RU2005118071A - Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей - Google Patents
Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей Download PDFInfo
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- RU2005118071A RU2005118071A RU2005118071/15A RU2005118071A RU2005118071A RU 2005118071 A RU2005118071 A RU 2005118071A RU 2005118071/15 A RU2005118071/15 A RU 2005118071/15A RU 2005118071 A RU2005118071 A RU 2005118071A RU 2005118071 A RU2005118071 A RU 2005118071A
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- 239000003446 ligand Substances 0.000 title claims abstract 19
- 230000002485 urinary effect Effects 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 14
- 239000012453 solvate Substances 0.000 claims abstract 14
- 150000001875 compounds Chemical class 0.000 claims abstract 9
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims abstract 7
- 239000003149 muscarinic antagonist Substances 0.000 claims abstract 7
- 239000003814 drug Substances 0.000 claims abstract 6
- 238000004519 manufacturing process Methods 0.000 claims abstract 4
- 229940124638 COX inhibitor Drugs 0.000 claims 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 229940127557 pharmaceutical product Drugs 0.000 claims 5
- 206010046543 Urinary incontinence Diseases 0.000 claims 4
- 229940123934 Reductase inhibitor Drugs 0.000 claims 3
- 239000000951 adrenergic alpha-1 receptor antagonist Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- RGFRGRZSMVXTLF-UHFFFAOYSA-N 4-[(3-fluorophenyl)methyl]pyrrolidin-1-ium-2-carboxylate Chemical compound C1NC(C(=O)O)CC1CC1=CC=CC(F)=C1 RGFRGRZSMVXTLF-UHFFFAOYSA-N 0.000 claims 2
- 229940113178 5 Alpha reductase inhibitor Drugs 0.000 claims 2
- 239000002677 5-alpha reductase inhibitor Substances 0.000 claims 2
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- OOGJQPCLVADCPB-HXUWFJFHSA-N tolterodine Chemical group C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 OOGJQPCLVADCPB-HXUWFJFHSA-N 0.000 claims 2
- 229960004045 tolterodine Drugs 0.000 claims 2
- BDIAUFOIMFAIPU-UHFFFAOYSA-N valepotriate Natural products CC(C)CC(=O)OC1C=C(C(=COC2OC(=O)CC(C)C)COC(C)=O)C2C11CO1 BDIAUFOIMFAIPU-UHFFFAOYSA-N 0.000 claims 2
- NDDZVQRQVFTNSN-UHFFFAOYSA-N 2-[3-(aminomethyl)-3-bicyclo[3.2.0]heptanyl]acetic acid Chemical compound C1C(CN)(CC(O)=O)CC2CCC21 NDDZVQRQVFTNSN-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229940111134 coxibs Drugs 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 206010029446 nocturia Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 1
- 229960001233 pregabalin Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- RGFRGRZSMVXTLF-UMJHXOGRSA-N OC([C@H]1NCC(Cc2cccc(F)c2)C1)=O Chemical compound OC([C@H]1NCC(Cc2cccc(F)c2)C1)=O RGFRGRZSMVXTLF-UMJHXOGRSA-N 0.000 description 1
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- 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
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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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
-
- 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
- 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
-
- 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
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- 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
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Pyrrole Compounds (AREA)
Claims (24)
1. Применение альфа-2-дельта лиганда, или его фармацевтически приемлемой соли или сольвата, для получения лекарственного средства для лечения СНМП, отличного от недержания мочи, связанного с ГМП и/или ДГПЖ.
2. Применение сочетания альфа-2-дельта лиганда с соединением, выбранным из
(i) антагониста α1-адренергического рецептора;
(ii) соединения, обладающего активностью NRI и/или SRI;
(iii) ингибитора HMG Со-А редуктазы;
(iv) ингибитора PDEV;
(v) мускаринового антагониста; или
(vi) ингибитора СОХ,
или его фармацевтически приемлемых солей или сольватов, для получения лекарственного средства для лечения СНМП, связанного с ГМП и/или ДГПЖ.
3. Применение по п.2, где альфа-2-дельта лиганд находится в сочетании с ингибитором СОХ, и ингибитор СОХ является ингибитором СОХ2.
4. Применение по п.2, где альфа-2-дельта лиганд находится в сочетании с мускариновым антагонистом.
5. Применение по п.4, где мускариновым антагонистом является толтеродином.
6. Применение сочетания альфа-2-дельта лиганда и ингибитора 5-α редуктазы человека, или его фармацевтически приемлемых солей или сольватов, для получения лекарственного средства для лечения СНМП, связанного с ДГПЖ.
7. Применение по любому из пп.2 или 6, где СНМП не является недержанием мочи.
8. Применение по любому из пп.1, 2 или 6, где СНМП связан с ДГПЖ.
9. Применение по любому из пп.1, 2 или 6, где СНМП связан с ГМП.
10. Применение по п.9, где при ГМП отсутствует недержание мочи.
11. Применение по любому из пп.1, 2 или 6, где СНМП является частыми позывами к мочеиспусканию.
12. Применение по любому из пп.1, 2 или 6, где СНМП представляет собой никтурию.
13. Применение по любому из пп.1, 2 или 6, где альфа-2-дельта лиганд выбран из
или его фармацевтически приемлемой соли или сольвата;
где каждый R1 и R2 независимо выбран из Н, прямого или разветвленного алкила из 1-6 атомов углерода, циклоалкила из 3-6 атомов углерода, фенила и бензила, при условии, кроме трициклооктанового соединения формулы (XVIII), что R1 и R2 одновременно не могут быть водородом; или выбран из
или его фармацевтически приемлемой соли или сольвата.
14. Применение по любому из пп.1, 2 или 6, где альфа-2-дельта лиганд выбран из габапентина (I)
или его фармацевтически приемлемой соли или сольвата.
15. Применение по любому из пп.1, 2 или 6, где альфа-2-дельта лигандом является прегабалин (II)
или его фармацевтически приемлемой соли или сольвата.
16. Применение по любому из пп.1, 2 или 6, где альфа-2-дельта лигандом является (1α, 3α, 5α)(3-аминометилбицикло[3.2.0]гепт-3-ил) уксусная кислота (III')
или его фармацевтически приемлемой соли или сольвата.
17. Применение по любому из пп.1, 2 или 6, где альфа-2-дельта лигандом является 4-(3-фторбензил)пирролидин-2-карбоновая кислота (XXXV)
или ее фармацевтически приемлемая соль или сольват.
18. Способ лечения СНМП, отличного от недержания мочи, связанного с ГМП и/или ДГПЖ, заключающийся во введении альфа-2-дельта лиганда, или его фармацевтически приемлемой соли или сольвата, пациенту при необходимости такого лечения.
19. Способ по п.18, где указанный лиганд такой, как определен в любом из пп.13-17.
20. Фармацевтический продукт, содержащий альфа-2-дельта лиганд и соединение, выбранное из
(i) антагониста α1-адренергического рецептора;
(ii) соединения, обладающего активностью NRI и/или SRI;
(iii) ингибитора HMG Со-А редуктазы;
(iv) ингибитора PDEV;
(v) антагониста мускаринового рецептора; или
(vi) ингибитора СОХ,
или его фармацевтически приемлемую соль или сольват, в виде объединенного лекарственного средства для одновременного, отдельного или последовательного применение для лечения СНМП, связанного с ГМП и/или ДГПЖ.
21. Фармацевтический продукт по п.20, где альфа-2-дельта лиганд такой, как определено в любом из пп.13-17, и находится в сочетании с мускариновым антагонистом.
22. Фармацевтический продукт по п.21, где альфа-2-дельта лиганд такой, как определено в любом из пп.13-17, и находится в сочетании с толтеродином.
23. Фармацевтический продукт, содержащий альфа-2-дельта лиганд и ингибитор 5-α редуктазы человека или его фармацевтически приемлемую соль или сольват, в виде объединенного лекарственного средства для одновременного, отдельного или последовательного применение для лечения СНМП, связанного ДГПЖ.
24. Фармацевтический продукт, содержащий альфа-2-дельта лиганд и соединение, выбранное из
(i) антагониста α1-адренергического рецептора;
(ii) соединения, обладающего активностью NRI и/или SRI;
(iii) ингибитора HMG Со-А редуктазы;
(iv) ингибитора PDEV;
(v) антагониста мускаринового рецептора; или
(vi) ингибитора СОХ;
и его фармацевтически приемлемую соль или сольват.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43349102P | 2002-12-13 | 2002-12-13 | |
| US60/433,491 | 2002-12-13 | ||
| GB0302657A GB0302657D0 (en) | 2003-02-05 | 2003-02-05 | Method of treatment |
| GB0302657.2 | 2003-02-05 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008108841/15A Division RU2008108841A (ru) | 2002-12-13 | 2008-03-06 | Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2005118071A true RU2005118071A (ru) | 2006-01-27 |
| RU2331438C2 RU2331438C2 (ru) | 2008-08-20 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005118071/15A RU2331438C2 (ru) | 2002-12-13 | 2003-12-03 | Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей |
| RU2008108841/15A RU2008108841A (ru) | 2002-12-13 | 2008-03-06 | Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей |
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| RU2008108841/15A RU2008108841A (ru) | 2002-12-13 | 2008-03-06 | Альфа-2-дельта лиганд для лечения симптомов нижних мочевыводящих путей |
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| EP (2) | EP1572173B1 (ru) |
| JP (2) | JP2006511606A (ru) |
| KR (3) | KR20070091049A (ru) |
| AT (1) | ATE465725T1 (ru) |
| AU (2) | AU2003303041B2 (ru) |
| BR (1) | BR0316572A (ru) |
| CA (2) | CA2509605C (ru) |
| CY (1) | CY1110114T1 (ru) |
| DE (1) | DE60332387D1 (ru) |
| DK (1) | DK1572173T3 (ru) |
| ES (1) | ES2341240T3 (ru) |
| HK (1) | HK1083010A1 (ru) |
| MX (1) | MXPA05006333A (ru) |
| MY (2) | MY146794A (ru) |
| NO (1) | NO20053355D0 (ru) |
| NZ (2) | NZ539972A (ru) |
| PL (1) | PL377657A1 (ru) |
| PT (1) | PT1572173E (ru) |
| RU (2) | RU2331438C2 (ru) |
| SI (1) | SI1572173T1 (ru) |
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| WO (1) | WO2004054560A1 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003301184A1 (en) * | 2002-12-20 | 2004-07-22 | Dynogen Pharmaceuticals Inc | METHODS OF TREATING NON-PAINFUL BLADDER DISORDERS USING Alpha2Delta SUBUNIT CALCIUM CHANNEL MODULATORS |
| EP1621193A3 (en) * | 2002-12-20 | 2006-08-02 | Dynogen Pharmaceuticals Inc. | Treatment of non-painful bladder disorders using alpha2-delta-subunit calcium channel modulators |
| US7084116B2 (en) | 2003-03-10 | 2006-08-01 | Dynogen Pharmaceuticals, Inc. | Methods for treating lower urinary tract disorders and the related disorders vulvodynia and vulvar vestibulitis using Cav2.2 subunit calcium channel modulators |
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