IL124309A - Aztidinylalkyl derivatives of the N-heterocyclic compounds, the process for their preparation and medicinal preparations containing them for the antagonists of tachycin - Google Patents

Aztidinylalkyl derivatives of the N-heterocyclic compounds, the process for their preparation and medicinal preparations containing them for the antagonists of tachycin

Info

Publication number: IL124309A
Authority: IL; Israel
Prior art keywords: alkyl; compound; formula; cycloalkyl; alkoxy
Prior art date: 1996-01-05

Application number

IL12430996A

Other languages

English (en)

Hebrew (he)

Other versions

IL124309A0 (en

Original Assignee

Pfizer Res And Dev Company

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1996-01-05

Filing date

1996-12-09

Publication date

2002-11-10

1996-12-09 Application filed by Pfizer Res And Dev Company filed Critical Pfizer Res And Dev Company

1996-12-09 Priority to IL14532496A priority Critical patent/IL145324A0/xx

1998-12-06 Publication of IL124309A0 publication Critical patent/IL124309A0/xx

2002-11-10 Publication of IL124309A publication Critical patent/IL124309A/en

Links

238000002360 preparation method Methods 0.000 title claims description 131
238000000034 method Methods 0.000 title claims description 61
102000003141 Tachykinin Human genes 0.000 title claims description 9
108060008037 tachykinin Proteins 0.000 title claims description 9
230000008569 process Effects 0.000 title claims description 5
239000008194 pharmaceutical composition Substances 0.000 title claims description 4
230000003042 antagnostic effect Effects 0.000 title description 2
125000006543 azetidinylalkyl group Chemical group 0.000 title description 2
150000002391 heterocyclic compounds Chemical class 0.000 title description 2
150000001875 compounds Chemical class 0.000 claims abstract description 291
125000000217 alkyl group Chemical group 0.000 claims abstract description 96
-1 fluoro (C1-C4) alkyl Chemical group 0.000 claims abstract description 95
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 66
150000003839 salts Chemical class 0.000 claims abstract description 57
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 38
229910052757 nitrogen Inorganic materials 0.000 claims abstract description 35
125000003118 aryl group Chemical group 0.000 claims abstract description 32
125000001153 fluoro group Chemical group F* 0.000 claims abstract description 29
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract description 28
125000001424 substituent group Chemical group 0.000 claims abstract description 20
125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims abstract description 18
125000005843 halogen group Chemical group 0.000 claims abstract description 16
125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 15
229910052760 oxygen Inorganic materials 0.000 claims abstract description 14
125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims abstract description 13
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract description 11
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract description 9
125000001589 carboacyl group Chemical group 0.000 claims abstract description 9
239000001301 oxygen Substances 0.000 claims abstract description 9
125000002947 alkylene group Chemical group 0.000 claims abstract description 6
125000000623 heterocyclic group Chemical group 0.000 claims abstract description 6
101100439665 Arabidopsis thaliana SWI2 gene Proteins 0.000 claims abstract description 5
125000001624 naphthyl group Chemical group 0.000 claims abstract description 5
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims abstract description 4
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract description 4
125000005842 heteroatom Chemical group 0.000 claims abstract description 4
125000001544 thienyl group Chemical group 0.000 claims abstract description 4
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 4
NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract description 3
125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims abstract description 3
125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims abstract description 3
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 3
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 3
125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 11
229910003844 NSO2 Inorganic materials 0.000 claims abstract 4
125000001041 indolyl group Chemical group 0.000 claims abstract 2
ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims description 88
238000006243 chemical reaction Methods 0.000 claims description 84
239000000203 mixture Substances 0.000 claims description 81
230000002829 reductive effect Effects 0.000 claims description 77
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 50
239000002253 acid Substances 0.000 claims description 48
208000035475 disorder Diseases 0.000 claims description 30
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 24
125000003545 alkoxy group Chemical group 0.000 claims description 21
125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 20
201000010099 disease Diseases 0.000 claims description 20
BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 20
101000831616 Homo sapiens Protachykinin-1 Proteins 0.000 claims description 18
102100024304 Protachykinin-1 Human genes 0.000 claims description 18
239000007858 starting material Substances 0.000 claims description 17
VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims description 16
239000005977 Ethylene Substances 0.000 claims description 16
229910052739 hydrogen Inorganic materials 0.000 claims description 14
QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Chemical group CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 14
125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims description 14
150000001412 amines Chemical class 0.000 claims description 13
206010020751 Hypersensitivity Diseases 0.000 claims description 12
208000002193 Pain Diseases 0.000 claims description 12
208000026935 allergic disease Diseases 0.000 claims description 12
208000004296 neuralgia Diseases 0.000 claims description 12
210000003169 central nervous system Anatomy 0.000 claims description 11
229910052721 tungsten Inorganic materials 0.000 claims description 11
238000010511 deprotection reaction Methods 0.000 claims description 10
229910000027 potassium carbonate Inorganic materials 0.000 claims description 10
ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 claims description 10
125000001246 bromo group Chemical group Br* 0.000 claims description 9
239000003814 drug Substances 0.000 claims description 9
125000006239 protecting group Chemical group 0.000 claims description 9
VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 8
230000000694 effects Effects 0.000 claims description 8
238000006268 reductive amination reaction Methods 0.000 claims description 8
201000004624 Dermatitis Diseases 0.000 claims description 7
239000005557 antagonist Substances 0.000 claims description 7
125000001309 chloro group Chemical group Cl* 0.000 claims description 7
230000003647 oxidation Effects 0.000 claims description 7
238000007254 oxidation reaction Methods 0.000 claims description 7
208000019901 Anxiety disease Diseases 0.000 claims description 6
208000001387 Causalgia Diseases 0.000 claims description 6
208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 6
208000000094 Chronic Pain Diseases 0.000 claims description 6
208000023890 Complex Regional Pain Syndromes Diseases 0.000 claims description 6
206010011224 Cough Diseases 0.000 claims description 6
208000011231 Crohn disease Diseases 0.000 claims description 6
206010012289 Dementia Diseases 0.000 claims description 6
206010012442 Dermatitis contact Diseases 0.000 claims description 6
208000032131 Diabetic Neuropathies Diseases 0.000 claims description 6
208000034347 Faecal incontinence Diseases 0.000 claims description 6
206010021639 Incontinence Diseases 0.000 claims description 6
208000022559 Inflammatory bowel disease Diseases 0.000 claims description 6
208000019693 Lung disease Diseases 0.000 claims description 6
MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 claims description 6
206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 6
201000004681 Psoriasis Diseases 0.000 claims description 6
208000028017 Psychotic disease Diseases 0.000 claims description 6
241000159243 Toxicodendron radicans Species 0.000 claims description 6
230000001154 acute effect Effects 0.000 claims description 6
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206010003246 arthritis Diseases 0.000 claims description 6
208000006673 asthma Diseases 0.000 claims description 6
208000010668 atopic eczema Diseases 0.000 claims description 6
206010009887 colitis Diseases 0.000 claims description 6
208000014439 complex regional pain syndrome type 2 Diseases 0.000 claims description 6
208000010247 contact dermatitis Diseases 0.000 claims description 6
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
201000003146 cystitis Diseases 0.000 claims description 6
208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 6
230000009610 hypersensitivity Effects 0.000 claims description 6
208000027866 inflammatory disease Diseases 0.000 claims description 6
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208000005877 painful neuropathy Diseases 0.000 claims description 6
208000033808 peripheral neuropathy Diseases 0.000 claims description 6
206010039083 rhinitis Diseases 0.000 claims description 6
208000000187 Abnormal Reflex Diseases 0.000 claims description 5
206010020745 hyperreflexia Diseases 0.000 claims description 5
230000035859 hyperreflexia Effects 0.000 claims description 5
238000011282 treatment Methods 0.000 claims description 5
125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 4
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 4
125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims description 4
230000002496 gastric effect Effects 0.000 claims description 4
125000002346 iodo group Chemical group I* 0.000 claims description 4
229910052717 sulfur Inorganic materials 0.000 claims description 4
ZNSMNVMLTJELDZ-UHFFFAOYSA-N Bis(2-chloroethyl)ether Chemical compound ClCCOCCCl ZNSMNVMLTJELDZ-UHFFFAOYSA-N 0.000 claims description 3
125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 3
239000003085 diluting agent Substances 0.000 claims description 3
238000007327 hydrogenolysis reaction Methods 0.000 claims description 3
230000007062 hydrolysis Effects 0.000 claims description 3
238000006460 hydrolysis reaction Methods 0.000 claims description 3
238000004519 manufacturing process Methods 0.000 claims description 3
CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 claims description 2
UOWHCAKKYIRMSX-UHFFFAOYSA-N [N].C1CNC1 Chemical group [N].C1CNC1 UOWHCAKKYIRMSX-UHFFFAOYSA-N 0.000 claims description 2
230000010933 acylation Effects 0.000 claims description 2
238000005917 acylation reaction Methods 0.000 claims description 2
150000008064 anhydrides Chemical class 0.000 claims description 2
229910052799 carbon Inorganic materials 0.000 claims description 2
238000009833 condensation Methods 0.000 claims description 2
230000005494 condensation Effects 0.000 claims description 2
238000001212 derivatisation Methods 0.000 claims description 2
239000012948 isocyanate Substances 0.000 claims description 2
150000002513 isocyanates Chemical class 0.000 claims description 2
125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
WJKHJLXJJJATHN-UHFFFAOYSA-N triflic anhydride Chemical compound FC(F)(F)S(=O)(=O)OS(=O)(=O)C(F)(F)F WJKHJLXJJJATHN-UHFFFAOYSA-N 0.000 claims description 2
125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
101100097467 Arabidopsis thaliana SYD gene Proteins 0.000 claims 1
101100495925 Schizosaccharomyces pombe (strain 972 / ATCC 24843) chr3 gene Proteins 0.000 claims 1
GRGCWBWNLSTIEN-UHFFFAOYSA-N trifluoromethanesulfonyl chloride Chemical compound FC(F)(F)S(Cl)(=O)=O GRGCWBWNLSTIEN-UHFFFAOYSA-N 0.000 claims 1
125000001072 heteroaryl group Chemical group 0.000 abstract description 4
125000004423 acyloxy group Chemical group 0.000 abstract description 3
125000000325 methylidene group Chemical group [H]C([H])=* 0.000 abstract 4
229910020008 S(O) Inorganic materials 0.000 abstract 3
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 abstract 2
RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 abstract 2
125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 abstract 2
125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 200
239000000243 solution Substances 0.000 description 153
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 123
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 117
239000002904 solvent Substances 0.000 description 92
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 80
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CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 70
VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 57
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 50
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238000005160 1H NMR spectroscopy Methods 0.000 description 38
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235000019341 magnesium sulphate Nutrition 0.000 description 35
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UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 30
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239000000741 silica gel Substances 0.000 description 26
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239000012074 organic phase Substances 0.000 description 17
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Classifications

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- 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
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- 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
- C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/30—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
- C07D211/32—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms

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Reproductive Health (AREA)
Heart & Thoracic Surgery (AREA)
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Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Pyrane Compounds (AREA)
Pyrrole Compounds (AREA)
Hydrogenated Pyridines (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Peptides Or Proteins (AREA)

IL12430996A 1996-01-05 1996-12-09 Aztidinylalkyl derivatives of the N-heterocyclic compounds, the process for their preparation and medicinal preparations containing them for the antagonists of tachycin IL124309A (en)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
IL14532496A IL145324A0 (en)	1996-01-05	1996-12-09	Azetidinylalkyl derivatives of n-containing heterocyclic compounds, process for their preparation and a pharmaceutical composition containing them for antagonizing tachykinin

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
GBGB9600235.7A GB9600235D0 (en)	1996-01-05	1996-01-05	Therapeutic agents
PCT/EP1996/005613 WO1997025322A1 (en)	1996-01-05	1996-12-09	3-azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

Publications (2)

Publication Number	Publication Date
IL124309A0 IL124309A0 (en)	1998-12-06
IL124309A true IL124309A (en)	2002-11-10

Family

ID=10786682

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
IL12430996A IL124309A (en)	1996-01-05	1996-12-09	Aztidinylalkyl derivatives of the N-heterocyclic compounds, the process for their preparation and medicinal preparations containing them for the antagonists of tachycin
IL14532496A IL145324A0 (en)	1996-01-05	1996-12-09	Azetidinylalkyl derivatives of n-containing heterocyclic compounds, process for their preparation and a pharmaceutical composition containing them for antagonizing tachykinin

Family Applications After (1)

Application Number	Title	Priority Date	Filing Date
IL14532496A IL145324A0 (en)	1996-01-05	1996-12-09	Azetidinylalkyl derivatives of n-containing heterocyclic compounds, process for their preparation and a pharmaceutical composition containing them for antagonizing tachykinin

Country Status (38)

Country	Link
US (1)	US6242438B1 (es)
EP (1)	EP0871623B1 (es)
JP (2)	JP3123611B2 (es)
KR (1)	KR100275402B1 (es)
AP (1)	AP709A (es)
AR (2)	AR005338A1 (es)
AT (1)	ATE232526T1 (es)
AU (1)	AU708282B2 (es)
BG (1)	BG102589A (es)
BR (1)	BR9612412A (es)
CA (1)	CA2237189C (es)
CO (1)	CO4750815A1 (es)
CZ (1)	CZ209398A3 (es)
DE (1)	DE69626220T2 (es)
DK (1)	DK0871623T3 (es)
DZ (1)	DZ2155A1 (es)
ES (1)	ES2190486T3 (es)
GB (1)	GB9600235D0 (es)
HR (1)	HRP970006A2 (es)
HU (1)	HUP9903590A3 (es)
IL (2)	IL124309A (es)
IS (1)	IS1876B (es)
MA (1)	MA26417A1 (es)
NO (1)	NO311838B1 (es)
NZ (1)	NZ324712A (es)
OA (1)	OA10863A (es)
PE (1)	PE29798A1 (es)
PL (1)	PL185723B1 (es)
RU (1)	RU2158264C2 (es)
SI (1)	SI0871623T1 (es)
SK (1)	SK89598A3 (es)
TN (1)	TNSN96174A1 (es)
TR (1)	TR199801268T2 (es)
TW (1)	TW472054B (es)
UY (1)	UY24429A1 (es)
WO (1)	WO1997025322A1 (es)
YU (1)	YU71496A (es)
ZA (1)	ZA9747B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
GB9714129D0 (en) *	1997-07-04	1997-09-10	Pfizer Ltd	Azetidines
AU1089599A (en) *	1997-10-15	1999-05-03	Coelacanth Chemical Corporation	Synthesis of azetidine derivatives
KR100610538B1 (ko) *	1997-12-04	2006-08-09	상꾜 가부시키가이샤	지환식 아실화 복소환 유도체
GB9821898D0 (en) *	1998-10-08	1998-12-02	Pfizer Ltd	Heterocycles
ATE367811T1 (de) *	2000-06-12	2007-08-15	Univ Rochester	Methode zur behandlung von hitzewallungen, durch verwendung eines tachikinin-rezeptor antagonisten
US6642226B2 (en) *	2001-02-06	2003-11-04	Hoffman-La Roche Inc.	Substituted phenyl-piperidine methanone compounds
GB0130261D0 (en) *	2001-12-18	2002-02-06	Pfizer Ltd	Lactams as tachykinin antagonists
EP1501826B1 (en) *	2002-02-01	2006-09-27	F. Hoffman-la Roche AG	Substituted indoles as alpha-1 agonists
US7674783B2 (en) *	2002-11-22	2010-03-09	Dimera Inc.	Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease
JP4660199B2 (ja) *	2002-12-23	2011-03-30	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	置換１−ピペリジン−４−イル−４−アゼチジン−３−イル−ピペラジン誘導体およびそれらのニューロキニン拮抗薬としての使用
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1996
- 1996-01-05 GB GBGB9600235.7A patent/GB9600235D0/en active Pending
- 1996-12-06 TW TW085115107A patent/TW472054B/zh not_active IP Right Cessation
- 1996-12-09 IL IL12430996A patent/IL124309A/en not_active IP Right Cessation
- 1996-12-09 KR KR1019980705159A patent/KR100275402B1/ko not_active Expired - Fee Related
- 1996-12-09 CA CA002237189A patent/CA2237189C/en not_active Expired - Fee Related
- 1996-12-09 AT AT96943119T patent/ATE232526T1/de not_active IP Right Cessation
- 1996-12-09 SI SI9630590T patent/SI0871623T1/xx unknown
- 1996-12-09 AU AU11950/97A patent/AU708282B2/en not_active Ceased
- 1996-12-09 IL IL14532496A patent/IL145324A0/xx unknown
- 1996-12-09 US US09/297,736 patent/US6242438B1/en not_active Expired - Fee Related
- 1996-12-09 CZ CZ982093A patent/CZ209398A3/cs unknown
- 1996-12-09 EP EP96943119A patent/EP0871623B1/en not_active Expired - Lifetime
- 1996-12-09 ES ES96943119T patent/ES2190486T3/es not_active Expired - Lifetime
- 1996-12-09 SK SK895-98A patent/SK89598A3/sk unknown
- 1996-12-09 HU HU9903590A patent/HUP9903590A3/hu unknown
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- 1996-12-09 JP JP09520769A patent/JP3123611B2/ja not_active Expired - Fee Related
- 1996-12-09 RU RU98114667/04A patent/RU2158264C2/ru not_active IP Right Cessation
- 1996-12-09 PL PL96327665A patent/PL185723B1/pl not_active IP Right Cessation
- 1996-12-09 WO PCT/EP1996/005613 patent/WO1997025322A1/en not_active Ceased
- 1996-12-09 TR TR1998/01268T patent/TR199801268T2/xx unknown
- 1996-12-09 DK DK96943119T patent/DK0871623T3/da active
- 1996-12-09 BR BR9612412A patent/BR9612412A/pt not_active Application Discontinuation
- 1996-12-09 DE DE69626220T patent/DE69626220T2/de not_active Expired - Fee Related
- 1996-12-19 AP APAP/P/1996/000901A patent/AP709A/en active
- 1996-12-27 PE PE1996000960A patent/PE29798A1/es not_active Application Discontinuation
- 1996-12-31 MA MA24446A patent/MA26417A1/fr unknown
- 1996-12-31 DZ DZ960200A patent/DZ2155A1/fr active
- 1996-12-31 TN TNTNSN96174A patent/TNSN96174A1/fr unknown
- 1996-12-31 YU YU71496A patent/YU71496A/sr unknown
1997
- 1997-01-02 AR ARP970100003A patent/AR005338A1/es unknown
- 1997-01-02 AR ARP970100004A patent/AR005339A1/es unknown
- 1997-01-03 HR HR9600235.7A patent/HRP970006A2/xx not_active Application Discontinuation
- 1997-01-03 UY UY24429A patent/UY24429A1/es not_active Application Discontinuation
- 1997-01-03 ZA ZA9747A patent/ZA9747B/xx unknown
- 1997-01-07 CO CO97000263A patent/CO4750815A1/es unknown
1998
- 1998-05-28 IS IS4760A patent/IS1876B/is unknown
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- 1998-06-30 BG BG102589A patent/BG102589A/xx unknown
2000
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Also Published As

Publication number	Publication date
AP709A (en)	1998-12-22
TNSN96174A1 (fr)	2005-03-15
BG102589A (en)	1999-09-30
SK89598A3 (en)	2000-02-14
IS4760A (is)	1998-05-28
DZ2155A1 (fr)	2002-10-26
UY24429A1 (es)	2001-08-27
AP9600901A0 (en)	1997-01-31
IL145324A0 (en)	2002-06-30
WO1997025322A1 (en)	1997-07-17
NO311838B1 (no)	2002-02-04
HUP9903590A3 (en)	2002-01-28
NO982651D0 (no)	1998-06-09
EP0871623B1 (en)	2003-02-12
HRP970006A2 (en)	1998-06-30
KR19990077027A (ko)	1999-10-25
CA2237189A1 (en)	1997-07-17
TR199801268T2 (xx)	1998-10-21
IS1876B (is)	2003-05-28
ZA9747B (en)	1998-09-30
TW472054B (en)	2002-01-11
EP0871623A1 (en)	1998-10-21
PE29798A1 (es)	1998-06-11
CO4750815A1 (es)	1999-03-31
PL185723B1 (pl)	2003-07-31
PL327665A1 (en)	1998-12-21
AR005338A1 (es)	1999-04-28
NO982651L (no)	1998-06-09
RU2158264C2 (ru)	2000-10-27
DK0871623T3 (da)	2003-03-31
AU1195097A (en)	1997-08-01
JP3123611B2 (ja)	2001-01-15
DE69626220T2 (de)	2003-08-28
BR9612412A (pt)	1999-07-13
ATE232526T1 (de)	2003-02-15
US6242438B1 (en)	2001-06-05
IL124309A0 (en)	1998-12-06
AR005339A1 (es)	1999-04-28
OA10863A (en)	2001-09-27
GB9600235D0 (en)	1996-03-06
NZ324712A (en)	1999-05-28
ES2190486T3 (es)	2003-08-01
JP3254205B2 (ja)	2002-02-04
CZ209398A3 (cs)	1999-04-14
AU708282B2 (en)	1999-07-29
DE69626220D1 (de)	2003-03-20
JPH11501667A (ja)	1999-02-09
KR100275402B1 (ko)	2000-12-15
YU71496A (en)	1999-11-22
HUP9903590A2 (hu)	2000-05-28
MA26417A1 (fr)	2004-12-20
JP2000344741A (ja)	2000-12-12
CA2237189C (en)	2002-09-03
SI0871623T1 (en)	2003-08-31

Legal Events

Date	Code	Title
2003-04-10	FF	Patent granted
2003-05-29	KB	Patent renewed
2007-08-19	MM9K	Patent not in force due to non-payment of renewal fees

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