566A1 (es) | 2012-04-02 | 2014-11-19 | Boehringer Ingelheim Int | Proceso para la produccion de inhibidores de crr |
| US20130261153A1 (en) | 2012-04-03 | 2013-10-03 | Boehringer Ingelheim International Gmbh | Use of ccr3-inhibitors |
| US10213421B2 (en) | 2012-04-04 | 2019-02-26 | Alkahest, Inc. | Pharmaceutical formulations comprising CCR3 antagonists |
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2011
- 2011-06-10 UA UAA201305572A patent/UA109290C2/ru unknown
- 2011-10-06 KR KR1020177037823A patent/KR102163874B1/ko active Active
- 2011-10-06 AR ARP110103717A patent/AR083353A1/es unknown
- 2011-10-06 SG SG2013013305A patent/SG188949A1/en unknown
- 2011-10-06 US US13/267,417 patent/US8742115B2/en active Active
- 2011-10-06 UY UY0001033655A patent/UY33655A/es unknown
- 2011-10-06 PT PT11764572T patent/PT2625174E/pt unknown
- 2011-10-06 ES ES11764572.1T patent/ES2535264T3/es active Active
- 2011-10-06 BR BR122021010665-7A patent/BR122021010665B1/pt active IP Right Grant
- 2011-10-06 WO PCT/EP2011/067437 patent/WO2012045803A1/en not_active Ceased
- 2011-10-06 KR KR1020137008683A patent/KR101844215B1/ko active Active
- 2011-10-06 TW TW100136338A patent/TWI546294B/zh active
- 2011-10-06 AP AP2013006679A patent/AP3268A/xx active
- 2011-10-06 MY MYPI2013000801A patent/MY167898A/en unknown
- 2011-10-06 AU AU2011311530A patent/AU2011311530B2/en active Active
- 2011-10-06 MX MX2013003785A patent/MX2013003785A/es active IP Right Grant
- 2011-10-06 RS RS20150131A patent/RS53858B1/sr unknown
- 2011-10-06 MA MA35770A patent/MA34545B1/fr unknown
- 2011-10-06 SI SI201130394T patent/SI2625174T1/sl unknown
- 2011-10-06 ME MEP-2015-17A patent/ME02040B/me unknown
- 2011-10-06 NZ NZ605827A patent/NZ605827A/en unknown
- 2011-10-06 EP EP11764572.1A patent/EP2625174B1/en active Active
- 2011-10-06 BR BR112013008211-9A patent/BR112013008211B1/pt active IP Right Grant
- 2011-10-06 PH PH1/2013/500644A patent/PH12013500644A1/en unknown
- 2011-10-06 JP JP2013532190A patent/JP5794713B2/ja active Active
- 2011-10-06 HU HUE11764572A patent/HUE024540T2/hu unknown
- 2011-10-06 PE PE2013000781A patent/PE20140188A1/es not_active Application Discontinuation
- 2011-10-06 KR KR1020197025850A patent/KR102239690B1/ko active Active
- 2011-10-06 DK DK11764572.1T patent/DK2625174T3/da active
- 2011-10-06 EA EA201300436A patent/EA029097B1/ru unknown
- 2011-10-06 HR HRP20150419TT patent/HRP20150419T1/hr unknown
- 2011-10-06 CN CN201180047995.1A patent/CN103140486B/zh active Active
- 2011-10-06 PL PL11764572T patent/PL2625174T3/pl unknown
- 2011-10-06 GE GEAP201113082A patent/GEP20166488B/en unknown
- 2011-10-06 CA CA2807255A patent/CA2807255C/en active Active
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2013
- 2013-01-17 IL IL224269A patent/IL224269A/en unknown
- 2013-02-19 CL CL2013000488A patent/CL2013000488A1/es unknown
- 2013-04-08 CO CO13090552A patent/CO6710910A2/es unknown
- 2013-05-03 EC ECSP13012600 patent/ECSP13012600A/es unknown
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2014
- 2014-01-22 US US14/160,646 patent/US20140135307A1/en not_active Abandoned
- 2014-12-17 US US14/572,889 patent/US9233950B2/en active Active
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2015
- 2015-04-07 CY CY20151100331T patent/CY1116168T1/el unknown
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