- [1,2,4]TRIAZOLO[4,3-B]PYRIDAZINES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES
-
The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
- -
-
-
- TRIAZOLO [4,3-B] PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER
-
The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
- -
-
-
- [1,2,4] TRIAZOLO [4,3-B] PYRIDAZINES AS LIGANDS OF THE ANDROGEN RECEPTOR
-
The invention concerns bicyclic compounds of Formula (I): wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
- -
-
-
- Synthesis and dopaminergic activity of some E-3-(piperidin-1-yl)-1-(4-substituted phenyl)prop-2-en-1-one derivatives
-
A convenient route for the synthesis of some 2-propen-1-one derivatives with E isomeric configuration is described. The activity of the synthesized compounds was evaluated through behavioral studies of apomorphine-induced licking in animal models. It was demonstrated that most of the synthesized compounds showed moderate activity in inhibition of lickings, among which 6a, was the most active compound at 30 mg/kg.
- Sakhteman, Amirhossein,Foroumadi, Alireza,Sharifzadeh, Mohammad,Amanlou, Masoud,Rayatnia, Farhoud,Shafiee, Abbas
-
scheme or table
p. 6908 - 6913
(2009/12/24)
-
- 2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
-
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
- -
-
Page/Page column 32
(2010/02/08)
-
- 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
-
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
- -
-
-
- New strong fibrates with piperidine moiety
-
New fibrates containing piperidine, 4-hydroxypiperidine, piperidin-3-ene, and piperazine moieties in the structures were synthesized and evaluated. Among the synthesized compounds, 2-[3-[1-(4-fluorobenzoyl)-piperidin-4yl]phenoxy]-2-methylpropanoic acid (9
- Komoto, Teruo,Hirota, Hiroyuki,Otsuka, Mari,Kotake, Jiro,Hasegawa, Susumu,Koya, Hidehiko,Sato, Susumu,Sakamoto, Takao
-
p. 1978 - 1985
(2007/10/03)
-
- Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4- hydroxybenzyl)piperidines, and (±)-3-(4-hydroxyphenyl)pyrrolidines: Selective antagonists at the 1A/2B NMDA receptor subtype
-
Antagonists at the 1A/2B subtype of the NMDA receptor (NR1A/2B) are typically small molecules that consist of a 4-benzyl- or a 4-phenylpiperidine with an ω-phenylalkyl substituent on the heterocyclic nitrogen. Many of these antagonists, for example ifenprodil (1), incorporate a 4-hydroxy substituent on the ω-phenyl group. In this study, the position of this 4- hydroxy substituent was transferred from the ω-phenyl group to the benzyl or phenyl group located on the 4-position of the piperidine ring. Analogues incorporating pyrrolidine in lieu of piperidine were also prepared. Electrical recordings using cloned receptors expressed in Xenopus oocytes show that high-potency antagonists at the NR1A/2B subtype are obtained employing N-(ω-phenylalkyl)-substituted 4-(4-hydroxyphenyl)piperidine, 4-(4- hydroxybenzyl)piperidine, and (±)3-(4-hydroxyphenyl)pyrrolidine as exemplified by 21 (IC50 = 0.022 μM), 33 (IC50 = 0.059 μM), and 40 (IC50 = 0.017 μM), respectively. These high-potency antagonists are > 1000 times more potent at the NR1A/2B subtype than at either the NR1A/2A or NR1A/2C subtypes. The binding affinities of 21 at α1-adrenergic receptors ([3H]prazosin, IC50 = 0.54 μM) and dopamine D2 receptors ([3H]raclopride, IC50 = 1.2 μM) are reduced by incorporating a hydroxy group onto the 4-position of the piperidine ring and the β-carbon of the N- alkyl spacer to give (±)-27: IC50 NR1A/2B, 0.026; α1, 14; D2, 105 μM. The high-potency phenolic antagonist 21 and its low-potency O-methylated analogue 18 are both potent anticonvulsants in a mouse maximal electroshock- induced seizure (MES) study (ED50 (iv) = 0.23 and 0.56 mg/kg, respectively). These data indicate that such compounds penetrate the blood- brain barrier but their MES activity may not be related to NMDA receptor antagonism.
- Guzikowski, Anthony P.,Tamiz, Amir P.,Acosta-Burruel, Manuel,Hong-Bae, Soo,Cai, Sui Xiong,Hawkinson, Jon E.,Keana, John F. W.,Kesten, Suzanne R.,Shipp, Christina T.,Tran, Minhtam,Whittemore, Edward R.,Woodward, Richard M.,Wright, Jon L.,Zhou, Zhang-Lin
-
p. 984 - 994
(2007/10/03)
-
- Aryl substituted heterocycles
-
The present invention concerns the novel use of aryl substituted heterocycles of formula I, set out below, which antagonize the pharmacological actions of one of ent endogenous neuropeptide tachykinins an the neurokinin 2 (NK2) receptor making them useful whenever such antagonism is desired, such as in the treatment of asthma and related conditions. The invention also provides pharmaceutical compositions containing the aryl substituted heterocycles for use in such treatment. Certain novel aryl substituted heterocycles of formula I and novel intermediates for their manufacture are also provided. STR1
- -
-
-
- Cyclic amide derivatives for treating asthma
-
Compounds of formula I STR1 wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
- -
-
-
- 2-pyrrolidinones, pharmaceutical compositions containing these compounds and processes for preparing them
-
The invention relates to cyclic imino derivatives of general formula wherein A, B, E, X2 to X5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.
- -
-
-