LV11431B - Central cholecystokinin antagonists for treatment of psychiatric disorders - Google Patents
Central cholecystokinin antagonists for treatment of psychiatric disorders Download PDFInfo
- Publication number
- LV11431B LV11431B LVP-96-32A LV960032A LV11431B LV 11431 B LV11431 B LV 11431B LV 960032 A LV960032 A LV 960032A LV 11431 B LV11431 B LV 11431B
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- LV
- Latvia
- Prior art keywords
- groups
- alkyl
- hydrogen
- phenyl
- independently
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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- 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
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/20—Hypnotics; Sedatives
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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Claims (6)
- LV 11431 Izgudrojuma formula 1. D.L-glutamīnskābes un D.L-asparagīnskābes farmakoloģiski aktīvo atvasinājumu ar formulu (I), (ΙΑ), (II) vai (III) vai to farmaceitiski pieņemamo sālu pielietojums anksiofītisku medikamentu ražošanai, kur formulās (I) un (IA) COOH CO-R2 CH2)n (I) I ch-nh-co-Ri (CH2)n (IA) CH-NH-CO-Ri COOH CO-R2 n ir 1 vai 2; R1 ir fenilgrupa, kas aizvietota ar: 1, 2 vai 3 lineārām vai sazarotām Ci^alkilgrupām, kas var būt vienādas vai dažādas, halogēna atomiem, ciāngrupu vai trifluormetilgrupu; R2 ir ņemts no rindas: morfolinilgrupa, piperidinilgrupa vai aminogrupa, kas aizvietota ar vienu vai divām lineārām vai sazarotām vai cikliskām Ci-ealkilgrupām, kas var būt vienādas vai dažādas;formulā (II) 1 R1 ir ūdeņraža atoms, lineāra vai sazarota Ci^alkilgrupa, Ci-5alkenilgrupa, Ci.5alkinilgrupa, -X12COO R6, -X11-C3.7Cikloalkilgrupa, -X12NR4R5, -X12CONR4R , -X12CN vai -X11C(X10)3; R2 ir ūdeņraža atoms, Ci^alkilgrupa, fenilgrupa, kas neobligāti aizvietota ar 1 - 2 halogēna atomiem, Ci.7alkilgrupām, Ci.7alkoksigrupām, Ci.7alkiltiogrupām, karboksilgrupām, karboksi-Ci-7alkilgrupām, nitro-grupām, trifluormetilgrupām vai hidroksilgrupām, 2-, 3- vai 4-piridil-grupa, -X12SCH3, -X12SOCH3, -X12S02CH3, -X12COORe; grupa -X12X2 R3 ir, -X11CX9X11R7, -X11NR18(CH2)qR7, -X11NR18CHCOOR®, -X11X9CX11R7, -NH(CH2)2.3NHR7, -NH(CH2)2.3NHCOR7, -X11NRieS02(CH2)qR7, -X11R7, OH OH I 0 ļ| -X11CHR7 11 ' 7 -X1 C-R7 I -X11CR7 R7 R7a ļ (CH2)q 0 -X11X9CX11R7, 0 -x11cx9x11r7 , | -x11nr18chcoor® , O O 0 nh2 X11X9CCHCH2R7, -X11X9Jx9aX11R7 -x11x9c-ch2-chr7, NHCOOR14 O X2 -X11X9C(CH2)qX9a— J^ļjj 3 , vai =CH-R7, X kur R4 un R5 neatkarīgi viens no otra ir R6 vai grupā NR4R5 kopā ar N atomu abi kopā veido neaizvietotu, mono- vai divaizvietotu, piesātinātu vai nepiesātinātu, vai arī ar benzola gredzenu kondensētu 4-7 locekļu heterociklu, pie kam minētais heterocikls var papildus saturēt otru heteroatomu no rindas: 0 un NCH3, bet minētie aizvietotāji ir neatkarīgi viens no otra ņemti no Ci^alkilgrupām; R® ir ūdeņraža atoms, Ci-7alkilgrupa, CjTcikloalkilgrupa, fenilgrupa vai fenil-Ci-7-alkilgrupa, kas fenilgrupā neobligāti aizvietota ar 1 - 2 halogēna atomiem, 2 LV 11431 Ci.7alkilgrupām, Ci-7alkoksigrupām, nitrogrupām vai trifiuormetilgrupām; R7 un R7a neatkarīgi viens no otra a- vai β-naftilgrupa; fenilgrupa, kas neobligāti aizvietota ar 1 - 2 halogēna atomiem, nitrogrupām, hidroksilgrupām, -X11NR4R5, Ci.7alkilgrupām, trifiuormetilgrupām, ciāngrupām, trifluormetiltiogrupām, etinilgrupām, acetoksigrupām, grupām CH2SCF3, -OCHF2, SH, -SC6H5, -PO3H, Ci-7alkoksigrupām vai Ci-7alkiltiogrupām;R8N N 09ir ūdeņraža atoms, Ci.7alkilgrupa, C3.7cikloalkilgrupa, -X12CONH2, -X12COOR6, -X12-C3-7Cikloalkilgrupa, -X12NR4R5, grupas -X12# -XUCO (CH2) 4f 3 -COCHNHCOOR11 vai -COCHNH- I 12 » 12 ch2r12 ch2r12 R9 un R10 neatkarīgi viens no otra ir ūdeņraža atoms, hidroksilgrupa vai metilgrupa; R11 un R12 neatkarīgi viens no otra ir Ci.7alkilgrupa vai C3-7Cikloalkilgrupa; R13 ir ūdeņraža atoms, Ci.7alkilgrupa, acilgrupa, O vai C3.7cikloalkilgrupa; R14 ir C1-7 alkilgrupa vai fenil-Ci-7alkilgrupa; R15 ir ūdeņraža atoms, C1.7 alkilgrupa, grupavai aminogrupa; R18 ir ūdeņraža atoms, C1.7 alkilgrupa vai acilgrupa; p ir 0, kad blakusesošā grupa =ISF ir nepiesātināta, un 1, kad blakusesošā grupa =N- ir piesātināta, izņemot tādu gadījumu, kad p = 1, R13 ir O un grupa =N- ir nepiesātināta; q ir 0-4; r ir 1 vai 2; XI ir ūdeņraža atoms, nitrogrupa, trifluormetilgrupa, ciāngrupa, hidroksilgrupa, halogēna atoms, Ci-7alkiltiogrupa, Ci^alkoksigrupa, -X11COOR6 vai -X11NR4R5; X2 un X3 neatkarīgi viens no otra ir ūdeņraža atoms, hidroksilgrupa, nitrogrupa, halogēna atoms, Ci-7alkiltiogrupa, Ci^alkilgrupa vai Ci-7alkoksigrupa: X4 irS, O, CH2, NRi8vaiNR8;. X5 ir ūdeņraža atoms, trifluormetilgrupa, ciāngrupa, -COOR6, nitrogrupa vai halogēna atoms; X6 ir O vai HH; X7 ir 0, S, HH vai NR15; X8 ir ūdeņraža atoms vai Ci.7alkilgrupa; X9 un X9a neatkarīgi viens no otra ir NR18vai O; X10 ir F, Cl vai Br; XII nav vispār, vai arī tas ir lineāra vai sazarota Ci^alkilēngrupa; X12 ir lineāra vai sazarota Ci.*alkilēngrupa; = ir piesātināta vai nepiesātināta saite; formulā (III)4 LV 11431 kur R3 R\ R2, R4, R5, R6, R8, R9 R10, R11, R12, R13, R14, R15, p, q, r, X1, X2, X3, X5, X6, X7, X8. X9, X10, X1f un X12 nozīmes ir jau minētās, ir -X11NR1^(CHi)qR16, -NH(CH2)2.3NHR7 -NH(CH2)2.3NHCOR7, -X11NR18CX9aX11R , -X11NR18S02(CH2)qR7, -X11C(=0)R7, grupas 0 0 0 -X11NR18CX11R7 -x11cx9x11r7 , II -x11x9cch-ch2r7 NHCOOR14 onh2 0 „ J I II -X11X9C-CHCH2R7 -X11X9C(CH2)qX9a— -X11C(=0)R R 7 ir a- vai β-naftilgrupa; fenilgrupa, kas neobligāti aizvietota ar 1 - 2 halogēna atomiem, nitrogrupām, hidroksilgrupām, grupām -X11NR4R5, Ci-7alkil-grupām, trifluormetilgrupām, ciāngrupām, trifluormetiltiogrupām, etinilgrupām, acetoksigrupām, grupām CH2SCF3, -OCHF2, SH, SPh, P03H, Ci.7alkoksigrupām, Ci.7alkiltiogrupām vai karboksil-grupām; 0 2-, 3- vai 4-piridilgrupa; ļj OCCS3/ grupa95 R16 ir oc- vai β-naftilgrupa vai 2-indolilgrupa; R18 ir ūdeņraža atoms vai Ci.7alkilgrupa; = ir piesātināta vai nepiesātināta saite.
- 2. Pielietojums pēc 1. punkta, kas atšķiras ar to, ka atvasinājums ir: DL-4-(3,4-dihlorbenzoilamino)-5-(dipentilamino)-5-oksopentānskābe, ^)-4-(3,4-dihlorbenzoilamino)-5-[(3-metoksipropil)pentilamino]-5-oksopentān-skābe, 3(S)-(-)-N-(2,3-dihidro-1 -metil-2-okso-5-fenil-1 H-1,4-benzodiazepin-3-il)-1 H-indol-2-karboksamīds, (R)-N-(2,3-dihidro-1-metil-2-okso-5-fenil-1 H-1,4-benzodiazepin-3-il)-N’-(3-metilfenil)urīnviela vai to farmaceitiski pieņemama sāls.
- 3. Atvasinājuma pēc 1. vai 2. punkta pielietojums tādu medikamentu ražošanai, kas paredzēti zīdītāju abstinences sindroma novēršanai vai ārstēšanai, pārtraucot hronisku ārstēšanu ar dizepāmu.
- 4. Atvasinājuma pēc 1. vai 2. punkta pielietojums tādu medikamentu ražošanai, kas paredzēti zīdītāju abstinences sindroma novēršanai vai ārstēšanai, pārtraucot hronisku kokaīna lietošanu.
- 5. Atvasinājuma pēc 1. vai 2. punkta pielietojums tādu medikamentu ražošanai, kas paredzēti zīdītāju abstinences sindroma novēršanai vai ārstēšanai, pārtraucot hronisku alkohola lietošanu.
- 6. Atvasinājuma pēc 1. vai 2. punkta pielietojums tādu medikamentu ražošanai, kas paredzēti zīdītāju abstinences sindroma novēršanai vai ārstēšanai, pārtraucot hronisku nikotīna lietošanu. 6
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38966589A | 1989-08-04 | 1989-08-04 | |
| US42189689A | 1989-10-16 | 1989-10-16 |
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| Publication Number | Publication Date |
|---|---|
| LV11431A LV11431A (lv) | 1996-08-20 |
| LV11431B true LV11431B (en) | 1996-12-20 |
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| Application Number | Title | Priority Date | Filing Date |
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| LVP-96-32A LV11431B (en) | 1989-08-04 | 1996-02-05 | Central cholecystokinin antagonists for treatment of psychiatric disorders |
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|---|---|
| US (1) | US5550126A (lv) |
| EP (2) | EP0411668B2 (lv) |
| JP (1) | JPH0374328A (lv) |
| AT (1) | ATE119040T1 (lv) |
| CY (1) | CY1983A (lv) |
| DE (1) | DE69017302T3 (lv) |
| DK (1) | DK0411668T4 (lv) |
| HK (1) | HK8197A (lv) |
| LV (1) | LV11431B (lv) |
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| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| EP2864336B1 (en) | 2012-06-06 | 2016-11-23 | Constellation Pharmaceuticals, Inc. | Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| AR094963A1 (es) | 2013-03-04 | 2015-09-09 | Ono Pharmaceutical Co | Reacción de oxidación excelente en el índice de conversión |
| CA2929858C (en) | 2013-11-22 | 2022-03-29 | CL BioSciences LLC | Gastrin antagonists (eg yf476, netazepide) for treatment and prevention of osteoporosis |
| PT3157928T (pt) | 2014-06-20 | 2019-05-30 | Constellation Pharmaceuticals Inc | Formas cristalinas de 2-((4s)-6-(4-clorofenil)-1-metil-4h-benzo[c] isoxazolo[4,5-e]azepin-4-il)acetamida |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE57892B1 (en) * | 1984-06-25 | 1993-05-05 | Rotta Research Lab | Glutamic and aspartic acid derivatives |
| CA1332410C (en) * | 1984-06-26 | 1994-10-11 | Roger M. Freidinger | Benzodiazepine analogs |
| US5004741A (en) * | 1984-06-26 | 1991-04-02 | Merck & Co., Inc. | Methods of antagonizing CCK or gastrin with benzodiazepine analogs |
| US4820834A (en) * | 1984-06-26 | 1989-04-11 | Merck & Co., Inc. | Benzodiazepine analogs |
| IT1215169B (it) * | 1985-12-17 | 1990-01-31 | Rotta Research Lab | Derivati alchil ossigenati degli acidi glutammico ed aspartico ad attivita antagonista su polipeptidi bioattivi e procedimento per la loro preparazione |
| IT1217123B (it) * | 1987-02-05 | 1990-03-14 | Rotta Research Lab | Derivati otticamente attivi dell acido 5 pentilammino 5 oxo pentanoico r ad attivita antagonista della colecistochinina e procedimento per la loro preparazione |
| ATE119040T1 (de) * | 1989-08-04 | 1995-03-15 | Merck Sharp & Dohme | Zentrale cholecystokinin-antagonisten zur behandlung von psychiatrischen krankheiten. |
| US5153191A (en) * | 1991-08-20 | 1992-10-06 | Warner-Lambert Company | Cholecystokinin antagonists useful for treating depression |
-
1990
- 1990-08-03 AT AT90114993T patent/ATE119040T1/de not_active IP Right Cessation
- 1990-08-03 DE DE69017302T patent/DE69017302T3/de not_active Expired - Fee Related
- 1990-08-03 JP JP2205335A patent/JPH0374328A/ja active Pending
- 1990-08-03 EP EP90114993A patent/EP0411668B2/en not_active Expired - Lifetime
- 1990-08-03 EP EP94106046A patent/EP0727215A3/en not_active Withdrawn
- 1990-08-03 DK DK90114993T patent/DK0411668T4/da active
-
1995
- 1995-01-30 US US08/380,467 patent/US5550126A/en not_active Expired - Fee Related
-
1996
- 1996-02-05 LV LVP-96-32A patent/LV11431B/en unknown
-
1997
- 1997-01-16 HK HK8197A patent/HK8197A/xx not_active IP Right Cessation
- 1997-09-05 CY CY198397A patent/CY1983A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ATE119040T1 (de) | 1995-03-15 |
| HK8197A (en) | 1997-01-24 |
| EP0727215A3 (en) | 1996-11-06 |
| US5550126A (en) | 1996-08-27 |
| EP0411668A2 (en) | 1991-02-06 |
| EP0411668B1 (en) | 1995-03-01 |
| DK0411668T4 (da) | 1999-08-09 |
| LV11431A (lv) | 1996-08-20 |
| DE69017302D1 (de) | 1995-04-06 |
| CY1983A (en) | 1997-09-05 |
| DK0411668T3 (da) | 1995-03-27 |
| DE69017302T2 (de) | 1995-09-28 |
| JPH0374328A (ja) | 1991-03-28 |
| EP0727215A2 (en) | 1996-08-21 |
| EP0411668A3 (en) | 1992-01-29 |
| DE69017302T3 (de) | 1999-08-05 |
| EP0411668B2 (en) | 1998-11-11 |
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